CompletedNCT01343706Updated Apr 25, 2024Results posted

Safety Tolerability and Pharmacokinetic of BI 409306

A Phase 1 interventional study of Placebo and Placebo in Healthy, sponsored by Boehringer Ingelheim. Completed at 1 site in Germany. Open to male participants aged 21 Years to 50 Years, including healthy volunteers. Per ClinicalTrials.gov, last updated 2024-04-25.

Sponsored by Boehringer Ingelheim · Phase 1, Interventional, and Treatment

Phase: Phase 1
Study type: Interventional
Enrollment: 80
Allocation: Randomized
Ages: 21 Years to 50 Years
Sex: Male

Study summary

The primary objective of the current study is to investigate the safety and tolerability of BI 409306 in healthy male genotyped volunteers following oral administration of single rising doses.

The secondary objectives are: (1) to explore dose proportionality of BI 409306 as immediate release solid oral dosage, (2) to explore the relative bioavailability of BI 409306 when administered as immediate release solid oral dosage compared to oral drinking solution and (3) to compare the safety and pharmacokinetic profiles between two different groups of genotyped subjects.

Conditions studied

Healthy

In context

Lead sponsor

Boehringer Ingelheim is the lead sponsor of 2,245 studies on the registry; 58 are open to participants now.

Of its 162 completed or terminated interventional studies of FDA-regulated products, 116 (72%) have results posted.

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

Who can participate

Ages eligible: 21 Years to 50 Years
Sexes eligible: Male
Accepts healthy volunteers: Yes

Inclusion criteria

Healthy males according to the following criteria: Based upon a complete medical history, including the physical examination, vital signs (blood pressure (BP), pulse rate (PR)), 12-lead electrocardiogram (ECG), clinical laboratory tests
Age > 21 and Age \< 50 years
Body Mass Index (BMI) > 18.5 and BMI \< 29.9 kg/m2

Exclusion criteria

Exclusion criteria:

Any finding of the medical examination (including BP, PR and ECG) deviating from normal and of clinical relevance
Any evidence of a clinically relevant concomitant disease
Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders
Surgery of the gastrointestinal tract (except appendectomy)
Diseases of the central nervous system (including but not limited to any kind of seizures, stroke or psychiatric disorders) within the past 6 month
History of relevant orthostatic hypotension, fainting spells or blackouts.
Chronic or relevant acute infections
History of relevant allergy/hypersensitivity (including allergy to drug or its excipients)
Use of drugs which might reasonably influence the results of the trial or that prolong the QT/QTc interval based on the knowledge at the time of protocol preparation within 10 days prior to administration or during the trial
Any laboratory value outside the reference range that is of clinical relevance
A marked baseline prolongation of QT/QTc interval (e.g., repeated demonstration of a QTc interval >450 ms);
A history of additional risk factors for Torsades de points (TdP) (e.g., heart failure, hypokalemia, family history of Long QT Syndrome)

Study design

Phase: Phase 1
Primary purpose: Treatment
Allocation: Randomized
Intervention model: Parallel assignment
Masking: Double
Enrollment: 80 participants (actual)

Study arms

Experimental
BI 409306 0.5 mg PiB [EM]
Extensive metaboliser \[EM\] subjects administered one single dose of 0.5 milligram (mg) BI 409306 powder in bottle (PiB) reconstituted for oral solution (0.5 mg /milliliter (mL)) in a volume of 80 mL of the solvent containing aqueous 0.5% tartaric acid solution orally with 240 mL water (160 mL containing the respective diluted volume of reconstituted solution and 80 mL drinking water) after an overnight fast of at least 10 hours.
Drug: BI 409306
Experimental
BI 409306 2 mg PiB [EM]
EM subjects administered one single dose of 2 mg BI 409306 PiB reconstituted for oral solution (0.5 mg/mL) in a volume of 80 mL of the solvent containing aqueous 0.5% tartaric acid solution orally with 240 mL water (160 mL containing the respective diluted volume of reconstituted solution and 80 milliliter drinking water) after an overnight fast of at least 10 hours.
Drug: BI 409306
Experimental
BI 409306 5 mg PiB followed by BI 409306 5 mg Tablet [EM]
EM subjects administered one single dose of 5 mg BI 409306 powder in bottle (PiB) reconstituted for oral solution (0.5 mg/ mL) in a volume of 80 mL of the solvent containing aqueous 0.5% tartaric acid solution orally with 240 mL water (160 mL containing the respective diluted volume of reconstituted solution and 80 mL drinking water) after an overnight fast of at least 10 hours in period 1; followed by a washout period of 5 days; followed by one single dose of 5 mg BI 409306 immediate release tablet administered orally with 240 mL water after an overnight fast of at least 10 hours in period 2.
Drug: BI 409306
Experimental
BI 409306 10 mg Tablet [EM]
EM subjects administered 2 immediate release tablets of 5 mg BI 409306 as a single dose (total dosage: 10 mg) orally with 240 mL water after an overnight fast of at least 10 hours.
Drug: BI 409306
Experimental
BI 409306 25 mg Tablet [EM]
EM subjects administered 5 immediate release tablets of 5 mg BI 409306 as a single dose (total dosage: 25 mg) orally with 240 mL water after an overnight fast of at least 10 hours.
Drug: BI 409306
Experimental
BI 409306 50 mg Tablet followed by BI 409306 50mg PiB [EM]
EM subjects administered one single dose of 50 mg BI 409306 immediate release tablet orally with 240 mL water in period 1; followed by a washout period of 5 days; followed by one single dose of 50 mg BI 409306 powder in bottle (PiB) reconstituted for oral solution (0.5 mg/mL) in a volume of 80 mL of the solvent containing aqueous 0.5% tartaric acid solution administered orally with 240 mL water (160 mL containing the respective diluted volume of reconstituted solution and 80 mL drinking water) after an overnight fast of at least 10 hours in period 2.
Drug: BI 409306
Experimental
BI 409306 100 mg Tablet [EM]
EM subjects administered 2 immediate release tablets of 50 mg BI 409306 as single dose (total dosage: 100 mg) orally with 240 mL water after an overnight fast of at least 10 hours.
Drug: BI 409306
Experimental
BI 409306 200 mg Tablet [EM]
EM subjects administered 1 immediate release tablet of 150 mg and 1 immediate release tablet of 50 mg of BI 409306 together as single dose (total dosage: 200 mg) orally with 240 mL water after an overnight fast of at least 10 hours.
Drug: BI 409306
Experimental
BI 409306 350 mg Tablet [EM]
EM subjects administered 2 immediate release tablet of 150 mg and 1 immediate release tablet of 50 mg of BI 409306 together as single dose (total dosage: 350 mg) orally with 240 mL water after an overnight fast of at least 10 hours.
Drug: BI 409306
Experimental
BI 409306 10 mg Tablet followed by BI 409306 100mg Tablet [PM]
Poor metaboliser \[PM\] subjects administered 2 immediate release tablets of 5 mg BI 409306 as single dose (total dosage: 10 mg) orally with 240 mL water after an overnight fast of at least 10 hours in period 1; followed by washout period of 5 days; followed by 2 immediate release tablets of 50 mg BI 409306 administered as single dose (total dosage: 100 mg) orally with 240 mL water after an overnight fast of at least 10 hours in period 2.
Drug: BI 409306
Placebo comparator
Placebo matching to BI 409306 PiB
Subjects administered one single dose of placebo matching to BI 409306 powder in bottle (PiB) after an overnight fast of at least 10 hours.
Drug: Placebo
Placebo comparator
Placebo matching to BI 409306 film-coated tablet
Subjects administered one single dose of placebo matching to the BI 409306 film-coated tablet (5 milligrams (mg), 50 mg, and 150 mg) orally with 240 mL water after an overnight fast of at least 10 hours.
Drug: Placebo

Interventions

DrugPlacebo
Solution for oral administration
DrugPlacebo
Immediate release solid oral dosage (film-coated tablet)
DrugBI 409306
Immediate release solid oral dosage (film-coated tablet)
DrugBI 409306
solution for oral administration

What researchers measure

Primary outcomes

Percentage of Subjects With Drug-related Adverse Events
Percentage of subjects with investigator defined drug-related Adverse Events (AEs)
Time frame: From first drug administration until 30 days after last drug administration; up to 31 days.
Percentage of Subjects With Clinical Relevant Abnormalities for Physical Examination, Vital Signs, Clinical Laboratory Tests, Oral Body Temperature and ECG
Percentage of subjects with Clinical Relevant abnormalities for Physical examination, Vital Signs blood pressure (BP), pulse rate (PR) respiratory rate (RR), orthostatic test), Clinical laboratory tests (haematology, clinical chemistry and urinalysis), Oral body temperature and ECG were reported.
Time frame: Day 4
Percentage of Subjects Per Category for Assessment of Tolerability by Investigator
The investigator assessed global clinical assessment and tolerability of BI 409306 were reported in possible categories were 'good', 'satisfactory', 'not satisfactory', and 'bad'.
Time frame: Day 4
Change From Baseline in Bond & Lader (B&L) Visual Analogue Scales (VAS)
The B\&L VAS scores were calculated from 16 item with each has a score range from 0 to 10 \[cm\]. The score of each of the 3 categories of effects ("alertness", "calmness", and "contentment") is a weighted average of the scores from the 16 items. The VAS score for alertness/calmness/contentment ranges from 0 to 10 (more alertness/calmness/contentment). The B\&L VAS data was analysed descriptively (change from baseline at 24 hour). The VAS assessment 2 h before drug administration was considered as baseline.
Time frame: At 24 hours

Secondary outcomes

Area Under the Concentration-time Curve of the BI 409306 in Plasma From Time 0 to Time of Last Quantifiable Data Point (AUC0-24)
AUC0-24, Area under the concentration-time curve of the BI 409306 in plasma over the time interval from 0 to the time of the last quantifiable data point is presented as geometric mean (gMean) and geometric coefficient of variation (gCV%). Pharmacokinetic samples were also collected at 48:00 and 72:00 hours after the drug administration for dose groups 10 mg onwards.
Time frame: Pharmacokinetic samples were collected at 2:00 (hour: minute) before 0.167, 0.333, 0.5, 0.75, 1:00, 1.50, 2:00, 2.50, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, and 24:00 hours after the drug administration.
Area Under the Concentration-time Curve of the BI 409306 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞)
AUC0-∞, Area under the concentration-time curve of the BI 409306 in plasma over the time interval from 0 extrapolated to infinity. Pharmacokinetic samples were also collected at 48:00 and 72:00 hours after the drug administration for dose groups 10 mg onwards.
Time frame: Pharmacokinetic samples were collected at 2:00 (hour: minute) before 0.167, 0.333, 0.5, 0.75, 1:00, 1.50, 2:00, 2.50, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, and 24:00 hours after the drug administration.
Maximum Measured Concentration of the BI 409306 in Plasma (Cmax)
Cmax, Maximum measured concentration of the BI 409306 in plasma. Pharmacokinetic samples were also collected at 48:00 and 72:00 hours after the drug administration for dose groups 10 mg onwards.
Time frame: Pharmacokinetic samples were collected at 2:00 (hour: minute) before 0.167, 0.333, 0.5, 0.75, 1:00, 1.50, 2:00, 2.50, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, and 24:00 hours after the drug administration.
Amount of BI 409306 Eliminated in Urine From the Time Point t1 to Time Point t2 (Ae0-4)
Ae0-4, Amount of BI 409306 eliminated in urine from the time point t1(0) to time point t2(4). Urine samples were obtained 24:00 to 48:00 and 48:00 to 72:00 hours after oral administration were obtained only from dose group 10 mg onwards.
Time frame: Urine samples were obtained pre-dose and sampling intervals 0:00 to 4:00, 4:00 to 8:00, 8:00 to 12:00 and 12:00 to 24:00 hours after oral administration.

Results

Posted Mar 12, 2024

Participant flow

In this Phase 1, single centre, placebo-controlled trial (within dose groups), total of 80 healthy subjects were entered and 79 (71 CYP2C19 Extensive metaboliser /8 Poor CYP2C19 metaboliser) subjects were treated in 10 sequential dose groups.

Participant flow — Overall Study
Milestone	Placebo Matching to BI 409306 [EM and PM]	BI 409306 0.5 mg PiB [EM]	BI 409306 2 mg PiB [EM]	BI 409306 5 mg PiB Followed by BI 409306 5 mg Tablet [EM]	BI 409306 10 mg Tablet [EM]	BI 409306 25 mg Tablet [EM]	BI 409306 50 mg Tablet Followed by BI 409306 50mg PiB [EM]	Placebo to BI 409306 50 mg Tablet Followed by BI 409306 50 mg PiB [EM]	BI 409306 100 mg Tablet [EM]	BI 409306 200 mg Tablet [EM]	BI 409306 350 mg Tablet [EM]	BI 409306 10 mg Tablet Followed by BI 409306 100mg Tablet [PM]
Started	18	6	6	6	6	6	6	2	6	6	6	6
Not treated	0	0	0	0	0	0	0	0	1	0	0	0
Completed	18	6	6	6	6	6	6	2	5	6	6	6
Not completed	0	0	0	0	0	0	0	0	1	0	0	0

Outcome measures

PrimaryPercentage of Subjects With Drug-related Adverse Events

Percentage of subjects with investigator defined drug-related Adverse Events (AEs)

Time frame:: From first drug administration until 30 days after last drug administration; up to 31 days.
Reported as:: Number · Percentage of subjects

Percentage of Subjects With Drug-related Adverse Events
Percentage of subjects	Placebo Matching to BI (Period 1)	Placebo Matching to BI (Period 2)	BI 409306 0.5 mg PiB [EM]	BI 409306 2 mg PiB [EM]	BI 409306 5 mg PiB [EM]	BI 409306 5 mg Tablet [EM]	BI 409306 10 mg Tablet [EM]	BI 409306 25 mg Tablet [EM]	BI 409306 50 mg Tablet [EM]	BI 409306 50 mg PiB [EM]	BI 409306 100 mg Tablet [EM]	BI 409306 200 mg Tablet [EM]	BI 409306 350 mg Tablet [EM]	BI 409306 10 mg Tablet [PM]	BI 409306 100 mg Tablet [PM]
Percentage of Subjects With Drug-related Adverse Events	0.0	0.0	0.0	33.3	0.0	16.7	0.0	0.0	0.0	0.0	40.0	66.7	66.7	33.3	50.0

PrimaryPercentage of Subjects With Clinical Relevant Abnormalities for Physical Examination, Vital Signs, Clinical Laboratory Tests, Oral Body Temperature and ECG

Percentage of subjects with Clinical Relevant abnormalities for Physical examination, Vital Signs blood pressure (BP), pulse rate (PR) respiratory rate (RR), orthostatic test), Clinical laboratory tests (haematology, clinical chemistry and urinalysis), Oral body temperature and ECG were reported.

Time frame:: Day 4
Reported as:: Number · Percentage of subjects

Percentage of Subjects With Clinical Relevant Abnormalities for Physical Examination, Vital Signs, Clinical Laboratory Tests, Oral Body Temperature and ECG
Percentage of subjects	Placebo Matching to BI (Period 1)	Placebo Matching to BI (Period 2)	BI 409306 0.5 mg PiB [EM]	BI 409306 2 mg PiB [EM]	BI 409306 5 mg PiB [EM]	BI 409306 5 mg Tablet EM	BI 409306 10 mg Tablet [EM]	BI 409306 25 mg Tablet [EM]	BI 409306 50 mg Tablet [EM]	BI 409306 50 mg PiB [EM]	BI 409306 100 mg Tablet [EM]	BI 409306 200 mg Tablet [EM]	BI 409306 350 mg Tablet [EM]	BI 409306 10 mg Tablet [PM]	BI 409306 100 mg Tablet [PM]
Percentage of Subjects With Clinical Relevant Abnormalities for Physical Examination, Vital Signs, Clinical Laboratory Tests, Oral Body Temperature and ECG	0	0	0	0	0	0	0	0	0	0	0	0	0	0	0

PrimaryPercentage of Subjects Per Category for Assessment of Tolerability by Investigator

The investigator assessed global clinical assessment and tolerability of BI 409306 were reported in possible categories were 'good', 'satisfactory', 'not satisfactory', and 'bad'.

Time frame:: Day 4
Reported as:: Number · Percentage of subjects

Percentage of Subjects Per Category for Assessment of Tolerability by Investigator
Percentage of subjects	BI 409306 2 mg PiB [EM]	BI 409306 50 mg Tablet Followed by BI 409306 50mg PiB [EM]	Placebo to BI 409306 50 mg Tablet Followed by BI 409306 50 mg PiB [EM]	BI 409306 100 mg Tablet [EM]	BI 409306 200 mg Tablet [EM]	BI 409306 350 mg Tablet [EM]	BI 409306 10 mg Tablet Followed by BI 409306 100mg Tablet [PM]
Good	0	6	2	5	6	4	4
Satisfactory	1	0	0	0	0	2	1
Not satisfactory	0	0	0	0	0	0	1
Bad	0	0	0	0	0	0	0
Not assessable	0	0	0	0	0	0	0

PrimaryChange From Baseline in Bond & Lader (B&L) Visual Analogue Scales (VAS)

The B\&L VAS scores were calculated from 16 item with each has a score range from 0 to 10 \[cm\]. The score of each of the 3 categories of effects ("alertness", "calmness", and "contentment") is a weighted average of the scores from the 16 items. The VAS score for alertness/calmness/contentment ranges from 0 to 10 (more alertness/calmness/contentment). The B\&L VAS data was analysed descriptively (change from baseline at 24 hour). The VAS assessment 2 h before drug administration was considered as baseline.

Time frame:: At 24 hours
Reported as:: Least squares mean · Score on a scale

Change From Baseline in Bond & Lader (B&L) Visual Analogue Scales (VAS)
Score on a scale	Placebo Matching to BI (Period 1)	Placebo Matching to BI (Period 2)	BI 409306 0.5 mg PiB [EM]	BI 409306 2 mg PiB [EM]	BI 409306 5 mg PiB [EM]	BI 409306 5 mg Tablet [EM]	BI 409306 10 mg Tablet [EM]	BI 409306 25 mg Tablet [EM]	BI 409306 50 mg Tablet [EM]	BI 409306 50 mg PiB [EM]	BI 409306 100 mg Tablet [EM]	BI 409306 200 mg Tablet [EM]	BI 409306 350 mg Tablet [EM]	BI 409306 10 mg Tablet [PM]	BI 409306 100 mg Tablet [PM]
Alertness	-0.33 ± 1.26	-0.04 ± 0.70	-0.84 ± 1.11	-1.18 ± 0.35	-0.13 ± 0.70	0.09 ± 0.56	-0.33 ± 0.73	-0.07 ± 0.97	-0.92 ± 1.25	-0.56 ± 0.54	-0.26 ± 0.95	-0.80 ± 0.55	-0.21 ± 0.39	-1.02 ± 1.24	-1.88 ± 1.58
Contentment	-0.30 ± 1.09	0.06 ± 0.45	-0.74 ± 1.02	-0.68 ± 0.23	-0.53 ± 0.68	-0.12 ± 0.71	0.04 ± 0.46	0.00 ± 0.76	-0.49 ± 0.84	-0.35 ± 0.75	-0.19 ± 0.73	-0.59 ± 0.59	-0.22 ± 0.50	-0.64 ± 1.23	-0.97 ± 0.71
Calmness	-0.35 ± 1.34	0.02 ± 0.21	-0.48 ± 1.20	-0.91 ± 0.99	-0.45 ± 0.89	-0.14 ± 1.59	0.25 ± 1.04	-0.39 ± 0.55	-0.75 ± 1.35	-0.47 ± 1.71	0.05 ± 1.31	-0.55 ± 1.55	-0.17 ± 0.34	-0.47 ± 1.06	-0.38 ± 0.59

SecondaryArea Under the Concentration-time Curve of the BI 409306 in Plasma From Time 0 to Time of Last Quantifiable Data Point (AUC0-24)

AUC0-24, Area under the concentration-time curve of the BI 409306 in plasma over the time interval from 0 to the time of the last quantifiable data point is presented as geometric mean (gMean) and geometric coefficient of variation (gCV%). Pharmacokinetic samples were also collected at 48:00 and 72:00 hours after the drug administration for dose groups 10 mg onwards.

Time frame:: Pharmacokinetic samples were collected at 2:00 (hour: minute) before 0.167, 0.333, 0.5, 0.75, 1:00, 1.50, 2:00, 2.50, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, and 24:00 hours after the drug administration.
Reported as:: Geometric mean · nanomol*hour/Litre [nmol*h/L]

Area Under the Concentration-time Curve of the BI 409306 in Plasma From Time 0 to Time of Last Quantifiable Data Point (AUC0-24)
nanomolhour/Litre [nmolh/L]	BI 409306 0.5 mg PiB [EM]	BI 409306 2 mg PiB [EM]	BI 409306 5 mg PiB [EM]	BI 409306 5 mg Tablet [EM]	BI 409306 10 mg Tablet [EM]	BI 409306 25 mg Tablet [EM]	BI 409306 50 mg Tablet [EM]	BI 409306 50 mg PiB [EM]	BI 409306 100 mg Tablet [EM]	BI 409306 200 mg Tablet [EM]	BI 409306 350 mg Tablet [EM]	BI 409306 10 mg Tablet [PM]	BI 409306 100 mg Tablet [PM]
Area Under the Concentration-time Curve of the BI 409306 in Plasma From Time 0 to Time of Last Quantifiable Data Point (AUC0-24)	3.96 ± 50.3	20.90 ± 41.30	76.70 ± 27.00	75.60 ± 32.29	96.00 ± 69.90	351.00 ± 49.30	539.00 ± 82.00	648.00 ± 42.90	1460.00 ± 68.50	3920.00 ± 44.40	7980.00 ± 17.10	476.00 ± 35.40	6060.00 ± 21.40

SecondaryArea Under the Concentration-time Curve of the BI 409306 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞)

AUC0-∞, Area under the concentration-time curve of the BI 409306 in plasma over the time interval from 0 extrapolated to infinity. Pharmacokinetic samples were also collected at 48:00 and 72:00 hours after the drug administration for dose groups 10 mg onwards.

Time frame:: Pharmacokinetic samples were collected at 2:00 (hour: minute) before 0.167, 0.333, 0.5, 0.75, 1:00, 1.50, 2:00, 2.50, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, and 24:00 hours after the drug administration.
Reported as:: Geometric mean · nanomol*hour/Litre [nmol*h/L]

Area Under the Concentration-time Curve of the BI 409306 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞)
nanomolhour/Litre [nmolh/L]	BI 409306 0.5 mg PiB [EM]	BI 409306 2 mg PiB [EM]	BI 409306 5 mg PiB [EM]	BI 409306 5 mg Tablet [EM]	BI 409306 10 mg Tablet [EM]	BI 409306 25 mg Tablet [EM]	BI 409306 50 mg Tablet [EM]	BI 409306 50 mg PiB [EM]	BI 409306 100 mg Tablet [EM]	BI 409306 200 mg Tablet [EM]	BI 409306 350 mg Tablet [EM]	BI 409306 10 mg Tablet [PM]	BI 409306 100 mg Tablet [PM]
Area Under the Concentration-time Curve of the BI 409306 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞)	3.95 ± 50.40	20.90 ± 41.30	76.70 ± 27.00	75.60 ± 32.20	95.90 ± 69.80	351.00 ± 49.40	539.00 ± 82.00	648.00 ± 42.90	1460.00 ± 68.50	3920.00 ± 44.40	7980.00 ± 17.10	476.00 ± 35.50	6060.00 ± 21.40

SecondaryMaximum Measured Concentration of the BI 409306 in Plasma (Cmax)

Cmax, Maximum measured concentration of the BI 409306 in plasma. Pharmacokinetic samples were also collected at 48:00 and 72:00 hours after the drug administration for dose groups 10 mg onwards.

Time frame:: Pharmacokinetic samples were collected at 2:00 (hour: minute) before 0.167, 0.333, 0.5, 0.75, 1:00, 1.50, 2:00, 2.50, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, and 24:00 hours after the drug administration.
Reported as:: Geometric mean · nanomol/Litre (nmol/L)

Maximum Measured Concentration of the BI 409306 in Plasma (Cmax)
nanomol/Litre (nmol/L)	BI 409306 0.5 mg PiB [EM]	BI 409306 2 mg PiB [EM]	BI 409306 5 mg PiB [EM]	BI 409306 5 mg Tablet [EM]	BI 409306 10 mg Tablet [EM]	BI 409306 25 mg Tablet [EM]	BI 409306 50 mg Tablet [EM]	BI 409306 50 mg PiB [EM]	BI 409306 100 mg Tablet [EM]	BI 409306 200 mg Tablet [EM]	BI 409306 350 mg Tablet [EM]	BI 409306 10 mg Tablet [PM]	BI 409306 100 mg Tablet [PM]
Maximum Measured Concentration of the BI 409306 in Plasma (Cmax)	3.54 ± 34.50	18.80 ± 50.80	56.40 ± 36.40	55.90 ± 40.90	99.80 ± 79.10	300.00 ± 85.00	479.00 ± 67.00	613.00 ± 40.70	1370.00 ± 87.30	2950.00 ± 89.50	5540.00 ± 29.50	223.00 ± 38.10	3120.00 ± 31.40

SecondaryAmount of BI 409306 Eliminated in Urine From the Time Point t1 to Time Point t2 (Ae0-4)

Ae0-4, Amount of BI 409306 eliminated in urine from the time point t1(0) to time point t2(4). Urine samples were obtained 24:00 to 48:00 and 48:00 to 72:00 hours after oral administration were obtained only from dose group 10 mg onwards.

Time frame:: Urine samples were obtained pre-dose and sampling intervals 0:00 to 4:00, 4:00 to 8:00, 8:00 to 12:00 and 12:00 to 24:00 hours after oral administration.
Reported as:: Geometric mean · nanomol [nmol]

Amount of BI 409306 Eliminated in Urine From the Time Point t1 to Time Point t2 (Ae0-4)
nanomol [nmol]	BI 409306 0.5 mg PiB [EM]	BI 409306 2 mg PiB [EM]	BI 409306 5 mg PiB [EM]	BI 409306 5 mg Tablet [EM]	BI 409306 10 mg Tablet [EM]	BI 409306 25 mg Tablet [EM]	BI 409306 50 mg Tablet [EM]	BI 409306 50 mg PiB [EM]	BI 409306 100 mg Tablet [EM]	BI 409306 200 mg Tablet [EM]	BI 409306 350 mg Tablet [EM]	BI 409306 10 mg Tablet [PM]	BI 409306 100 mg Tablet [PM]
Amount of BI 409306 Eliminated in Urine From the Time Point t1 to Time Point t2 (Ae0-4)	—	31.00 ± 46.50	93.60 ± 26.00	98.10 ± 24.20	148.00 ± 60.20	—	840.00 ± 56.90	953.00 ± 48.10	1920.00 ± 53.00	4340.00 ± 48.80	8830.00 ± 24.00	418.00 ± 14.30	5700.00 ± 23.30

Adverse events

Collected over From first drug administration until 30 days after last drug administration; up to 31 days.. Non-serious events are listed at a 5% frequency threshold.

Adverse event summary by group
Group	Deaths	Serious	Other
Placebo Matching to BI (Period 1)	0/20 (0%)	0/20 (0%)	2/20 (10%)
Placebo Matching to BI (Period 2)	0/4 (0%)	0/4 (0%)	1/4 (25%)
BI 409306 0.5 mg PiB [EM]	0/6 (0%)	0/6 (0%)	0/6 (0%)
BI 409306 2 mg PiB [EM]	0/6 (0%)	0/6 (0%)	2/6 (33.3%)
BI 409306 5 mg PiB [EM]	0/6 (0%)	0/6 (0%)	0/6 (0%)
BI 409306 5 mg Tablet [EM]	0/6 (0%)	0/6 (0%)	1/6 (16.7%)
BI 409306 10 mg Tablet [EM]	0/6 (0%)	0/6 (0%)	0/6 (0%)
BI 409306 25 mg Tablet [EM]	0/6 (0%)	0/6 (0%)	0/6 (0%)
BI 409306 50 mg Tablet [EM]	0/6 (0%)	0/6 (0%)	2/6 (33.3%)
BI 409306 50mg PiB [EM]	0/8 (0%)	0/8 (0%)	0/8 (0%)
BI 409306 100 mg Tablet [EM]	0/5 (0%)	0/5 (0%)	2/5 (40%)
BI 409306 200 mg Tablet [EM]	0/6 (0%)	0/6 (0%)	4/6 (66.7%)
BI 409306 350 mg Tablet [EM]	0/6 (0%)	0/6 (0%)	4/6 (66.7%)
BI 409306 10 mg Tablet [PM]	0/6 (0%)	0/6 (0%)	3/6 (50%)
BI 409306 100 mg Tablet [PM]	0/6 (0%)	0/6 (0%)	3/6 (50%)

Most frequent other events

Showing 10 of 19

Most frequent other events
Event	Placebo Matching to BI (Period 1)	Placebo Matching to BI (Period 2)	BI 409306 0.5 mg PiB [EM]	BI 409306 2 mg PiB [EM]	BI 409306 5 mg PiB [EM]	BI 409306 5 mg Tablet [EM]	BI 409306 10 mg Tablet [EM]	BI 409306 25 mg Tablet [EM]	BI 409306 50 mg Tablet [EM]	BI 409306 50mg PiB [EM]	BI 409306 100 mg Tablet [EM]	BI 409306 200 mg Tablet [EM]	BI 409306 350 mg Tablet [EM]	BI 409306 10 mg Tablet [PM]	BI 409306 100 mg Tablet [PM]
PhotopsiaEye disorders	0/20	0/4	0/6	0/6	0/6	0/6	0/6	0/6	0/6	0/8	1/5	2/6	2/6	0/6	1/6
HeadacheNervous system disorders	1/20	0/4	0/6	1/6	0/6	1/6	0/6	0/6	0/6	0/8	0/5	1/6	0/6	2/6	2/6
DizzinessNervous system disorders	0/20	1/4	0/6	1/6	0/6	0/6	0/6	0/6	0/6	0/8	0/5	0/6	0/6	0/6	0/6
Sinus tachycardiaCardiac disorders	0/20	0/4	0/6	0/6	0/6	0/6	0/6	0/6	0/6	0/8	1/5	0/6	1/6	0/6	0/6
PhotophobiaEye disorders	0/20	0/4	0/6	0/6	0/6	0/6	0/6	0/6	0/6	0/8	1/5	1/6	1/6	0/6	0/6
ParaesthesiaNervous system disorders	0/20	0/4	0/6	0/6	0/6	0/6	0/6	0/6	0/6	0/8	1/5	0/6	0/6	0/6	0/6
ParosmiaNervous system disorders	0/20	0/4	0/6	0/6	0/6	0/6	0/6	0/6	0/6	0/8	1/5	0/6	0/6	0/6	0/6
ExtrasystolesCardiac disorders	0/20	0/4	0/6	0/6	0/6	0/6	0/6	0/6	1/6	0/8	0/5	0/6	0/6	0/6	0/6
PalpitationsCardiac disorders	0/20	0/4	0/6	0/6	0/6	0/6	0/6	0/6	1/6	0/8	0/5	0/5	0/6	0/6	0/6
ChromatopsiaEye disorders	0/20	0/4	0/6	0/6	0/6	0/6	0/6	0/6	0/6	0/8	0/5	0/6	1/6	0/6	1/6

Baseline characteristics

Treated set (TS): The treated set includes all subjects who were dispensed study medication and were documented to have taken at least one dose of investigational treatment.

Age, Continuous
Age, Continuous(Years)	Placebo Matching to BI 409306 [EM and PM]	BI 409306 0.5 mg PiB [EM]	BI 409306 2 mg PiB [EM]	BI 409306 5 mg PiB Followed by BI 409306 5 mg Tablet [EM]	BI 409306 10 mg Tablet [EM]	BI 409306 25 mg Tablet [EM]	BI 409306 50 mg Tablet Followed by BI 409306 50mg PiB [EM]	Placebo to BI 409306 50 mg Tablet Followed by BI 409306 50 mg PiB [EM]	BI 409306 100 mg Tablet [EM]	BI 409306 200 mg Tablet [EM]	BI 409306 350 mg Tablet [EM]	BI 409306 10 mg Tablet Followed by BI 409306 100mg Tablet [PM]	Total
Mean	38.2 ± 5.6	36.5 ± 9.2	37.5 ± 6.5	35.7 ± 8.2	30.5 ± 5.9	32.2 ± 6.5	40.3 ± 6.1	37.5 ± 3.5	31.4 ± 7.3	38.5 ± 6.7	39.2 ± 8.8	39.5 ± 7.5	36.7 ± 7.1

Sex: Female, Male
Sex: Female, Male(Participants)	Placebo Matching to BI 409306 [EM and PM]	BI 409306 0.5 mg PiB [EM]	BI 409306 2 mg PiB [EM]	BI 409306 5 mg PiB Followed by BI 409306 5 mg Tablet [EM]	BI 409306 10 mg Tablet [EM]	BI 409306 25 mg Tablet [EM]	BI 409306 50 mg Tablet Followed by BI 409306 50mg PiB [EM]	Placebo to BI 409306 50 mg Tablet Followed by BI 409306 50 mg PiB [EM]	BI 409306 100 mg Tablet [EM]	BI 409306 200 mg Tablet [EM]	BI 409306 350 mg Tablet [EM]	BI 409306 10 mg Tablet Followed by BI 409306 100mg Tablet [PM]	Total
Female	0	0	0	0	0	0	0	0	0	0	0	0	0
Male	18	6	6	6	6	6	6	2	5	6	6	6	79

Race (NIH/OMB)
Race (NIH/OMB)(Participants)	Placebo Matching to BI 409306 [EM and PM]	BI 409306 0.5 mg PiB [EM]	BI 409306 2 mg PiB [EM]	BI 409306 5 mg PiB Followed by BI 409306 5 mg Tablet [EM]	BI 409306 10 mg Tablet [EM]	BI 409306 25 mg Tablet [EM]	BI 409306 50 mg Tablet Followed by BI 409306 50mg PiB [EM]	Placebo to BI 409306 50 mg Tablet Followed by BI 409306 50 mg PiB [EM]	BI 409306 100 mg Tablet [EM]	BI 409306 200 mg Tablet [EM]	BI 409306 350 mg Tablet [EM]	BI 409306 10 mg Tablet Followed by BI 409306 100mg Tablet [PM]	Total
American Indian or Alaska Native	0	0	0	0	0	0	0	0	0	0	0	0	0
Asian	0	0	0	0	0	0	0	0	0	0	0	0	0
Native Hawaiian or Other Pacific Islander	0	0	0	0	0	0	0	0	0	0	0	0	0
Black or African American	0	0	0	0	0	0	0	0	0	0	0	0	0
White	18	6	6	6	6	6	6	2	5	6	6	6	79
More than one race	0	0	0	0	0	0	0	0	0	0	0	0	0
Unknown or Not Reported	0	0	0	0	0	0	0	0	0	0	0	0	0

Study locations

1 site

1289.1.1 Boehringer Ingelheim Investigational Site
Ingelheim, Germany

References and documents

Individual participant data

Plan to share: No — Clinical studies sponsored by Boehringer Ingelheim, phases I to IV, interventional and non-interventional, are in scope for sharing of the raw clinical study data and clinical study documents. Exceptions might apply, e.g. studies in products where Boehringer Ingelheim is not the license holder; studies regarding pharmaceutical formulations and associated analytical methods, and studies pertinent to pharmacokinetics using human biomaterials; studies conducted in a single center or targeting rare diseases (in case of low number of patients and therefore limitations with anonymization). For more details refer to: https://www.mystudywindow.com/msw/datatransparency

No publications or documents are linked to this record.

Updates

Tracking since Sep 25, 2026

No changes since tracking began. The registry record was last updated on Apr 25, 2024, before this site started recording changes on Sep 25, 2026. Its history is on ClinicalTrials.gov ↗

Registry details

Key details

Study ID: NCT01343706
Lead sponsor: Boehringer Ingelheim
Responsible party: Sponsor
First posted: Apr 28, 2011
Start date: Apr 1, 2011
Primary completion: Aug 1, 2011
Completion: Aug 5, 2011
Results posted: Mar 12, 2024
Last update: Apr 25, 2024

Study contacts

Boehringer Ingelheim

study chair · Boehringer Ingelheim

View the source record on ClinicalTrials.gov ↗

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