Phase 1
Completed N=16
A Study Investigating the Absolute Oral Bioavailability of Balovaptan After Single and Multiple Daily Oral Doses of Balovaptan in Healthy Volunteers
Healthy Volunteers
Source: ClinicalTrials.gov NCT03764449 ↗
Enrolled (actual)
16
Serious AEs
0.0%
Results posted
Feb 2020
Primary outcomePrimary: Absolute Bioavailability of Oral Balovaptan at Dose Level A (Cohort 1) — 100.6 Percentage
Summary
This study was a non-randomized, open-label, parallel group, two-treatment study in healthy volunteers to investigate the absolute oral bioavailability of balovaptan. The study was conducted at 1 site in the Netherlands.
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Absolute Bioavailability of Oral Balovaptan at Dose Level A (Cohort 1) |
100.6 | — |
| SECONDARY Absolute Bioavailability of Oral Balovaptan at Dose Level B (Cohort 2) |
108.2 | — |
| SECONDARY Absolute Bioavailability of Oral Balovaptan at Dose A and Dose B |
82.3; 103.1 | — |
| SECONDARY Maximum Plasma Concentration (Cmax) of IV Balovaptan |
688; 1601; 1591; 1974 | — |
| SECONDARY Cmax of Oral Balovaptan |
36.9; 443; 108; 643 | — |
| SECONDARY Cmax of M2 Metabolites |
3.87; 23.6; 20.3; 105 | — |
| SECONDARY Cmax of M3 Metabolites |
6.18; 57.9; 57.2; 260 | — |
| SECONDARY Time to Maximum Observed Plasma Concentration (Tmax) of IV Balovaptan |
0.25; 0.25; 0.25; 0.25 | — |
| SECONDARY Tmax of Oral Balovaptan |
1.23; 1.00; 1.28; 1.11 | — |
| SECONDARY Tmax of M2 Metabolites |
24.0; 24.0; 4.50; 3.38 | — |
| SECONDARY Tmax of M3 Metabolites |
48.0; 12.0; 2.13; 1.88 | — |
| SECONDARY Apparent Terminal Half-Life (t1/2) of IV Balovaptan |
35.2; 19.5; 27.7; 15.7 | — |
| SECONDARY T1/2 of Oral Balovaptan |
38.8; 29.1; 31.2; 22.7 | — |
| SECONDARY T1/2 of M2 Metabolites |
48.5; 35.7; 36.3; 28.5 | — |
| SECONDARY T1/2 of M3 Metabolites |
93.0; 68.2; 60.3; 33.7 | — |
| SECONDARY Area Under the Plasma Concentration-Time Curve From Time Zero to the Last Measurable Plasma Concentration Time Point (AUC0-last) of IV Balovaptan |
8087; 9372 | — |
| SECONDARY AUC0-last of Oral Balovaptan |
937; 5497 | — |
| SECONDARY AUC0-last of M2 Metabolites |
297; 1751 | — |
| SECONDARY AUC0-last of M3 Metabolites |
754; 3908 | — |
| SECONDARY Area Under the Plasma Concentration-Time Curve From Time Zero Extrapolated to Infinity (AUC0-inf) of IV Balovaptan |
8929; 9569; 15492; 10430 | — |
| SECONDARY AUC0-inf of Oral Balovaptan |
1008; 5550 | — |
| SECONDARY AUC0-inf of M2 Metabolites |
520; 1819 | — |
| SECONDARY AUC0-inf of M3 Metabolites |
1122; 4221 | — |
| SECONDARY Area Under the Plasma Concentration-Time Curve Over the Dosing Interval at Steady State (AUC0-24) of IV Balovaptan |
4400; 6690; 9898; 7908 | — |
| SECONDARY AUC0-24 of Oral Balovaptan |
458; 3632; 1322; 5505 | — |
| SECONDARY AUC0-24 of M2 Metabolites |
54.7; 427; 404; 2087 | — |
| SECONDARY AUC0-24 of M3 Metabolites |
106; 1188; 1102; 4727 | — |
| SECONDARY Last Measurable Plasma Concentration (Clast) of IV Balovaptan |
13.6; 6.62; 12.5; 6.92 | — |
| SECONDARY Clast of Oral Balovaptan |
1.22; 1.22; 3.51; 3.40 | — |
| SECONDARY Clast of M2 Metabolites |
1.24; 1.25; 3.19; 9.95 | — |
| SECONDARY Clast of M3 Metabolites |
1.43; 2.74; 11.9; 17.6 | — |
| SECONDARY Time of Last Measurable Plasma Concentration (Tlast) of IV Balovaptan |
106.75; 100.75; 106.75; 82.75 | — |
| SECONDARY Tlast of Oral Balovaptan |
132.00; 156.00; 108.00; 108.00 | — |
| SECONDARY Tlast of M2 Metabolites |
120.00; 168.00; 108.00; 108.00 | — |
| SECONDARY Tlast of M3 Metabolites |
216.00; 216.00; 108.00; 108.00 | — |
| SECONDARY Terminal Elimination Rate Constant (λz) of IV Balovaptan |
0.0197; 0.0356; 0.0250; 0.0442 | — |
| SECONDARY λz of Oral Balovaptan |
0.0179; 0.0239; 0.0222; 0.0306 | — |
| SECONDARY λz of M2 Metabolites |
0.0143; 0.0194; 0.0191; 0.0244 | — |
| SECONDARY λz of M3 Metabolites |
0.0075; 0.0102; 0.0115; 0.0206 | — |
| SECONDARY Total Body Clearance (CL) of IV Balovaptan |
9.98; 9.75; 6.23; 9.36 | — |
| SECONDARY Volume of Distribution (Vss) of IV Balovaptan |
396; 197; 166; 154 | — |
| SECONDARY Percentage of Participants With Treatment-Emergent Adverse Events |
50; 75; 63; 88 | — |
Eligibility Criteria
Inclusion Criteria
- Healthy male and female subjects. Healthy status is defined by absence of evidence of any active or chronic disease following a detailed medical and surgical history, a complete physical examination including vital signs, 12-lead ECG, hematology, blood chemistry, urinalysis, and serology.
- Body Mass Index of 18 to 30 kg/m2, inclusive.
- For women of childbearing potential: agreement to use at least 2 acceptable contraceptive methods during the treatment period and for 90 days after the last dose of study drug.
- For men: agreement to use contraceptive measures, and agreement to refrain from donating sperm until 90 days after the last dose of study drug.
Exclusion Criteria
- Female subjects who are pregnant or lactating.
- Any condition or disease detected during the medical interview/physical examination that would render the subject unsuitable for the study, place the subject at undue risk or interfere with the ability of the subject to complete the study in the opinion of the Investigator.
Data sourced from ClinicalTrials.gov (NCT03764449). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication. Informational only — not medical advice.