Phase 1
Completed N=50
Pharmacokinetics and Safety Study of Omecamtiv Mecarbil in Healthy Japanese Adults
Healthy Volunteer
Source: ClinicalTrials.gov NCT02601001 ↗
Enrolled (actual)
50
Serious AEs
0.0%
Results posted
May 2021
Primary outcomePrimary: Dosing Period 1: Maximum Observed Plasma Concentration (Cmax) of Omecamtiv Mecarbil After First and Last Dose in Period 1 — 77.4; 79.5; 256; 259 ng/mL
Summary
The purpose of this study is to evaluate the pharmacokinetics (PK), safety, and tolerability of omecamtiv mecarbil in healthy volunteers in Japan.
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Dosing Period 1: Maximum Observed Plasma Concentration (Cmax) of Omecamtiv Mecarbil After First and Last Dose in Period 1 |
77.4; 79.5; 256; 259 | — |
| PRIMARY Dosing Period 1: Time to Maximum Observed Plasma Concentration (Tmax) of Omecamtiv Mecarbil After First and Last Dose in Period 1 |
4.0; 3.0; 2.0; 2.0 | — |
| PRIMARY Dosing Period 1: Area Under the Concentration-time Curve for a Dosing Interval of 12 Hours (AUC0-12) for Omecamtiv Mecarbil After First and Last Dose in Period 1 |
687; 677; 2570; 2670 | — |
| PRIMARY Dosing Period 1: Predose Omecamtiv Mecarbil Plasma Concentration |
190; 192 | — |
| PRIMARY Dosing Period 1: Accumulation Ratio |
3.66; 3.79 | — |
| PRIMARY Dosing Period 2: Maximum Observed Plasma Concentration (Cmax) of Omecamtiv Mecarbil After First and Last Dose in Period 2 |
96.5; 107; 84.9; 154; 335; 341 | — |
| PRIMARY Dosing Period 2: Time to Maximum Observed Plasma Concentration (Tmax) of Omecamtiv Mecarbil After First and Last Dose in Period 2 |
4.0; 2.0; 4.0; 3.0; 2.0; 3.0 | — |
| PRIMARY Dosing Period 2: AUC(0-12) for Omecamtiv Mecarbil After First and Last Dose in Period 2 |
902; 950; 841; 1330; 3520; 3500 | — |
| PRIMARY Dosing Period 2: Predose Omecamtiv Mecarbil Plasma Concentration |
271; 256; 245; 401 | — |
| PRIMARY Dosing Period 2: Accumulation Ratio |
4.12; 3.81; 4.53; 4.11 | — |
| SECONDARY Number of Participants With Treatment-emergent Adverse Events |
6; 4; 7; 4; 3; 0 | — |
| SECONDARY Number of Participants With Grade 3 or Higher Laboratory Toxicities |
0; 0; 0; 0; 0 | — |
| SECONDARY Maximum Increase From Baseline in Fridericia-Corrected QT Interval (QTcF) In Dosing Period 1 |
10; 7; 13; 7; 13; 0 | — |
| SECONDARY Maximum Increase From Baseline in Fridericia-Corrected QT Interval (QTcF) In Dosing Period 2 |
10; 7; 13; 7; 12; 0 | — |
Eligibility Criteria
Inclusion Criteria
- No history or evidence of clinically relevant medical disorders as determined by the Investigator, and in good health as determined by a pre-study physical examination and medical history with no clinically significant abnormalities, normal vital signs and no history or presence of a clinically significant abnormal electrocardiogram finding
- Subjects' pre-study clinical laboratory findings (including creatine phosphokinase) should be within normal range or if outside of the normal range, are deemed not clinically significant by the Investigator.
Exclusion Criteria
- A clinically significant disorder/disease, including gastro intestinal abnormalities that might interfere with absorption
- An unstable medical condition, defined as having been hospitalized within 28 days before day 1, major surgery within 6 months before day 1, or otherwise unstable in the judgment of the Investigator
- History or evidence of any other clinically significant disorder, condition, or disease that, in the opinion of the Investigator or Medical Monitor would pose a risk to subject safety or interfere with the study evaluation, procedures, or completion
- History of malignancy of any type other than surgically excised non-melanomatous skin cancers or in situ cervical cancer within 5 years before the day of dosing
- Use of any prescription or over-the-counter medications within 14 days or 5 half-lives (whichever time period is greater), prior to receiving the first dose of omecamtiv mecarbil (acetaminophen up to 2 grams per day for analgesia and hormone replacement therapy (e.g., estrogen) will be allowed
- Use of any known inhibitors of CYP3A4/p-glycoprotein (P-gp) or CYP2D6 within 14 days or 5 half-lives, whichever is longer; or use of grapefruit juice or grapefruit containing products within 7 days prior to receiving the first dose of omecamtiv mecarbil
- Use of any known CYP3A4 inducers within 30 days or 5 half-lives, whichever is longer, before receiving omecamtiv mecarbil
Data sourced from ClinicalTrials.gov (NCT02601001). 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.