CompletedNCT02853435Updated Oct 8, 2020Results posted

To Assess Bioavailability, Food Effect and Pharmacokinetics of Gepotidacin Tablets: A Phase I, Single-Dose, 2 Part Study in Healthy Subjects.

A Phase 1 interventional study of Gepotidacin RC Tablet and Gepotidacin HSWG Tablet in Infections, Bacterial, sponsored by GlaxoSmithKline. Completed at 2 sites in United States. Open to participants aged 18 Years to 64 Years, including healthy volunteers. Per ClinicalTrials.gov, last updated 2020-10-08.

Sponsored by GlaxoSmithKline · Phase 1, Interventional, and Treatment

Phase: Phase 1
Study type: Interventional
Enrollment: 48
Allocation: Randomized
Ages: 18 Years to 64 Years
Sex: All

Study summary

This study is divided in 2 parts. Part 1a is being conducted to evaluate the safety, tolerability, and relative bioavailability of the 2 free base tablet formulations (roller compacted [RC] and high shear wet granulation [HSWG]) compared to the reference capsule formulation under fasted conditions. This is a 3-period; cross-over study that will guide which gepotidacin formulation will be used for future studies. Following review of pharmacokinetic (PK) and safety data in Part 1a, a decision will be made whether to proceed with Parts 1b and 2.

Part 1b is a 2-period, cross-over study and will assess the effect of food on the PK of the selected gepotidacin tablet formulation from Part 1a. In Part 2, the PK of the selected gepotidacin tablet formulation from Part 1a in Japanese (2a) and Chinese (2b) subjects will be evaluated under fasted conditions.

The duration of the study (from Screening to the Follow-up visit) will be approximately 44 days (Part 1a), 41 days (Part 1b) and 38 days (Part 2a and 2b each), respectively. The approximate number of subjects enrolled in Part 1a will be 27 (9 subjects in each of the 3 treatment sequences), 16 in Part 1b (8 subjects in each of the 2 treatment sequences) and 12 Japanese and 12 Chinese subjects in Part 2a and 2b, respectively.

Conditions studied

Infections, Bacterial

Browse trials for

Bacterial Infections 658

Keywords

Cross-over
Gepotidacin
Pharmacokinetics
Relative Bioavailability
non-compartmental PK analysis
High shear wet granulation

In context

Bacterial Infections

658 studies on the registry are indexed under Bacterial Infections; 100 are open to participants now.

This study's enrollment of 48 is below the median of 84 across 405 interventional studies indexed under Bacterial Infections.

Browse Bacterial Infections studies →

Lead sponsor

GlaxoSmithKline is the lead sponsor of 3,562 studies on the registry; 117 are open to participants now.

Of its 258 completed or terminated interventional studies of FDA-regulated products, 232 (90%) have results posted.

Counted across the registry records on this site, refreshed daily.

Who can participate

Ages eligible: 18 Years to 64 Years
Sexes eligible: All
Accepts healthy volunteers: Yes

Inclusion criteria

Male or female subjects between 18 and 64 years of age inclusive, at the time of signing the informed consent.
Healthy as determined by the investigator based on medical history, clinical laboratory results (serum chemistry, hematology, urinalysis, and serology), vital sign measurements, 12-lead ECG results, and physical examination findings. A subject with a clinical abnormality or laboratory parameters outside the reference range for the population being studied may be included only if the investigator feels and documents that the finding is unlikely to introduce additional risk factors and will not interfere with the study procedures.
Additional inclusion criteria for Japanese subjects (Part 2a only): the subject was a non-naturalized Japanese citizen and held a Japanese passport, the subject had 2 Japanese parents and 4 Japanese grandparents who were all non naturalized Japanese citizens, as confirmed by interview and the subject had been living outside of Japan for up to 10 years as confirmed by interview.
Additional inclusion criteria for Chinese subjects (Part 2b only): the subject was a non-naturalized Chinese citizen and held a Chinese passport, the subject had 2 Chinese parents and 4 Chinese grandparents who were all non naturalized Chinese citizens, as confirmed by interview, the subject had been living outside of China for up to 10 years as confirmed by interview.
Body weight for subjects in Part 1a and 1b: more than equal to (>=) 50 kilogram (kg) and body mass index (BMI) within the range 19 and 32 kilogram per meter square (kg/m\^2), inclusive and for Japanese and Chinese subjects (Part 2a and 2b): >=50 kg and BMI within the range 18 and 32 kg/m\^2, inclusive.
Male or female: a female subject is eligible to participate if she is not pregnant (as confirmed by a negative serum human chorionic gonadotrophin test, not lactating, and at least one of the following conditions applies. Non-reproductive potential defined as: pre-menopausal females with one of the following: documented tubal ligation, documented hysteroscopic tubal occlusion procedure with follow-up confirmation of bilateral tubal occlusion, hysterectomy, documented bilateral oophorectomy and postmenopausal defined as 12 months of spontaneous amenorrhea (in questionable cases a blood sample with simultaneous follicle-stimulating hormone and estradiol levels consistent with menopause). Females on hormone replacement therapy (HRT) and whose menopausal status is in doubt will be required to use one of the highly effective contraception methods if they wish to continue their HRT during the study. Otherwise, they must discontinue HRT to allow confirmation of post-menopausal status prior to study enrolment. Reproductive potential and agrees to follow one of the options listed in the Modified List of Highly Effective Methods for Avoiding Pregnancy in Females of Reproductive Potential from 30 days prior to the first dose of study medication and until completion of the Follow-up visit.
Capable of giving signed informed consent which includes compliance with the requirements and restrictions listed in the consent form and in this protocol.

Exclusion criteria

Exclusion Criteria

Subject has a clinically significant abnormality in past medical history or at the Screening physical examination that in the investigator's opinion may place the subject at risk or interfere with outcome variables of the study. This includes, but is not limited to, history or current cardiac, hepatic, renal, neurologic, gastrointestinal, respiratory, hematologic, or immunologic disease.
Subject has any surgical or medical condition (active or chronic) that may interfere with drug absorption, distribution, metabolism, or excretion of the study drug, or any other condition that may place the subject at risk, in the opinion of the investigator.
QTc more than (>) 450 millisecond (msec).
Use of a systemic antibiotic within 30 days of Screening.
Within 2 months before Screening, either a confirmed history of Clostridium difficile diarrhea infection or a past positive Clostridium difficile toxin test.
Current or chronic history of liver disease, or known hepatic or biliary abnormalities (with the exception of Gilbert's syndrome or asymptomatic gallstones).
History of sensitivity to heparin or heparin-induced thrombocytopenia (if the clinic uses heparin to maintain intravenous cannula patency).
Subjects cannot use any over-the-counter, or prescription medication (except for hormonal contraceptives and/or acetaminophen), vitamin supplement, or herbal medication within 7 days (or 5 half-lives, whichever is longer) before dosing and during the study.
History of regular alcohol consumption within 6 months of screening defined as an average weekly intake of >21 units (or an average daily intake of >3 units) for males or an average weekly intake of >14 units (or an average daily intake >2 units) for females. One unit is equivalent to 270 milliliter (mL) of full strength beer, 470 mL of light beer, 30 mL of spirits, or 100 mL of wine.
Urinary cotinine level indicative of smoking or history or regular use of tobacco- or nicotine containing products within 3 months before screening.
History of sensitivity to any of the study medications, or components thereof, or a history of drug or other allergy that, in the opinion of the investigator or medical monitor, contraindicates their participation.
Presence of hepatitis B surface antigen, positive hepatitis C antibody test result at screening or within 3 months prior to first dose of study treatment.
Female subject has a positive pregnancy test result or is lactating at Screening or upon admission to the clinic.
ALT >1.5×upper limit of normal (ULN)
Bilirubin >1.5×ULN (isolated bilirubin >1.5×ULN is acceptable if bilirubin is fractionated and direct bilirubin less than [\<] 35 percent [%]).
Urinalysis positive for blood without other cause identified.
A positive pre-study drug/alcohol screen.
A positive test for human immunodeficiency virus antibody.
Subject has clinically significant abnormal findings in serum chemistry, hematology, or urinalysis results obtained at Screening or Day -1.
Donation of blood in excess of 500 mL within 12 weeks prior to dosing or participation in the study would result in donation of blood or blood products in excess of 500 mL within a 56 day period.
Previous exposure to gepotidacin within 12 months prior to the first dosing day.
Exclusion criteria for screening and baseline 12-lead ECG (a single repeat is allowed for eligibility determination): male subjects with heart rate \<40 and >100 beats per minute (bpm), female subjects with heart rate \<50 and >100 bpm, PR interval \<120 and >220 msec for male and female subjects, QRS duration \<70 and >120 msec in both male and female subjects and corrected QT interval using Bazett's formula (QTcB) or corrected QT interval using Fridericia's formula (QTcF) >450 msec in both male and female subjects. Evidence of previous myocardial infarction (does not include ST segment changes associated with repolarization). Any conduction abnormality (including but not specific to left or right complete bundle branch block, atrioventricular block [second degree or higher], Wolf Parkinson White syndrome), sinus pauses >3 seconds, non-sustained or sustained ventricular tachycardia (>=3 consecutive ventricular ectopic beats) or any significant arrhythmia which, in the opinion of the principal investigator and GlaxoSmithKline medical monitor, will interfere with the safety of the individual subject.
The subject has participated in a clinical trial and has received an investigational product within the following time period prior to the first dosing day in the current study: 30 days, 5 half-lives or twice the duration of the biological effect of the investigational product (whichever is longer).
Subject is unable to comply with all study procedures, in the opinion of the investigator.
The subject should not participate in the study, in the opinion of the investigator or sponsor.

Study design

Phase: Phase 1
Primary purpose: Treatment
Allocation: Randomized
Intervention model: Crossover assignment
Masking: None (open label)
Enrollment: 48 participants (actual)

Study arms

Experimental
Part1a: Gepotidacin 1500 mg-Sequence A-capsules, B-RC, C-HSWG
Subjects will be receive treatment sequence (ABC) which is a single dose of gepotidacin 1500 mg (three tablets of 500 mg) reference capsule (Treatment A) in Period 1, 1500 mg (two tablets of 750 mg) RC tablet (Treatment B) in Period 2 or 1500 mg (two tablets of 750 mg) HSWG tablet (Treatment C) in Period 3, according to randomization. There will be a washout period of at least 3 days between doses.
Drug: Gepotidacin RC Tablet · Drug: Gepotidacin HSWG Tablet · Drug: Gepotidacin Capsule
Experimental
Part1a: Gepotidacin 1500 mg-Sequence C-HSWG, A-capsules, B-RC)
Subjects will receive treatment sequence (CAB) to receive a single dose of gepotidacin 1500 mg (two tablets of 750 mg) HSWG tablet (Treatment C) in Period 1, 1500 mg (three tablets of 500 mg) reference capsule (Treatment A) in Period 2 or 1500 mg (two tablets of 750 mg) RC tablet (Treatment B) in Period 3 according to randomization. There will be a washout period of at least 3 days between doses.
Drug: Gepotidacin RC Tablet · Drug: Gepotidacin HSWG Tablet · Drug: Gepotidacin Capsule
Experimental
Part1a: Gepotidacin 1500 mg-Sequence B-RC, C-HSWG, A-capsules)
Subjects will receive treatment sequence (BCA) to receive a single dose of gepotidacin 1500 mg (two tablets of 750 mg) RC tablet (Treatment B) in period 1, 1500 mg (two tablets of 750 mg) HSWG tablet (Treatment C) in Period 2, or 1500 mg (three tablets of 500 mg) (Treatment A) in Period 3 reference capsule according to randomization.. There will be a washout period of at least 3 days between doses.
Drug: Gepotidacin RC Tablet · Drug: Gepotidacin HSWG Tablet · Drug: Gepotidacin Capsule
Experimental
Part1b: Gepotidacin 1500 mg-Sequence DE-fasted followed by fed
Subjects will receive treatment sequence (DE) according to randomization which is a single 1500 mg (two tablets of 750 mg) dose of gepotidacin tablet (RC or HSWG) selected from Part 1a under fasted condition (Treatment D) in Period 1 followed by fed conditions (Treatment E) in period 2. There will be a washout period of at least 3 days between doses.
Drug: Gepotidacin RC Tablet · Drug: Gepotidacin HSWG Tablet
Experimental
Part1b: Gepotidacin 1500 mg-Sequence ED-fed followed by fasted
Subjects will be receive treatment sequence (ED) according to randomization which is single 1500 mg (two tablets of 750 mg) dose of gepotidacin tablet (RC or HSWG) selected from Part 1a under fed condition (Treatment E) in period 1 followed by fasted conditions (Treatment D) in Period 2. There will be a washout period of at least 3 days between doses.
Drug: Gepotidacin RC Tablet · Drug: Gepotidacin HSWG Tablet
Experimental
Part 2a: Gepotidacin 1500 mg (RC or HSWG)- Japanese subjects
Japanese subjects will receive a single 1500 mg (two tablets of 750 mg) dose of gepotidacin tablet (RC or HSWG) selected from Part 1a.
Drug: Gepotidacin RC Tablet · Drug: Gepotidacin HSWG Tablet
Experimental
Part 2b: Gepotidacin 1500 mg (RC or HSWG)- Chinese subjects
Chinese subjects will receive a single 1500 mg (two tablets of 750 mg) dose of gepotidacin tablet (RC or HSWG) selected from Part 1a.
Drug: Gepotidacin RC Tablet · Drug: Gepotidacin HSWG Tablet

Interventions

DrugGepotidacin RC Tablet
The tablet is a capsule shape white film coated tablet with no identifying markings. This is an immediate release tablet containing gepotidacin 750 mg (free base) and inactive formulation excipients administered orally with 240 mL of water. Up to an additional 100 mL of water may be given to assist in swallowing tablets.
DrugGepotidacin HSWG Tablet
The tablet is an oval shape white film coated tablet with no identifying markings. This is an immediate release tablets containing gepotidacin 750 mg (free base) and inactive formulation excipients administered orally with 240 mL of water. Up to an additional 100 mL of water may be given to assist in swallowing tablets.
DrugGepotidacin Capsule
It is a pink gelatin size 00 capsule with no identifying markings containing slightly agglomerated pale yellow to grayish yellow to yellowish gray powder. This is an immediate release capsules containing gepotidacin 500 mg (mesylate salt) and inactive formulation excipients administered orally with 240 mL of water. Up to an additional 100 mL of water may be given to assist in swallowing capsules.

What researchers measure

Primary outcomes

Area Under the Concentration-time Curve From Time 0 (Pre-dose) Extrapolated to Infinite Time (AUC [0-infinity]) of Plasma Gepotidacin for Part 1a
Blood samples for pharmacokinetic (PK) analysis of gepotidacin were collected at Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in Part 1a. For each sample, 3 milliliters (mL) of blood was drawn via an indwelling catheter and/or direct venipuncture into tubes containing ethylenediaminetetraacetate anticoagulant. PK parameters were determined from the plasma concentration-time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher. The PK Parameter Population consisted of all participants in the PK Population, for whom valid and evaluable PK parameters were derived. Statistics has been presented on geometric least square (LS) means.
Time frame: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Area Under the Concentration-time Curve (AUC) From Time 0 (Pre-dose) to Time of the Last Quantifiable Concentration (AUC [0-t]) of Plasma Gepotidacin for Part 1a
Blood samples for PK analysis of gepotidacin were collected at Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in Part 1a. For each sample, 3 mL of blood was drawn via an indwelling catheter and/or direct venipuncture into tubes containing ethylenediaminetetraacetate anticoagulant. PK parameters were determined from the plasma concentration-time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher. Statistics has been presented on geometric LS means.
Time frame: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Relative Bioavailability of Drug (Frel) of Plasma Gepotidacin for Part 1a
Blood samples for PK analysis of gepotidacin were collected at Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in Part 1a. For each sample, 3 mL of blood was drawn via an indwelling catheter and/or direct venipuncture into tubes containing ethylenediaminetetraacetate anticoagulant. PK parameters were determined from the plasma concentration-time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher. NA indicates data was not available as this was the reference capsule the Frel of each tablet type was being compared to.
Time frame: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Maximum Observed Concentration (Cmax) Determined Directly From the Concentration Time Data of Plasma Gepotidacin for Part 1a
Blood samples for PK analysis of gepotidacin were collected at Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in Part 1a. For each sample, 3 mL of blood was drawn via an indwelling catheter and/or direct venipuncture into tubes containing ethylenediaminetetraacetate anticoagulant. PK parameters were determined from the plasma concentration-time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher. Statistics has been presented on geometric LS means.
Time frame: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Time to First Occurrence of Cmax (Tmax) of Plasma Gepotidacin for Part 1a
Blood samples for PK analysis of gepotidacin were collected at Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in Part 1a. For each sample, 3 mL of blood was drawn via an indwelling catheter and/or direct venipuncture into tubes containing ethylenediaminetetraacetate anticoagulant. PK parameters were determined from the plasma concentration-time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher.
Time frame: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Lag Time Before Observation of Drug Concentrations in Sampled Matrix (Tlag) of Plasma Gepotidacin for Part 1a
Blood samples for PK analysis of gepotidacin were collected at Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in Part 1a. For each sample, 3 mL of blood was drawn via an indwelling catheter and/or direct venipuncture into tubes containing ethylenediaminetetraacetate anticoagulant. PK parameters were determined from the plasma concentration-time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher.
Time frame: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Terminal Phase Half-life (t1/2) of Plasma Gepotidacin for Part 1a
Blood samples for PK analysis of gepotidacin were collected at Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in Part 1a. For each sample, 3 mL of blood was drawn via an indwelling catheter and/or direct venipuncture into tubes containing ethylenediaminetetraacetate anticoagulant. PK parameters were determined from the plasma concentration-time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher.
Time frame: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Total Unchanged Drug (Total Amount of Drug Excreted in Urine [Ae Total]) for Part 1a
PK urine samples were collected at 0 (predose), 0 to 2, 2 ot 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, 36 to 48 hours. PK parameters were determined from the urine concentration- time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher
Time frame: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours
Percentage of the Given Dose of Drug Excreted in Urine (fe%) of Plasma Gepotidacin for Part 1a
PK urine samples were collected at 0 (pre-dose), 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, 36 to 48 hours. PK parameters were determined from the urine concentration- time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher.
Time frame: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours
Renal Clearance of Drug in Urine (CLr) for Part 1a
PK urine samples were collected at 0 (pre-dose), 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, 36 to 48 hours. PK parameters were determined from the urine concentration- time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher.
Time frame: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours
Amount of Drug Excreted in Urine in a Time Intervals for Pre-dose, 0 to 2 Hours, 2 to 4 Hours, 4 to 6 Hours, 6 to 8 Hours, 8 to 12 Hours, 12 to 24 Hours, 24 to 36 Hours, and 36 to 48 Hours (Ae [t1-t2]) for Part 1a
PK urine samples were collected at 0 (pre-dose), 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, 36 to 48 hours. PK parameters were determined from the urine concentration- time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher. Only those participants available at the specific time points were analyzed (represented by n = X in the category titles).
Time frame: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours
Area Under the Urine Concentration-time Curve Over Time 0 (Pre-dose) to 12 Hours (AUC [0-12]) for Part 1a
PK urine samples were collected at 0 (pre-dose), 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, 36 to 48 hours. PK parameters were determined from the urine concentration- time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher
Time frame: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours.
Area Under the Urine Concentration-time Curve Over Time 0 (Pre-dose) to 24 Hours (AUC [0-24]) After Dosing for Part 1a
PK urine samples were collected at 0 (pre-dose), 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, 36 to 48 hours. PK parameters were determined from the urine concentration- time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher
Time frame: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours
Area Under the Urine Concentration-time Curve Over Time 0 (Pre-dose) to 48 Hours (AUC [0-48]) After Dosing for Part 1a
PK urine samples were collected at 0 (pre-dose), 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, 36 to 48 hours. PK parameters were determined from the urine concentration- time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher. Only those participants with data available at the indicated time point were analyzed.
Time frame: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours
AUC (0-infinity) of Plasma Gepotidacin for Part 1b
Blood samples for PK analysis of gepotidacin was planned to be collected at Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in Part 1b. Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.
Time frame: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
AUC (0-t) of Plasma Gepotidacin for Part 1b
Blood samples for PK analysis of gepotidacin was planned to be collected at Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in Part 1b. Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.
Time frame: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Cmax of Plasma Gepotidacin for Part 1b
Blood samples for PK analysis of gepotidacin was planned to be collected at Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in Part 1b. Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.
Time frame: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Tmax of Plasma Gepotidacin for Part 1b
Blood samples for PK analysis of gepotidacin was planned to be collected at Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in Part 1b. Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.
Time frame: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Tlag of Plasma Gepotidacin for Part 1b
Blood samples for PK analysis of gepotidacin was planned to be collected at Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in Part 1b. Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.
Time frame: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
t1/2 of Plasma Gepotidacin for Part 1b
Blood samples for PK analysis of gepotidacin was planned to be collected at Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in Part 1b. Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.
Time frame: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
AUC (0-infinity) of Plasma Gepotidacin for Part 2
Blood samples for PK analysis of gepotidacin were collected at Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in Part 2. For each sample, 3 mL of blood was drawn via an indwelling catheter and/or direct venipuncture into tubes containing ethylenediaminetetraacetate anticoagulant. PK parameters were determined from the plasma concentration-time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher.
Time frame: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
AUC (0-t) of Plasma Gepotidacin for Part 2
Blood samples for PK analysis of gepotidacin were collected at Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in Part 2. For each sample, 3 mL of blood was drawn via an indwelling catheter and/or direct venipuncture into tubes containing ethylenediaminetetraacetate anticoagulant. PK parameters were determined from the plasma concentration-time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher.
Time frame: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Cmax of Plasma Gepotidacin for Part 2
Blood samples for PK analysis of gepotidacin were collected at Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in Part 2. For each sample, 3 mL of blood was drawn via an indwelling catheter and/or direct venipuncture into tubes containing ethylenediaminetetraacetate anticoagulant. PK parameters were determined from the plasma concentration-time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher.
Time frame: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Tlag of Plasma Gepotidacin for Part 2
Blood samples for PK analysis of gepotidacin were collected at Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in Part 2. For each sample, 3 mL of blood was drawn via an indwelling catheter and/or direct venipuncture into tubes containing ethylenediaminetetraacetate anticoagulant. PK parameters were determined from the plasma concentration-time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher.
Time frame: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Tmax of Plasma Gepotidacin for Part 2
Blood samples for PK analysis of gepotidacin were collected at Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in Part 2. For each sample, 3 mL of blood was drawn via an indwelling catheter and/or direct venipuncture into tubes containing ethylenediaminetetraacetate anticoagulant. PK parameters were determined from the plasma concentration-time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher.
Time frame: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
t1/2 of Plasma Gepotidacin for Part 2
Blood samples for PK analysis of gepotidacin were collected at Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in Part 2. For each sample, 3 mL of blood was drawn via an indwelling catheter and/or direct venipuncture into tubes containing ethylenediaminetetraacetate anticoagulant. PK parameters were determined from the plasma concentration-time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher.
Time frame: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Total Unchanged Drug (Ae Total) for Part 2
PK urine samples were collected at 0 (pre-dose), 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, 36 to 48 hours. PK parameters were determined from the urine concentration- time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher.
Time frame: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours.
Ae (t1-t2) for Part 2
PK urine samples were collected at 0 (pre-dose), 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, 36 to 48 hours. PK parameters were determined from the urine concentration- time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher.
Time frame: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours.
AUC (0-12) for Part 2
PK urine samples were collected at 0 (pre-dose), 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, 36 to 48 hours. PK parameters were determined from the urine concentration- time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher.
Time frame: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours.
AUC (0-24) for Part 2
PK urine samples were collected at 0 (pre-dose), 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, 36 to 48 hours. PK parameters were determined from the urine concentration- time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher.
Time frame: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours.
AUC (0-48) for Part 2
PK urine samples were collected at pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, 36 to 48 hours. PK parameters were determined from the urine concentration- time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher.
Time frame: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours.
fe% for Part 2
PK urine samples were collected at pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, 36 to 48 hours. PK parameters were determined from the urine concentration- time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher.
Time frame: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours.
CLr for Part 2
PK urine samples were collected at pre-dose), 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, 36 to 48 hours. PK parameters were determined from the urine concentration- time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher.
Time frame: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours.
AUC (0-infinity) of Plasma Gepotidacin for Part 3
Blood samples for PK analysis of gepotidacin were collected at Pre-dose, 0, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in Part 3. For each sample, 3 mL of blood was drawn via an indwelling catheter and/or direct venipuncture into tubes containing ethylenediaminetetraacetate anticoagulant. PK parameters were determined from the plasma concentration-time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher.
Time frame: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
AUC (0-t) of Plasma Gepotidacin for Part 3
Blood samples for PK analysis of gepotidacin were collected at Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in Part 3. For each sample, 3 mL of blood was drawn via an indwelling catheter and/or direct venipuncture into tubes containing ethylenediaminetetraacetate anticoagulant. PK parameters were determined from the plasma concentration-time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher.
Time frame: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Cmax of Plasma Gepotidacin for Part 3
Blood samples for PK analysis of gepotidacin were collected at Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in Part 3. For each sample, 3 mL of blood was drawn via an indwelling catheter and/or direct venipuncture into tubes containing ethylenediaminetetraacetate anticoagulant. PK parameters were determined from the plasma concentration-time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher.
Time frame: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Tmax of Plasma Gepotidacin for Part 3
Blood samples for PK analysis of gepotidacin were collected at Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in Part 3. For each sample, 3 mL of blood was drawn via an indwelling catheter and/or direct venipuncture into tubes containing ethylenediaminetetraacetate anticoagulant. PK parameters were determined from the plasma concentration-time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher.
Time frame: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Tlag of Plasma Gepotidacin for Part 3
Blood samples for PK analysis of gepotidacin were collected at Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in Part 3. For each sample, 3 mL of blood was drawn via an indwelling catheter and/or direct venipuncture into tubes containing ethylenediaminetetraacetate anticoagulant. PK parameters were determined from the plasma concentration-time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher.
Time frame: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
t1/2 of Plasma Gepotidacin for Part 3
Blood samples for PK analysis of gepotidacin were collected at Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in Part 3. For each sample, 3 mL of blood was drawn via an indwelling catheter and/or direct venipuncture into tubes containing ethylenediaminetetraacetate anticoagulant. PK parameters were determined from the plasma concentration-time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher.
Time frame: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Total Unchanged Drug (Ae Total) for Part 3
PK urine samples were collected at pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, 36 to 48 hours. PK parameters were determined from the urine concentration- time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher
Time frame: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours
Urine Ae (t1-t2) for Part 3
PK urine samples were collected at pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, 36 to 48 hours. PK parameters were determined from the urine concentration- time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher. Only those participants available at the specific time points were analyzed (represented by n = X in the category titles).
Time frame: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours.
Urine AUC (0-12) for Part 3
PK urine samples were collected at pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, 36 to 48 hours. PK parameters were determined from the urine concentration- time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher.
Time frame: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours.
Urine AUC (0-24) for Part 3
PK urine samples were collected at pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, 36 to 48 hours. PK parameters were determined from the urine concentration- time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher.
Time frame: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours.
Urine AUC (0-48) for Part 3
PK urine samples were collected at pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, 36 to 48 hours. PK parameters were determined from the urine concentration- time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher.
Time frame: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours.
fe% for Part 3
PK urine samples were collected at pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, 36 to 48 hours. PK parameters were determined from the urine concentration- time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher.
Time frame: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours.
CLr for Part 3
PK urine samples were collected at pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, 36 to 48 hours. PK parameters were determined from the urine concentration- time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher
Time frame: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours.

Secondary outcomes

Number of Participants With Non-serious Adverse Events (AEs) and Serious Adverse Events (SAEs) for Part 1a
AE is any untoward medical occurrence in a participant or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. An SAE is any untoward medical occurrence that, at any dose results in death, is life-threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, or is a congenital anomaly/birth defect or is medically significant. Participants with non-serious AEs and SAEs has been reported. Safety Population comprised of all participants who received at least 1 dose of study medication and had at least 1 post dose safety assessment.
Time frame: Up to 14 days
Change From Baseline in Clinical Chemistry Parameters Serum Glucose, Serum Calcium, Serum Carbon Dioxide, Serum Chloride, Serum Potassium, Serum Sodium and Serum Urea Nitrogen for Part 1a
Blood samples were collected for the assessment of chemistry parameters namely serum glucose, serum calcium, serum carbon dioxide, serum chloride, serum potassium, serum sodium and serum urea nitrogen for Part 1a. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles).
Time frame: Baseline and up to 14 days
Change From Baseline in Clinical Chemistry Parameters Serum Alanine Aminotransferase (ALT), Serum Alkaline Phosphatase (AP), Serum Aspartate Aminotransferase (AST) and Serum Creatinine Kinase (CK) for Part 1a
Blood samples were collected for the assessment of chemistry parameters namely serum ALT, serum AP, serum AST and serum CK for Part 1a. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose-visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles).
Time frame: Baseline and up to 14 days
Change From Baseline in Clinical Chemistry Parameters Serum Albumin and Serum Protein for Part 1a
Blood samples were collected for the assessment of chemistry parameters namely serum albumin and serum protein for Part 1a. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose-visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles).
Time frame: Baseline and up to 14 days
Change From Baseline in Clinical Chemistry Parameters Serum Bilirubin, Serum Creatinine and Serum Direct Bilirubin for Part 1a
Blood samples were collected for the assessment of chemistry parameters namely serum bilirubin, serum creatinine and serum direct bilirubin Part 1a. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles).
Time frame: Baseline and up to 14 days
Change From Baseline in Hematology Parameters Blood Basophils, Blood Eosinophils, Blood Leukocytes, Blood Lymphocytes, Blood Monocytes, Blood Neutrophils and Blood Platelets for Part 1a
Blood samples were collected for the assessment of hematology parameters namely blood basophils, blood eosinophils, blood leukocytes, blood lymphocytes, blood monocytes, blood neutrophils and blood platelets for Part 1a. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles).
Time frame: Baseline and up to 14 days
Change From Baseline in Hematology Parameters Blood Erythrocyte (Ery.) Mean Corpuscular Hemoglobin Concentration (MCHC) and Blood Hemoglobin for Part 1a
Blood samples were collected for the assessment of hematology parameters namely blood Ery. MCHC and blood hemoglobin for Part 1a. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose-visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles).
Time frame: Baseline and up to 14 days
Change From Baseline in Hematology Parameter Blood Ery. Mean Corpuscular Hemoglobin (MCH) for Part 1a
Blood samples were collected for the assessment of hematology parameter namely blood Ery. MCH for Part 1a. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles).
Time frame: Baseline and up to 14 days
Change From Baseline in Hematology Parameter Blood Ery. Mean Corpuscular Volume (MCV) for Part 1a
Blood samples were collected for the assessment of hematology parameter namely blood Ery. MCV for Part 1a. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles).
Time frame: Baseline and up to 14 days
Change From Baseline in Hematology Parameter Blood Ery. for Part 1a
Blood samples were collected for the assessment of hematology parameter namely blood Ery. for Part 1a. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles).
Time frame: Baseline and up to 14 days
Change From Baseline in Hematology Parameter Blood Hematocrit for Part 1a
Blood samples were collected for the assessment of hematology parameter namely blood hematocrit for Part 1a. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles).
Time frame: Baseline and up to 14 days
Change From Baseline in Vital Sign Parameters Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP) for Part 1a
Single vital signs were measured in semi-supine position after 5 minutes rest and included SBP, DBP. Baseline was defined as assessments performed on Day 1 (pre-dose). Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles).
Time frame: Baseline and up to 14 days
Change From Baseline in Vital Sign Parameter Heart Rate for Part 1a
Single vital signs were measured in semi-supine position after 5 minutes rest and included heart rate. Baseline was defined as assessments performed on Day 1 (pre-dose). Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles).
Time frame: Baseline and up to 14 days
Change From Baseline in Electrocardiogram (ECG) Parameter Heart Rate for Part 1a
A 12 lead ECG was measured in semi-supine position after 5 minutes rest using an ECG machine that automatically calculated the heart rate. Baseline was defined as assessments performed on Day 1 (pre-dose). Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles).
Time frame: Baseline and up to 14 days
Change From Baseline in ECG Parameters PR Interval, QRS Duration, QT Interval, Corrected QT Interval Using Bazett's Formula (QTcB) and Corrected QT Interval Using Fridericia's Formula (QTcF) for Part 1a
A 12 lead ECG was measured in semi-supine position after 5 minutes rest using an ECG machine that measured PR interval, QRS duration, QT interval, QTcB and QTcF for Part 1a. Baseline was defined as assessments performed on Day 1 (pre-dose). Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles).
Time frame: Baseline and up to 14 days
Number of Participants With Abnormal Values on Urinalysis by Dipstick Analysis Part 1a
Urinalysis parameters assessed were urine ketones, urine glucose, urine occult blood, urine pH, urine specific gravity and urine protein. In this dipstick test, the level of ketones, glucose, occult blood, pH, specific gravity and protein in urine samples was recorded as negative trace, 1+, 3+, 5+, 6+, 7+ and 8+ (the plus sign increases with a higher level of ketones, occult blood, pH or specific gravity in the urine: 1+=slightly positive, 3+ to 5+=positive, 6+ and above=high positive). Urine samples were collected for the measurement of urinalysis parameters by dipstick method up-to follow-up (5 to 7 days post last dose) in Part 1a. Only categories with significant values have been presented.
Time frame: Up to 14 days
Number of Participants With AEs and SAEs for Part 1b
AE is any untoward medical occurrence in a participant or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. An SAE is any untoward medical occurrence that, at any dose results in death, is life-threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, or is a congenital anomaly/birth defect or is medically significant. Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.
Time frame: Up to 11 days
Change From Baseline in Clinical Chemistry Parameters Serum Glucose, Serum Calcium, Serum Carbon Dioxide, Serum Chloride, Serum Potassium, Serum Sodium and Serum Urea Nitrogen for Part 1b
Blood samples were collected for the assessment of chemistry parameters namely serum glucose, serum calcium, serum carbon dioxide, serum chloride, serum potassium, serum sodium and serum urea nitrogen for Part 1b. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose-visit value from the Baseline value. Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.
Time frame: Baseline and up to 11 days
Change From Baseline in Clinical Chemistry Parameters Serum ALT, Serum AP, Serum AST and Serum CK for Part 1b
Blood samples were collected for the assessment of chemistry parameters namely serum ALT, serum AP, serum AST and serum CK for Part 1b. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.
Time frame: Baseline and up to 11 days
Change From Baseline in Clinical Chemistry Parameters Serum Albumin and Serum Protein for Part 1b
Blood samples were collected for the assessment of chemistry parameters namely serum albuim and serum protein for Part 1b. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.
Time frame: Baseline and up to 11 days
Change From Baseline in Clinical Chemistry Parameters Serum Bilirubin, Serum Creatinine and Serum Direct Bilirubin in Part 1b
Blood samples were collected for the assessment of chemistry parameters namely serum ALT, serum AP, serum AST and serum CK for Part 1b. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.
Time frame: Baseline and up to 11 days
Change From Baseline in Hematology Parameters Blood Basophils, Blood Eosinophils, Blood Leukocytes, Blood Lymphocytes, Blood Monocytes, Blood Neutrophils and Blood Platelets for Part 1b
Blood samples were collected for the assessment of hematology parameters namely blood basophils, blood eosinophils, blood leukocytes, blood lymphocytes, blood monocytes, blood neutrophils and blood platelets for Part 1b. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.
Time frame: Baseline and up to 11 days
Change From Baseline in Hematology Parameters Blood Ery. MCHC and Blood Hemoglobin for Part 1b
Blood samples were collected for the assessment of hematology parameters namely blood Ery. MCHC and blood hemoglobin for Part 1b. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.
Time frame: Baseline and up to 11 days
Change From Baseline in Hematology Parameter Blood Ery. MCH for Part 1b
Blood samples were collected for the assessment of hematology parameter namely blood Ery. MCH for Part 1a. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.
Time frame: Baseline and up to 11 days
Change From Baseline in Hematology Parameter Blood Ery. MCV for Part 1b
Blood samples were collected for the assessment of hematology parameter namely blood Ery. MCV for Part 1a. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.
Time frame: Baseline and up to 11 days
Change From Baseline in Hematology Parameter Blood Ery. for Part 1b
Blood samples were collected for the assessment of hematology parameter namely blood Ery. for Part 1b. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.
Time frame: Baseline and up to 11 days
Change From Baseline in Hematology Parameter Blood Hematocrit for Part 1b
Blood samples were collected for the assessment of hematology parameter namely blood hematocrit for Part 1b. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.
Time frame: Baseline and up to 11 days
Change From Baseline in Vital Sign Parameters SBP and DBP for Part 1b
Single vital signs were measured in semi-supine position after 5 minutes rest and included SBP, DBP. Baseline was defined as assessments performed on Day 1 (pre-dose). Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.
Time frame: Baseline and up to 11 days
Change From Baseline in Vital Sign Parameter Heart Rate for Part 1b
Single vital signs were measured in semi-supine position after 5 minutes rest and included heart rate. Baseline was defined as assessments performed on Day 1 (pre-dose). Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.
Time frame: Baseline and up to 11 days
Change From Baseline in ECG Parameter Heart Rate for Part 1b
A 12 lead ECG was measured in semi-supine position after 5 minutes rest using an ECG machine that automatically calculated the heart rate. Baseline was defined as assessments performed on Day 1 (pre-dose). Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.
Time frame: Baseline and up to 11 days
Change From Baseline in ECG Parameters PR Interval, QRS Duration, QT Interval, QTcB and QTcF for Part 1b
A 12 lead ECG was measured in semi-supine position after 5 minutes rest using an ECG machine that measured PR interval, QRS duration, QT interval, QTcB and QTcF for Part 1b. Baseline was defined as assessments performed on Day 1 (pre-dose). Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.
Time frame: Baseline and up to 11 days
Number of Participants With Abnormal Values on Urinalysis by Dipstick Analysis Part 1b
Urinalysis parameters assessed were urine ketones, urine glucose, urine occult blood, urine pH, urine specific gravity and urine protein. In this dipstick test, the level of ketones, glucose, occult blood, pH, specific gravity and protein in urine samples was recorded as negative trace, 1+, 3+, 5+, 6+, 7+ and 8+ (the plus sign increases with a higher level of ketones, occult blood, pH or specific gravity in the urine: 1+=slightly positive, 3+ to 5+=positive, 6+ and above=high positive). Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.
Time frame: Up to 11 days
Number of Participants With Non-serious AEs and SAEs for Part 2
AE is any untoward medical occurrence in a participant or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. An SAE is any untoward medical occurrence that, at any dose results in death, is life-threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, or is a congenital anomaly/birth defect or is medically significant.
Time frame: Up to 11 days
Change From Baseline in Clinical Chemistry Parameters Serum Glucose, Serum Calcium, Serum Carbon Dioxide, Serum Chloride, Serum Potassium, Serum Sodium and Serum Urea Nitrogen in Part 2
Blood samples were collected for the assessment of chemistry parameters namely serum glucose, serum calcium, serum carbon dioxide, serum chloride, serum potassium, serum sodium and serum urea nitrogen for Part 2. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose-visit value from the Baseline value. NA indicates participants crossed-over as follow-up visit occurred after Period 2.
Time frame: Baseline and up to 11 days
Change From Baseline in Clinical Chemistry Parameters Serum ALT, Serum AP, Serum AST and Serum CK in Part 2
Blood samples were collected for the assessment of chemistry parameters namely serum ALT, serum AP, serum AST and serum CK for Part 2. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. NA indicates participants crossed-over as follow-up visit occurred after Period 2.
Time frame: Baseline and up to 11 days
Change From Baseline in Clinical Chemistry Parameters Serum Albumin and Serum Protein for Part 2
Blood samples were collected for the assessment of chemistry parameters namely serum albumin and serum protein for Part 2. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose-visit value from the Baseline value. NA indicates participants crossed-over as follow-up visit occurred after Period 2.
Time frame: Baseline and up to 11 days
Change From Baseline in Clinical Chemistry Parameters Serum Bilirubin, Serum Creatinine and Serum Direct Bilirubin for Part 2
Blood samples were collected for the assessment of chemistry parameters namely serum bilirubin, serum creatinine and serum direct bilirubin for Part 2. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. NA indicates participants crossed-over as follow-up visit occurred after Period 2.
Time frame: Baseline and up to 11 days
Change From Baseline in Clinical Chemistry Parameter Serum Estradiol for Part 2
Blood samples were collected for the assessment of chemistry parameter namely serum estradiol for Part 2. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the indicated time point were analyzed. NA indicates standard deviation was not calculated as a single participant was analyzed.
Time frame: Baseline and up to 11 days
Change From Baseline in Hematology Parameters Blood Basophils, Blood Eosinophils, Blood Leukocytes, Blood Lymphocytes, Blood Monocytes, Blood Neutrophils and Blood Platelets for Part 2
Blood samples were collected for the assessment of hematology parameters namely blood basophils, blood eosinophils, blood leukocytes, blood lymphocytes, blood monocytes, blood neutrophils and blood platelets for Part 2. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. NA indicates participants crossed-over as follow-up visit occurred after Period 2.
Time frame: Baseline and up to 11 days
Change From Baseline in Hematology Parameters Ery. MCHC and Blood Hemoglobin for Part 2
Blood samples were collected for the assessment of hematology parameters namely blood Ery. MCHC and blood hemoglobin for Part 2. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. NA indicates participants crossed-over as follow-up visit occurred after Period 2.
Time frame: Baseline and up to 11 days
Change From Baseline in Hematology Parameter Blood Ery. MCH for Part 2
Blood samples were collected for the assessment of hematology parameter namely blood Ery. MCH for Part 2. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. NA indicates participants crossed-over as follow-up visit occurred after Period 2.
Time frame: Baseline and up to 11 days
Change From Baseline in Hematology Parameter Blood Ery. MCV for Part 2
Blood samples were collected for the assessment of hematology parameter namely blood Ery. MCV for Part 2. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. NA indicates participants crossed-over as follow-up visit occurred after Period 2.
Time frame: Baseline and up to 11 days
Change From Baseline in Hematology Parameter Blood Ery. for Part 2
Blood samples were collected for the assessment of hematology parameter namely blood Ery. for Part 2. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. NA indicates participants crossed-over as follow-up visit occurred after Period 2.
Time frame: Baseline and up to 11 days
Change From Baseline in Hematology Parameter Blood Hematocrit for Part 2
Blood samples were collected for the assessment of hematology parameter namely blood hematocrit for Part 2. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. NA indicates participants crossed-over as follow-up visit occurred after Period 2.
Time frame: Baseline and up to 11 days
Change From Baseline in Vital Sign Parameters SBP and DBP for Part 2
Single vital signs were measured in semi-supine position after 5 minutes rest and included SBP, DBP. Baseline was defined as assessments performed on Day 1 (pre-dose). Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. NA indicates participants crossed-over as follow-up visit occurred after Period 2.
Time frame: Baseline and up to 11 days
Change From Baseline in Vital Sign Parameter Heart Rate for Part 2
Single vital signs were measured in semi-supine position after 5 minutes rest and included heart rate. Baseline was defined as assessments performed on Day 1 (pre-dose). Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. NA indicates participants crossed-over as follow-up visit occurred after Period 2.
Time frame: Baseline and up to 11 days
Change From Baseline in ECG Parameter Heart Rate for Part 2
A 12 lead ECG was measured in semi-supine position after 5 minutes rest using an ECG machine that automatically calculated the heart rate. Baseline was defined as assessments performed on Day 1 (pre-dose). Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. NA indicates participants crossed-over as follow-up visit occurred after Period 2.
Time frame: Baseline and up to 11 days
Change From Baseline in ECG Parameters PR Interval, QRS Duration, QT Interval, QTcB and QTcF for Part 2
A 12 lead ECG was measured in semi-supine position after 5 minutes rest using an ECG machine that measured PR interval, QRS duration, QT interval, QTcB and QTcF for Part 2. Baseline was defined as assessments performed on Day 1 (pre-dose). Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. NA indicates participants crossed-over as follow-up visit occurred after Period 2.
Time frame: Baseline and up to 11 days
Number of Participants With Abnormal Values on Urinalysis by Dipstick Analysis Part 2
Urinalysis parameters assessed were urine ketones, urine glucose, urine occult blood, urine pH, urine specific gravity and urine protein. In this dipstick test, the level of ketones, glucose, occult blood, pH, specific gravity and protein in urine samples was recorded as negative trace, 1+, 3+, 4+ 5+, 6+, 7+ and 8+ (the plus sign increases with a higher level of ketones, occult blood, pH or specific gravity in the urine: 1+=slightly positive, 3+ to 5+=positive, 6+ and above=high positive). Urine samples were collected for the measurement of urinalysis parameters by dipstick method up-to follow-up (5 to 7 days post last dose) in Part 2. Only categories with significant values have been presented.
Time frame: Baseline and up to 11 days
Number of Participants With Non-serious AEs and SAEs for Part 3
AE is any untoward medical occurrence in a participant or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. An SAE is any untoward medical occurrence that, at any dose results in death, is life-threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, or is a congenital anomaly/birth defect or is medically significant.
Time frame: Up to 14 days
Change From Baseline in Clinical Chemistry Parameters Serum Glucose, Serum Calcium, Serum Carbon Dioxide, Serum Chloride, Serum Potassium, Serum Sodium and Serum Urea Nitrogen for Part 3
Blood samples were collected for the assessment of chemistry parameters namely serum glucose, serum calcium, serum carbon dioxide, serum chloride, serum potassium, serum sodium and serum urea nitrogen for Part 3. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles). Data points with null value for participants analyzed indicate data not collected for respective category and treatment arm.
Time frame: Baseline and up to 14 days
Change From Baseline in Clinical Chemistry Parameters Serum ALT, Serum AP, Serum AST and Serum CK for Part 3
Blood samples were collected for the assessment of chemistry parameters namely serum ALT, serum AP, serum AST and serum CK for Part 3. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles). Data points with null value for participants analyzed indicate data not collected for respective category and treatment arm.
Time frame: Baseline and up to 14 days
Change From Baseline in Clinical Chemistry Parameters Serum Albumin and Serum Protein for Part 3
Blood samples were collected for the assessment of chemistry parameters namely serum albumin and serum protein for Part 3. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles). Data points with null value for participants analyzed indicate data not collected for respective category and treatment arm.
Time frame: Baseline and up to 14 days
Change From Baseline in Clinical Chemistry Parameters Serum Bilirubin and Serum Creatinine for Part 3
Blood samples were collected for the assessment of chemistry parameters namely serum bilirubin and serum creatinine for Part 3. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles). Data points with null value for participants analyzed indicate data not collected for respective category and treatment arm
Time frame: Baseline and up to 14 days
Change From Baseline in Hematology Parameters Blood Basophils, Blood Eosinophils, Blood Leukocytes, Blood Lymphocytes, Blood Monocytes, Blood Neutrophils and Blood Platelets for Part 3
Blood samples were collected for the assessment of hematology parameters namely blood basophils, blood eosinophils, blood leukocytes, blood lymphocytes, blood monocytes, blood neutrophils and blood platelets for Part 3. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles). Data points with null value for participants analyzed indicate data not collected for respective category and treatment arm.
Time frame: Baseline and up to 14 days
Change From Baseline in Hematology Parameters Blood Ery. MCHC and Blood Hemoglobin for Part 3
Blood samples were collected for the assessment of hematology parameters namely blood Ery. MCHC and blood hemoglobin for Part 3. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles). Data points with null value for participants analyzed indicate data not collected for respective category and treatment arm.
Time frame: Baseline and up to 14 days
Change From Baseline in Hematology Parameter Blood Ery. MCH for Part 3
Blood samples were collected for the assessment of hematology parameter namely blood Ery. MCH for Part 1a. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles). Data points with null value for participants analyzed indicate data not collected for respective category and treatment arm.
Time frame: Baseline and up to 14 days
Change From Baseline in Hematology Parameter Blood Ery. Mean Corpuscular Volume (MCV) for Part 3
Blood samples were collected for the assessment of hematology parameter namely blood Ery. MCV for Part 3. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles). Data points with null value for participants analyzed indicate data not collected for respective category and treatment arm.
Time frame: Baseline and up to 14 days
Change From Baseline in Hematology Parameter Blood Ery. for Part 3
Blood samples were collected for the assessment of hematology parameter namely blood Ery. for Part 1a. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles). Data points with null value for participants analyzed indicate data not collected for respective category and treatment arm.
Time frame: Baseline and up to 14 days
Change From Baseline in Hematology Parameter Blood Hematocrit for Part 3
Blood samples were collected for the assessment of hematology parameter namely blood hematocrit for Part 3. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles). Data points with null value for participants analyzed indicate data not collected for respective category and treatment arm.
Time frame: Baseline and up to 14 days
Change From Baseline in Vital Sign Parameters SBP and DBP for Part 3
Single vital signs were measured in semi-supine position after 5 minutes rest and included SBP, DBP. Baseline was defined as assessments performed on Day 1 (pre-dose). Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles). Data points with null value for participants analyzed indicate data not collected for respective category and treatment arm.
Time frame: Baseline and up to 14 days
Change From Baseline in Vital Sign Parameter Heart Rate for Part 3
Single vital signs were measured in semi-supine position after 5 minutes rest and included heart rate. Baseline was defined as assessments performed on Day 1 (pre-dose). Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles). Data points with null value for participants analyzed indicate data not collected for respective category and treatment arm.
Time frame: Baseline and up to 14 days
Change From Baseline in ECG Parameter Heart Rate for Part 3
A 12 lead ECG was measured in semi-supine position after 5 minutes rest using an ECG machine that automatically calculated the heart rate. Baseline was defined as assessments performed on Day 1 (pre-dose). Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles). Data points with null value for participants analyzed indicate data not collected for respective category and treatment arm.
Time frame: Baseline and up to 14 days
Change From Baseline in ECG Parameters PR Interval, QRS Duration, QT Interval, QTcB and QTcF for Part 3
A 12 lead ECG was measured in semi-supine position after 5 minutes rest using an ECG machine that measured PR interval, QRS duration, QT interval, QTcB and QTcF for Part 3. Baseline was defined as assessments performed on Day 1 (pre-dose). Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles). Data points with null value for participants analyzed indicate data not collected for respective category and treatment arm.
Time frame: Baseline and up to 14 days
Number of Participants With Abnormal Values on Urinalysis by Dipstick Analysis Part 3
Urinalysis parameters assessed were urine ketones, urine glucose, urine occult blood, urine pH, urine specific gravity and urine protein. In this dipstick test, the level of ketones, glucose, occult blood, pH, specific gravity and protein in urine samples was recorded as negative trace, 1+, 3+, 5+, 6+, 7+ and 8+ (the plus sign increases with a higher level of ketones, occult blood, pH or specific gravity in the urine: 1+=slightly positive, 3+ to 5+=positive, 6+ and above=high positive). Urine samples were collected for the measurement of urinalysis parameters by dipstick method up-to follow-up (5 to 7 days post last dose) in Part 3. Only categories with significant values have been presented.
Time frame: Up to 14 days

Results

Posted Nov 14, 2018

Participant flow

This study was conducted across 2 centers in the United States from 04-August-2016 to 18-October-2017. Since the relative bio-availability of the roller compacted(RC) tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.

Part 1a, Period 1 (3 Days)

Participant flow — Part 1a, Period 1 (3 Days)
Milestone	Gepotidacin-R Then Gepotidacin RC Then Gepotidacin HSWG	Gepotidacin HSWG Then Gepotidacin- R Then Gepotidacin RC	Gepotidacin-RC Then Gepotidacin HSWG Then Gepotidacin-R
Started	9	9	8
Completed	9	9	8
Not completed	0	0	0

Part 1a, Washout Period 1 (3 Days)

Participant flow — Part 1a, Washout Period 1 (3 Days)
Milestone	Gepotidacin-R Then Gepotidacin RC Then Gepotidacin HSWG	Gepotidacin HSWG Then Gepotidacin- R Then Gepotidacin RC	Gepotidacin-RC Then Gepotidacin HSWG Then Gepotidacin-R
Started	9	9	8
Completed	9	9	8
Not completed	0	0	0

Part 1a, Period 2 (3 Days)

Participant flow — Part 1a, Period 2 (3 Days)
Milestone	Gepotidacin-R Then Gepotidacin RC Then Gepotidacin HSWG	Gepotidacin HSWG Then Gepotidacin- R Then Gepotidacin RC	Gepotidacin-RC Then Gepotidacin HSWG Then Gepotidacin-R
Started	9	9	8
Completed	9	9	8
Not completed	0	0	0

Part 1a, Washout Period 2 (3 Days)

Participant flow — Part 1a, Washout Period 2 (3 Days)
Milestone	Gepotidacin-R Then Gepotidacin RC Then Gepotidacin HSWG	Gepotidacin HSWG Then Gepotidacin- R Then Gepotidacin RC	Gepotidacin-RC Then Gepotidacin HSWG Then Gepotidacin-R
Started	9	9	8
Completed	9	9	8
Not completed	0	0	0

Part 1a, Period 3 (3 Days)

Participant flow — Part 1a, Period 3 (3 Days)
Milestone	Gepotidacin-R Then Gepotidacin RC Then Gepotidacin HSWG	Gepotidacin HSWG Then Gepotidacin- R Then Gepotidacin RC	Gepotidacin-RC Then Gepotidacin HSWG Then Gepotidacin-R
Started	9	9	8
Completed	9	9	8
Not completed	0	0	0

Part 2, Period 1 (3 Days)

Participant flow — Part 2, Period 1 (3 Days)
Milestone	Gepotidacin-R Then Gepotidacin RC Then Gepotidacin HSWG	Gepotidacin HSWG Then Gepotidacin- R Then Gepotidacin RC	Gepotidacin-RC Then Gepotidacin HSWG Then Gepotidacin-R	Gepotidacin 1500 mg RC Then Gepotidacin 3000 mg RC	Gepotidacin 1500 Then Gepotidacin 2250 Then Gepotidacin 3000	Placebo Then Placebo Then Placebo
Started	0	0	0	10	0	0
Completed	0	0	0	10	0	0
Not completed	0	0	0	0	0	0

Part 2, Washout Period 1 (3 Days)

Participant flow — Part 2, Washout Period 1 (3 Days)
Milestone	Gepotidacin-R Then Gepotidacin RC Then Gepotidacin HSWG	Gepotidacin HSWG Then Gepotidacin- R Then Gepotidacin RC	Gepotidacin-RC Then Gepotidacin HSWG Then Gepotidacin-R	Gepotidacin 1500 mg RC Then Gepotidacin 3000 mg RC	Gepotidacin 1500 Then Gepotidacin 2250 Then Gepotidacin 3000	Placebo Then Placebo Then Placebo
Started	0	0	0	10	0	0
Completed	0	0	0	10	0	0
Not completed	0	0	0	0	0	0

Part 2, Period 2 (3 Days)

Participant flow — Part 2, Period 2 (3 Days)
Milestone	Gepotidacin-R Then Gepotidacin RC Then Gepotidacin HSWG	Gepotidacin HSWG Then Gepotidacin- R Then Gepotidacin RC	Gepotidacin-RC Then Gepotidacin HSWG Then Gepotidacin-R	Gepotidacin 1500 mg RC Then Gepotidacin 3000 mg RC	Gepotidacin 1500 Then Gepotidacin 2250 Then Gepotidacin 3000	Placebo Then Placebo Then Placebo
Started	0	0	0	10	0	0
Completed	0	0	0	10	0	0
Not completed	0	0	0	0	0	0

Part 3, Period 1 (3 Days)

Participant flow — Part 3, Period 1 (3 Days)
Milestone	Gepotidacin 1500 Then Gepotidacin 2250 Then Gepotidacin 3000	Placebo Then Placebo Then Placebo
Started	10	2
Completed	10	2
Not completed	0	0

Part 3, Washout Period 1 (3 Days)

Participant flow — Part 3, Washout Period 1 (3 Days)
Milestone	Gepotidacin 1500 Then Gepotidacin 2250 Then Gepotidacin 3000	Placebo Then Placebo Then Placebo
Started	10	2
Completed	10	2
Not completed	0	0

Part 3, Period 2 (3 Days)

Participant flow — Part 3, Period 2 (3 Days)
Milestone	Gepotidacin 1500 Then Gepotidacin 2250 Then Gepotidacin 3000	Placebo Then Placebo Then Placebo
Started	10	2
Completed	10	2
Not completed	0	0

Part 3, Washout Period 2 (3 Days)

Participant flow — Part 3, Washout Period 2 (3 Days)
Milestone	Gepotidacin 1500 Then Gepotidacin 2250 Then Gepotidacin 3000	Placebo Then Placebo Then Placebo
Started	10	2
Completed	9	2
Not completed	1	0
Withdrew: Withdrawal by subject	1	0

Part 3, Period 3 (3 Days)

Participant flow — Part 3, Period 3 (3 Days)
Milestone	Gepotidacin 1500 Then Gepotidacin 2250 Then Gepotidacin 3000	Placebo Then Placebo Then Placebo
Started	9	2
Completed	9	2
Not completed	0	0

Outcome measures

PrimaryArea Under the Concentration-time Curve From Time 0 (Pre-dose) Extrapolated to Infinite Time (AUC [0-infinity]) of Plasma Gepotidacin for Part 1a

Blood samples for pharmacokinetic (PK) analysis of gepotidacin were collected at Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in Part 1a. For each sample, 3 milliliters (mL) of blood was drawn via an indwelling catheter and/or direct venipuncture into tubes containing ethylenediaminetetraacetate anticoagulant. PK parameters were determined from the plasma concentration-time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher. The PK Parameter Population consisted of all participants in the PK Population, for whom valid and evaluable PK parameters were derived. Statistics has been presented on geometric least square (LS) means.

Time frame:: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Reported as:: Geometric mean · hours*nanograms/milliliter

Area Under the Concentration-time Curve From Time 0 (Pre-dose) Extrapolated to Infinite Time (AUC [0-infinity]) of Plasma Gepotidacin for Part 1a
hours*nanograms/milliliter	Gepotidacin 1500 mg - R Capsules	Gepotidacin 1500 mg RC Tablets	Gepotidacin 1500 mg HSWG Tablets
Area Under the Concentration-time Curve From Time 0 (Pre-dose) Extrapolated to Infinite Time (AUC [0-infinity]) of Plasma Gepotidacin for Part 1a	16733 ± 25.7	17495 ± 23.0	18646 ± 24.0

Statistical analysis

Gepotidacin 1500 mg - R Capsules vs Gepotidacin 1500 mg RC Tablets · Ratio of geometric ls means: 1.0417 · 90% CI 0.9809 to 1.1063A mixed effects model with treatment, sequence, period as fixed effects and participant within sequence as random effect was performed on the natural log-transformed parameters AUC(0-inf).
Gepotidacin 1500 mg - R Capsules vs Gepotidacin 1500 mg HSWG Tablets · Ratio of geometric ls means: 1.1108 · 90% CI 1.0459 to 1.1797A mixed effects model with treatment, sequence, period as fixed effects and participant within sequence as random effect was performed on the natural log-transformed parameters AUC(0-inf).

PrimaryArea Under the Concentration-time Curve (AUC) From Time 0 (Pre-dose) to Time of the Last Quantifiable Concentration (AUC [0-t]) of Plasma Gepotidacin for Part 1a

Blood samples for PK analysis of gepotidacin were collected at Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in Part 1a. For each sample, 3 mL of blood was drawn via an indwelling catheter and/or direct venipuncture into tubes containing ethylenediaminetetraacetate anticoagulant. PK parameters were determined from the plasma concentration-time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher. Statistics has been presented on geometric LS means.

Time frame:: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Reported as:: Geometric mean · hours*nanograms/milliliters

Area Under the Concentration-time Curve (AUC) From Time 0 (Pre-dose) to Time of the Last Quantifiable Concentration (AUC [0-t]) of Plasma Gepotidacin for Part 1a
hours*nanograms/milliliters	Gepotidacin 1500 mg - R Capsules	Gepotidacin 1500 mg RC Tablets	Gepotidacin 1500 mg HSWG Tablets
Area Under the Concentration-time Curve (AUC) From Time 0 (Pre-dose) to Time of the Last Quantifiable Concentration (AUC [0-t]) of Plasma Gepotidacin for Part 1a	16409 ± 26.2	17125 ± 23.4	18317 ± 24.1

Statistical analysis

Gepotidacin 1500 mg - R Capsules vs Gepotidacin 1500 mg RC Tablets · Ratio of geometric ls means: 1.0408 · 90% CI 0.9792 to 1.1062A mixed effects model with treatment, sequence, period as fixed effects and participant within sequence as random effect was performed on the natural log-transformed parameters AUC(0-t).
Gepotidacin 1500 mg - R Capsules vs Gepotidacin 1500 mg HSWG Tablets · Ratio of geometric ls means: 1.1138 · 90% CI 1.0479 to 1.1838A mixed effects model with treatment, sequence, period as fixed effects and participant within sequence as random effect was performed on the natural log-transformed parameters AUC(0-t).

PrimaryRelative Bioavailability of Drug (Frel) of Plasma Gepotidacin for Part 1a

Blood samples for PK analysis of gepotidacin were collected at Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in Part 1a. For each sample, 3 mL of blood was drawn via an indwelling catheter and/or direct venipuncture into tubes containing ethylenediaminetetraacetate anticoagulant. PK parameters were determined from the plasma concentration-time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher. NA indicates data was not available as this was the reference capsule the Frel of each tablet type was being compared to.

Time frame:: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Reported as:: Geometric mean · Ratio of AUC (0-infinity)

Relative Bioavailability of Drug (Frel) of Plasma Gepotidacin for Part 1a
Ratio of AUC (0-infinity)	Gepotidacin 1500 mg - R Capsules	Gepotidacin 1500 mg RC Tablets	Gepotidacin 1500 mg HSWG Tablets
Relative Bioavailability of Drug (Frel) of Plasma Gepotidacin for Part 1a	NA ± NA	1.05 ± 22.3	1.11 ± 16.5

PrimaryMaximum Observed Concentration (Cmax) Determined Directly From the Concentration Time Data of Plasma Gepotidacin for Part 1a

Time frame:: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Reported as:: Geometric mean · nanograms/milliliter

Maximum Observed Concentration (Cmax) Determined Directly From the Concentration Time Data of Plasma Gepotidacin for Part 1a
nanograms/milliliter	Gepotidacin 1500 mg - R Capsules	Gepotidacin 1500 mg RC Tablets	Gepotidacin 1500 mg HSWG Tablets
Maximum Observed Concentration (Cmax) Determined Directly From the Concentration Time Data of Plasma Gepotidacin for Part 1a	4648 ± 43.8	4487 ± 43.6	5349 ± 46.8

Statistical analysis

Gepotidacin 1500 mg - R Capsules vs Gepotidacin 1500 mg RC Tablets · Ratio of geometric ls means: 0.9586 · 90% CI 0.8440 to 1.0888A mixed effects model with treatment, sequence, period as fixed effects and participant within sequence as random effect was performed on the natural log-transformed parameters Cmax.
Gepotidacin 1500 mg - R Capsules vs Gepotidacin 1500 mg HSWG Tablets · Ratio of geometric ls means: 1.1487 · 90% CI 1.0113 to 1.3047A mixed effects model with treatment, sequence, period as fixed effects and participant within sequence as random effect was performed on the natural log-transformed parameters Cmax.

PrimaryTime to First Occurrence of Cmax (Tmax) of Plasma Gepotidacin for Part 1a

Time frame:: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Reported as:: Median · hours

Time to First Occurrence of Cmax (Tmax) of Plasma Gepotidacin for Part 1a
hours	Gepotidacin 1500 mg - R Capsules	Gepotidacin 1500 mg RC Tablets	Gepotidacin 1500 mg HSWG Tablets
Time to First Occurrence of Cmax (Tmax) of Plasma Gepotidacin for Part 1a	1.50 (1.00 to 4.00)	1.50 (0.50 to 4.00)	1.00 (0.50 to 3.00)

Statistical analysis

Gepotidacin 1500 mg - R Capsules vs Gepotidacin 1500 mg RC Tablets · Wilcoxon signed-rank test. · p = 0.309 (The p-value is from Wilcoxon signed-rank test.) · Median difference (final values): -0.233 · 90% CI -0.267 to 0.000The median, median difference and 90% CI of the median difference are from Hodge-Lehmann estimate.
Gepotidacin 1500 mg - R Capsules vs Gepotidacin 1500 mg HSWG Tablets · Wilcoxon signed-rank test. · p = <0.001 (The p-value is from Wilcoxon signed-rank test.) · Median difference (final values): -0.492 · 90% CI -0.500 to -0.250The median, median difference and 90% CI of the median difference are from Hodge-Lehmann estimate.

PrimaryLag Time Before Observation of Drug Concentrations in Sampled Matrix (Tlag) of Plasma Gepotidacin for Part 1a

Time frame:: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Reported as:: Median · hours

Lag Time Before Observation of Drug Concentrations in Sampled Matrix (Tlag) of Plasma Gepotidacin for Part 1a
hours	Gepotidacin 1500 mg - R Capsules	Gepotidacin 1500 mg RC Tablets	Gepotidacin 1500 mg HSWG Tablets
Lag Time Before Observation of Drug Concentrations in Sampled Matrix (Tlag) of Plasma Gepotidacin for Part 1a	0.00 (0.00 to 0.00)	0.00 (0.00 to 0.50)	0.00 (0.00 to 0.50)

PrimaryTerminal Phase Half-life (t1/2) of Plasma Gepotidacin for Part 1a

Time frame:: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Reported as:: Geometric mean · hours

Terminal Phase Half-life (t1/2) of Plasma Gepotidacin for Part 1a
hours	Gepotidacin 1500 mg - R Capsules	Gepotidacin 1500 mg RC Tablets	Gepotidacin 1500 mg HSWG Tablets
Terminal Phase Half-life (t1/2) of Plasma Gepotidacin for Part 1a	10.29 ± 13.7	10.24 ± 15.2	10.24 ± 12.1

PrimaryTotal Unchanged Drug (Total Amount of Drug Excreted in Urine [Ae Total]) for Part 1a

PK urine samples were collected at 0 (predose), 0 to 2, 2 ot 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, 36 to 48 hours. PK parameters were determined from the urine concentration- time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher

Time frame:: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours
Reported as:: Geometric mean · milligrams

Total Unchanged Drug (Total Amount of Drug Excreted in Urine [Ae Total]) for Part 1a
milligrams	Gepotidacin 1500 mg - R Capsules	Gepotidacin 1500 mg RC Tablets	Gepotidacin 1500 mg HSWG Tablets
Total Unchanged Drug (Total Amount of Drug Excreted in Urine [Ae Total]) for Part 1a	274.925 ± 28.6	286.751 ± 22.2	284.510 ± 30.0

PrimaryPercentage of the Given Dose of Drug Excreted in Urine (fe%) of Plasma Gepotidacin for Part 1a

PK urine samples were collected at 0 (pre-dose), 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, 36 to 48 hours. PK parameters were determined from the urine concentration- time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher.

Time frame:: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours
Reported as:: Geometric mean · Percentage dose of drug excreted

Percentage of the Given Dose of Drug Excreted in Urine (fe%) of Plasma Gepotidacin for Part 1a
Percentage dose of drug excreted	Gepotidacin 1500 mg - R Capsules	Gepotidacin 1500 mg RC Tablets	Gepotidacin 1500 mg HSWG Tablets
Percentage of the Given Dose of Drug Excreted in Urine (fe%) of Plasma Gepotidacin for Part 1a	18.329 ± 28.6	19.116 ± 22.2	18.968 ± 30.0

PrimaryRenal Clearance of Drug in Urine (CLr) for Part 1a

Time frame:: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours
Reported as:: Geometric mean · liters/hour

Renal Clearance of Drug in Urine (CLr) for Part 1a
liters/hour	Gepotidacin 1500 mg - R Capsules	Gepotidacin 1500 mg RC Tablets	Gepotidacin 1500 mg HSWG Tablets
Renal Clearance of Drug in Urine (CLr) for Part 1a	16.761 ± 21.7	16.740 ± 19.6	15.532 ± 22.3

PrimaryAmount of Drug Excreted in Urine in a Time Intervals for Pre-dose, 0 to 2 Hours, 2 to 4 Hours, 4 to 6 Hours, 6 to 8 Hours, 8 to 12 Hours, 12 to 24 Hours, 24 to 36 Hours, and 36 to 48 Hours (Ae [t1-t2]) for Part 1a

Time frame:: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours
Reported as:: Geometric mean · milligrams

Amount of Drug Excreted in Urine in a Time Intervals for Pre-dose, 0 to 2 Hours, 2 to 4 Hours, 4 to 6 Hours, 6 to 8 Hours, 8 to 12 Hours, 12 to 24 Hours, 24 to 36 Hours, and 36 to 48 Hours (Ae [t1-t2]) for Part 1a
milligrams	Gepotidacin 1500 mg - R Capsules	Gepotidacin 1500 mg RC Tablets	Gepotidacin 1500 mg HSWG Tablets
Ae (0-2), n=26,25,26	65.817 ± 95.1	60.915 ± 102.9	85.584 ± 67.7
Ae (2-4),n=26,24,25	72.734 ± 67.3	77.650 ± 33.6	67.419 ± 72.0
Ae (4-6),n=25,25,26	36.019 ± 44.2	45.313 ± 61.1	39.361 ± 39.1
Ae (6-8),n=25,26,26	22.817 ± 37.4	26.061 ± 24.9	22.755 ± 28.7
Ae (8-12),n=26,26,26	21.515 ± 57.3	25.609 ± 27.7	16.590 ± 75.5
Ae (12-24),n=26,26,26	19.224 ± 60.4	22.536 ± 26.9	19.432 ± 32.9
Ae (24-36),n=26,26,26	8.145 ± 35.0	9.787 ± 27.8	8.185 ± 44.4
Ae (36-48),n=26,26,26	4.633 ± 31.4	4.517 ± 57.7	4.319 ± 41.0

PrimaryArea Under the Urine Concentration-time Curve Over Time 0 (Pre-dose) to 12 Hours (AUC [0-12]) for Part 1a

Time frame:: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours.
Reported as:: Geometric mean · micrograms*hours/milliliter

Area Under the Urine Concentration-time Curve Over Time 0 (Pre-dose) to 12 Hours (AUC [0-12]) for Part 1a
micrograms*hours/milliliter	Gepotidacin 1500 mg - R Capsules	Gepotidacin 1500 mg RC Tablets	Gepotidacin 1500 mg HSWG Tablets
Area Under the Urine Concentration-time Curve Over Time 0 (Pre-dose) to 12 Hours (AUC [0-12]) for Part 1a	1904 ± 82.7	1948 ± 61.2	2156 ± 74.8

PrimaryArea Under the Urine Concentration-time Curve Over Time 0 (Pre-dose) to 24 Hours (AUC [0-24]) After Dosing for Part 1a

Time frame:: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours
Reported as:: Geometric mean · micrograms*hours/milliliter

Area Under the Urine Concentration-time Curve Over Time 0 (Pre-dose) to 24 Hours (AUC [0-24]) After Dosing for Part 1a
micrograms*hours/milliliter	Gepotidacin 1500 mg - R Capsules	Gepotidacin 1500 mg RC Tablets	Gepotidacin 1500 mg HSWG Tablets
Area Under the Urine Concentration-time Curve Over Time 0 (Pre-dose) to 24 Hours (AUC [0-24]) After Dosing for Part 1a	2373 ± 74.9	2464 ± 56.3	2599 ± 69.0

PrimaryArea Under the Urine Concentration-time Curve Over Time 0 (Pre-dose) to 48 Hours (AUC [0-48]) After Dosing for Part 1a

Time frame:: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours
Reported as:: Geometric mean · micrograms*hours/milliliter

Area Under the Urine Concentration-time Curve Over Time 0 (Pre-dose) to 48 Hours (AUC [0-48]) After Dosing for Part 1a
micrograms*hours/milliliter	Gepotidacin 1500 mg - R Capsules	Gepotidacin 1500 mg RC Tablets	Gepotidacin 1500 mg HSWG Tablets
Area Under the Urine Concentration-time Curve Over Time 0 (Pre-dose) to 48 Hours (AUC [0-48]) After Dosing for Part 1a	2597 ± 69.5	2725 ± 54.4	2768 ± 64.0

PrimaryAUC (0-infinity) of Plasma Gepotidacin for Part 1b

Blood samples for PK analysis of gepotidacin was planned to be collected at Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in Part 1b. Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.

Time frame:: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period

No measurements were reported for this outcome.

PrimaryAUC (0-t) of Plasma Gepotidacin for Part 1b

Time frame:: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period

No measurements were reported for this outcome.

PrimaryCmax of Plasma Gepotidacin for Part 1b

Time frame:: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period

No measurements were reported for this outcome.

PrimaryTmax of Plasma Gepotidacin for Part 1b

Time frame:: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period

No measurements were reported for this outcome.

PrimaryTlag of Plasma Gepotidacin for Part 1b

Time frame:: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period

No measurements were reported for this outcome.

Primaryt1/2 of Plasma Gepotidacin for Part 1b

Time frame:: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period

No measurements were reported for this outcome.

PrimaryAUC (0-infinity) of Plasma Gepotidacin for Part 2

Blood samples for PK analysis of gepotidacin were collected at Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in Part 2. For each sample, 3 mL of blood was drawn via an indwelling catheter and/or direct venipuncture into tubes containing ethylenediaminetetraacetate anticoagulant. PK parameters were determined from the plasma concentration-time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher.

Time frame:: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Reported as:: Geometric mean · hours*nanograms/milliliter

AUC (0-infinity) of Plasma Gepotidacin for Part 2
hours*nanograms/milliliter	Gepotidacin RC 1500 mg Tablets	Gepotidacin RC 3000 mg Tablets
AUC (0-infinity) of Plasma Gepotidacin for Part 2	23137 ± 34.1	46537 ± 20.9

PrimaryAUC (0-t) of Plasma Gepotidacin for Part 2

Time frame:: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Reported as:: Geometric mean · hours*nanograms/milliliter

AUC (0-t) of Plasma Gepotidacin for Part 2
hours*nanograms/milliliter	Gepotidacin RC 1500 mg Tablets	Gepotidacin RC 3000 mg Tablets
AUC (0-t) of Plasma Gepotidacin for Part 2	22777 ± 34.4	46120 ± 21.1

PrimaryCmax of Plasma Gepotidacin for Part 2

Time frame:: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Reported as:: Geometric mean · nanograms/milliliter

Cmax of Plasma Gepotidacin for Part 2
nanograms/milliliter	Gepotidacin RC 1500 mg Tablets	Gepotidacin RC 3000 mg Tablets
Cmax of Plasma Gepotidacin for Part 2	9177 ± 94.8	15335 ± 28.6

PrimaryTlag of Plasma Gepotidacin for Part 2

Time frame:: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Reported as:: Median · hours

Tlag of Plasma Gepotidacin for Part 2
hours	Gepotidacin RC 1500 mg Tablets	Gepotidacin RC 3000 mg Tablets
Tlag of Plasma Gepotidacin for Part 2	0.00 (0.00 to 0.00)	0.00 (0.00 to 0.00)

PrimaryTmax of Plasma Gepotidacin for Part 2

Time frame:: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Reported as:: Median · hours

Tmax of Plasma Gepotidacin for Part 2
hours	Gepotidacin RC 1500 mg Tablets	Gepotidacin RC 3000 mg Tablets
Tmax of Plasma Gepotidacin for Part 2	1.00 (0.50 to 2.00)	0.56 (0.50 to 2.50)

Primaryt1/2 of Plasma Gepotidacin for Part 2

Time frame:: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Reported as:: Geometric mean · hours

t1/2 of Plasma Gepotidacin for Part 2
hours	Gepotidacin RC 1500 mg Tablets	Gepotidacin RC 3000 mg Tablets
t1/2 of Plasma Gepotidacin for Part 2	10.73 ± 10.9	8.81 ± 8.4

PrimaryTotal Unchanged Drug (Ae Total) for Part 2

Time frame:: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours.
Reported as:: Geometric mean · milligrams

Total Unchanged Drug (Ae Total) for Part 2
milligrams	Gepotidacin RC 1500 mg Tablets	Gepotidacin RC 3000 mg Tablets
Total Unchanged Drug (Ae Total) for Part 2	203.853 ± 38.8	546.263 ± 51.8

PrimaryAe (t1-t2) for Part 2

Time frame:: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours.
Reported as:: Geometric mean · milligrams

Ae (t1-t2) for Part 2
milligrams	Gepotidacin RC 1500 mg Tablets	Gepotidacin RC 3000 mg Tablets
Ae (0-2)	50.893 ± 289.7	115.793 ± 73.0
Ae (2-4)	47.995 ± 42.7	131.013 ± 92.1
Ae (4-6)	21.381 ± 47.5	97.651 ± 139.4
Ae (6-8)	11.759 ± 88.2	40.670 ± 36.2
Ae (8-12)	12.519 ± 104.6	29.474 ± 96.0
Ae (12-24)	9.810 ± 226.4	30.849 ± 83.9
Ae (24-36)	3.710 ± 111.0	9.754 ± 51.0
Ae (36-48)	2.743 ± 114.7	3.652 ± 136.1

PrimaryAUC (0-12) for Part 2

Time frame:: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours.
Reported as:: Geometric mean · micrograms*hours/milliliter

AUC (0-12) for Part 2
micrograms*hours/milliliter	Gepotidacin RC 1500 mg Tablets	Gepotidacin RC 3000 mg Tablets
AUC (0-12) for Part 2	1298 ± 110.8	4758 ± 64.6

PrimaryAUC (0-24) for Part 2

Time frame:: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours.
Reported as:: Geometric mean · micrograms*hours/milliliter

AUC (0-24) for Part 2
micrograms*hours/milliliter	Gepotidacin RC 1500 mg Tablets	Gepotidacin RC 3000 mg Tablets
AUC (0-24) for Part 2	1714 ± 88.8	5594 ± 61.9

PrimaryAUC (0-48) for Part 2

PK urine samples were collected at pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, 36 to 48 hours. PK parameters were determined from the urine concentration- time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher.

Time frame:: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours.
Reported as:: Geometric mean · micrograms*hours/milliliter

AUC (0-48) for Part 2
micrograms*hours/milliliter	Gepotidacin RC 1500 mg Tablets	Gepotidacin RC 3000 mg Tablets
AUC (0-48) for Part 2	1875 ± 83.6	5845 ± 61.1

Primaryfe% for Part 2

Time frame:: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours.
Reported as:: Geometric mean · Percentage dose of drug excreted

fe% for Part 2
Percentage dose of drug excreted	Gepotidacin RC 1500 mg Tablets	Gepotidacin RC 3000 mg Tablets
fe% for Part 2	13.591 ± 38.8	18.207 ± 51.8

PrimaryCLr for Part 2

PK urine samples were collected at pre-dose), 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, 36 to 48 hours. PK parameters were determined from the urine concentration- time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher.

Time frame:: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours.
Reported as:: Geometric mean · liters/hour

CLr for Part 2
liters/hour	Gepotidacin RC 1500 mg Tablets	Gepotidacin RC 3000 mg Tablets
CLr for Part 2	8.950 ± 41.5	11.834 ± 32.0

PrimaryAUC (0-infinity) of Plasma Gepotidacin for Part 3

Blood samples for PK analysis of gepotidacin were collected at Pre-dose, 0, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in Part 3. For each sample, 3 mL of blood was drawn via an indwelling catheter and/or direct venipuncture into tubes containing ethylenediaminetetraacetate anticoagulant. PK parameters were determined from the plasma concentration-time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher.

Time frame:: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Reported as:: Geometric mean · hours*nanograms/milliliter

AUC (0-infinity) of Plasma Gepotidacin for Part 3
hours*nanograms/milliliter	Gepotidacin RC 1500 mg Fed	Gepotidacin RC 2250 mg Fed	Gepotidacin RC 3000 mg Fed
AUC (0-infinity) of Plasma Gepotidacin for Part 3	22921 ± 19.9	37235 ± 17.2	50178 ± 21.9

PrimaryAUC (0-t) of Plasma Gepotidacin for Part 3

Blood samples for PK analysis of gepotidacin were collected at Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in Part 3. For each sample, 3 mL of blood was drawn via an indwelling catheter and/or direct venipuncture into tubes containing ethylenediaminetetraacetate anticoagulant. PK parameters were determined from the plasma concentration-time data and were calculated by standard non-compartmental analysis according to current working practices and using Phoenix WinNonlin Version 6.2.1 or higher.

Time frame:: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Reported as:: Geometric mean · hours*nanograms/milliliter

AUC (0-t) of Plasma Gepotidacin for Part 3
hours*nanograms/milliliter	Gepotidacin RC 1500 mg Fed	Gepotidacin RC 2250 mg Fed	Gepotidacin RC 3000 mg Fed
AUC (0-t) of Plasma Gepotidacin for Part 3	22709 ± 20.0	36938 ± 17.2	49789 ± 21.7

PrimaryCmax of Plasma Gepotidacin for Part 3

Time frame:: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Reported as:: Geometric mean · nanograms/milliliter

Cmax of Plasma Gepotidacin for Part 3
nanograms/milliliter	Gepotidacin RC 1500 mg Fed	Gepotidacin RC 2250 mg Fed	Gepotidacin RC 3000 mg Fed
Cmax of Plasma Gepotidacin for Part 3	6502 ± 27.7	9812 ± 21.1	12889 ± 21.1

PrimaryTmax of Plasma Gepotidacin for Part 3

Time frame:: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Reported as:: Median · hours

Tmax of Plasma Gepotidacin for Part 3
hours	Gepotidacin RC 1500 mg Fed	Gepotidacin RC 2250 mg Fed	Gepotidacin RC 3000 mg Fed
Tmax of Plasma Gepotidacin for Part 3	2.25 (1.00 to 4.00)	2.05 (1.50 to 4.00)	2.00 (1.00 to 3.00)

PrimaryTlag of Plasma Gepotidacin for Part 3

Time frame:: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Reported as:: Median · hours

Tlag of Plasma Gepotidacin for Part 3
hours	Gepotidacin RC 1500 mg Fed	Gepotidacin RC 2250 mg Fed	Gepotidacin RC 3000 mg Fed
Tlag of Plasma Gepotidacin for Part 3	0.50 (0.00 to 0.50)	0.00 (0.00 to 0.00)	0.00 (0.00 to 0.00)

Primaryt1/2 of Plasma Gepotidacin for Part 3

Time frame:: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 hours (Day 1), 24, 36 hours (Day 2) and 48 hours (Day 3) in each treatment period
Reported as:: Geometric mean · hours

t1/2 of Plasma Gepotidacin for Part 3
hours	Gepotidacin RC 1500 mg Fed	Gepotidacin RC 2250 mg Fed	Gepotidacin RC 3000 mg Fed
t1/2 of Plasma Gepotidacin for Part 3	9.23 ± 9.7	8.19 ± 7.2	7.93 ± 10.6

PrimaryTotal Unchanged Drug (Ae Total) for Part 3

Time frame:: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours
Reported as:: Geometric mean · milligrams

Total Unchanged Drug (Ae Total) for Part 3
milligrams	Gepotidacin RC 1500 mg Fed	Gepotidacin RC 2250 mg Fed	Gepotidacin RC 3000 mg Fed
Total Unchanged Drug (Ae Total) for Part 3	390.099 ± 34.3	613.635 ± 32.2	895.556 ± 27.8

PrimaryUrine Ae (t1-t2) for Part 3

Time frame:: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours.
Reported as:: Geometric mean · milligrams

Urine Ae (t1-t2) for Part 3
milligrams	Gepotidacin RC 1500 mg Fed	Gepotidacin RC 2250 mg Fed	Gepotidacin RC 3000 mg Fed
Ae (0-2), n=10,10,9	27.763 ± 536.8	54.827 ± 264.1	142.546 ± 96.7
Ae (2-4), n=10,10,9	132.423 ± 67.6	247.448 ± 45.5	333.805 ± 43.0
Ae (4-6),n=9,10,9	63.314 ± 61.4	113.386 ± 36.9	175.739 ± 36.5
Ae (6-8),n=10,10,9	54.631 ± 57.4	48.536 ± 93.3	70.582 ± 70.7
Ae (8-12),n=10,10,9	35.322 ± 37.1	48.906 ± 41.0	47.392 ± 85.2
Ae (12-24),n=10,10,9	14.201 ± 40.3	22.931 ± 65.9	36.214 ± 65.8
Ae (24-36),n=10,10,9	6.510 ± 49.0	8.463 ± 55.4	12.642 ± 50.7
Ae (36-48),n=10,10,8	3.265 ± 53.3	3.150 ± 71.5	5.641 ± 42.4

PrimaryUrine AUC (0-12) for Part 3

Time frame:: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours.
Reported as:: Geometric mean · micrograms*hours/milliliter

Urine AUC (0-12) for Part 3
micrograms*hours/milliliter	Gepotidacin RC 1500 mg Fed	Gepotidacin RC 2250 mg Fed	Gepotidacin RC 3000 mg Fed
Urine AUC (0-12) for Part 3	1573 ± 48.3	2812 ± 42.4	3517 ± 52.4

PrimaryUrine AUC (0-24) for Part 3

Time frame:: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours.
Reported as:: Geometric mean · micrograms*hours/milliliter

Urine AUC (0-24) for Part 3
micrograms*hours/milliliter	Gepotidacin RC 1500 mg Fed	Gepotidacin RC 2250 mg Fed	Gepotidacin RC 3000 mg Fed
Urine AUC (0-24) for Part 3	1879 ± 51.8	3301 ± 45.5	4197 ± 54.1

PrimaryUrine AUC (0-48) for Part 3

Time frame:: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours.
Reported as:: Geometric mean · micrograms*hours/milliliter

Urine AUC (0-48) for Part 3
micrograms*hours/milliliter	Gepotidacin RC 1500 mg Fed	Gepotidacin RC 2250 mg Fed	Gepotidacin RC 3000 mg Fed
Urine AUC (0-48) for Part 3	2024 ± 54.3	3455 ± 46.6	4390 ± 54.1

Primaryfe% for Part 3

Time frame:: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours.
Reported as:: Geometric mean · Percentage dose of drug excreted

fe% for Part 3
Percentage dose of drug excreted	Gepotidacin RC 1500 mg Fed	Gepotidacin RC 2250 mg Fed	Gepotidacin RC 3000 mg Fed
fe% for Part 3	26.008 ± 34.3	27.273 ± 32.2	29.858 ± 27.8

PrimaryCLr for Part 3

Time frame:: Pre-dose, 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12, 12 to 24, 24 to 36, and 36 to 48 hours.
Reported as:: Geometric mean · liters/hour

CLr for Part 3
liters/hour	Gepotidacin RC 1500 mg Fed	Gepotidacin RC 2250 mg Fed	Gepotidacin RC 3000 mg Fed
CLr for Part 3	17.196 ± 24.8	16.598 ± 26.5	17.969 ± 21.2

SecondaryNumber of Participants With Non-serious Adverse Events (AEs) and Serious Adverse Events (SAEs) for Part 1a

AE is any untoward medical occurrence in a participant or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. An SAE is any untoward medical occurrence that, at any dose results in death, is life-threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, or is a congenital anomaly/birth defect or is medically significant. Participants with non-serious AEs and SAEs has been reported. Safety Population comprised of all participants who received at least 1 dose of study medication and had at least 1 post dose safety assessment.

Time frame:: Up to 14 days
Reported as:: Count of participants · Participants

Number of Participants With Non-serious Adverse Events (AEs) and Serious Adverse Events (SAEs) for Part 1a
Participants	Gepotidacin 1500 mg - R Capsules	Gepotidacin 1500 mg RC Tablets	Gepotidacin 1500 mg HSWG Tablets
Non serious AE	8	5	9
SAE	0	0	0

SecondaryChange From Baseline in Clinical Chemistry Parameters Serum Glucose, Serum Calcium, Serum Carbon Dioxide, Serum Chloride, Serum Potassium, Serum Sodium and Serum Urea Nitrogen for Part 1a

Blood samples were collected for the assessment of chemistry parameters namely serum glucose, serum calcium, serum carbon dioxide, serum chloride, serum potassium, serum sodium and serum urea nitrogen for Part 1a. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles).

Time frame:: Baseline and up to 14 days
Reported as:: Mean · millimoles/liter

Change From Baseline in Clinical Chemistry Parameters Serum Glucose, Serum Calcium, Serum Carbon Dioxide, Serum Chloride, Serum Potassium, Serum Sodium and Serum Urea Nitrogen for Part 1a
millimoles/liter	Gepotidacin 1500 mg - R Capsules	Gepotidacin 1500 mg RC Tablets	Gepotidacin 1500 mg HSWG Tablets
Serum glucose, Day 3 (48 hour), n=26, 26, 26	0.010 ± 0.2837	0.049 ± 0.3253	0.094 ± 0.2699
Serum glucose, Follow-up, n=8, 9, 9	0.099 ± 0.3911	0.304 ± 0.5180	0.381 ± 0.3850
Serum calcium, Day 3 (48 hour), n=26, 26, 26	0.050 ± 0.0968	0.054 ± 0.0802	0.051 ± 0.0700
Serum calcium, Follow-up, n=8, 9, 9	0.003 ± 0.0861	-0.019 ± 0.0692	-0.046 ± 0.0865
Serum carbon dioxide, Day 3 (48 hour),n=26, 26, 26	-0.2 ± 1.39	-0.2 ± 1.22	0.0 ± 1.22
Serum carbon dioxide, Follow-up, n=8, 9, 9	-1.4 ± 1.19	-1.7 ± 1.58	-1.6 ± 1.33
Serum chloride, Day 3 (48 hour),n=26, 26, 26	-1.0 ± 1.78	-1.1 ± 2.00	-1.0 ± 2.27
Serum chloride, Follow-up, n=8, 9, 9	1.3 ± 1.75	0.7 ± 1.32	1.6 ± 2.24
Serum potassium, Day 3 (48 hour), n=26,26,26	-0.06 ± 0.297	-0.04 ± 0.270	-0.06 ± 0.298
Serum potassium, Follow-up, n=8,9,9,	-0.18 ± 0.306	-0.09 ± 0.237	-0.24 ± 0.371
Serum sodium, Day 3 (48 hour), n=26,26,26	-0.3 ± 1.70	-0.7 ± 1.67	-0.5 ± 1.98
Serum sodium, Follow-up, n=8,9,9	-1.0 ± 2.39	-1.3 ± 2.35	-0.6 ± 1.74
Serum urea nitrogen, Day 3 (48 hour), n=26,26,26	-0.250 ± 1.0929	-0.307 ± 1.0021	-0.332 ± 1.0598
Serum urea nitrogen, Follow-up, n=8,9,9	-0.043 ± 1.4732	-0.354 ± 1.0294	-0.223 ± 1.0126

SecondaryChange From Baseline in Clinical Chemistry Parameters Serum Alanine Aminotransferase (ALT), Serum Alkaline Phosphatase (AP), Serum Aspartate Aminotransferase (AST) and Serum Creatinine Kinase (CK) for Part 1a

Blood samples were collected for the assessment of chemistry parameters namely serum ALT, serum AP, serum AST and serum CK for Part 1a. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose-visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles).

Time frame:: Baseline and up to 14 days
Reported as:: Mean · International units/liter

Change From Baseline in Clinical Chemistry Parameters Serum Alanine Aminotransferase (ALT), Serum Alkaline Phosphatase (AP), Serum Aspartate Aminotransferase (AST) and Serum Creatinine Kinase (CK) for Part 1a
International units/liter	Gepotidacin 1500 mg - R Capsules	Gepotidacin 1500 mg RC Tablets	Gepotidacin 1500 mg HSWG Tablets
Serum ALT, Day 3 (48 hour), n=26, 26, 26	-1.1 ± 7.04	-0.1 ± 7.30	-0.3 ± 6.54
Serum ALT, Follow-up, n=8, 9, 9	-3.0 ± 10.76	0.1 ± 11.57	5.4 ± 5.05
Serum AP, Day 3 (48 hour), n=26, 26, 26	7.7 ± 5.69	8.3 ± 5.40	9.0 ± 6.25
Serum AP, Follow-up, n=8, 9, 9	2.6 ± 6.07	7.2 ± 7.71	7.4 ± 4.75
Serum AST, Day 3 (48 hour),n=26, 26, 26	-0.6 ± 4.11	-0.2 ± 4.01	-0.5 ± 3.99
Serum AST, Follow-up, n=8, 9, 9	-0.1 ± 4.94	1.7 ± 7.18	3.1 ± 4.40
Serum CK, Day 3 (48 hour),n=26, 26, 26	-28.7 ± 43.65	-26.4 ± 47.32	-30.2 ± 41.96
Serum CK, Follow-up, n=8, 9, 9	8.0 ± 42.32	29.0 ± 107.27	13.2 ± 26.16

SecondaryChange From Baseline in Clinical Chemistry Parameters Serum Albumin and Serum Protein for Part 1a

Blood samples were collected for the assessment of chemistry parameters namely serum albumin and serum protein for Part 1a. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose-visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles).

Time frame:: Baseline and up to 14 days
Reported as:: Mean · grams/liter

Change From Baseline in Clinical Chemistry Parameters Serum Albumin and Serum Protein for Part 1a
grams/liter	Gepotidacin 1500 mg - R Capsules	Gepotidacin 1500 mg RC Tablets	Gepotidacin 1500 mg HSWG Tablets
Serum albumin, Day 3 (48 hour), n=26, 26, 26	1.5 ± 2.27	1.8 ± 1.98	1.8 ± 2.36
Serum albumin, Follow-up, n=8, 9, 9	-0.3 ± 2.55	-0.7 ± 1.87	-0.6 ± 2.46
Serum protein, Day 3 (48 hour), n=26, 26, 26	1.8 ± 4.68	1.9 ± 3.10	2.1 ± 3.98
Serum protein, Follow-up, n=8, 9, 9	-2.1 ± 4.29	-2.6 ± 3.32	-2.1 ± 4.43

SecondaryChange From Baseline in Clinical Chemistry Parameters Serum Bilirubin, Serum Creatinine and Serum Direct Bilirubin for Part 1a

Blood samples were collected for the assessment of chemistry parameters namely serum bilirubin, serum creatinine and serum direct bilirubin Part 1a. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles).

Time frame:: Baseline and up to 14 days
Reported as:: Mean · micromoles/liter

Change From Baseline in Clinical Chemistry Parameters Serum Bilirubin, Serum Creatinine and Serum Direct Bilirubin for Part 1a
micromoles/liter	Gepotidacin 1500 mg - R Capsules	Gepotidacin 1500 mg RC Tablets	Gepotidacin 1500 mg HSWG Tablets
Serum bilirubin, Day 3 (48 hour), n=26, 26, 26	2.08 ± 2.746	1.59 ± 3.511	1.98 ± 3.018
Serum bilirubin, Follow-up, n=8, 9, 9	2.34 ± 3.608	-1.08 ± 1.943	-1.19 ± 4.431
Serum creatinine, Day 3 (48 hour), n=26, 26, 26	1.49 ± 5.758	2.14 ± 6.793	2.31 ± 6.564
Serum creatinine, Follow-up, n=8, 9, 9	4.86 ± 5.349	2.28 ± 9.930	3.93 ± 5.859
Serum direct bilirubin, Day 3 (48 hour),n=26,26,26	0.25 ± 0.422	0.17 ± 0.528	0.18 ± 0.482
Serum direct bilirubin, Follow-up, n=8, 9, 9	0.46 ± 0.707	-0.14 ± 0.384	-0.09 ± 0.677

SecondaryChange From Baseline in Hematology Parameters Blood Basophils, Blood Eosinophils, Blood Leukocytes, Blood Lymphocytes, Blood Monocytes, Blood Neutrophils and Blood Platelets for Part 1a

Blood samples were collected for the assessment of hematology parameters namely blood basophils, blood eosinophils, blood leukocytes, blood lymphocytes, blood monocytes, blood neutrophils and blood platelets for Part 1a. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles).

Time frame:: Baseline and up to 14 days
Reported as:: Mean · 10^9 cells/liter

Change From Baseline in Hematology Parameters Blood Basophils, Blood Eosinophils, Blood Leukocytes, Blood Lymphocytes, Blood Monocytes, Blood Neutrophils and Blood Platelets for Part 1a
10^9 cells/liter	Gepotidacin 1500 mg - R Capsules	Gepotidacin 1500 mg RC Tablets	Gepotidacin 1500 mg HSWG Tablets
Blood basophils, Day 3 (48 hour), n=26, 26, 26	0.004 ± 0.0344	0.004 ± 0.0344	-0.004 ± 0.0344
Blood basophils, Follow-up, n=8, 9, 9	0.000 ± 0.0000	0.000 ± 0.0500	0.000 ± 0.0000
Blood eosinophils, Day 3 (48 hour), n=26, 26, 26	0.008 ± 0.0688	0.008 ± 0.0935	0.004 ± 0.0958
Blood eosinophils, Follow-up, n=8, 9, 9	0.025 ± 0.0463	0.044 ± 0.0527	0.033 ± 0.1323
Blood leukocytes, Day 3 (48 hour),n=26, 26, 26	-0.388 ± 0.7464	-0.300 ± 0.6957	-0.400 ± 0.6675
Blood leukocytes, Follow-up, n=8, 9, 9	-0.175 ± 0.4862	0.000 ± 1.2728	-0.400 ± 0.3841
Blood lymphocytes, Day 3 (48 hour),n=26, 26, 26	-0.050 ± 0.2832	0.015 ± 0.3081	-0.008 ± 0.4127
Blood lymphocytes, Follow-up, n=8, 9, 9	0.025 ± 0.2866	-0.100 ± 0.4444	0.011 ± 0.2147
Blood monocytes, Day 3 (48 hour),n=26, 26, 26	-0.065 ± 0.0977	-0.069 ± 0.0970	-0.096 ± 0.0871
Blood monocytes, Follow-up, n=8, 9, 9	0.050 ± 0.0926	0.033 ± 0.1323	-0.056 ± 0.0527
Blood neutrophils, Day 3 (48 hour),n=26, 26, 26	-0.254 ± 0.5907	-0.238 ± 0.5845	-0.288 ± 0.4702
Blood neutrophils, Follow-up, n=8, 9, 9	-0.213 ± 0.5330	0.089 ± 0.7976	-0.356 ± 0.4187
Blood platelets, Day 3 (48 hour),n=26, 26, 26	11.5 ± 14.76	17.4 ± 16.43	14.5 ± 17.85
Blood platelets, Follow-up, n=8, 9, 9	3.8 ± 17.90	1.8 ± 17.89	9.8 ± 26.48

SecondaryChange From Baseline in Hematology Parameters Blood Erythrocyte (Ery.) Mean Corpuscular Hemoglobin Concentration (MCHC) and Blood Hemoglobin for Part 1a

Blood samples were collected for the assessment of hematology parameters namely blood Ery. MCHC and blood hemoglobin for Part 1a. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose-visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles).

Time frame:: Baseline and up to 14 days
Reported as:: Mean · grams/liter

Change From Baseline in Hematology Parameters Blood Erythrocyte (Ery.) Mean Corpuscular Hemoglobin Concentration (MCHC) and Blood Hemoglobin for Part 1a
grams/liter	Gepotidacin 1500 mg - R Capsules	Gepotidacin 1500 mg RC Tablets	Gepotidacin 1500 mg HSWG Tablets
Blood Ery. MCHC, Day 3 (48 hour), n=26, 26, 26	0.4 ± 4.78	0.9 ± 4.27	0.4 ± 5.56
Blood Ery. MCHC, Follow-up, n=8, 9, 9	2.5 ± 6.63	4.1 ± 3.33	3.0 ± 5.52
Blood hemoglobin, Day 3 (48 hour), n=26, 26, 26	8.0 ± 7.21	8.5 ± 6.59	8.4 ± 7.26
Blood hemoglobin, Follow-up, n=8, 9, 9	-3.8 ± 6.45	-4.4 ± 6.29	-2.3 ± 8.03

SecondaryChange From Baseline in Hematology Parameter Blood Ery. Mean Corpuscular Hemoglobin (MCH) for Part 1a

Blood samples were collected for the assessment of hematology parameter namely blood Ery. MCH for Part 1a. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles).

Time frame:: Baseline and up to 14 days
Reported as:: Mean · picograms

Change From Baseline in Hematology Parameter Blood Ery. Mean Corpuscular Hemoglobin (MCH) for Part 1a
picograms	Gepotidacin 1500 mg - R Capsules	Gepotidacin 1500 mg RC Tablets	Gepotidacin 1500 mg HSWG Tablets
Blood Ery.MCH, Day 3 (48 hour), n=26, 26, 26	-0.03 ± 0.360	0.00 ± 0.280	-0.02 ± 0.400
Blood Ery. MCH, Follow-up, n=8, 9, 9	-0.03 ± 0.512	0.14 ± 0.270	0.04 ± 0.317

SecondaryChange From Baseline in Hematology Parameter Blood Ery. Mean Corpuscular Volume (MCV) for Part 1a

Blood samples were collected for the assessment of hematology parameter namely blood Ery. MCV for Part 1a. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles).

Time frame:: Baseline and up to 14 days
Reported as:: Mean · femtoliters

Change From Baseline in Hematology Parameter Blood Ery. Mean Corpuscular Volume (MCV) for Part 1a
femtoliters	Gepotidacin 1500 mg - R Capsules	Gepotidacin 1500 mg RC Tablets	Gepotidacin 1500 mg HSWG Tablets
Blood Ery. MCV, Day 3 (48 hour), n=26, 26, 26	-0.21 ± 0.471	-0.26 ± 0.568	-0.23 ± 0.586
Blood Ery. MCV, Follow-up, n=8, 9, 9	-0.73 ± 0.618	-0.58 ± 0.549	-0.72 ± 0.800

SecondaryChange From Baseline in Hematology Parameter Blood Ery. for Part 1a

Blood samples were collected for the assessment of hematology parameter namely blood Ery. for Part 1a. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles).

Time frame:: Baseline and up to 14 days
Reported as:: Mean · 10^12 cells/liter

Change From Baseline in Hematology Parameter Blood Ery. for Part 1a
10^12 cells/liter	Gepotidacin 1500 mg - R Capsules	Gepotidacin 1500 mg RC Tablets	Gepotidacin 1500 mg HSWG Tablets
Blood Ery. , Day 3 (48 hour), n=26, 26, 26	0.279 ± 0.2597	0.293 ± 0.2450	0.296 ± 0.2538
Blood Ery. , Follow-up, n=8, 9, 9	-0.130 ± 0.2045	-0.190 ± 0.2258	-0.101 ± 0.2538

SecondaryChange From Baseline in Hematology Parameter Blood Hematocrit for Part 1a

Blood samples were collected for the assessment of hematology parameter namely blood hematocrit for Part 1a. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles).

Time frame:: Baseline and up to 14 days
Reported as:: Mean · Percentage of red blood cells in blood

Change From Baseline in Hematology Parameter Blood Hematocrit for Part 1a
Percentage of red blood cells in blood	Gepotidacin 1500 mg - R Capsules	Gepotidacin 1500 mg RC Tablets	Gepotidacin 1500 mg HSWG Tablets
Blood hematocrit , Day 3 (48 hour), n=26, 26, 26	2.32 ± 2.212	2.43 ± 2.110	2.48 ± 2.200
Blood hematocrit, Follow-up, n=8, 9, 9	-1.50 ± 1.628	-1.87 ± 1.781	-1.20 ± 2.029

SecondaryChange From Baseline in Vital Sign Parameters Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP) for Part 1a

Single vital signs were measured in semi-supine position after 5 minutes rest and included SBP, DBP. Baseline was defined as assessments performed on Day 1 (pre-dose). Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles).

Time frame:: Baseline and up to 14 days
Reported as:: Mean · millimeters of mercury

Change From Baseline in Vital Sign Parameters Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP) for Part 1a
millimeters of mercury	Gepotidacin 1500 mg - R Capsules	Gepotidacin 1500 mg RC Tablets	Gepotidacin 1500 mg HSWG Tablets
SBP, Day 1 (2 hours), n=26, 26, 26,	1.8 ± 6.88	-1.3 ± 7.24	1.1 ± 5.25
SBP, Day 2 (24 hours), n=26, 26, 26	0.1 ± 6.82	-2.8 ± 10.21	-1.8 ± 5.31
SBP, Day 3 (48 hours), n=26, 26, 26	5.3 ± 7.93	-1.3 ± 7.12	-0.2 ± 6.46
SBP, Follow-up, n=8,9,9	18.0 ± 11.28	9.4 ± 6.09	6.9 ± 7.83
DBP, Day 1 (2 hours), n=26, 26, 26,	3.2 ± 7.04	1.0 ± 5.59	2.2 ± 6.34
DBP, Day 2 (24 hours), n=26, 26, 26	2.3 ± 8.11	-0.4 ± 7.41	0.0 ± 6.87
DBP, Day 3 (48 hours), n=26, 26, 26	2.2 ± 7.65	2.8 ± 6.29	1.0 ± 7.19
DBP, Follow-up, n=8,9,9	8.3 ± 7.36	6.4 ± 5.73	7.4 ± 4.85

SecondaryChange From Baseline in Vital Sign Parameter Heart Rate for Part 1a

Single vital signs were measured in semi-supine position after 5 minutes rest and included heart rate. Baseline was defined as assessments performed on Day 1 (pre-dose). Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles).

Time frame:: Baseline and up to 14 days
Reported as:: Mean · beats/minute

Change From Baseline in Vital Sign Parameter Heart Rate for Part 1a
beats/minute	Gepotidacin 1500 mg - R Capsules	Gepotidacin 1500 mg RC Tablets	Gepotidacin 1500 mg HSWG Tablets
Heart rate, Day 1 (2 hours), n=26, 26, 26,	-0.7 ± 7.59	0.0 ± 4.61	1.7 ± 3.61
Heart rate, Day 2 (24 hours), n=26, 26, 26	-0.7 ± 7.11	0.6 ± 5.87	1.7 ± 3.82
Heart rate, Day 3 (48 hours), n=26, 26, 26	-0.2 ± 8.18	-0.2 ± 6.20	3.2 ± 5.46
Heart rate, Follow-up, n=8,9,9	-0.1 ± 3.04	0.2 ± 7.56	5.7 ± 5.15

SecondaryChange From Baseline in Electrocardiogram (ECG) Parameter Heart Rate for Part 1a

A 12 lead ECG was measured in semi-supine position after 5 minutes rest using an ECG machine that automatically calculated the heart rate. Baseline was defined as assessments performed on Day 1 (pre-dose). Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles).

Time frame:: Baseline and up to 14 days
Reported as:: Mean · beats per minute

Change From Baseline in Electrocardiogram (ECG) Parameter Heart Rate for Part 1a
beats per minute	Gepotidacin 1500 mg - R Capsules	Gepotidacin 1500 mg RC Tablets	Gepotidacin 1500 mg HSWG Tablets
ECG Heart rate, Day 1 (2 hours), n=26, 26, 26,	-1.1 ± 6.33	-1.0 ± 6.05	0.4 ± 3.60
ECG Heart rate, Day 2 (24 hours), n=26, 26, 26	0.2 ± 5.85	-0.4 ± 8.02	0.3 ± 3.96
ECG Heart rate, Day 3 (48 hours), n=26, 26, 26	0.0 ± 6.39	-0.6 ± 7.00	1.0 ± 4.04
ECG Heart rate, Follow-up, n=8,9,9	-1.0 ± 4.11	0.7 ± 8.82	3.6 ± 6.56

SecondaryChange From Baseline in ECG Parameters PR Interval, QRS Duration, QT Interval, Corrected QT Interval Using Bazett's Formula (QTcB) and Corrected QT Interval Using Fridericia's Formula (QTcF) for Part 1a

A 12 lead ECG was measured in semi-supine position after 5 minutes rest using an ECG machine that measured PR interval, QRS duration, QT interval, QTcB and QTcF for Part 1a. Baseline was defined as assessments performed on Day 1 (pre-dose). Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles).

Time frame:: Baseline and up to 14 days
Reported as:: Mean · milliseconds

Change From Baseline in ECG Parameters PR Interval, QRS Duration, QT Interval, Corrected QT Interval Using Bazett's Formula (QTcB) and Corrected QT Interval Using Fridericia's Formula (QTcF) for Part 1a
milliseconds	Gepotidacin 1500 mg - R Capsules	Gepotidacin 1500 mg RC Tablets	Gepotidacin 1500 mg HSWG Tablets
PR interval, Day 1 (2 hours), n=26, 26, 26	-2.5 ± 12.28	-3.2 ± 11.79	-3.8 ± 6.01
PR interval, Day 2 (24 hours), n=26, 26, 26	1.7 ± 13.77	-0.1 ± 8.80	-0.5 ± 9.20
PR interval,, Day 3 (48 hours), n=26, 26, 26	1.2 ± 9.64	-0.3 ± 7.74	2.0 ± 12.51
PR interval, Follow-up, n=8,9,9	4.0 ± 14.89	-3.1 ± 9.98	-9.2 ± 7.41
QRS duration, Day 1 (2 hours), n=26, 26, 26,	1.3 ± 4.65	0.1 ± 5.61	-0.4 ± 4.64
QRS duration, Day 2 (24 hours), n=26, 26, 26	0.3 ± 3.64	-1.0 ± 5.62	-0.5 ± 5.07
QRS duration, Day 3 (48 hours), n=26, 26, 26	0.1 ± 4.47	-0.1 ± 5.42	-1.8 ± 5.28
QRS duration, Follow-up, n=8,9,9	-0.4 ± 7.21	2.1 ± 8.31	0.9 ± 2.26
QT interval Day 1 (2 hours), n=26, 26, 26,	9.6 ± 14.42	6.4 ± 12.07	8.8 ± 11.28
QT interval, Day 2 (24 hours), n=26, 26, 26	1.5 ± 11.55	2.1 ± 15.22	2.4 ± 8.40
QT interval, Day 3 (48 hours), n=26, 26, 26	1.8 ± 12.95	-0.5 ± 14.55	-0.7 ± 10.80
QT interval, Follow-up, n=8,9,9	17.5 ± 22.99	5.2 ± 29.79	-3.6 ± 17.81
QTcB interval, Day 1 (2 hours), n=26, 26, 26,	6.6 ± 14.07	4.3 ± 14.96	10.3 ± 11.26
QTcB, Day 2 (24 hours), n=26, 26, 26	1.8 ± 12.63	1.7 ± 13.74	3.8 ± 9.86
QTcB, Day 3 (48 hours), n=26, 26, 26	2.0 ± 12.56	-1.6 ± 13.26	2.9 ± 9.76
QTcB, Follow-up, n=8,9,9	13.9 ± 19.95	2.9 ± 19.62	6.0 ± 11.51
QTcF interval, Day 1 (2 hours), n=26, 26, 26,	7.5 ± 10.56	4.8 ± 11.05	10.0 ± 9.57
QTcF, Day 2 (24 hours), n=26, 26, 26	1.7 ± 9.11	2.0 ± 9.73	3.4 ± 7.21
QTcF, Day 3 (48 hours), n=26, 26, 26	2.0 ± 8.30	-1.3 ± 9.93	1.8 ± 8.20
QTcF, Follow-up, n=8,9,9	15.4 ± 20.16	4.9 ± 18.84	4.6 ± 7.65

SecondaryNumber of Participants With Abnormal Values on Urinalysis by Dipstick Analysis Part 1a

Urinalysis parameters assessed were urine ketones, urine glucose, urine occult blood, urine pH, urine specific gravity and urine protein. In this dipstick test, the level of ketones, glucose, occult blood, pH, specific gravity and protein in urine samples was recorded as negative trace, 1+, 3+, 5+, 6+, 7+ and 8+ (the plus sign increases with a higher level of ketones, occult blood, pH or specific gravity in the urine: 1+=slightly positive, 3+ to 5+=positive, 6+ and above=high positive). Urine samples were collected for the measurement of urinalysis parameters by dipstick method up-to follow-up (5 to 7 days post last dose) in Part 1a. Only categories with significant values have been presented.

Time frame:: Up to 14 days
Reported as:: Count of participants · Participants

Number of Participants With Abnormal Values on Urinalysis by Dipstick Analysis Part 1a
Participants	Gepotidacin 1500 mg - R Capsules	Gepotidacin 1500 mg RC Tablets	Gepotidacin 1500 mg HSWG Tablets
Urine Ketones, Day 3 (48 hours), 1+	1	0	0
Urine pH, Day 3 (48 hours), 5+	4	4	4
Urine pH, Day 3 (48 hours), 6+	18	16	14
Urine pH, Day 3 (48 hours), 7+	3	6	8
Urine pH, Day 3 (48 hours), 8+	1	0	0
Urine pH, Follow-up, 5+	2	4	3
Urine pH, Follow-up, 6+	5	5	4
Urine pH, Follow-up, 7+	1	0	2
Urine Specific gravity, Day 3 (48 hours), 1+	26	26	26
Urine Specific gravity, Follow-up, 1+	8	9	9

SecondaryNumber of Participants With AEs and SAEs for Part 1b

AE is any untoward medical occurrence in a participant or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. An SAE is any untoward medical occurrence that, at any dose results in death, is life-threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, or is a congenital anomaly/birth defect or is medically significant. Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.

Time frame:: Up to 11 days

No measurements were reported for this outcome.

SecondaryChange From Baseline in Clinical Chemistry Parameters Serum Glucose, Serum Calcium, Serum Carbon Dioxide, Serum Chloride, Serum Potassium, Serum Sodium and Serum Urea Nitrogen for Part 1b

Blood samples were collected for the assessment of chemistry parameters namely serum glucose, serum calcium, serum carbon dioxide, serum chloride, serum potassium, serum sodium and serum urea nitrogen for Part 1b. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose-visit value from the Baseline value. Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.

Time frame:: Baseline and up to 11 days

No measurements were reported for this outcome.

SecondaryChange From Baseline in Clinical Chemistry Parameters Serum ALT, Serum AP, Serum AST and Serum CK for Part 1b

Blood samples were collected for the assessment of chemistry parameters namely serum ALT, serum AP, serum AST and serum CK for Part 1b. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.

Time frame:: Baseline and up to 11 days

No measurements were reported for this outcome.

SecondaryChange From Baseline in Clinical Chemistry Parameters Serum Albumin and Serum Protein for Part 1b

Blood samples were collected for the assessment of chemistry parameters namely serum albuim and serum protein for Part 1b. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.

Time frame:: Baseline and up to 11 days

No measurements were reported for this outcome.

SecondaryChange From Baseline in Clinical Chemistry Parameters Serum Bilirubin, Serum Creatinine and Serum Direct Bilirubin in Part 1b

Time frame:: Baseline and up to 11 days

No measurements were reported for this outcome.

SecondaryChange From Baseline in Hematology Parameters Blood Basophils, Blood Eosinophils, Blood Leukocytes, Blood Lymphocytes, Blood Monocytes, Blood Neutrophils and Blood Platelets for Part 1b

Blood samples were collected for the assessment of hematology parameters namely blood basophils, blood eosinophils, blood leukocytes, blood lymphocytes, blood monocytes, blood neutrophils and blood platelets for Part 1b. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.

Time frame:: Baseline and up to 11 days

No measurements were reported for this outcome.

SecondaryChange From Baseline in Hematology Parameters Blood Ery. MCHC and Blood Hemoglobin for Part 1b

Blood samples were collected for the assessment of hematology parameters namely blood Ery. MCHC and blood hemoglobin for Part 1b. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.

Time frame:: Baseline and up to 11 days

No measurements were reported for this outcome.

SecondaryChange From Baseline in Hematology Parameter Blood Ery. MCH for Part 1b

Blood samples were collected for the assessment of hematology parameter namely blood Ery. MCH for Part 1a. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.

Time frame:: Baseline and up to 11 days

No measurements were reported for this outcome.

SecondaryChange From Baseline in Hematology Parameter Blood Ery. MCV for Part 1b

Blood samples were collected for the assessment of hematology parameter namely blood Ery. MCV for Part 1a. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.

Time frame:: Baseline and up to 11 days

No measurements were reported for this outcome.

SecondaryChange From Baseline in Hematology Parameter Blood Ery. for Part 1b

Blood samples were collected for the assessment of hematology parameter namely blood Ery. for Part 1b. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.

Time frame:: Baseline and up to 11 days

No measurements were reported for this outcome.

SecondaryChange From Baseline in Hematology Parameter Blood Hematocrit for Part 1b

Blood samples were collected for the assessment of hematology parameter namely blood hematocrit for Part 1b. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.

Time frame:: Baseline and up to 11 days

No measurements were reported for this outcome.

SecondaryChange From Baseline in Vital Sign Parameters SBP and DBP for Part 1b

Single vital signs were measured in semi-supine position after 5 minutes rest and included SBP, DBP. Baseline was defined as assessments performed on Day 1 (pre-dose). Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.

Time frame:: Baseline and up to 11 days

No measurements were reported for this outcome.

SecondaryChange From Baseline in Vital Sign Parameter Heart Rate for Part 1b

Single vital signs were measured in semi-supine position after 5 minutes rest and included heart rate. Baseline was defined as assessments performed on Day 1 (pre-dose). Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.

Time frame:: Baseline and up to 11 days

No measurements were reported for this outcome.

SecondaryChange From Baseline in ECG Parameter Heart Rate for Part 1b

A 12 lead ECG was measured in semi-supine position after 5 minutes rest using an ECG machine that automatically calculated the heart rate. Baseline was defined as assessments performed on Day 1 (pre-dose). Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.

Time frame:: Baseline and up to 11 days

No measurements were reported for this outcome.

SecondaryChange From Baseline in ECG Parameters PR Interval, QRS Duration, QT Interval, QTcB and QTcF for Part 1b

A 12 lead ECG was measured in semi-supine position after 5 minutes rest using an ECG machine that measured PR interval, QRS duration, QT interval, QTcB and QTcF for Part 1b. Baseline was defined as assessments performed on Day 1 (pre-dose). Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.

Time frame:: Baseline and up to 11 days

No measurements were reported for this outcome.

SecondaryNumber of Participants With Abnormal Values on Urinalysis by Dipstick Analysis Part 1b

Urinalysis parameters assessed were urine ketones, urine glucose, urine occult blood, urine pH, urine specific gravity and urine protein. In this dipstick test, the level of ketones, glucose, occult blood, pH, specific gravity and protein in urine samples was recorded as negative trace, 1+, 3+, 5+, 6+, 7+ and 8+ (the plus sign increases with a higher level of ketones, occult blood, pH or specific gravity in the urine: 1+=slightly positive, 3+ to 5+=positive, 6+ and above=high positive). Since the relative bio-availability of the RC tablet formulation under fasted and fed conditions had been previously evaluated in Study BTZ117349 (NCT02045849), Part 1b was not conducted.

Time frame:: Up to 11 days

No measurements were reported for this outcome.

SecondaryNumber of Participants With Non-serious AEs and SAEs for Part 2

Time frame:: Up to 11 days
Reported as:: Count of participants · Participants

Number of Participants With Non-serious AEs and SAEs for Part 2
Participants	Gepotidacin RC 1500 mg Tablets	Gepotidacin RC 3000 mg Tablets
Non serious AE	6	9
SAE	0	0

SecondaryChange From Baseline in Clinical Chemistry Parameters Serum Glucose, Serum Calcium, Serum Carbon Dioxide, Serum Chloride, Serum Potassium, Serum Sodium and Serum Urea Nitrogen in Part 2

Blood samples were collected for the assessment of chemistry parameters namely serum glucose, serum calcium, serum carbon dioxide, serum chloride, serum potassium, serum sodium and serum urea nitrogen for Part 2. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose-visit value from the Baseline value. NA indicates participants crossed-over as follow-up visit occurred after Period 2.

Time frame:: Baseline and up to 11 days
Reported as:: Mean · millimoles/liter

Change From Baseline in Clinical Chemistry Parameters Serum Glucose, Serum Calcium, Serum Carbon Dioxide, Serum Chloride, Serum Potassium, Serum Sodium and Serum Urea Nitrogen in Part 2
millimoles/liter	Gepotidacin RC 1500 mg Tablets	Gepotidacin RC 3000 mg Tablets
Serum glucose, Day 3 (48 hour)	-0.146 ± 0.4421	-0.133 ± 0.3665
Serum glucose, Follow-up	NA ± NA	-0.211 ± 0.5005
Serum calcium, Day 3 (48 hour)	-0.027 ± 0.1055	-0.009 ± 0.0684
Serum calcium, Follow-up	NA ± NA	-0.011 ± 0.0638
Serum carbon dioxide, Day 3 (48 hour)	1.5 ± 1.96	-1.4 ± 1.71
Serum carbon dioxide, Follow-up	NA ± NA	-0.4 ± 1.78
Serum chloride, Day 3 (48 hour)	-1.5 ± 1.96	-1.2 ± 2.04
Serum chloride, Follow-up	NA ± NA	0.1 ± 2.13
Serum potassium, Day 3 (48 hour)	-0.03 ± 0.437	-0.16 ± 0.517
Serum potassium, Follow-up	NA ± NA	0.01 ± 0.446
Serum sodium, Day 3 (48 hour)	-1.1 ± 1.45	-0.9 ± 2.02
Serum sodium, Follow-up	NA ± NA	0.4 ± 2.22
Serum urea nitrogen, Day 3 (48 hour)	0.678 ± 0.8489	1.321 ± 1.2692
Serum urea nitrogen, Follow-up	NA ± NA	0.216 ± 1.7478

SecondaryChange From Baseline in Clinical Chemistry Parameters Serum ALT, Serum AP, Serum AST and Serum CK in Part 2

Blood samples were collected for the assessment of chemistry parameters namely serum ALT, serum AP, serum AST and serum CK for Part 2. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. NA indicates participants crossed-over as follow-up visit occurred after Period 2.

Time frame:: Baseline and up to 11 days
Reported as:: Mean · International units/liter

Change From Baseline in Clinical Chemistry Parameters Serum ALT, Serum AP, Serum AST and Serum CK in Part 2
International units/liter	Gepotidacin RC 1500 mg Tablets	Gepotidacin RC 3000 mg Tablets
Serum ALT, Day 3 (48 hour)	-0.2 ± 1.55	1.3 ± 3.16
Serum ALT, Follow-up	NA ± NA	3.1 ± 5.95
Serum AP, Day 3 (48 hour)	-0.3 ± 5.44	-0.3 ± 4.00
Serum AP, Follow-up	NA ± NA	-1.7 ± 2.95
Serum AST, Day 3 (48 hour)	0.5 ± 2.92	1.0 ± 2.71
Serum AST, Follow-up	NA ± NA	3.5 ± 4.81
Serum CK, Day 3 (48 hour)	-22.7 ± 26.45	-25.7 ± 15.81
Serum CK, Follow-up	NA ± NA	-9.8 ± 13.99

SecondaryChange From Baseline in Clinical Chemistry Parameters Serum Albumin and Serum Protein for Part 2

Blood samples were collected for the assessment of chemistry parameters namely serum albumin and serum protein for Part 2. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose-visit value from the Baseline value. NA indicates participants crossed-over as follow-up visit occurred after Period 2.

Time frame:: Baseline and up to 11 days
Reported as:: Mean · grams/liter

Change From Baseline in Clinical Chemistry Parameters Serum Albumin and Serum Protein for Part 2
grams/liter	Gepotidacin RC 1500 mg Tablets	Gepotidacin RC 3000 mg Tablets
Serum albumin, Day 3 (48 hour)	-0.9 ± 3.38	0.0 ± 1.70
Serum albumin, Follow-up	NA ± NA	-1.5 ± 2.17
Serum protein, Day 3 (48 hour)	0.0 ± 5.29	-2.1 ± 4.63
Serum protein, Follow-up,	NA ± NA	-1.8 ± 2.70

SecondaryChange From Baseline in Clinical Chemistry Parameters Serum Bilirubin, Serum Creatinine and Serum Direct Bilirubin for Part 2

Blood samples were collected for the assessment of chemistry parameters namely serum bilirubin, serum creatinine and serum direct bilirubin for Part 2. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. NA indicates participants crossed-over as follow-up visit occurred after Period 2.

Time frame:: Baseline and up to 11 days
Reported as:: Mean · micromoles/liter

Change From Baseline in Clinical Chemistry Parameters Serum Bilirubin, Serum Creatinine and Serum Direct Bilirubin for Part 2
micromoles/liter	Gepotidacin RC 1500 mg Tablets	Gepotidacin RC 3000 mg Tablets
Serum bilirubin, Day 3 (48 hour)	-1.02 ± 2.944	-3.62 ± 2.968
Serum bilirubin	NA ± NA	-0.68 ± 4.207
Serum creatinine, Day 3 (48 hour)	-1.76 ± 8.147	-4.42 ± 6.254
Serum creatinine	NA ± NA	-3.55 ± 7.458
Serum direct bilirubin, Day 3 (48 hour)	-0.51 ± 1.147	-1.02 ± 0.878
Serum direct bilirubin, Follow-up	NA ± NA	-0.34 ± 1.075

SecondaryChange From Baseline in Clinical Chemistry Parameter Serum Estradiol for Part 2

Blood samples were collected for the assessment of chemistry parameter namely serum estradiol for Part 2. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the indicated time point were analyzed. NA indicates standard deviation was not calculated as a single participant was analyzed.

Time frame:: Baseline and up to 11 days
Reported as:: Mean · picomoles/liter

Change From Baseline in Clinical Chemistry Parameter Serum Estradiol for Part 2
picomoles/liter	Gepotidacin RC 1500 mg Tablets	Gepotidacin RC 3000 mg Tablets
Change From Baseline in Clinical Chemistry Parameter Serum Estradiol for Part 2	NA ± NA	0.00 ± NA

SecondaryChange From Baseline in Hematology Parameters Blood Basophils, Blood Eosinophils, Blood Leukocytes, Blood Lymphocytes, Blood Monocytes, Blood Neutrophils and Blood Platelets for Part 2

Blood samples were collected for the assessment of hematology parameters namely blood basophils, blood eosinophils, blood leukocytes, blood lymphocytes, blood monocytes, blood neutrophils and blood platelets for Part 2. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. NA indicates participants crossed-over as follow-up visit occurred after Period 2.

Time frame:: Baseline and up to 11 days
Reported as:: Mean · 10^9 cells/liter

Change From Baseline in Hematology Parameters Blood Basophils, Blood Eosinophils, Blood Leukocytes, Blood Lymphocytes, Blood Monocytes, Blood Neutrophils and Blood Platelets for Part 2
10^9 cells/liter	Gepotidacin RC 1500 mg Tablets	Gepotidacin RC 3000 mg Tablets
Blood basophils, Day 3 (48 hour)	0.002 ± 0.0092	0.009 ± 0.0129
Blood basophils, Follow-up	NA ± NA	0.004 ± 0.0097
Blood eosinophils, Day 3 (48 hour)	0.036 ± 0.0626	0.052 ± 0.0839
Blood eosinophils, Follow-up	NA ± NA	0.021 ± 0.0671
Blood leukocytes, Day 3 (48 hour)	0.129 ± 0.7779	0.039 ± 0.8843
Blood leukocytes, Follow-up	NA ± NA	-0.183 ± 0.7906
Blood lymphocytes, Day 3 (48 hour)	0.222 ± 0.1707	0.243 ± 0.2165
Blood lymphocytes, Follow-up	NA ± NA	-0.038 ± 0.2875
Blood monocytes, Day 3 (48 hour)	-0.020 ± 0.0651	-0.013 ± 0.0732
Blood monocytes, Follow-up	NA ± NA	0.045 ± 0.0546
Blood neutrophils, Day 3 (48 hour)	-0.112 ± 0.6906	-0.251 ± 0.6701
Blood neutrophils, Follow-up	NA ± NA	-0.213 ± 0.8126
Blood platelets, Day 3 (48 hour)	-7.4 ± 38.14	-0.6 ± 33.37
Blood platelets, Follow-up	NA ± NA	2.1 ± 31.49

SecondaryChange From Baseline in Hematology Parameters Ery. MCHC and Blood Hemoglobin for Part 2

Blood samples were collected for the assessment of hematology parameters namely blood Ery. MCHC and blood hemoglobin for Part 2. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. NA indicates participants crossed-over as follow-up visit occurred after Period 2.

Time frame:: Baseline and up to 11 days
Reported as:: Mean · grams/liter

Change From Baseline in Hematology Parameters Ery. MCHC and Blood Hemoglobin for Part 2
grams/liter	Gepotidacin RC 1500 mg Tablets	Gepotidacin RC 3000 mg Tablets
Blood Ery. MCHC, Day 3 (48 hour)	-6.6 ± 4.35	-6.6 ± 3.20
Blood Ery. MCHC, Follow-up	NA ± NA	-6.2 ± 5.87
Blood hemoglobin, Day 3 (48 hour)	2.8 ± 9.43	0.9 ± 5.55
Blood hemoglobin, Follow-up	NA ± NA	-5.9 ± 3.67

SecondaryChange From Baseline in Hematology Parameter Blood Ery. MCH for Part 2

Blood samples were collected for the assessment of hematology parameter namely blood Ery. MCH for Part 2. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. NA indicates participants crossed-over as follow-up visit occurred after Period 2.

Time frame:: Baseline and up to 11 days
Reported as:: Mean · picograms

Change From Baseline in Hematology Parameter Blood Ery. MCH for Part 2
picograms	Gepotidacin RC 1500 mg Tablets	Gepotidacin RC 3000 mg Tablets
Blood Ery.MCH, Day 3 (48 hour)	-0.25 ± 0.331	-0.06 ± 0.378
Blood Ery. MCH, Follow-up	NA ± NA	-0.15 ± 0.488

SecondaryChange From Baseline in Hematology Parameter Blood Ery. MCV for Part 2

Blood samples were collected for the assessment of hematology parameter namely blood Ery. MCV for Part 2. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. NA indicates participants crossed-over as follow-up visit occurred after Period 2.

Time frame:: Baseline and up to 11 days
Reported as:: Mean · femtoliters

Change From Baseline in Hematology Parameter Blood Ery. MCV for Part 2
femtoliters	Gepotidacin RC 1500 mg Tablets	Gepotidacin RC 3000 mg Tablets
Blood Ery. MCV, Day 3 (48 hour)	1.17 ± 1.610	1.69 ± 1.371
Blood Ery. MCV, Follow-up	NA ± NA	1.28 ± 1.834

SecondaryChange From Baseline in Hematology Parameter Blood Ery. for Part 2

Blood samples were collected for the assessment of hematology parameter namely blood Ery. for Part 2. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. NA indicates participants crossed-over as follow-up visit occurred after Period 2.

Time frame:: Baseline and up to 11 days
Reported as:: Mean · 10^12 cells/liter

Change From Baseline in Hematology Parameter Blood Ery. for Part 2
10^12 cells/liter	Gepotidacin RC 1500 mg Tablets	Gepotidacin RC 3000 mg Tablets
Blood Ery., Day 3 (48 hour)	0.118 ± 0.2839	0.033 ± 0.1675
Blood Ery., Follow-up	NA ± NA	-0.175 ± 0.1099

SecondaryChange From Baseline in Hematology Parameter Blood Hematocrit for Part 2

Blood samples were collected for the assessment of hematology parameter namely blood hematocrit for Part 2. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. NA indicates participants crossed-over as follow-up visit occurred after Period 2.

Time frame:: Baseline and up to 11 days
Reported as:: Mean · Percentage of red blood cells in blood

Change From Baseline in Hematology Parameter Blood Hematocrit for Part 2
Percentage of red blood cells in blood	Gepotidacin RC 1500 mg Tablets	Gepotidacin RC 3000 mg Tablets
Blood hematocrit , Day 3 (48 hour)	1.6 ± 2.871	1.02 ± 1.713
Blood hematocrit, Follow-up	NA ± NA	-1.09 ± 1.079

SecondaryChange From Baseline in Vital Sign Parameters SBP and DBP for Part 2

Time frame:: Baseline and up to 11 days
Reported as:: Mean · millimeters of mercury

Change From Baseline in Vital Sign Parameters SBP and DBP for Part 2
millimeters of mercury	Gepotidacin RC 1500 mg Tablets	Gepotidacin RC 3000 mg Tablets
SBP, Day 1 (2 hours)	-8.4 ± 15.78	6.7 ± 10.49
SBP, Day 2 (24 hours)	-9.6 ± 13.55	-3.1 ± 12.90
SBP, Day 3 (48 hours)	-4.1 ± 17.99	-4.2 ± 11.03
SBP, Follow-up	NA ± NA	-2.0 ± 17.81
DBP, Day 1 (2 hours)	-6.7 ± 6.13	-0.3 ± 6.95
DBP, Day 2 (24 hours)	-5.4 ± 8.72	-3.5 ± 6.92
DBP, Day 3 (48 hours)	-1.9 ± 7.98	-1.7 ± 6.62
DBP, Follow-up	NA ± NA	-0.1 ± 11.35

SecondaryChange From Baseline in Vital Sign Parameter Heart Rate for Part 2

Time frame:: Baseline and up to 11 days
Reported as:: Mean · beats/minute

Change From Baseline in Vital Sign Parameter Heart Rate for Part 2
beats/minute	Gepotidacin RC 1500 mg Tablets	Gepotidacin RC 3000 mg Tablets
Heart rate, Day 1 (2 hours)	0.1 ± 7.84	3.2 ± 6.48
Heart rate, Day 2 (24 hours)	-3.8 ± 12.38	-1.4 ± 6.90
Heart rate, Day 3 (48 hours)	-3.0 ± 11.22	3.4 ± 6.29
Heart rate, Follow-up	NA ± NA	-0.3 ± 9.06

SecondaryChange From Baseline in ECG Parameter Heart Rate for Part 2

A 12 lead ECG was measured in semi-supine position after 5 minutes rest using an ECG machine that automatically calculated the heart rate. Baseline was defined as assessments performed on Day 1 (pre-dose). Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. NA indicates participants crossed-over as follow-up visit occurred after Period 2.

Time frame:: Baseline and up to 11 days
Reported as:: Mean · beats/minute

Change From Baseline in ECG Parameter Heart Rate for Part 2
beats/minute	Gepotidacin RC 1500 mg Tablets	Gepotidacin RC 3000 mg Tablets
ECG Heart rate, Day 1 (2 hours)	5.4 ± 10.13	4.9 ± 5.02
ECG Heart rate, Day 2 (24 hours)	-1.2 ± 8.75	-1.1 ± 6.71
ECG Heart rate, Day 3 (48 hours)	2.1 ± 11.00	3.4 ± 5.38
ECG Heart rate, Follow-up	NA ± NA	-1.6 ± 8.18

SecondaryChange From Baseline in ECG Parameters PR Interval, QRS Duration, QT Interval, QTcB and QTcF for Part 2

A 12 lead ECG was measured in semi-supine position after 5 minutes rest using an ECG machine that measured PR interval, QRS duration, QT interval, QTcB and QTcF for Part 2. Baseline was defined as assessments performed on Day 1 (pre-dose). Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. NA indicates participants crossed-over as follow-up visit occurred after Period 2.

Time frame:: Baseline and up to 11 days
Reported as:: Mean · milliseconds

Change From Baseline in ECG Parameters PR Interval, QRS Duration, QT Interval, QTcB and QTcF for Part 2
milliseconds	Gepotidacin RC 1500 mg Tablets	Gepotidacin RC 3000 mg Tablets
PR interval, Day 1 (2 hours)	-1.7 ± 13.92	0.5 ± 11.49
PR interval, Day 2 (24 hours)	7.2 ± 11.44	-2.7 ± 7.23
PR interval, Day 3 (48 hours)	5.1 ± 11.46	3.0 ± 11.71
PR interval, Follow-up	NA ± NA	-1.2 ± 15.37
QRS duration, Day 1 (2 hours)	0.4 ± 5.19	3.9 ± 4.28
QRS duration, Day 2 (24 hours)	0.3 ± 4.57	-0.2 ± 4.73
QRS duration, Day 3 (48 hours)	-0.2 ± 4.54	0.7 ± 4.06
QRS duration, Follow-up	NA ± NA	1.6 ± 3.60
QT interval Day 1 (2 hours)	-4.0 ± 16.21	5.1 ± 16.04
QT interval, Day 2 (24 hours)	4.8 ± 21.63	11.7 ± 17.31
QT interval, Day 3 (48 hours)	-1.0 ± 20.48	-3.4 ± 14.95
QT interval, Follow-up	NA ± NA	9.5 ± 17.37
QTcB interval, Day 1 (2 hours)	15.2 ± 18.23	20.7 ± 14.17
QTcB, Day 2 (24 hours)	3.4 ± 11.64	9.5 ± 8.24
QTcB, Day 3 (48 hours)	6.6 ± 16.26	6.0 ± 13.00
QTcB, Follow-up	NA ± NA	5.7 ± 13.44
QTcF interval, Day 1 (2 hours)	8.6 ± 9.56	15.2 ± 13.09
QTcF, Day 2 (24 hours)	4.0 ± 10.23	10.4 ± 8.75
QTcF, Day 3 (48 hours)	4.0 ± 8.60	2.4 ± 11.64
QTcF, Follow-up	NA ± NA	7.0 ± 9.36

SecondaryNumber of Participants With Abnormal Values on Urinalysis by Dipstick Analysis Part 2

Urinalysis parameters assessed were urine ketones, urine glucose, urine occult blood, urine pH, urine specific gravity and urine protein. In this dipstick test, the level of ketones, glucose, occult blood, pH, specific gravity and protein in urine samples was recorded as negative trace, 1+, 3+, 4+ 5+, 6+, 7+ and 8+ (the plus sign increases with a higher level of ketones, occult blood, pH or specific gravity in the urine: 1+=slightly positive, 3+ to 5+=positive, 6+ and above=high positive). Urine samples were collected for the measurement of urinalysis parameters by dipstick method up-to follow-up (5 to 7 days post last dose) in Part 2. Only categories with significant values have been presented.

Time frame:: Baseline and up to 11 days
Reported as:: Count of participants · Participants

Number of Participants With Abnormal Values on Urinalysis by Dipstick Analysis Part 2
Participants	Gepotidacin RC 1500 mg Tablets	Gepotidacin RC 3000 mg Tablets
Urine Ketones, Follow-up, Trace	0	1
Urine Occult blood, Day 3 (48 hours), 1+	0	1
Urine Occult blood, Trace, Day 3 (48 hours),	2	0
Urine Occult blood, Follow-up, 1+	0	1
Urine pH, Day 3 (48 hours), 5+	2	7
Urine pH, Day 3 (48 hours), 6+	6	2
Urine pH, Day 3 (48 hours), 7+	1	1
Urine pH, Day 3 (48 hours), 8+	1	0
Urine pH, Follow-up, 5+	0	3
Urine pH, Follow-up, 6+	0	6
Urine pH, Follow-up, 8+	0	1
Urine Specific gravity, Day 3 (48 hours), 1+	10	10
Urine Specific gravity, Follow-up, 1+	0	10

SecondaryNumber of Participants With Non-serious AEs and SAEs for Part 3

Time frame:: Up to 14 days
Reported as:: Count of participants · Participants

Number of Participants With Non-serious AEs and SAEs for Part 3
Participants	Gepotidacin RC 1500 mg Fed	Gepotidacin RC 2250 mg Fed	Gepotidacin RC 3000 mg Fed	Placebo
Non seriou AE	0	1	6	0
SAE	0	0	0	0

SecondaryChange From Baseline in Clinical Chemistry Parameters Serum Glucose, Serum Calcium, Serum Carbon Dioxide, Serum Chloride, Serum Potassium, Serum Sodium and Serum Urea Nitrogen for Part 3

Blood samples were collected for the assessment of chemistry parameters namely serum glucose, serum calcium, serum carbon dioxide, serum chloride, serum potassium, serum sodium and serum urea nitrogen for Part 3. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles). Data points with null value for participants analyzed indicate data not collected for respective category and treatment arm.

Time frame:: Baseline and up to 14 days
Reported as:: Mean · millimoles/liter

Change From Baseline in Clinical Chemistry Parameters Serum Glucose, Serum Calcium, Serum Carbon Dioxide, Serum Chloride, Serum Potassium, Serum Sodium and Serum Urea Nitrogen for Part 3
millimoles/liter	Gepotidacin RC 1500 mg Fed	Gepotidacin RC 2250 mg Fed	Gepotidacin RC 3000 mg Fed	Placebo
Glucose,Period 1,Day 3(48 hour),n=10,0,0,2	0.038 ± 0.3178	—	—	-0.305 ± 0.4313
Glucose,Period 2,Day 3 (48 hour),n=0,10,0,2	—	-0.071 ± 0.2993	—	-0.415 ± 0.2758
Glucose,Period 3,Day 3 (48 hour),n=0,0,9,2	—	—	-0.197 ± 0.2355	-0.335 ± 0.1626
Glucose, Follow-up, n=0,0,9,2	—	—	-0.050 ± 0.2744	-0.390 ± 0.3960
Calcium,Period1, Day 3 (48 hour),n=10,0,0,2	-0.057 ± 0.0887	—	—	-0.075 ± 0.1061
Calcium,Period 2,Day 3 (48 hour),n=0,10,0,2	—	-0.046 ± 0.0819	—	-0.115 ± 0.0919
Calcium,Period 3,Day 3 (48 hour),n=0,0,9,2	—	—	-0.028 ± 0.0502	-0.105 ± 0.0354
Calcium, Follow-up, n=0,0, 9, 2	—	—	-0.039 ± 0.0742	-0.040 ± 0.0141
Carbon dioxide,Period 1,Day 3(48 hour),n=10,0,0,2	-0.6 ± 1.51	—	—	0.5 ± 0.71
Carbon dioxide,Period 2,Day 3(48 hour),n=0,10,0,2	—	-0.7 ± 1.64	—	2.5 ± 2.12
Carbon dioxide,Period 3,Day 3(48 hour),n=0,0,9,2	—	—	-1.1 ± 1.36	1.5 ± 0.71
Carbon dioxide, Follow-up, n=0,0,9,2	—	—	0.2 ± 2.28	1.5 ± 0.71
Chloride, Period 1, Day 3 (48 hour),n=10,0,0,2	0.8 ± 1.23	—	—	1.0 ± 2.83
Chloride, Period 2, Day 3 (48 hour),n=0,10,0,2	—	0.8 ± 1.75	—	-2.0 ± 0.00
Chloride, Period 3, Day 3 (48 hour),n=0,0,9,2	—	—	0.1 ± 1.96	-1.5 ± 0.71
Chloride, Follow-up,n=0,0,9,2	—	—	0.2 ± 2.95	-2.0 ± 0.00
Potassium, Period 1, Day 3 (48 hour), n=10,0,0,2	-0.21 ± 0.536	—	—	-0.10 ± 0.283
Potassium, Period 2, Day 3 (48 hour), n=0,10,0,2	—	-0.19 ± 0.381	—	-0.40 ± 1.131
Potassium, Period 3, Day 3 (48 hour), n=0,0,9,2	—	—	-0.28 ± 0.561	-0.30 ± 1.273
Potassium, Follow-up, n=0,0,9,2	—	—	-0.21 ± 0.359	-0.15 ± 0.919
Sodium, Period 1, Day 3 (48 hour), n=10,0,0,2	0.6 ± 2.12	—	—	2.5 ± 2.12
Sodium, Period 2, Day 3 (48 hour), n=0,10,0,2	—	0.1 ± 2.38	—	-1.0 ± 2.83
Sodium, Period 3, Day 3 (48 hour), n=0,0,9,2	—	—	0.3 ± 1.94	-2.0 ± 4.24
Sodium, Follow-up, n=0,0,9,2	—	—	-0.1 ± 1.90	-2.5 ± 2.12
Urea nitrogen,Period 1,Day 3 (48 hour),n=10,0,0,2	0.606 ± 1.0760	—	—	0.535 ± 0.2475
Urea nitrogen,Period 2,Day 3 (48 hour),n=0,10,0,2	—	0.677 ± 1.3401	—	1.610 ± 0.7637
Urea nitrogen,Period 3,Day 3 (48 hour),n=0,0,9,2	—	—	0.474 ± 1.4617	1.075 ± 0.0071
Urea nitrogen, Follow-up, n=0,0,9,2	—	—	0.356 ± 1.2998	2.320 ± 2.7860

SecondaryChange From Baseline in Clinical Chemistry Parameters Serum ALT, Serum AP, Serum AST and Serum CK for Part 3

Blood samples were collected for the assessment of chemistry parameters namely serum ALT, serum AP, serum AST and serum CK for Part 3. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles). Data points with null value for participants analyzed indicate data not collected for respective category and treatment arm.

Time frame:: Baseline and up to 14 days
Reported as:: Mean · International units/liter

Change From Baseline in Clinical Chemistry Parameters Serum ALT, Serum AP, Serum AST and Serum CK for Part 3
International units/liter	Gepotidacin RC 1500 mg Fed	Gepotidacin RC 2250 mg Fed	Gepotidacin RC 3000 mg Fed	Placebo
ALT, Period 1, Day 3 (48 hour), n=10,0,0,2	0.1 ± 2.73	—	—	-2.5 ± 2.12
ALT, Period 2, Day 3 (48 hour), n=0,10,0,2	—	2.2 ± 3.36	—	-4.0 ± 7.07
ALT, Period 3, Day 3 (48 hour), n=0,0,9,2,	—	—	6.0 ± 3.74	-4.5 ± 9.19
ALT, Follow-up, n=0,0,9,2	—	—	5.9 ± 4.11	-5.0 ± 11.31
AP, Period 1, Day 3 (48 hour), n=10,0,0,2,	-3.6 ± 2.07	—	—	-9.0 ± 5.66
AP, Period 2, Day 3 (48 hour), n=0,10,0,2	—	-2.5 ± 4.62	—	-2.0 ± 4.24
Serum AP, Day 3 (48 hour), n=0,0,9,2	—	—	0.6 ± 3.88	-0.5 ± 0.71
AP, Follow-up, n=0,0,9,2	—	—	1.8 ± 3.96	3.5 ± 3.54
AST, Period 1, Day 3 (48 hour),n=10,0,0,2	1.3 ± 3.06	—	—	-3.5 ± 2.12
AST, Period 2, Day 3 (48 hour),n=0,10,0,2	—	1.7 ± 2.50	—	-5.0 ± 4.24
AST, Period 3, Day 3 (48 hour),n=0,0,9,2	—	—	4.2 ± 2.68	-5.0 ± 5.66
AST, Follow-up, n=0,0,9,2	—	—	2.6 ± 2.46	-4.0 ± 7.07
CK, Period 1, Day 3 (48 hour),n=10,0,0,2	-28.1 ± 17.60	—	—	-22.5 ± 14.85
CK, Period 2, Day 3 (48 hour),n=0,10,0,2	—	-11.8 ± 65.84	—	-33.5 ± 23.33
CK, Period 3, Day 3 (48 hour),n=0,0,9,2	—	—	-14.3 ± 20.27	-21.5 ± 9.19
CK, Follow-up, n=0,0,9,2	—	—	3.7 ± 26.87	1.0 ± 11.31

SecondaryChange From Baseline in Clinical Chemistry Parameters Serum Albumin and Serum Protein for Part 3

Blood samples were collected for the assessment of chemistry parameters namely serum albumin and serum protein for Part 3. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles). Data points with null value for participants analyzed indicate data not collected for respective category and treatment arm.

Time frame:: Baseline and up to 14 days
Reported as:: Mean · grams/liter

Change From Baseline in Clinical Chemistry Parameters Serum Albumin and Serum Protein for Part 3
grams/liter	Gepotidacin RC 1500 mg Fed	Gepotidacin RC 2250 mg Fed	Gepotidacin RC 3000 mg Fed	Placebo
Albumin, Part 1, Day 3 (48 hour), n=10,0,0,2	-2.0 ± 2.54	—	—	-2.0 ± 0.00
Albumin, Period 2, Day 3 (48 hour), n=0,10,0,2	—	-2.0 ± 1.05	—	-3.0 ± 1.41
Albumin, Period 3, Day 3 (48 hour), n=0,0,9,2	—	—	-0.6 ± 3.05	-2.5 ± 0.71
Albumin, Follow-up, n=0,0,9,2	—	—	-0.3 ± 3.12	-0.5 ± 2.12
Protein, Period 1, Day 3 (48 hour), n=10,0,0,2	-3.0 ± 2.31	—	—	-4.5 ± 0.71
Protein, Period 2, Day 3 (48 hour), n=0,10,0,2	—	-2.2 ± 3.01	—	-5.0 ± 1.41
Protein, Period 3, Day 3 (48 hour), n=0,0,9,2	—	—	-0.6 ± 3.97	-4.5 ± 0.71
Protein, Follow-up, n=0,0,9,2	—	—	-0.6 ± 4.64	-1.0 ± 5.66

SecondaryChange From Baseline in Clinical Chemistry Parameters Serum Bilirubin and Serum Creatinine for Part 3

Blood samples were collected for the assessment of chemistry parameters namely serum bilirubin and serum creatinine for Part 3. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles). Data points with null value for participants analyzed indicate data not collected for respective category and treatment arm

Time frame:: Baseline and up to 14 days
Reported as:: Mean · micromoles/liter

Change From Baseline in Clinical Chemistry Parameters Serum Bilirubin and Serum Creatinine for Part 3
micromoles/liter	Gepotidacin RC 1500 mg Fed	Gepotidacin RC 2250 mg Fed	Gepotidacin RC 3000 mg Fed	Placebo
Bilirubin, Period 1, Day 3 (48 hour), n=10,0,0,2	-2.43 ± 3.364	—	—	-0.85 ± 1.202
Bilirubin, Period 2, Day 3 (48 hour), n=0,10,0,2,	—	-3.11 ± 3.793	—	-1.70 ± 0.000
Bilirubin, Period 3, Day 3 (48 hour), n=0,0,9,2	—	—	-2.28 ± 3.844	0.85 ± 1.202
Bilirubin, Follow-up, n=0,0,9,2	—	—	-1.53 ± 2.757	-1.70 ± 0.000
Creatinine, Period 1,Day 3 (48 hour), n=10,0,0,2	-1.75 ± 8.101	—	—	-17.65 ± 12.516
Creatinine, Period 2,Day 3 (48 hour), n=0,10,0,2	—	-1.75 ± 6.958	—	-17.60 ± 0.000
Creatinine, Period 3,Day 3 (48 hour), n=0,0,9,2	—	—	0.01 ± 7.636	-13.20 ± 6.223
Creatinine, Follow-up, n=0,0,9,2	—	—	2.97 ± 6.258	-4.40 ± 6.223

SecondaryChange From Baseline in Hematology Parameters Blood Basophils, Blood Eosinophils, Blood Leukocytes, Blood Lymphocytes, Blood Monocytes, Blood Neutrophils and Blood Platelets for Part 3

Blood samples were collected for the assessment of hematology parameters namely blood basophils, blood eosinophils, blood leukocytes, blood lymphocytes, blood monocytes, blood neutrophils and blood platelets for Part 3. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles). Data points with null value for participants analyzed indicate data not collected for respective category and treatment arm.

Time frame:: Baseline and up to 14 days
Reported as:: Mean · 10^9 cells/liter

Change From Baseline in Hematology Parameters Blood Basophils, Blood Eosinophils, Blood Leukocytes, Blood Lymphocytes, Blood Monocytes, Blood Neutrophils and Blood Platelets for Part 3
10^9 cells/liter	Gepotidacin RC 1500 mg Fed	Gepotidacin RC 2250 mg Fed	Gepotidacin RC 3000 mg Fed	Placebo
Basophils, Period 1, Day 3 (48 hour), n=10,0,0,2	0.004 ± 0.0158	—	—	0.000 ± 0.0141
Basophils, Period 2, Day 3 (48 hour), n=0,10,0,2,	—	0.009 ± 0.0120	—	-0.010 ± 0.0141
Basophils, Period 3, Day 3 (48 hour), n=0,0,9,2	—	—	0.009 ± 0.0162	0.005 ± 0.0071
Basophils, Follow-up, n=0,0,9,2	—	—	0.008 ± 0.0186	0.015 ± 0.0071
Eosinophils, Period 1, Day 3 (48 hour),n=10,0,0,2	0.053 ± 0.0254	—	—	0.060 ± 0.0707
Eosinophils, Period 2,Day 3 (48 hour), n=0,10,0,2	—	0.068 ± 0.0421	—	0.055 ± 0.0778
Eosinophils, Period 3,Day 3 (48 hour), n=0,0,9,2	—	—	0.053 ± 0.0487	0.040 ± 0.0990
Eosinophils, Follow-up, n=0,0,9,2	—	—	0.022 ± 0.0192	0.045 ± 0.1061
Leukocytes, Period 1, Day 3 (48 hour),n=10,0,0,2	0.581 ± 0.6524	—	—	-1.000 ± 0.8202
Leukocytes, Period 2, Day 3 (48 hour),n=0,10,0,2	—	0.730 ± 0.8427	—	-1.415 ± 1.0819
Leukocytes, Period 3, Day 3 (48 hour),n=0,0,9,2	—	—	0.966 ± 0.7001	-1.670 ± 0.9475
Leukocytes, Follow-up, n=0,0,9,2	—	—	0.132 ± 0.8490	-1.630 ± 0.2121
Lymphocytes, Period 1,Day 3 (48 hour),n=10,0,0,2	0.209 ± 0.2885	—	—	0.060 ± 0.2263
Lymphocytes, Period 2,Day 3 (48 hour),n=0,10,0,2	—	0.144 ± 0.3405	—	-0.035 ± 0.2192
Lymphocytes, Period 3,Day 3 (48 hour),n=0,0,9,2	—	—	-0.009 ± 0.3207	-0.100 ± 0.2404
Lymphocytes, Follow-up, n=0,0, 9, 2	—	—	-0.089 ± 0.1928	-0.050 ± 0.0283
Monocytes, Period 1, Day 3 (48 hour),n=10,0,0,2,	0.022 ± 0.0598	—	—	-0.025 ± 0.0354
Monocytes, Period 2, Day 3 (48 hour),n=0,10,0,2	—	0.010 ± 0.0615	—	-0.080 ± 0.0424
Monocytes, Period 3, Day 3 (48 hour),n=0,0,9,2	—	—	0.042 ± 0.0427	-0.110 ± 0.0000
Monocytes, Follow-up, n=0,0,9,2	—	—	-0.002 ± 0.0452	-0.100 ± 0.0424
Neutrophils, Period 1,Day 3 (48 hour),n=10,0,0,2	0.292 ± 0.8198	—	—	-1.100 ± 1.1597
Neutrophils, Period 2,Day 3 (48 hour),n=0,10,0,2	—	0.489 ± 0.7302	—	-1.350 ± 0.8910
Neutrophils, Period 3,Day 3 (48 hour),n=0,0,9,2	—	—	0.850 ± 0.8456	-1.505 ± 0.7990
Neutrophils, Follow-up, n=0,0,9,2	—	—	0.184 ± 0.8251	-1.545 ± 0.3606
Platelets, Period 1, Day 3 (48 hour),n=10,0,0,2	-4.7 ± 13.19	—	—	-10.5 ± 10.61
Platelets, Period 2, Day 3 (48 hour),n=0,10,0,2	—	-22.2 ± 41.82	—	-5.0 ± 5.66
Platelets, Period 3, Day 3 (48 hour),n=0,0,9,2	—	—	-6.0 ± 19.80	-15.0 ± 8.49
Platelets, Follow-up, n=0,0,9,2	—	—	2.4 ± 21.93	4.0 ± 8.49

SecondaryChange From Baseline in Hematology Parameters Blood Ery. MCHC and Blood Hemoglobin for Part 3

Blood samples were collected for the assessment of hematology parameters namely blood Ery. MCHC and blood hemoglobin for Part 3. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles). Data points with null value for participants analyzed indicate data not collected for respective category and treatment arm.

Time frame:: Baseline and up to 14 days
Reported as:: Mean · grams/liter

Change From Baseline in Hematology Parameters Blood Ery. MCHC and Blood Hemoglobin for Part 3
grams/liter	Gepotidacin RC 1500 mg Fed	Gepotidacin RC 2250 mg Fed	Gepotidacin RC 3000 mg Fed	Placebo
Ery. MCHC, Period 1, Day 3 (48 hour), n=10,0,0,2	-2.9 ± 5.67	—	—	-2.0 ± 9.90
Ery. MCHC, Period 2, Day 3 (48 hour), n=0,10,0,2	—	-3.2 ± 3.49	—	-1.5 ± 4.95
Ery. MCHC, Period 3, Day 3 (48 hour), n=0,0,9,2	—	—	-5.3 ± 5.22	-6.5 ± 2.12
Ery. MCHC, Follow-up, n=0,0,9,2	—	—	-1.2 ± 4.94	0.0 ± 0.00
Hemoglobin, Period 1,Day 3 (48 hour), n=10,0,0,2	-1.4 ± 6.70	—	—	-7.5 ± 0.71
Hemoglobin, Period 2, Day 3 (48 hour), n=0,10,0,2	—	-3.4 ± 9.35	—	-11.5 ± 0.71
Hemoglobin, Period 3,Day 3 (48 hour), n=0,0,9,2	—	—	-2.1 ± 6.47	-10.5 ± 0.71
Hemoglobin, Follow-up, n=0,0,9,2	—	—	-6.0 ± 7.62	-6.5 ± 7.78

SecondaryChange From Baseline in Hematology Parameter Blood Ery. MCH for Part 3

Time frame:: Baseline and up to 14 days
Reported as:: Mean · picograms

Change From Baseline in Hematology Parameter Blood Ery. MCH for Part 3
picograms	Gepotidacin RC 1500 mg Fed	Gepotidacin RC 2250 mg Fed	Gepotidacin RC 3000 mg Fed	Placebo
Ery.MCH, Period 1, Day 3 (48 hour), n=10,0,0,2	0.08 ± 0.397	—	—	0.25 ± 0.071
Ery.MCH, Period 2, Day 3 (48 hour), n=0,10,0,2	—	0.08 ± 0.270	—	0.15 ± 0.212
Ery.MCH, Period 3 Day 3 (48 hour), n=0,0,9,2	—	—	-0.12 ± 0.380	0.00 ± 0.283
Ery. MCH, Follow-up, n=0,0,9,2	—	—	0.31 ± 0.483	0.00 ± 0.424

SecondaryChange From Baseline in Hematology Parameter Blood Ery. Mean Corpuscular Volume (MCV) for Part 3

Blood samples were collected for the assessment of hematology parameter namely blood Ery. MCV for Part 3. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles). Data points with null value for participants analyzed indicate data not collected for respective category and treatment arm.

Time frame:: Baseline and up to 14 days
Reported as:: Mean · femtoliters

Change From Baseline in Hematology Parameter Blood Ery. Mean Corpuscular Volume (MCV) for Part 3
femtoliters	Gepotidacin RC 1500 mg Fed	Gepotidacin RC 2250 mg Fed	Gepotidacin RC 3000 mg Fed	Placebo
Ery. MCV, Period 1, Day 3 (48 hour), n=10,0,0,2	1.10 ± 1.152	—	—	1.30 ± 2.970
Ery. MCV, Period 2, Day 3 (48 hour), n=0,10,0,2	—	1.14 ± 0.857	—	0.70 ± 2.121
Ery. MCV, Period 3, Day 3 (48 hour), n=0,0,9,2	—	—	1.16 ± 1.167	1.80 ± 0.000
Ery. MCV, Follow-up, n=0,0,9,2	—	—	1.31 ± 1.430	0.00 ± 1.131

SecondaryChange From Baseline in Hematology Parameter Blood Ery. for Part 3

Time frame:: Baseline and up to 14 days
Reported as:: Mean · 10^12 cells/liter

Change From Baseline in Hematology Parameter Blood Ery. for Part 3
10^12 cells/liter	Gepotidacin RC 1500 mg Fed	Gepotidacin RC 2250 mg Fed	Gepotidacin RC 3000 mg Fed	Placebo
Ery., Period 1, Day 3 (48 hour), n=10,0,0,2	-0.065 ± 0.2576	—	—	-0.275 ± 0.0354
Ery.,Period 2, Day 3 (48 hour), n=0,10,0,2	—	-0.138 ± 0.3381	—	-0.390 ± 0.0566
Ery., Period 3, Day 3 (48 hour), n=0,0,9,2	—	—	-0.060 ± 0.2536	-0.340 ± 0.0566
Ery., Follow-up, n=0,0,9,2	—	—	-0.253 ± 0.3347	-0.210 ± 0.3111

SecondaryChange From Baseline in Hematology Parameter Blood Hematocrit for Part 3

Blood samples were collected for the assessment of hematology parameter namely blood hematocrit for Part 3. Baseline was defined as assessments performed on Day -1. Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles). Data points with null value for participants analyzed indicate data not collected for respective category and treatment arm.

Time frame:: Baseline and up to 14 days
Reported as:: Mean · Percentage of red blood cells in blood

Change From Baseline in Hematology Parameter Blood Hematocrit for Part 3
Percentage of red blood cells in blood	Gepotidacin RC 1500 mg Fed	Gepotidacin RC 2250 mg Fed	Gepotidacin RC 3000 mg Fed	Placebo
Hematocrit, Period 1,Day 3 (48 hour), n=10,0,0,2	-0.02 ± 2.170	—	—	-2 ± 0.990
Hematocrit, Period 2,Day 3 (48 hour), n=0,10,0,2	—	-0.65 ± 2.991	—	-3.3 ± 0.424
Hematocrit, Period 3,Day 3 (48 hour), n=0,0,9,2	—	—	0.02 ± 2.299	-2.35 ± 0.495
Hematocrit, Follow-up, n=0,0,9,2	—	—	-1.67 ± 2.545	-1.95 ± 2.333

SecondaryChange From Baseline in Vital Sign Parameters SBP and DBP for Part 3

Time frame:: Baseline and up to 14 days
Reported as:: Mean · millimeters of mercury

Change From Baseline in Vital Sign Parameters SBP and DBP for Part 3
millimeters of mercury	Gepotidacin RC 1500 mg Fed	Gepotidacin RC 2250 mg Fed	Gepotidacin RC 3000 mg Fed	Placebo
SBP, Period 1, Day 1 (2 hours), n=10,0,0,2	4.6 ± 10.94	—	—	6.0 ± 7.07
SBP, Period 1, Day 2 (24 hours), n=10,0,0,2	-4.3 ± 11.13	—	—	0.5 ± 3.54
SBP, Period 1, Day 3 (48 hours), n=10,0,0,2	-4.8 ± 8.63	—	—	-1.5 ± 0.71
SBP, Period 2, Day 1 (2 hours), n=0,10,0,2	—	3.5 ± 11.18	—	10.5 ± 6.36
SBP, Period 2, Day 2 (24 hours), n=0,10,0,2	—	-2.0 ± 9.71	—	6.0 ± 7.07
SBP, Period 2, Day 3 (48 hours), n=0,10,0,2	—	1.2 ± 9.37	—	-3.5 ± 4.95
SBP, Period 3, Day 1 (2 hours), n=0,0,9,2	—	—	7.4 ± 12.89	-1.0 ± 1.41
SBP, Period 3, Day 2 (24 hours), n=0,0,9,2	—	—	4.1 ± 8.19	-0.5 ± 2.12
SBP, Period 3, Day 3 (48 hours), n=0,0,9,2	—	—	-0.7 ± 10.65	0.0 ± 12.73
SBP, Follow-up, n=0,0,9,2	—	—	5.1 ± 7.42	-4.5 ± 3.54
DBP, Period 1, Day 1 (2 hours), n=10,0,0,2	3.4 ± 9.63	—	—	5.0 ± 8.49
DBP, Period 1, Day 2 (24 hours), n=10,0,0,2	-4.4 ± 7.56	—	—	0.0 ± 7.07
DBP, Period 1, Day 3 (48 hours), n=10,0,0,2	-3.7 ± 7.73	—	—	2.0 ± 2.83
DBP, Period 2, Day 1 (2 hours), n=0,10,0,2	—	-3.4 ± 7.73	—	-4.5 ± 0.71
DBP, Period 2, Day 2 (24 hours), n=0,10,0,2	—	-2.6 ± 8.97	—	-4.0 ± 0.00
DBP, Period 2, Day 3 (48 hours), n=0,10,0,2	—	0.7 ± 8.81	—	-4.5 ± 0.71
DBP, Period 3, Day 1 (2 hours), n=0,0,9,2	—	—	-2.8 ± 13.58	4.0 ± 9.90
DBP, Period 3, Day 2 (24 hours), n=0,0,9,2	—	—	-3.2 ± 3.96	4.0 ± 0.00
DBP, Period 3, Day 3 (48 hours), n=0,0,9,2	—	—	-1.3 ± 9.34	3.0 ± 5.66
DBP, Follow-up, n=0,0,9,2	—	—	2.2 ± 9.80	2.5 ± 3.54

SecondaryChange From Baseline in Vital Sign Parameter Heart Rate for Part 3

Time frame:: Baseline and up to 14 days
Reported as:: Mean · beats/minute

Change From Baseline in Vital Sign Parameter Heart Rate for Part 3
beats/minute	Gepotidacin RC 1500 mg Fed	Gepotidacin RC 2250 mg Fed	Gepotidacin RC 3000 mg Fed	Placebo
Heart rate, Period 1, Day 1 (2 hours), n=10,0,0,2	1.6 ± 8.88	—	—	1.0 ± 15.56
Heart rate, Period 2, Day 2 (24 hours), n=10,0,0,2	0.1 ± 7.37	—	—	-4.5 ± 16.26
Heart rate, Period 1, Day 3 (48 hours), n=10,0,0,2	-3.2 ± 8.27	—	—	-4.0 ± 15.56
Heart rate, Period 2, Day 1 (2 hours), n=0,10,0,2	—	4.9 ± 6.47	—	5.0 ± 8.49
Heart rate, Period 2, Day 2 (24 hours), n=0,10,0,2	—	0.9 ± 4.89	—	2.0 ± 7.07
Heart rate, Period 2, Day 3 (48 hours), n=0,10,0,2	—	3.0 ± 4.35	—	-2.5 ± 0.71
Heart rate, Period 3, Day 1 (2 hours), n=0,0,9,2	—	—	4.6 ± 7.65	7.0 ± 11.31
Heart rate, Period 3, Day 2 (24 hours), n=0,0,9,2	—	—	1.1 ± 6.27	0.5 ± 3.54
Heart rate, Period 3, Day 3 (48 hours), n=0,0,9,2	—	—	3.2 ± 9.92	6.5 ± 12.02
Heart rate, Follow-up, n=0,0,9,2	—	—	-4.2 ± 8.83	0.5 ± 0.71

SecondaryChange From Baseline in ECG Parameter Heart Rate for Part 3

Time frame:: Baseline and up to 14 days
Reported as:: Mean · beats/minute

Change From Baseline in ECG Parameter Heart Rate for Part 3
beats/minute	Gepotidacin RC 1500 mg Fed	Gepotidacin RC 2250 mg Fed	Gepotidacin RC 3000 mg Fed	Placebo
ECG Heart rate,Period1,Day 1 (2 hours),n=10,0,0,2	8.0 ± 7.15	—	—	5.0 ± 8.49
ECG Heart rate,Period1,Day 2 (24 hours),n=10,0,0,2	-0.3 ± 4.11	—	—	-4.0 ± 4.24
ECG Heart rate,Period1,Day 3 (48 hours),n=10,0,0,2	4.8 ± 6.75	—	—	0.0 ± 9.90
ECG Heart rate,Period2,Day 1 (2 hours),n=0,10,0,2	—	6.4 ± 8.88	—	10.0 ± 7.07
ECG Heart rate,Period2,Day 2 (24 hours),n=0,10,0,2	—	-0.2 ± 8.78	—	8.0 ± 8.49
ECG Heart rate,Period2,Day 3 (48 hours),n=0,10,0,2	—	-0.5 ± 10.32	—	3.0 ± 5.66
ECG Heart rate,Period3,Day 1 (2 hours),n=0,0,9,2	—	—	8.0 ± 7.04	5.5 ± 6.36
ECG Heart rate,Period3,Day 2 (24 hours),n=0,0,9,2	—	—	4.6 ± 13.61	12.0 ± 15.56
ECG Heart rate,Period3,Day 3 (48 hours),n=0,0,9,2	—	—	1.4 ± 5.98	5.0 ± 9.90
ECG Heart rate, Follow-up, n=0,0,9,2	—	—	-3.8 ± 6.72	-1.0 ± 0.00

SecondaryChange From Baseline in ECG Parameters PR Interval, QRS Duration, QT Interval, QTcB and QTcF for Part 3

A 12 lead ECG was measured in semi-supine position after 5 minutes rest using an ECG machine that measured PR interval, QRS duration, QT interval, QTcB and QTcF for Part 3. Baseline was defined as assessments performed on Day 1 (pre-dose). Change from Baseline was calculated by subtracting the post-dose visit value from the Baseline value. Only those participants with data available at the specified time were analyzed (represented by n=x in the category titles). Data points with null value for participants analyzed indicate data not collected for respective category and treatment arm.

Time frame:: Baseline and up to 14 days
Reported as:: Mean · milliseconds

Change From Baseline in ECG Parameters PR Interval, QRS Duration, QT Interval, QTcB and QTcF for Part 3
milliseconds	Gepotidacin RC 1500 mg Fed	Gepotidacin RC 2250 mg Fed	Gepotidacin RC 3000 mg Fed	Placebo
PR interval, Period1,Day 1 (2 hours),n=10,0,0,2	-3.3 ± 12.58	—	—	-1.0 ± 5.66
PR interval, Period1,Day 2 (24 hours),n=10,0,0,2	-1.9 ± 7.82	—	—	-1.0 ± 5.66
PR interval,Period1,Day 3 (48 hours), n=10,0,0,2	-3.7 ± 9.08	—	—	0.0 ± 4.24
PR interval,Period 2,Day 1 (2 hours),n=0,10,0,2	—	-7.5 ± 12.70	—	-8.5 ± 0.71
PR interval,Period 2, Day 2 (24 hours),n=0,10,0,2	—	-2.2 ± 9.02	—	1.0 ± 4.24
PR interval, Period2, Day 3 (48 hours),n=0,10,0,2	—	-3.5 ± 13.92	—	3.0 ± 1.41
PR interval,Period 3,Day 1 (2 hours),n=0,0,9,2	—	—	-0.1 ± 6.77	-4.0 ± 14.14
PR interval,Period 3,Day 2 (24 hours),n=0,0,9,2	—	—	4.8 ± 13.94	0.5 ± 7.78
PR interval,Period 3,Day 3 (48 hours), n=0,0,9,2	—	—	0.3 ± 16.18	4.0 ± 16.97
PR interval, Follow-up, n=0,0,9,2	—	—	6.1 ± 11.95	-6.0 ± 24.04
QRS duration,Period 1,Day 1 (2 hours),n=10,0,0,2	2.0 ± 10.73	—	—	3.5 ± 9.19
QRS duration,Period 1,Day 2 (24 hours),n=10,0,0,2	4.3 ± 8.63	—	—	-3.0 ± 7.07
QRS duration,Period 1,Day 3 (48 hours),n=10,0,0,2	0.5 ± 10.50	—	—	2.0 ± 4.24
QRS duration,Period 2,Day 1 (2 hours),n=0,10,0,2	—	1.8 ± 4.71	—	2.0 ± 7.07
QRS duration,Period 2, Day 2 (24 hours),n=0,10,0,2	—	0.4 ± 7.07	—	-2.5 ± 19.09
QRS duration,Period 2, Day 3 (48 hours),n=0,10,0,2	—	-1.1 ± 6.40	—	1.5 ± 3.54
QRS duration,Period 3,Day 1(2 hours),n=0,0,9,2	—	—	2.9 ± 4.65	1.5 ± 4.95
QRS duration,Period 3,Day 2(24 hours),n=0,0,9,2	—	—	-2.6 ± 4.39	8.0 ± 8.49
QRS duration,Period3, Day 3(48 hours),n=0,0,9,2	—	—	-1.1 ± 8.74	3.5 ± 14.85
QRS duration, Follow-up, n=0,0,9,2	—	—	-0.7 ± 6.52	4.5 ± 7.78
QT interval,Period 1, Day 1(2 hours),n=10,0,0,2	-9.2 ± 19.47	—	—	-15.0 ± 19.80
QT interval,Period 1,Day 2(24 hours),n=10,0,0,2	7.9 ± 19.45	—	—	-6.0 ± 24.04
QT interval,Period 1, Day 3(48 hours),n=10,0,0,2	0.4 ± 22.89	—	—	-0.5 ± 12.02
QT interval,Period 2, Day 1 (2 hours),n=0,10,0,2	—	-4.0 ± 22.45	—	-14.5 ± 23.33
QT interval,Period 2, Day 2 (24 hours),n=0,10,0,2	—	3.7 ± 15.93	—	-12.5 ± 31.82
QT interval,Period 2, Day 3 (48 hours),n=0,10,0,2	—	0.0 ± 26.86	—	-3.0 ± 2.83
QT interval,Period 3, Day 1 (2 hours),n=0,0,9,2	—	—	-7.9 ± 11.61	-12.5 ± 31.82
QT interval,Period 3, Day 2 (24 hours),n=0,0,9,2	—	—	-6.2 ± 24.03	-15.0 ± 28.28
QT interval,Period 3, Day 3 (48 hours),n=0,0,9,2	—	—	-3.0 ± 15.28	-15.0 ± 36.77
QT interval, Follow-up, n=0,0,9,2	—	—	11.4 ± 17.84	8.5 ± 6.36
QTcB ,Period 1, Day 1 (2 hours), n=10,0,0,2	16.4 ± 25.48	—	—	-1.0 ± 2.83
QTcB, Period 1, Day 2 (24 hours), n=10,0,0,2	8.6 ± 16.10	—	—	-19.5 ± 9.19
QTcB, Period 1, Day 3 (48 hours), n=10,0,0,2	15.7 ± 14.70	—	—	-1.0 ± 19.80
QTcB, Period 2, Day 1 (2 hours), n=0,10,0,2	—	15.1 ± 20.18	—	15.0 ± 8.49
QTcB, Period 2, Day 2 (24 hours), n=0,10,0,2	—	5.1 ± 13.98	—	9.5 ± 12.02
QTcB, Period 2, Day 3 (48 hours), n=0,10,0,2	—	1.8 ± 12.99	—	5.5 ± 13.44
QTcB, Period 3, Day 1 (2 hours), n=0,0,9,2	—	—	14.9 ± 21.83	4.0 ± 14.14
QTcB, Period 3, Day 2 (24 hours), n=0,0,9,2	—	—	5.8 ± 11.14	18.5 ± 12.02
QTcB, Period 3, Day 3 (48 hours), n=0,0,9,2	—	—	2.1 ± 10.02	-3.0 ± 8.49
QTcB, Follow-up, n=0,0,9,2	—	—	1.9 ± 14.88	6.5 ± 6.36
QTcF, Period 1, Day 1 (2 hours), n=10,0,0,2	7.7 ± 20.94	—	—	-6.0 ± 5.66
QTcF, Period 1, Day 2 (24 hours), n=10,0,0,2	8.3 ± 16.09	—	—	-15.0 ± 14.14
QTcF, Period 1, Day 3 (48 hours), n=10,0,0,2	10.5 ± 14.75	—	—	-1.0 ± 8.49
QTcF, Period 2, Day 1 (2 hours), n=0,10,0,2	—	8.4 ± 17.65	—	5.0 ± 14.14
QTcF, Period 2, Day 2 (24 hours), n=0,10,0,2	—	4.5 ± 7.09	—	2.5 ± 19.09
QTcF, Period 2, Day 3 (48 hours), n=0,10,0,2	—	1.2 ± 10.25	—	2.5 ± 7.78
QTcF, Period 3, Day 1 (2 hours), n=0,0,9,2	—	—	6.8 ± 16.15	-1.5 ± 20.51
QTcF, Period 3, Day 2 (24 hours), n=0,0,9,2	—	—	1.2 ± 4.99	7.0 ± 2.83
QTcF, Period 3, Day 3 (48 hours), n=0,0,9,2	—	—	0.2 ± 9.18	-7.0 ± 18.38
QTcF, Follow-up, n=0,0,9,2	—	—	5.2 ± 13.55	7.0 ± 7.07

SecondaryNumber of Participants With Abnormal Values on Urinalysis by Dipstick Analysis Part 3

Urinalysis parameters assessed were urine ketones, urine glucose, urine occult blood, urine pH, urine specific gravity and urine protein. In this dipstick test, the level of ketones, glucose, occult blood, pH, specific gravity and protein in urine samples was recorded as negative trace, 1+, 3+, 5+, 6+, 7+ and 8+ (the plus sign increases with a higher level of ketones, occult blood, pH or specific gravity in the urine: 1+=slightly positive, 3+ to 5+=positive, 6+ and above=high positive). Urine samples were collected for the measurement of urinalysis parameters by dipstick method up-to follow-up (5 to 7 days post last dose) in Part 3. Only categories with significant values have been presented.

Time frame:: Up to 14 days
Reported as:: Count of participants · Participants

Number of Participants With Abnormal Values on Urinalysis by Dipstick Analysis Part 3
Participants	Gepotidacin RC 1500 mg Fed	Gepotidacin RC 2250 mg Fed	Gepotidacin RC 3000 mg Fed	Placebo
Urine Ketones, Follow-up, 1+	0	0	1	0
Urine Occult blood,Trace,Period 1, Day 3 (48hours)	2	0	0	0
Urine Occult blood,Period 1,Day 3 (48hours), 1+	0	0	0	1
Urine Occult blood,Period 1,Day 3 (48hours), 3+	1	0	0	0
Urine Occult blood,Trace,Period 2,Day 3 (48hours)	0	1	0	0
Urine Occult blood,Period 2,Day 3 (48hours), 1+	0	1	0	0
Urine Occult blood,Trace,Period 3,Day 3 (48hours)	0	0	2	0
Urine Occult blood,Period 3,Day 3 (48hours), 1+	0	0	1	0
Urine Occult blood, Follow-up, 4+	0	0	1	0
Urine pH, Period 1 Day 3 (48 hours), 5+	0	0	0	1
Urine pH, Period 1, Day 3 (48 hours), 6+	4	0	0	1
Urine pH, Period 1, Day 3 (48 hours), 7+	5	0	0	1
Urine pH, Period 1, Day 3 (48 hours), 8+	1	0	0	0
Urine pH, Period 2, Day 3 (48 hours), 5+	0	6	0	2
Urine pH, Period 2, Day 3 (48 hours), 6+	0	2	0	0
Urine pH, Period 2, Day 3 (48 hours), 7+	0	2	0	0
Urine pH, Period 3, Day 3 (48 hours), 5+	0	0	3	0
Urine pH, Period 3, Day 3 (48 hours), 6+	0	0	5	2
Urine pH, Period 3, Day 3 (48 hours), 7+	0	0	1	0
Urine pH, Follow-up, 5+	0	0	3	1
Urine pH, Follow-up, 6+	0	0	2	1
Urine pH, Follow-up, 7+	0	0	4	0
Urine Specific gravity, Period1,Day 3(48 hours),1+	10	0	0	2
Urine Specific gravity, Period2,Day 3(48 hours),1+	0	10	0	2
Urine Specific gravity,Period 3,Day 3(48 hours),1+	0	0	9	2
Urine Specific gravity, Follow-up, 1+	0	0	9	2

Adverse events

Collected over Non-serious AEs and SAEs were collected from Day 1 until follow-up (Up to 14 days in Part 1a, 11 days in Part 1b and 2 and 14 days in Part 3).. Non-serious events are listed at a 5% frequency threshold.

Adverse event summary by group
Group	Deaths	Serious	Other
Gepotidacin 1500 mg - R Capsules	0/26 (0%)	0/26 (0%)	8/26 (30.8%)
Gepotidacin 1500 mg RC Tablets	0/26 (0%)	0/26 (0%)	5/26 (19.2%)
Gepotidacin 1500 mg HSWG Tablets	0/26 (0%)	0/26 (0%)	9/26 (34.6%)
Gepotidacin RC 1500 mg Tablets	0/10 (0%)	0/10 (0%)	6/10 (60%)
Gepotidacin RC 3000 mg Tablets	0/10 (0%)	0/10 (0%)	9/10 (90%)
Gepotidacin RC 1500 mg Fed	0/10 (0%)	0/10 (0%)	0/10 (0%)
Gepotidacin RC 2250 mg Fed	0/10 (0%)	0/10 (0%)	1/10 (10%)
Gepotidacin RC 3000 mg Fed	0/9 (0%)	0/9 (0%)	6/9 (66.7%)
Placebo	0/2 (0%)	0/2 (0%)	0/2 (0%)

Most frequent other events

Showing 10 of 13

Most frequent other events
Event	Gepotidacin 1500 mg - R Capsules	Gepotidacin 1500 mg RC Tablets	Gepotidacin 1500 mg HSWG Tablets	Gepotidacin RC 1500 mg Tablets	Gepotidacin RC 3000 mg Tablets	Gepotidacin RC 1500 mg Fed	Gepotidacin RC 2250 mg Fed	Gepotidacin RC 3000 mg Fed	Placebo
DiarrhoeaGastrointestinal disorders	6/26	5/26	6/26	5/10	9/10	0/10	0/10	1/9	0/2
NauseaGastrointestinal disorders	1/26	1/26	2/26	0/10	6/10	0/10	0/10	4/9	0/2
VomitingGastrointestinal disorders	0/26	0/26	0/26	0/10	5/10	0/10	0/10	1/9	0/2
DizzinessNervous system disorders	1/26	0/26	0/26	1/10	4/10	0/10	0/10	1/9	0/2
HeadacheNervous system disorders	0/26	0/26	1/26	2/10	3/10	0/10	0/10	2/9	0/2
Abdominal discomfortGastrointestinal disorders	0/26	0/26	0/26	0/10	0/10	0/10	0/10	2/9	0/2
Faeces softGastrointestinal disorders	0/26	0/26	0/26	0/10	0/10	0/10	1/10	2/9	0/2
Abdominal painGastrointestinal disorders	2/26	2/26	5/26	0/10	1/10	0/10	0/10	0/9	0/2
Abdominal pain upperGastrointestinal disorders	0/26	0/26	0/26	0/10	1/10	0/10	0/10	0/9	0/2
Paraesthesia oralGastrointestinal disorders	0/26	0/26	0/26	0/10	1/10	0/10	0/10	0/9	0/2

Baseline characteristics

Age, Continuous
Age, Continuous(Years)	Total Participants-Part 1a	Total Participants-Part 2	Total Participants- Part 3	Total
Mean	39.5 ± 10.64	55.6 ± 6.43	37.8 ± 7.93	42.5 ± 11.39

Sex: Female, Male
Sex: Female, Male(Participants)	Total Participants-Part 1a	Total Participants-Part 2	Total Participants- Part 3	Total
Female	5	8	6	19
Male	21	2	6	29

Race/Ethnicity, Customized
Race/Ethnicity, Customized(Participants)	Total Participants-Part 1a	Total Participants-Part 2	Total Participants- Part 3	Total
Black or African American	10	0	0	10
White - White/Caucasian/European Heritage	16	0	0	16
Asian - Japanese Heritage	0	10	12	22

Study locations

2 sites

GSK Investigational Site
Anaheim, California 92801, United States
GSK Investigational Site
Austin, Texas 78744, United States

References and documents

Publications

Barth A, Hossain M, Brimhall DB, Perry CR, Tiffany CA, Xu S, Dumont EF. Pharmacokinetics of Oral Formulations of Gepotidacin (GSK2140944), a Triazaacenaphthylene Bacterial Type II Topoisomerase Inhibitor, in Healthy Adult and Adolescent Participants. Antimicrob Agents Chemother. 2022 Jan 18;66(1):e0126321. doi: 10.1128/AAC.01263-21. Epub 2021 Oct 11. PubMed 34633853 ↗

Study documents

Study protocol · Sep 5, 2017
Statistical analysis plan · Nov 27, 2017

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Updates

Tracking since Sep 25, 2026

No changes since tracking began. The registry record was last updated on Oct 8, 2020, before this site started recording changes on Sep 25, 2026. Its history is on ClinicalTrials.gov ↗

Registry details

Key details

Study ID: NCT02853435
Lead sponsor: GlaxoSmithKline
Responsible party: Sponsor
First posted: Aug 3, 2016
Start date: Aug 4, 2016
Primary completion: Oct 17, 2017
Completion: Oct 17, 2017
Results posted: Nov 14, 2018
Last update: Oct 8, 2020

Study contacts

GSK Clinical Trials

study director · GlaxoSmithKline

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Data monitoring committee: No

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To Assess Bioavailability, Food Effect and Pharmacokinetics of Gepotidacin Tablets: A Phase I, Single-Dose, 2 Part Study in Healthy Subjects.

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