A Phase 1 interventional study of Fosnetupitant 235 mg solution and Akynzeo solution in Healthy Volunteers, sponsored by Helsinn Healthcare SA. Terminated at 1 site in Switzerland. Open to participants aged 18 Years to 55 Years, including healthy volunteers. Per ClinicalTrials.gov, last updated 2025-05-04.
Sponsored by Helsinn Healthcare SA · Phase 1, Interventional, and Health services research
This clinical trial will include two parts, i.e., Part A and Part B.
The goal of the Part A is to define the shortest safe and tolerable duration of an intravenous injection of Fosnetupitant 235 mg solution among 4 durations tested in male and female adult healthy volunteers. In study part A, researchers will compare Fosnetupitant 235 mg solution to Akynzeo® solution.
The duration determined in Part A will be investigated in study Part B.
The Part B of the study was not performed.
The registered product Akynzeo® (235 mg fosnetupitant/0.25 mg palonosetron) solution for intravenous injection, used before chemotherapy, is to be diluted up to a final volume of 50 mL and administered during 30 min infusion. With the aim to facilitate and improve the use of this kind of products, the Sponsor Helsinn focused on the development of a ready to use solution, not requiring additional dilutions, and to be administered as a bolus injection. The product developed by Helsinn is a liquid formulation for infusion, containing exclusively fosnetupitant 235 mg free base.
Aim of the present open label, single dose, two parts (part A and part B) phase I study is to evaluate the safety and the pharmacokinetic profile of this new product, i.e., Fosnetupitant 235 mg ready to use solution for intravenous injection. In addition, the pharmacokinetic profile of fosnetupitant, netupitant (fosnetupitant is rapidly converted in netupitant after intravenous administration) and netupitant metabolites (M1, M2 and M3) will be investigated after a 30-min infusion of the registered Akynzeo® liquid formulation.
Part A of the study:
In cohort 1, 10 healthy volunteers will receive a dose of Fosnetupitant 235 mg solution as a one single 30-min intravenous infusion and additional 10 subjects will receive a single intravenous dose of Akynzeo® solution as a one single 30-min intravenous infusion, according to a parallel group design.
In each of 3 consecutive cohorts (cohorts 2, 3 and 4), 10 healthy volunteers will receive a single intravenous dose of Fosnetupitant 235 mg solution at a predefined infusion duration and will be sequentially treated as 3 subgroups of 3, 3, and 4 subjects, respectively.
A staggered approach with decreasing infusion time duration will be applied, from cohort 1 to cohort 4, to the administration of Fosnetupitant free base 235 mg solution, as follows:
Cohort 1: 30 min Cohort 2: 15 min Cohort 3: 5 min Cohort 4: 2 min
At the end of cohort 1 and of each subgroup of cohorts 2, 3 and 4, safety and tolerability results will be evaluated by the Investigator and the study Sponsor Medical Expert. Predefined stopping rules will be considered for deciding about continuing with the next cohort treatment and a shorter injection duration of Fosnetupitant 235 mg solution. Specifically, after cohort 1, if the injection duration of 30 min proves to be safe and well tolerated, 15 min injection duration will be tested in cohort 2. If the injection duration of 15 min proves to be safe and well-tolerated, 5 min injection duration will be tested in cohort 3. If the injection duration of 5 min proves to be safe and well tolerated, a 2 min injection will be tested in cohort 4.
The selected shortest (safe and tolerable) injection duration determined in Part A will be investigated in study Part B.
The study was prematurely terminated after the end of Part A and study Part B was not performed.
Helsinn Healthcare SA is the lead sponsor of 32 studies on the registry; 1 is open to participants now.
Of its 8 completed or terminated interventional studies of FDA-regulated products, 7 (88%) have results posted.
Counted across the registry records on this site, refreshed daily.
Go through the criteria one by one — yes, no or not sure — and take the list to your doctor or the study team. Kept in this browser only.
and fertility (women only): women of defined as a non-menopausal woman who has not had a bilateral oophorectomy or medically documented ovarian failure and/or at risk for pregnancy must agree, signing the informed consent form, to use a highly effective method of contraception throughout the study and to continue for 14 days after the last dose of the study treatment. Highly effective contraceptive measures include:
Women of non-child-bearing potential or in status defined as such when there is either:
Contraception (men only): men will either be sterile or agree to use one of the following approved methods of contraception from the first study drug administration until at least 14 days after the last administration, also in case their partner is currently pregnant:
Exclusion criteria
Underlined terms in the criteria open these too. Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Before you join, the study team explains what taking part involves — its purpose, what happens, the risks and possible benefits — and answers your questions, so you can decide freely. Consent is usually recorded on a form (the informed consent form, ICF) signed by you or, where the law allows, by someone legally authorised to decide for you.
You can keep asking questions during the study, you are told of new information that matters, and you can choose to leave at any time.
Weight in kilograms divided by height in metres squared. Example: 70 kg and 1.75 m gives 70 ÷ (1.75 × 1.75) ≈ 22.9.
What counts as overweight or obesity differs between countries (some use lower cut-offs), so go by the range the study states.
Ways of preventing pregnancy. “Highly effective” methods fail less than 1% of the time a year when used correctly — for example an IUD or an implant.
Criteria usually say which methods count and how long to keep using them after the last dose, sometimes for male participants too. Some studies accept a partner’s vasectomy if it was confirmed successful and that person is the participant’s only sexual partner.
Able to become pregnant: from the first period until menopause, unless permanently unable to through surgery (removal of the womb, or of both ovaries or both fallopian tubes).
Criteria for people of childbearing potential usually ask for a negative pregnancy test and for contraception during the study and for a time after it.
Periods have stopped for good: usually no period for 12 months in a row without another medical reason, sometimes confirmed by a blood test (FSH).
A recording of the heart’s electrical activity, taken with stickers on the chest, arms and legs. It takes a few minutes and does not hurt.
Judged by the study doctor to matter for your health or for the study. It is a doctor’s decision, so ask the study team if you are unsure whether something counts.
On an ECG, the QT interval is the time the heart’s lower chambers take to activate electrically and recover in each beat. QTc is that time adjusted for heart rate (QTcF by Fridericia’s formula, QTcB by Bazett’s). Some medicines lengthen it, and a long QTc can raise the risk of a dangerous heart rhythm.
The study may name a correction formula and a limit in milliseconds, often around 450–480.
An allergy, or another reaction of the immune system, to a substance. “Hypersensitivity to the study drug” means a known allergic reaction to it — not every side effect a medicine can have.
CYP3A is a group of enzymes, mainly CYP3A4, in the liver and gut that break down many medicines. Some medicines, supplements and foods (grapefruit, St John’s wort) slow them down or speed them up, which changes how much of a study drug stays in the body.
Studies list them so they can be avoided or switched; bring a list of everything you take, including supplements.
A drug or device being studied in a clinical trial.
It may be new, or already approved and being studied for another use, dose or form. Criteria often leave out people who took part in another study of one within a recent period, commonly 30 days or five half-lives.
Informed consent
Before you join, the study team explains what taking part involves — its purpose, what happens, the risks and possible benefits — and answers your questions, so you can decide freely. Consent is usually recorded on a form (the informed consent form, ICF) signed by you or, where the law allows, by someone legally authorised to decide for you.
You can keep asking questions during the study, you are told of new information that matters, and you can choose to leave at any time.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
BMI (body mass index)
Weight in kilograms divided by height in metres squared. Example: 70 kg and 1.75 m gives 70 ÷ (1.75 × 1.75) ≈ 22.9.
What counts as overweight or obesity differs between countries (some use lower cut-offs), so go by the range the study states.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Contraception
Ways of preventing pregnancy. “Highly effective” methods fail less than 1% of the time a year when used correctly — for example an IUD or an implant.
Criteria usually say which methods count and how long to keep using them after the last dose, sometimes for male participants too. Some studies accept a partner’s vasectomy if it was confirmed successful and that person is the participant’s only sexual partner.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Childbearing potential
Able to become pregnant: from the first period until menopause, unless permanently unable to through surgery (removal of the womb, or of both ovaries or both fallopian tubes).
Criteria for people of childbearing potential usually ask for a negative pregnancy test and for contraception during the study and for a time after it.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Postmenopausal
Periods have stopped for good: usually no period for 12 months in a row without another medical reason, sometimes confirmed by a blood test (FSH).
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
ECG (electrocardiogram)
A recording of the heart’s electrical activity, taken with stickers on the chest, arms and legs. It takes a few minutes and does not hurt.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Clinically significant
Judged by the study doctor to matter for your health or for the study. It is a doctor’s decision, so ask the study team if you are unsure whether something counts.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
QT and QTc
On an ECG, the QT interval is the time the heart’s lower chambers take to activate electrically and recover in each beat. QTc is that time adjusted for heart rate (QTcF by Fridericia’s formula, QTcB by Bazett’s). Some medicines lengthen it, and a long QTc can raise the risk of a dangerous heart rhythm.
The study may name a correction formula and a limit in milliseconds, often around 450–480.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Hypersensitivity
An allergy, or another reaction of the immune system, to a substance. “Hypersensitivity to the study drug” means a known allergic reaction to it — not every side effect a medicine can have.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
CYP3A (CYP3A4) inhibitors and inducers
CYP3A is a group of enzymes, mainly CYP3A4, in the liver and gut that break down many medicines. Some medicines, supplements and foods (grapefruit, St John’s wort) slow them down or speed them up, which changes how much of a study drug stays in the body.
Studies list them so they can be avoided or switched; bring a list of everything you take, including supplements.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Investigational drug or device
A drug or device being studied in a clinical trial.
It may be new, or already approved and being studied for another use, dose or form. Criteria often leave out people who took part in another study of one within a recent period, commonly 30 days or five half-lives.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Fosnetupitant free base 235 mg administered as single 30 min intravenous infusion or 235 mg fosnetupitant/0.25 mg palonosetron in 20 mL injection solution administered undiluted as a single 30 min intravenous infusion
Drug: Fosnetupitant 235 mg solution · Drug: Akynzeo solution
Fosnetupitant free base 235 mg administered as single 15 min intravenous infusion
Drug: Fosnetupitant 235 mg solution
Fosnetupitant free base 235 mg administered as single 5 min intravenous infusion
Drug: Fosnetupitant 235 mg solution
Fosnetupitant free base 235 mg administered as single 2 min intravenous infusion
Drug: Fosnetupitant 235 mg solution
Fosnetupitant free base 235 mg (corresponding to 260 mg of the chloride hydrochloride salt) in 20 mL ready to use injectable solution for intravenous administration
Also known as: Helsinn Fosnetupitant solution
235 mg fosnetupitant (corresponding to 260 mg of the chloride hydrochloride salt) / 0.25 mg palonosetron in 20 mL injectable solution
Also known as: IV Akynzeo®
Study Part A: Number of Treatment-emergent Adverse Events
Number of treatment-emergent adverse events (TEAEs) collected up to 24 h post-dose.
Time frame: From screening visit (day of informed consent signature) up to 24 h after the investigational medicinal product administration (a maximum of 21 days)
Study Part A: Number of Subjects With Treatment-emergent Adverse Events
Number of subjects with treatment-emergent adverse events (TEAEs) collected up to 24 h post-dose.
Time frame: From screening visit (day of informed consent signature) up to 24 h after the investigational medicinal product administration (a maximum of 21 days)
Study Part A: Type of Treatment-emergent Adverse Events
Type of treatment-emergent adverse events (TEAEs) collected up to 24 h post-dose.
Time frame: From screening visit (day of informed consent signature) up to 24 h after the investigational medicinal product administration (a maximum of 21 days)
Study Part A: Systolic Blood Pressure
Systolic blood pressure in mmHg measured after 5 min at rest in sitting position
Time frame: Screening visit/day -1 (enrolment day)/day 1 (treatment day) at pre-administration, at the end of administration and 1, 2, 4, 24 h after the end of administration/final visit (7 days after the treatment)
Study Part A: Diastolic Blood Pressure
Diastolic blood pressure in mmHg measured after 5 min at rest in sitting position
Time frame: Screening visit/day -1 (enrolment day)/day 1 (treatment day) at pre-administration, at the end of administration and 1, 2, 4, 24 h after the end of administration/final visit (7 days after the treatment)
Study Part A: Pulse Rate
Pulse rate in bpm measured after 5 min at rest in sitting position
Time frame: Screening visit/day -1 (enrolment day)/day 1 (treatment day) at pre-administration, at the end of administration and 1, 2, 4, 24 h after the end of administration/final visit (7 days after the treatment)
Study Part A: Weight
Body weight in kilograms
Time frame: Screening visit (day of informed consent signature)/final visit (7 days after the treatment)
Study Part A: Full Physical Examination Through Apparatus/Systems Check
General appearance, Chest/respiratory, Gastrointestinal, Head, eyes, ears, nose and throat, Heart/cardiovascular, Lymph nodes, Metabolic/endocrine, Musculoskeletal/extremities, Neck (including thyroid), Neurological/psychiatric, Skin/dermatologic systems are checked. Any abnormalities are recorded.
Time frame: Screening visit (day of informed consent signature)/final visit (7 days after the treatment)
Study Part A: Short Physical Examination Through Apparatus/Systems Check
General appearance, Chest/respiratory, Heart/cardiovascular, Lymph nodes, Neurologic/psychiatric, Skin/dermatologic systems are checked. Any abnormalities are recorded.
Time frame: Day 2 (24 h after the end of investigational product administration)
Study Part A: ECGs - Heart Rate
Heart rate in beats/min recorded in supine position after 5 min at rest
Time frame: Screening visit/ day 1 (treatment day) at pre-administration, at the end of administration and 1, 2, 4, 24 h after the end of administration/final visit (7 days after the treatment)
Study Part A: ECGs - PR Interval
PR interval in ms recorded in supine position after 5 min at rest
Time frame: Screening visit/ day 1 (treatment day) at pre-administration, at the end of administration and 1, 2, 4, 24 h after the end of administration/final visit (7 days after the treatment)
Study Part A: ECGs - RR Interval
RR interval in ms recorded in supine position after 5 min at rest
Time frame: Screening visit/ day 1 (treatment day) at pre-administration, at the end of administration and 1, 2, 4, 24 h after the end of administration/final visit (7 days after the treatment)
Study Part A: ECGs - QRS Duration
QRS duration in ms recorded in supine position after 5 min at rest
Time frame: Screening visit/ day 1 (treatment day) at pre-administration, at the end of administration and 1, 2, 4, 24 h after the end of administration/final visit (7 days after the treatment)
Study Part A: ECGs - QT Interval
QT interval in ms recorded in supine position after 5 min at rest
Time frame: Screening visit/ day 1 (treatment day) at pre-administration, at the end of administration and 1, 2, 4, 24 h after the end of administration/final visit (7 days after the treatment)
Study Part A: ECGs - QTcB Interval
QTcB interval in ms recorded in supine position after 5 min at rest
Time frame: Screening visit/ day 1 (treatment day) at pre-administration, at the end of administration and 1, 2, 4, 24 h after the end of administration/final visit (7 days after the treatment)
Study Part A: ECGs - QTcF Interval
QTcF interval in ms recorded in supine position after 5 min at rest
Time frame: Screening visit/ day 1 (treatment day) at pre-administration, at the end of administration and 1, 2, 4, 24 h after the end of administration/final visit (7 days after the treatment)
Study Part A: Clinical Laboratory Tests (Blood Chemistry, Haematology, Urinalysis)
Leukocytes and leukocyte differential count, erythrocytes, haemoglobin, haematocrit, MCV, MCH, MCHC, thrombocytes, electrolytes (sodium, potassium, calcium, chloride, inorganic phosphorus), enzymes (alkaline phosphatase, γ-GT, AST, ALT), substrates/metabolites (total bilirubin, creatinine, glucose, urea, uric acid, total cholesterol, triglycerides), total proteins, urine chemical analysis (pH, specific weight, appearance, color, nitrites, proteins, glucose, urobilinogen, bilirubin, ketones, hematic pigments, leukocytes), urine sediment (analysis performed only if positive: leukocytes, erythrocytes, flat cells, round cells, crystals, cylinders, mucus, bacteria, glomerular erythrocytes). Any abnormalities are recorded.
Time frame: Screening visit (day of informed consent signature)/final visit (7 days after the treatment)
Study Part A: Cmax
Maximum plasma concentration measured for plasma fosnetupitant, netupitant and its main metabolites (M1, M2 and M3)
Time frame: Day 1 (treatment day) at pre-administration, at 2, 5, 10, 15, 20, 30 and 45 min and at 1, 1.5, 2, 3, 4, 8, 12, 24 h after the administration
Study Part A: C0
Plasma concentration at the end of the administration measured for plasma fosnetupitant, netupitant and its main metabolites (M1, M2 and M3)
Time frame: Day 1 (treatment day) at pre-administration, at 2, 5, 10, 15, 20, 30 and 45 min and at 1, 1.5, 2, 3, 4, 8, 12, 24 h after the administration
Study Part A: Tmax
Time to achieve the maximum plasma concentration measured for plasma fosnetupitant, netupitant and its main metabolites (M1, M2 and M3)
Time frame: Day 1 (treatment day) at pre-administration, at 2, 5, 10, 15, 20, 30 and 45 min and at 1, 1.5, 2, 3, 4, 8, 12, 24 h after the administration
Study Part A: Clast
Last measurable plasma concentration measured for plasma fosnetupitant, netupitant and its main metabolites (M1, M2 and M3)
Time frame: Day 1 (treatment day) at pre-administration, at 2, 5, 10, 15, 20, 30 and 45 min and at 1, 1.5, 2, 3, 4, 8, 12, 24 h after the administration
Study Part A: Tlast
Time of last measurable plasma concentration measured for plasma fosnetupitant, netupitant and its main metabolites (M1, M2 and M3)
Time frame: Day 1 (treatment day) at pre-administration, at 2, 5, 10, 15, 20, 30 and 45 min and at 1, 1.5, 2, 3, 4, 8, 12, 24 h after the administration
Study Part A: AUC0-t
Area under the concentration-time curve from time zero to time of last measurable plasma concentration measured for plasma fosnetupitant, netupitant and its main metabolites (M1, M2 and M3)
Time frame: Day 1 (treatment day) at pre-administration, at 2, 5, 10, 15, 20, 30 and 45 min and at 1, 1.5, 2, 3, 4, 8, 12, 24 h after the administration
Study Part A: AUC0-24
Area under the plasma concentration-time curve from time zero to 24 h after the administration measured for plasma fosnetupitant, netupitant and its main metabolites (M1, M2 and M3)
Time frame: Day 1 (treatment day) at pre-administration, at 2, 5, 10, 15, 20, 30 and 45 min and at 1, 1.5, 2, 3, 4, 8, 12, 24 h after the administration
Study Part A: Terminal Elimination Rate Constant
Terminal elimination rate constant, calculated, if feasible, by log-linear regression using at least 3 points, C0 and Cmax excluded and measured for plasma fosnetupitant, netupitant and its main metabolites (M1, M2 and M3). Calculation was not feasible for M1 and M3, therefore these analytes are not reported in the Outcome Measure Data Table.
Time frame: Day 1 (treatment day) at pre-administration, at 2, 5, 10, 15, 20, 30 and 45 min and at 1, 1.5, 2, 3, 4, 8, 12, 24 h after the administration
Study Part A: t1/2
Apparent terminal half-life calculated, if feasible, by as ln2/terminal elimination rate constant and measured for plasma fosnetupitant, netupitant and its main metabolites (M1, M2 and M3). Calculation was not feasible for M1 and M3, therefore these analytes are not reported in the Outcome Measure Data Table.
Time frame: Day 1 (treatment day) at pre-administration, at 2, 5, 10, 15, 20, 30 and 45 min and at 1, 1.5, 2, 3, 4, 8, 12, 24 h after the administration
Study Part A: Systemic Clearance
Systemic clearance measured for plasma fosnetupitant, netupitant and its main metabolites (M1, M2 and M3). Calculation was not feasible for M1 and M3, therefore these analytes are not reported in the Outcome Measure Data Table.
Time frame: Day 1 (treatment day) at pre-administration, at 2, 5, 10, 15, 20, 30 and 45 min and at 1, 1.5, 2, 3, 4, 8, 12, 24 h after the administration
Study Part A: Vz
Apparent volume of distribution in the post-distribution phase measured for plasma fosnetupitant, netupitant and its main metabolites (M1, M2 and M3). Calculation was not feasible for M1 and M3, therefore these analytes are not reported in the Outcome Measure Data Table.
Time frame: Day 1 (treatment day) at pre-administration, at 2, 5, 10, 15, 20, 30 and 45 min and at 1, 1.5, 2, 3, 4, 8, 12, 24 h after the administration
Study Part A: MRT
Mean residence time measured for plasma fosnetupitant, netupitant and its main metabolites (M1, M2 and M3). Calculation was not feasible for M1 and M3, therefore these analytes are not reported in the Outcome Measure Data Table.
Time frame: Day 1 (treatment day) at pre-administration, at 2, 5, 10, 15, 20, 30 and 45 min and at 1, 1.5, 2, 3, 4, 8, 12, 24 h after the administration
Participants were recruited at the Phase I Unit from 12 June 2023 to 14 October 2023 and enrolled in the study from 17 June 2023 to 16 October 2023.
| Milestone | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 |
|---|---|---|---|---|---|
| Started | 10 | 10 | 10 | 10 | 10 |
| Completed | 9 | 10 | 10 | 10 | 10 |
| Not completed | 1 | 0 | 0 | 0 | 0 |
| Withdrew: Withdrawal by subject | 1 | 0 | 0 | 0 | 0 |
Number of treatment-emergent adverse events (TEAEs) collected up to 24 h post-dose.
| Number of TEAE | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 |
|---|---|---|---|---|---|
| Study Part A: Number of Treatment-emergent Adverse Events | 7 | 4 | 3 | 1 | 4 |
Number of subjects with treatment-emergent adverse events (TEAEs) collected up to 24 h post-dose.
| Number of subjects with TEAE | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 |
|---|---|---|---|---|---|
| Study Part A: Number of Subjects With Treatment-emergent Adverse Events | 5 | 3 | 2 | 1 | 4 |
Type of treatment-emergent adverse events (TEAEs) collected up to 24 h post-dose.
| Number of TEAE | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 |
|---|---|---|---|---|---|
| Gastrointestinal disorders | 2 | 1 | 0 | 0 | 0 |
| General disorders and administration site conditions | 2 | 2 | 0 | 1 | 0 |
| Nervous system disorders | 2 | 1 | 2 | 0 | 4 |
| Psychiatric disorders | 1 | 0 | 0 | 0 | 0 |
| Investigations | 0 | 0 | 1 | 0 | 0 |
Systolic blood pressure in mmHg measured after 5 min at rest in sitting position
| mmHg | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 |
|---|---|---|---|---|---|
| Screening visit | 119.7 ± 9.4 | 118.8 ± 9.7 | 122.6 ± 12.5 | 122.6 ± 12.5 | 119.1 ± 8.9 |
| Day -1 (enrolment day) | 113.1 ± 6.2 | 116.7 ± 6.6 | 122.0 ± 12.5 | 122.0 ± 12.5 | 118.8 ± 9.7 |
| Day 1 (treatment day) at pre-administration | 112.5 ± 8.2 | 112.8 ± 12.9 | 114.2 ± 12.2 | 114.2 ± 12.2 | 115.6 ± 10.7 |
| Day 1 (treatment day) at the end of administration | 107.7 ± 12.3 | 111.5 ± 8.5 | 113.6 ± 10.6 | 113.6 ± 10.6 | 113.2 ± 13.5 |
| Day 1 (treatment day) at 1 h after the end of administration | 110.4 ± 8.2 | 111.7 ± 10.6 | 113.4 ± 11.9 | 113.4 ± 11.9 | 112.3 ± 10.2 |
| Day 1 (treatment day) at 2 h after the end of administration | 106.6 ± 6.9 | 109.8 ± 11.6 | 114.1 ± 10.8 | 114.1 ± 10.8 | 112.4 ± 7.6 |
| Day 1 (treatment day) at 4 h after the end of administration | 108.3 ± 10.5 | 107.6 ± 9.5 | 113.8 ± 12.7 | 113.8 ± 12.7 | 109.8 ± 9.6 |
| Day 1 (treatment day) at 24 h after the end of administration | 108.5 ± 8.2 | 112.9 ± 11.7 | 116.7 ± 10.8 | 116.7 ± 10.8 | 115.8 ± 10.6 |
| Final visit (7 days after the treatment) | 114.4 ± 9.3 | 111.1 ± 11.8 | 116.2 ± 8.7 | 116.2 ± 8.7 | 120.5 ± 10.9 |
Diastolic blood pressure in mmHg measured after 5 min at rest in sitting position
| mmHg | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 |
|---|---|---|---|---|---|
| Screening visit | 72.3 ± 6.5 | 76.8 ± 6.9 | 80.4 ± 8.0 | 80.4 ± 8.0 | 76.7 ± 7.5 |
| Day -1 (enrolment day) | 68.9 ± 8.6 | 77.7 ± 5.8 | 76.1 ± 7.0 | 76.1 ± 7.0 | 74.8 ± 6.9 |
| Day 1 (treatment day) at pre-administration | 72.1 ± 9.0 | 74.9 ± 9.2 | 76.0 ± 10.1 | 76.0 ± 10.1 | 71.9 ± 10.5 |
| Day 1 (treatment day) at the end of administration | 62.4 ± 11.1 | 71.7 ± 8.3 | 75.2 ± 10.1 | 75.2 ± 10.1 | 70.1 ± 9.3 |
| Day 1 (treatment day) at 1 h after the end of administration | 63.9 ± 6.4 | 73.4 ± 8.3 | 76.7 ± 8.8 | 76.7 ± 8.8 | 72.5 ± 7.2 |
| Day 1 (treatment day) at 2 h after the end of administration | 64.5 ± 8.5 | 72.8 ± 7.3 | 74.8 ± 11.2 | 74.8 ± 11.2 | 71.5 ± 9.2 |
| Day 1 (treatment day) at 4 h after the end of administration | 65.9 ± 6.6 | 68.9 ± 8.8 | 76.6 ± 9.8 | 76.6 ± 9.8 | 70.7 ± 8.5 |
| Day 1 (treatment day) at 24 h after the end of administration | 67.0 ± 9.4 | 72.7 ± 7.9 | 77.5 ± 8.8 | 77.5 ± 8.8 | 73.2 ± 7.7 |
| Final visit (7 days after the treatment) | 70.1 ± 7.2 | 74.4 ± 7.5 | 77.7 ± 7.1 | 77.7 ± 7.1 | 77.4 ± 6.4 |
Pulse rate in bpm measured after 5 min at rest in sitting position
| Beats/min | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 |
|---|---|---|---|---|---|
| Screening visit | 60.9 ± 7.3 | 65.3 ± 7.8 | 61.0 ± 10.5 | 61.0 ± 10.5 | 68.3 ± 7.3 |
| Day -1 (enrolment day) | 68.4 ± 8.9 | 74.9 ± 8.6 | 75.6 ± 11.7 | 75.6 ± 11.7 | 77.7 ± 8.8 |
| Day 1 (treatment day) at pre-administration | 60.0 ± 5.6 | 62.4 ± 8.6 | 59.0 ± 9.4 | 59.0 ± 9.4 | 65.2 ± 7.2 |
| Day 1 (treatment day) at the end of administration | 58.3 ± 7.5 | 64.2 ± 8.6 | 59.5 ± 7.7 | 59.5 ± 7.7 | 62.0 ± 10.1 |
| Day 1 (treatment day) at 1 h after the end of administration | 59.3 ± 10.4 | 62.8 ± 5.4 | 59.3 ± 7.8 | 59.3 ± 7.8 | 62.4 ± 8.9 |
| Day 1 (treatment day) at 2 h after the end of administration | 56.4 ± 6.8 | 61.4 ± 6.8 | 58.5 ± 7.8 | 58.5 ± 7.8 | 62.1 ± 9.2 |
| Day 1 (treatment day) at 4 h after the end of administration | 56.8 ± 7.2 | 62.7 ± 7.5 | 56.4 ± 7.2 | 56.4 ± 7.2 | 62.8 ± 7.9 |
| Day 1 (treatment day) at 24 h after the end of administration | 58.8 ± 9.8 | 65.5 ± 7.9 | 60.9 ± 9.0 | 60.9 ± 9.0 | 67.8 ± 6.5 |
| Final visit (7 days after the treatment) | 56.8 ± 8.1 | 62.9 ± 6.8 | 61.5 ± 7.4 | 61.5 ± 7.4 | 72.3 ± 10.5 |
Body weight in kilograms
| Kilograms | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 |
|---|---|---|---|---|---|
| Screening visit | 65.94 ± 9.50 | 69.83 ± 15.15 | 71.98 ± 13.16 | 71.98 ± 13.16 | 71.30 ± 11.66 |
| Final visit (7 days after the treatment) | 66.68 ± 9.49 | 70.08 ± 14.67 | 72.44 ± 13.72 | 72.44 ± 13.72 | 71.40 ± 11.48 |
General appearance, Chest/respiratory, Gastrointestinal, Head, eyes, ears, nose and throat, Heart/cardiovascular, Lymph nodes, Metabolic/endocrine, Musculoskeletal/extremities, Neck (including thyroid), Neurological/psychiatric, Skin/dermatologic systems are checked. Any abnormalities are recorded.
| Participants | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 |
|---|---|---|---|---|---|
| Screening visit — Normal | 10 | 7 | 9 | 10 | 9 |
| Screening visit — Abnormal not clinically significant | 0 | 3 | 1 | 0 | 1 |
| Final visit (7 days after the treatment) — Normal | 10 | 7 | 10 | 10 | 10 |
| Final visit (7 days after the treatment) — Abnormal not clinically significant | 0 | 3 | 0 | 0 | 0 |
General appearance, Chest/respiratory, Heart/cardiovascular, Lymph nodes, Neurologic/psychiatric, Skin/dermatologic systems are checked. Any abnormalities are recorded.
| Participants | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 |
|---|---|---|---|---|---|
| Normal | 9 | 7 | 10 | 10 | 10 |
| Abnormal not clinically significant | 1 | 3 | 0 | 0 | 0 |
Heart rate in beats/min recorded in supine position after 5 min at rest
| Participants | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 |
|---|---|---|---|---|---|
| Screening visit — Normal | 3 | 4 | 2 | 3 | 5 |
| Screening visit — Abnormal not clinically significant | 7 | 6 | 8 | 7 | 5 |
| Day 1 (treatment day) at pre-administration — Normal | 1 | 4 | 2 | 2 | 2 |
| Day 1 (treatment day) at pre-administration — Abnormal not clinically significant | 9 | 6 | 8 | 8 | 8 |
| Day 1 (treatment day) at the end of administration — Normal | 2 | 3 | 2 | 2 | 2 |
| Day 1 (treatment day) at the end of administration — Abnormal not clinically significant | 8 | 7 | 8 | 8 | 8 |
| Day 1 (treatment day) at 1 h after the end of administration — Normal | 1 | 2 | 2 | 1 | 2 |
| Day 1 (treatment day) at 1 h after the end of administration — Abnormal not clinically significant | 9 | 8 | 8 | 9 | 8 |
| Day 1 (treatment day) at 2 h after the end of administration — Normal | 0 | 2 | 2 | 2 | 2 |
| Day 1 (treatment day) at 2 h after the end of administration — Abnormal not clinically significant | 10 | 8 | 8 | 8 | 8 |
| Day 1 (treatment day) at 4 h after the end of administration — Normal | 1 | 2 | 1 | 1 | 2 |
| Day 1 (treatment day) at 4 h after the end of administration — Abnormal not clinically significant | 9 | 8 | 9 | 9 | 8 |
| Day 1 (treatment day) at 24 h after the end of administration — Normal | 0 | 4 | 2 | 3 | 5 |
| Day 1 (treatment day) at 24 h after the end of administration — Abnormal not clinically significant | 10 | 6 | 8 | 7 | 5 |
| Final visit (7 days after the treatment) — Normal | 2 | 7 | 3 | 2 | 4 |
| Final visit (7 days after the treatment) — Abnormal not clinically significant | 8 | 3 | 7 | 8 | 6 |
PR interval in ms recorded in supine position after 5 min at rest
| Participants | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 |
|---|---|---|---|---|---|
| Screening visit — Normal | 3 | 4 | 2 | 3 | 5 |
| Screening visit — Abnormal, not clinically significant | 7 | 6 | 8 | 7 | 5 |
| Day 1 (treatment day) at pre-administration — Normal | 1 | 4 | 2 | 2 | 2 |
| Day 1 (treatment day) at pre-administration — Abnormal, not clinically significant | 9 | 6 | 8 | 8 | 8 |
| Day 1 (treatment day) at the end of administration — Normal | 2 | 3 | 2 | 2 | 2 |
| Day 1 (treatment day) at the end of administration — Abnormal, not clinically significant | 8 | 7 | 8 | 8 | 8 |
| Day 1 (treatment day) at 1 h after the end of administration — Normal | 1 | 2 | 2 | 1 | 2 |
| Day 1 (treatment day) at 1 h after the end of administration — Abnormal, not clinically significant | 9 | 8 | 8 | 9 | 8 |
| Day 1 (treatment day) at 2 h after the end of administration — Normal | 0 | 2 | 2 | 2 | 2 |
| Day 1 (treatment day) at 2 h after the end of administration — Abnormal, not clinically significant | 10 | 8 | 8 | 8 | 8 |
| Day 1 (treatment day) at 4 h after the end of administration — Normal | 1 | 2 | 1 | 1 | 2 |
| Day 1 (treatment day) at 4 h after the end of administration — Abnormal, not clinically significant | 9 | 8 | 9 | 9 | 8 |
| Day 1 (treatment day) at 24 h after the end of administration — Normal | 0 | 4 | 2 | 3 | 5 |
| Day 1 (treatment day) at 24 h after the end of administration — Abnormal, not clinically significant | 10 | 6 | 8 | 7 | 5 |
| Final visit (7 days after the treatment) — Normal | 2 | 7 | 3 | 2 | 4 |
| Final visit (7 days after the treatment) — Abnormal, not clinically significant | 8 | 3 | 7 | 8 | 6 |
RR interval in ms recorded in supine position after 5 min at rest
| Participants | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 |
|---|---|---|---|---|---|
| Screening visit — Normal | 3 | 4 | 2 | 3 | 5 |
| Screening visit — Abnormal, not clinically significant | 7 | 6 | 8 | 7 | 5 |
| Day 1 (treatment day) at pre-administration — Normal | 1 | 4 | 2 | 2 | 2 |
| Day 1 (treatment day) at pre-administration — Abnormal, not clinically significant | 9 | 6 | 8 | 8 | 8 |
| Day 1 (treatment day) at the end of administration — Normal | 2 | 3 | 2 | 2 | 2 |
| Day 1 (treatment day) at the end of administration — Abnormal, not clinically significant | 8 | 7 | 8 | 8 | 8 |
| Day 1 (treatment day) at 1 h after the end of administration — Normal | 1 | 2 | 2 | 1 | 2 |
| Day 1 (treatment day) at 1 h after the end of administration — Abnormal, not clinically significant | 9 | 8 | 8 | 9 | 8 |
| Day 1 (treatment day) at 2 h after the end of administration — Normal | 0 | 2 | 2 | 2 | 2 |
| Day 1 (treatment day) at 2 h after the end of administration — Abnormal, not clinically significant | 10 | 8 | 8 | 8 | 8 |
| Day 1 (treatment day) at 4 h after the end of administration — Normal | 1 | 2 | 1 | 1 | 2 |
| Day 1 (treatment day) at 4 h after the end of administration — Abnormal, not clinically significant | 9 | 8 | 9 | 9 | 8 |
| Day 1 (treatment day) at 24 h after the end of administration — Normal | 0 | 4 | 2 | 3 | 5 |
| Day 1 (treatment day) at 24 h after the end of administration — Abnormal, not clinically significant | 10 | 6 | 8 | 7 | 5 |
| Final visit (7 days after the treatment) — Normal | 2 | 7 | 3 | 2 | 4 |
| Final visit (7 days after the treatment) — Abnormal, not clinically significant | 8 | 3 | 7 | 8 | 6 |
QRS duration in ms recorded in supine position after 5 min at rest
| Participants | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 |
|---|---|---|---|---|---|
| Screening visit — Normal | 3 | 4 | 2 | 3 | 5 |
| Screening visit — Abnormal not clinically significant | 7 | 6 | 8 | 7 | 5 |
| Day 1 (treatment day) at pre-administration — Normal | 1 | 4 | 2 | 2 | 2 |
| Day 1 (treatment day) at pre-administration — Abnormal not clinically significant | 9 | 6 | 8 | 8 | 8 |
| Day 1 (treatment day) at the end of administration — Normal | 2 | 3 | 2 | 2 | 2 |
| Day 1 (treatment day) at the end of administration — Abnormal not clinically significant | 8 | 7 | 8 | 8 | 8 |
| Day 1 (treatment day) at 1 h after the end of administration — Normal | 1 | 2 | 2 | 1 | 2 |
| Day 1 (treatment day) at 1 h after the end of administration — Abnormal not clinically significant | 9 | 8 | 8 | 9 | 8 |
| Day 1 (treatment day) at 2 h after the end of administration — Normal | 0 | 2 | 2 | 2 | 2 |
| Day 1 (treatment day) at 2 h after the end of administration — Abnormal not clinically significant | 10 | 8 | 8 | 8 | 8 |
| Day 1 (treatment day) at 4 h after the end of administration — Normal | 1 | 2 | 1 | 1 | 2 |
| Day 1 (treatment day) at 4 h after the end of administration — Abnormal not clinically significant | 9 | 8 | 9 | 9 | 8 |
| Day 1 (treatment day) at 24 h after the end of administration — Normal | 0 | 4 | 2 | 3 | 5 |
| Day 1 (treatment day) at 24 h after the end of administration — Abnormal not clinically significant | 10 | 6 | 8 | 7 | 5 |
| Final visit (7 days after the treatment) — Normal | 2 | 7 | 3 | 2 | 4 |
| Final visit (7 days after the treatment) — Abnormal not clinically significant | 8 | 3 | 7 | 8 | 6 |
QT interval in ms recorded in supine position after 5 min at rest
| Participants | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 |
|---|---|---|---|---|---|
| Screening visit — Normal | 3 | 4 | 2 | 3 | 5 |
| Screening visit — Abnormal, not clinically significant | 7 | 6 | 8 | 7 | 5 |
| Day 1 (treatment day) at pre-administration — Normal | 1 | 4 | 2 | 2 | 2 |
| Day 1 (treatment day) at pre-administration — Abnormal, not clinically significant | 9 | 6 | 8 | 8 | 8 |
| Day 1 (treatment day) at the end of administration — Normal | 2 | 3 | 2 | 2 | 2 |
| Day 1 (treatment day) at the end of administration — Abnormal, not clinically significant | 8 | 7 | 8 | 8 | 8 |
| Day 1 (treatment day) at 1 h after the end of administration — Normal | 1 | 2 | 2 | 1 | 2 |
| Day 1 (treatment day) at 1 h after the end of administration — Abnormal, not clinically significant | 9 | 8 | 8 | 9 | 8 |
| Day 1 (treatment day) at 2 h after the end of administration — Normal | 0 | 2 | 2 | 2 | 2 |
| Day 1 (treatment day) at 2 h after the end of administration — Abnormal, not clinically significant | 10 | 8 | 8 | 8 | 8 |
| Day 1 (treatment day) at 4 h after the end of administration — Normal | 1 | 2 | 1 | 1 | 2 |
| Day 1 (treatment day) at 4 h after the end of administration — Abnormal, not clinically significant | 9 | 8 | 9 | 9 | 8 |
| Day 1 (treatment day) at 24 h after the end of administration — Normal | 0 | 4 | 2 | 3 | 5 |
| Day 1 (treatment day) at 24 h after the end of administration — Abnormal, not clinically significant | 10 | 6 | 8 | 7 | 5 |
| Final visit (7 days after the treatment) — Normal | 2 | 7 | 3 | 2 | 4 |
| Final visit (7 days after the treatment) — Abnormal, not clinically significant | 8 | 3 | 7 | 8 | 6 |
QTcB interval in ms recorded in supine position after 5 min at rest
| Participants | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 |
|---|---|---|---|---|---|
| Screening visit — Normal | 3 | 4 | 2 | 3 | 5 |
| Screening visit — Abnormal not clinically significant | 7 | 6 | 8 | 7 | 5 |
| Day 1 (treatment day) at pre-administration — Normal | 1 | 4 | 2 | 2 | 2 |
| Day 1 (treatment day) at pre-administration — Abnormal not clinically significant | 9 | 6 | 8 | 8 | 8 |
| Day 1 (treatment day) at the end of administration — Normal | 2 | 3 | 2 | 2 | 2 |
| Day 1 (treatment day) at the end of administration — Abnormal not clinically significant | 8 | 7 | 8 | 8 | 8 |
| Day 1 (treatment day) at 1 h after the end of administration — Normal | 1 | 2 | 2 | 1 | 2 |
| Day 1 (treatment day) at 1 h after the end of administration — Abnormal not clinically significant | 9 | 8 | 8 | 9 | 8 |
| Day 1 (treatment day) at 2 h after the end of administration — Normal | 0 | 2 | 2 | 2 | 2 |
| Day 1 (treatment day) at 2 h after the end of administration — Abnormal not clinically significant | 10 | 8 | 8 | 8 | 8 |
| Day 1 (treatment day) at 4 h after the end of administration — Normal | 1 | 2 | 1 | 1 | 2 |
| Day 1 (treatment day) at 4 h after the end of administration — Abnormal not clinically significant | 9 | 8 | 9 | 9 | 8 |
| Day 1 (treatment day) at 24 h after the end of administration — Normal | 0 | 4 | 2 | 3 | 5 |
| Day 1 (treatment day) at 24 h after the end of administration — Abnormal not clinically significant | 10 | 6 | 8 | 7 | 5 |
| Final visit (7 days after the treatment) — Normal | 2 | 7 | 3 | 2 | 4 |
| Final visit (7 days after the treatment) — Abnormal not clinically significant | 8 | 3 | 7 | 8 | 6 |
QTcF interval in ms recorded in supine position after 5 min at rest
| Participants | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 |
|---|---|---|---|---|---|
| Screening visit — Normal | 3 | 4 | 2 | 3 | 5 |
| Screening visit — Abnormal not clinically significant | 7 | 6 | 8 | 7 | 5 |
| Day 1 (treatment day) at pre-administration — Normal | 1 | 4 | 2 | 2 | 2 |
| Day 1 (treatment day) at pre-administration — Abnormal not clinically significant | 9 | 6 | 8 | 8 | 8 |
| Day 1 (treatment day) at the end of administration — Normal | 2 | 3 | 2 | 2 | 2 |
| Day 1 (treatment day) at the end of administration — Abnormal not clinically significant | 8 | 7 | 8 | 8 | 8 |
| Day 1 (treatment day) at 1 h after the end of administration — Normal | 1 | 2 | 2 | 1 | 2 |
| Day 1 (treatment day) at 1 h after the end of administration — Abnormal not clinically significant | 9 | 8 | 8 | 9 | 8 |
| Day 1 (treatment day) at 2 h after the end of administration — Normal | 0 | 2 | 2 | 2 | 2 |
| Day 1 (treatment day) at 2 h after the end of administration — Abnormal not clinically significant | 10 | 8 | 8 | 8 | 8 |
| Day 1 (treatment day) at 4 h after the end of administration — Normal | 1 | 2 | 1 | 1 | 2 |
| Day 1 (treatment day) at 4 h after the end of administration — Abnormal not clinically significant | 9 | 8 | 9 | 9 | 8 |
| Day 1 (treatment day) at 24 h after the end of administration — Normal | 0 | 4 | 2 | 3 | 5 |
| Day 1 (treatment day) at 24 h after the end of administration — Abnormal not clinically significant | 10 | 6 | 8 | 7 | 5 |
| Final visit (7 days after the treatment) — Normal | 2 | 7 | 3 | 2 | 4 |
| Final visit (7 days after the treatment) — Abnormal not clinically significant | 8 | 3 | 7 | 8 | 6 |
Leukocytes and leukocyte differential count, erythrocytes, haemoglobin, haematocrit, MCV, MCH, MCHC, thrombocytes, electrolytes (sodium, potassium, calcium, chloride, inorganic phosphorus), enzymes (alkaline phosphatase, γ-GT, AST, ALT), substrates/metabolites (total bilirubin, creatinine, glucose, urea, uric acid, total cholesterol, triglycerides), total proteins, urine chemical analysis (pH, specific weight, appearance, color, nitrites, proteins, glucose, urobilinogen, bilirubin, ketones, hematic pigments, leukocytes), urine sediment (analysis performed only if positive: leukocytes, erythrocytes, flat cells, round cells, crystals, cylinders, mucus, bacteria, glomerular erythrocytes). Any abnormalities are recorded.
| Participants | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 |
|---|---|---|---|---|---|
| Screening visit - blood — Normal | 5 | 2 | 2 | 3 | 1 |
| Screening visit - blood — Abnormal not clinically significant | 5 | 8 | 8 | 7 | 9 |
| Screening visit - blood — Abnormal clinically significant | 0 | 0 | 0 | 0 | 0 |
| Screening visit - urine — Normal | 3 | 3 | 4 | 3 | 2 |
| Screening visit - urine — Abnormal not clinically significant | 7 | 7 | 6 | 7 | 8 |
| Screening visit - urine — Abnormal clinically significant | 0 | 0 | 0 | 0 | 0 |
| Final visit (7 days after the treatment) - blood — Normal | 2 | 4 | 1 | 1 | 0 |
| Final visit (7 days after the treatment) - blood — Abnormal not clinically significant | 8 | 6 | 8 | 9 | 10 |
| Final visit (7 days after the treatment) - blood — Abnormal clinically significant | 0 | 0 | 1 | 0 | 0 |
| Final visit (7 days after the treatment) - urine — Normal | 3 | 3 | 3 | 4 | 3 |
| Final visit (7 days after the treatment) - urine — Abnormal not clinically significant | 7 | 7 | 7 | 6 | 7 |
| Final visit (7 days after the treatment) - urine — Abnormal clinically significant | 0 | 0 | 0 | 0 | 0 |
Maximum plasma concentration measured for plasma fosnetupitant, netupitant and its main metabolites (M1, M2 and M3)
| ng/mL | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 |
|---|---|---|---|---|---|
| Fosnetupitant | 8486.000 ± 2095.382 | 8920.000 ± 1722.892 | 23650.000 ± 20971.899 | 32540.000 ± 6607.437 | 37500.000 ± 11243.270 |
| Netupitant | 767.400 ± 136.572 | 893.400 ± 283.232 | 1050.100 ± 260.591 | 1170.700 ± 276.310 | 1382.700 ± 315.816 |
| Metabolite M1 | 23.910 ± 5.324 | 22.380 ± 8.433 | 22.012 ± 6.687 | 21.930 ± 6.958 | 22.910 ± 7.610 |
| Metabolite M2 | 135.730 ± 58.257 | 150.110 ± 72.607 | 102.450 ± 44.216 | 118.160 ± 49.015 | 146.490 ± 88.541 |
| Metabolite M3 | 46.880 ± 11.936 | 48.450 ± 17.019 | 46.570 ± 16.137 | 47.680 ± 14.446 | 52.100 ± 27.347 |
Plasma concentration at the end of the administration measured for plasma fosnetupitant, netupitant and its main metabolites (M1, M2 and M3)
| ng/mL | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 |
|---|---|---|---|---|---|
| Fosnetupitant | 8486.000 ± 2095.382 | 8920.000 ± 1722.892 | 23650.000 ± 20971.899 | 32540.000 ± 6607.437 | 33557.000 ± 15972.519 |
| Netupitant | 743.100 ± 173.921 | 893.400 ± 283.232 | 946.100 ± 419.234 | 1019.400 ± 319.820 | 596.810 ± 383.903 |
| Metabolite M1 | 1.714 ± 2.229 | 1.753 ± 1.969 | 0.337 ± 1.066 | 0.000 ± 0.000 | 0.000 ± 0.000 |
| Metabolite M2 | 28.150 ± 10.059 | 49.121 ± 34.243 | 32.300 ± 22.563 | 25.680 ± 11.219 | 12.706 ± 6.689 |
| Metabolite M3 | 6.214 ± 4.144 | 6.799 ± 2.989 | 0.727 ± 1.711 | 0.000 ± 0.000 | 0.000 ± 0.000 |
Time to achieve the maximum plasma concentration measured for plasma fosnetupitant, netupitant and its main metabolites (M1, M2 and M3)
| h | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 |
|---|---|---|---|---|---|
| Fosnetupitant | 0.5 (0.5 to 0.5) | 0.5 (0.5 to 0.5) | 0.25 (0.25 to 0.3) | 0.08 (0.08 to 0.08) | 0.05 (0.033 to 0.08) |
| Netupitant | 0.5 (0.5 to 2) | 0.5 (0.5 to 0.5) | 0.25 (0.25 to 0.33) | 0.125 (0.08 to 0.17) | 0.08 (0.08 to 0.17) |
| Metabolite M1 | 12 (2 to 24) | 10 (2 to 24) | 12 (1.5 to 24) | 12 (4 to 24) | 12 (8 to 24) |
| Metabolite M2 | 2 (2 to 4) | 2 (1.5 to 3) | 2.5 (0.33 to 3) | 2 (1.5 to 3) | 1.75 (1.5 to 4) |
| Metabolite M3 | 24 (12 to 24) | 24 (2 to 24) | 24 (12 to 24) | 24 (12 to 24) | 24 (12 to 24) |
Last measurable plasma concentration measured for plasma fosnetupitant, netupitant and its main metabolites (M1, M2 and M3)
| ng/mL | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 |
|---|---|---|---|---|---|
| Fosnetupitant | 79.780 ± 71.819 | 49.410 ± 35.149 | 97.140 ± 122.226 | 45.620 ± 28.083 | 34.330 ± 16.176 |
| Netupitant | 149.150 ± 111.842 | 122.490 ± 40.233 | 136.340 ± 39.724 | 123.740 ± 28.843 | 137.270 ± 66.827 |
| Metabolite M1 | 21.150 ± 3.876 | 20.380 ± 7.875 | 20.532 ± 6.667 | 19.990 ± 5.977 | 21.440 ± 7.826 |
| Metabolite M2 | 20.090 ± 10.519 | 18.850 ± 7.890 | 14.534 ± 4.789 | 18.770 ± 5.515 | 17.067 ± 7.953 |
| Metabolite M3 | 46.370 ± 12.315 | 48.020 ± 17.273 | 44.960 ± 15.634 | 47.080 ± 14.763 | 52.060 ± 27.374 |
Time of last measurable plasma concentration measured for plasma fosnetupitant, netupitant and its main metabolites (M1, M2 and M3)
| h | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 |
|---|---|---|---|---|---|
| Fosnetupitant | 0.83 ± 0.118 | 0.95 ± 0.23 | 1.075 ± 1.048 | 0.6 ± 0.316 | 0.633 ± 0.35 |
| Netupitant | 24 ± 0 | 24 ± 0 | 24 ± 0 | 24 ± 0 | 24 ± 0 |
| Metabolite M1 | 24 ± 0 | 24 ± 0 | 24 ± 0 | 24 ± 0 | 24 ± 0 |
| Metabolite M2 | 24 ± 0 | 24 ± 0 | 24 ± 0 | 24 ± 0 | 24 ± 0 |
| Metabolite M3 | 24 ± 0 | 24 ± 0 | 24 ± 0 | 24 ± 0 | 24 ± 0 |
Area under the concentration-time curve from time zero to time of last measurable plasma concentration measured for plasma fosnetupitant, netupitant and its main metabolites (M1, M2 and M3)
| h x ng/mL | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 |
|---|---|---|---|---|---|
| Fosnetupitant | 3217.286 ± 780.235 | 3374.275 ± 658.088 | 4807.383 ± 4537.620 | 3662.088 ± 630.455 | 3839.681 ± 859.368 |
| Netupitant | 5404.315 ± 1227.399 | 5232.178 ± 1119.310 | 5792.056 ± 1520.649 | 5344.307 ± 1385.625 | 5656.305 ± 1998.286 |
| Metabolite M1 | 468.997 ± 113.819 | 456.214 ± 173.046 | 436.089 ± 142.089 | 426.440 ± 122.749 | 447.497 ± 143.611 |
| Metabolite M2 | 1234.204 ± 767.496 | 1260.320 ± 477.244 | 959.756 ± 382.755 | 1137.332 ± 331.659 | 1182.642 ± 560.829 |
| Metabolite M3 | 833.606 ± 164.142 | 895.624 ± 304.534 | 831.375 ± 306.679 | 826.377 ± 156.114 | 935.410 ± 441.878 |
Area under the plasma concentration-time curve from time zero to 24 h after the administration measured for plasma fosnetupitant, netupitant and its main metabolites (M1, M2 and M3)
| h x ng/mL | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 |
|---|---|---|---|---|---|
| Fosnetupitant | 3228.246 ± 781.172 | 3382.473 ± 657.505 | 4833.636 ± 4577.777 | 3668.069 ± 631.004 | 3844.251 ± 859.498 |
| Netupitant | 5404.315 ± 1227.399 | 5232.178 ± 1119.310 | 5792.056 ± 1520.649 | 5344.307 ± 1385.625 | 5656.305 ± 1998.286 |
| Metabolite M1 | 468.997 ± 113.819 | 456.214 ± 173.046 | 436.089 ± 142.089 | 426.440 ± 122.749 | 447.497 ± 143.611 |
| Metabolite M2 | 1234.204 ± 767.496 | 1260.320 ± 477.244 | 959.756 ± 382.755 | 1137.332 ± 331.659 | 1182.642 ± 560.829 |
| Metabolite M3 | 833.606 ± 164.142 | 895.624 ± 304.534 | 831.375 ± 306.679 | 826.377 ± 156.114 | 935.410 ± 441.878 |
Terminal elimination rate constant, calculated, if feasible, by log-linear regression using at least 3 points, C0 and Cmax excluded and measured for plasma fosnetupitant, netupitant and its main metabolites (M1, M2 and M3). Calculation was not feasible for M1 and M3, therefore these analytes are not reported in the Outcome Measure Data Table.
| 1/h | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 |
|---|---|---|---|---|---|
| Fosnetupitant | 12.157 ± 0.662 | 11.734 ± 0.754 | 14.979 ± 5.582 | 18.613 ± 3.868 | 19.141 ± 5.429 |
| Netupitant | 0.034 ± 0.012 | 0.034 ± 0.007 | 0.033 ± 0.012 | 0.039 ± 0.005 | 0.032 ± 0.014 |
| Metabolite M2 | 0.063 ± 0.014 | 0.061 ± 0.018 | 0.058 ± 0.017 | 0.059 ± 0.013 | 0.061 ± 0.015 |
Apparent terminal half-life calculated, if feasible, by as ln2/terminal elimination rate constant and measured for plasma fosnetupitant, netupitant and its main metabolites (M1, M2 and M3). Calculation was not feasible for M1 and M3, therefore these analytes are not reported in the Outcome Measure Data Table.
| h | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 |
|---|---|---|---|---|---|
| Fosnetupitant | 0.057 ± 0.003 | 0.059 ± 0.004 | 0.080 ± 0.115 | 0.039 ± 0.011 | 0.040 ± 0.017 |
| Netupitant | 22.104 ± 7.005 | 21.356 ± 4.151 | 25.176 ± 14.727 | 18.017 ± 2.747 | 30.061 ± 24.561 |
| Metabolite M2 | 11.538 ± 2.490 | 12.855 ± 5.985 | 12.918 ± 4.023 | 12.468 ± 3.215 | 12.248 ± 3.863 |
Systemic clearance measured for plasma fosnetupitant, netupitant and its main metabolites (M1, M2 and M3). Calculation was not feasible for M1 and M3, therefore these analytes are not reported in the Outcome Measure Data Table.
| mL/h | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 |
|---|---|---|---|---|---|
| Fosnetupitant | 61821.940 ± 16436.343 | 66942.974 ± 12370.822 | 65171.229 ± 21219.721 | 65651.064 ± 9975.506 | 63748.966 ± 13353.411 |
| Netupitant | 27219.010 ± 3356.654 | 28693.446 ± 7660.440 | 24200.268 ± 6832.625 | 27596.213 ± 6404.903 | 26994.542 ± 10531.874 |
| Metabolite M2 | 172324.405 ± 50962.753 | 162039.804 ± 57537.646 | 211825.621 ± 68310.261 | 174034.336 ± 64374.511 | 182468.624 ± 68658.409 |
Apparent volume of distribution in the post-distribution phase measured for plasma fosnetupitant, netupitant and its main metabolites (M1, M2 and M3). Calculation was not feasible for M1 and M3, therefore these analytes are not reported in the Outcome Measure Data Table.
| mL | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 |
|---|---|---|---|---|---|
| Fosnetupitant | 5129.653 ± 1631.449 | 5765.916 ± 1352.379 | 4796.595 ± 1491.027 | 3728.124 ± 1263.039 | 3572.355 ± 1199.382 |
| Netupitant | 848022.360 ± 215723.734 | 872978.816 ± 264673.002 | 772482.708 ± 205893.262 | 719627.108 ± 219903.292 | 944544.565 ± 311425.672 |
| Metabolite M2 | 2895427.080 ± 954908.605 | 2820832.784 ± 1000428.130 | 4109459.426 ± 2374558.032 | 3083100.830 ± 1154481.625 | 3122087.067 ± 1170365.896 |
Mean residence time measured for plasma fosnetupitant, netupitant and its main metabolites (M1, M2 and M3). Calculation was not feasible for M1 and M3, therefore these analytes are not reported in the Outcome Measure Data Table.
| h | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 |
|---|---|---|---|---|---|
| Fosnetupitant | 0.253 ± 0.001 | 0.254 ± 0.002 | 0.275 ± 0.038 | 0.109 ± 0.014 | 0.086 ± 0.014 |
| Netupitant | 28.529 ± 9.761 | 26.760 ± 5.780 | 33.752 ± 21.148 | 24.493 ± 3.866 | 40.753 ± 34.769 |
| Metabolite M2 | 14.343 ± 2.220 | 15.895 ± 7.651 | 16.347 ± 5.492 | 16.299 ± 3.936 | 14.975 ± 4.858 |
Collected over The reporting period for adverse events is the period starting from the time of informed consent signature and lasting until the final visit. Adverse events were collected for each participant for the whole period of the study (i.e., a maximum of 28 days).. Non-serious events are listed at a 0% frequency threshold.
| Group | Deaths | Serious | Other |
|---|---|---|---|
| Study Part A - Cohort 1 - Akynzeo | 0/10 (0%) | 0/10 (0%) | 5/10 (50%) |
| Study Part A - Cohort 1 - Fosnetupitant | 0/10 (0%) | 0/10 (0%) | 3/10 (30%) |
| Study Part A - Cohort 2 | 0/10 (0%) | 0/10 (0%) | 2/10 (20%) |
| Study Part A - Cohort 3 | 0/10 (0%) | 0/10 (0%) | 1/10 (10%) |
| Study Part A - Cohort 4 | 0/10 (0%) | 0/10 (0%) | 4/10 (40%) |
| Event | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 |
|---|---|---|---|---|---|
| ConstipationGastrointestinal disorders | 2/10 | 0/10 | 0/10 | 0/10 | 0/10 |
| FatigueGeneral disorders | 2/10 | 0/10 | 0/10 | 0/10 | 0/10 |
| HeadacheNervous system disorders | 0/10 | 1/10 | 1/10 | 0/10 | 2/10 |
| NauseaGastrointestinal disorders | 0/10 | 1/10 | 0/10 | 0/10 | 0/10 |
| Infusion site painGeneral disorders | 0/10 | 1/10 | 0/10 | 0/10 | 0/10 |
| Injection site discomfortGeneral disorders | 0/10 | 1/10 | 0/10 | 0/10 | 0/10 |
| Influenza like illnessGeneral disorders | 0/10 | 0/10 | 0/10 | 1/10 | 0/10 |
| DizzinessNervous system disorders | 1/10 | 0/10 | 1/10 | 0/10 | 1/10 |
| PresyncopeNervous system disorders | 1/10 | 0/10 | 0/10 | 0/10 | 0/10 |
| DysgeusiaNervous system disorders | 0/10 | 0/10 | 0/10 | 0/10 | 1/10 |
| Age, Continuous(years) | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 | Total |
|---|---|---|---|---|---|---|
| Mean | 31.7 ± 8.9 | 40.7 ± 8.2 | 38.9 ± 13.2 | 37.9 ± 10.8 | 38.1 ± 13.5 | 37.5 ± 11.1 |
| Sex: Female, Male(Participants) | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 | Total |
|---|---|---|---|---|---|---|
| Female | 4 | 6 | 3 | 3 | 4 | 20 |
| Male | 6 | 4 | 7 | 7 | 6 | 30 |
| Race (NIH/OMB)(Participants) | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 | Total |
|---|---|---|---|---|---|---|
| American Indian or Alaska Native | 0 | 0 | 0 | 0 | 0 | 0 |
| Asian | 0 | 0 | 0 | 0 | 0 | 0 |
| Native Hawaiian or Other Pacific Islander | 0 | 0 | 0 | 0 | 0 | 0 |
| Black or African American | 0 | 0 | 1 | 0 | 0 | 1 |
| White | 10 | 10 | 9 | 8 | 9 | 46 |
| More than one race | 0 | 0 | 0 | 2 | 1 | 3 |
| Unknown or Not Reported | 0 | 0 | 0 | 0 | 0 | 0 |
| Region of Enrollment(participants) | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 | Total |
|---|---|---|---|---|---|---|
| Switzerland | 10 | 10 | 10 | 10 | 10 | 10 |
| Body weight(kilograms) | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 | Total |
|---|---|---|---|---|---|---|
| Mean | 65.94 ± 9.50 | 69.83 ± 15.15 | 71.98 ± 13.16 | 75.20 ± 11.24 | 71.30 ± 11.66 | 70.85 ± 12.16 |
| Height(centimeters) | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 | Total |
|---|---|---|---|---|---|---|
| Mean | 171.0 ± 8.1 | 168.0 ± 9.3 | 170.1 ± 8.4 | 174.0 ± 10.4 | 169.4 ± 9.1 | 170.5 ± 9.0 |
| Body mass index(kilograms/square meters) | Study Part A - Cohort 1 - Akynzeo | Study Part A - Cohort 1 - Fosnetupitant | Study Part A - Cohort 2 | Study Part A - Cohort 3 | Study Part A - Cohort 4 | Total |
|---|---|---|---|---|---|---|
| Mean | 22.46 ± 2.20 | 24.49 ± 3.36 | 24.69 ± 2.65 | 24.74 ± 2.26 | 24.83 ± 3.42 | 24.24 ± 2.86 |
PDFs hosted by the registry, ClinicalTrials.gov.
Plan to share: No — No need to share IPD
Ran from Jun 2023 to primary completion in Oct 2023, 4 months.
Results were first posted in May 2025, 1 year 6 months after primary completion.
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