Phase 1
Completed N=15
A Performance and Bioavailability Study of Entrectinib in Healthy Volunteers.
Source: ClinicalTrials.gov NCT03961100 ↗Enrolled (actual)
15
Serious AEs
0.0%
Results posted
Sep 2020
Primary outcomePrimary: Area Under the Concentration-Time Curve From Time 0 to Infinity (AUC0-inf) of Entrectinib — 41500; 46600; 43400; 9860 nmol*h/L
Summary
This study will evaluate the bioavailability, palatability, safety and tolerability of entrectinib in healthy volunteers. Part 1 of the study will explore the performance of entrectinib multi-particle formulation. Part 2 will evaluate the effect of drug substance particle size on entrectinib bioavailability.
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Area Under the Concentration-Time Curve From Time 0 to Infinity (AUC0-inf) of Entrectinib |
41500; 46600; 43400; 9860; 10100 | — |
| PRIMARY AUC0-inf of Entrectinib Active Metabolite M5 |
12400; 12200; 13600; 3900; 3780 | — |
| PRIMARY Maximum Plasma Concentration (Cmax) of Entrectinib |
1930; 1940; 1880; 494; 522 | — |
| PRIMARY Cmax of Entrectinib Active Metabolite M5 |
398; 325; 360; 100; 113 | — |
| SECONDARY Percentage of Participants With Treatment-Emergent Adverse Events (TEAEs) |
100; 93.3; 100; 31.3; 37.5 | — |
Eligibility Criteria
Inclusion Criteria
- A body mass index (BMI) between 18.0 and 32.0 kilogram per square meter (kg/m2), inclusive, and weighing >/=50 kg.
- Agreement to comply with measures to prevent pregnancy and restrictions on egg and sperm donation
Exclusion Criteria
- Women of childbearing potential, women who are pregnant or breastfeeding, or intending to become pregnant during the study or within 14 days after the final dose of entrectinib or have a pregnant partner
- A clinical significant medical history of gastrointestinal surgery (e.g., gastric bypass) or other gastrointestinal disorder (e.g., malabsorption syndrome) that might affect absorption of medicines from the gastrointestinal tract
- Presence of a clinically significant disease, illness, medical condition or disorder, or any other medical history determined by the investigator to be clinically significant and relevant
- Clinically significant change in health status, or any major illness, or clinically significant acute infection or febrile illness
- Use of moderate or potent inhibitors or inducers of CYP P450 3A4 enzyme or P-gp transporter, or use of other prohibited medications
- Participation in any other clinical study involving an investigational medicinal product (IMP) or device
- A positive test result for hepatitis B, hepatitis C (HCV), or human immunodeficiency virus (HIV)
- Current smokers and those who have smoked, or users of e-cigarettes and nicotine replacement products within the last 12 months
- Known history of clinically significant hypersensitivity, or severe allergic reaction, to entrectinib or related compounds
Data sourced from ClinicalTrials.gov (NCT03961100). 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.