A Randomized, Phase I, Cross-Over Study to Assess the Relative Bioavailability of Single-Dose Cobimetinib (GDC-0973) in Tablet vs. Capsule Formulation

Phase 1

Completed

• Conditions: Healthy Volunteer
• Interventions: Drug: cobimetinib

• Registration Number: NCT02136524
• Lead Sponsor: Genentech, Inc.

Brief Summary

This study will be a Phase 1, open-label, randomized, 2-period, 2-treatment sequence crossover study to determine the relative bioavailability of cobimetinib administered as a single dose of the tablet formulation relative to a single dose of the capsule formulation to healthy male and female participants. A minimum of 24 participants (12 participants per sequence) will complete the study. Participants will be randomly assigned to 2 possible sequences (i.e., I: A/B, II: B/A) where the treatments are as follows: Treatment A: One cobimetinib tablet administered as a single oral dose after at least an 8-hour fast; Treatment B: Four cobimetinib capsules administered as a single oral dose after at least an 8-hour fast. The study is expected to last approximately 7 weeks.

Detailed Description

Not available

Study Timeline

• Study Start: 2014-04
• Primary Completion: 2014-05
• Study Completion: 2014-05
• Study First Submitted: 2014-05-09
• Study First Submitted QC: 2014-05-09
• Study First Posted: 2014-05-13
• Status Verified: 2016-11
• Last Update Submitted: 2016-11-01
• Last Update Posted: 2016-11-02

Recruitment & Eligibility

• Status: COMPLETED
• Sex: All
• Target Recruitment: 28

Inclusion Criteria

• Healthy male and female volunteers between 18 and 55 years of age, inclusive
• Body mass index between 18.5 to 32.0 kg/m2, inclusive;
• Adequate renal, liver, and hematologic function
• Participants who are in good health as determined by no clinically significant findings from medical history, 12-lead ECG, vital signs, and clinical laboratory evaluations

Exclusion Criteria

• Significant history or clinical manifestation of any metabolic, allergic, dermatological, hepatic, renal, hematological, pulmonary, cardiovascular, gastrointestinal, neurological, or psychiatric disorder (as determined by the Investigator)

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: CROSSOVER

Arm && Interventions

Group	Intervention	Description
Tablet formulation	cobimetinib	-
Capsule formulation	cobimetinib	-

Primary Outcome Measures

Name	Time	Method
Apparent terminal elimination rate constant	Days 1 to 10 and 15 to 25 (1 to 10 of the second crossover sequence)
Half-life (t1/2)	Days 1 to 10 and 15 to 25 (1 to 10 of the second crossover sequence)
Apparent clearance (CL/F)	Days 1 to 10 and 15 to 25 (1 to 10 of the second crossover sequence)
Maximum observed concentration (Cmax)	Days 1 to 10 and 15 to 25 (1 to 10 of the second crossover sequence)
Time to maximum concentration (tmax)	Days 1 to 10 and 15 to 25 (1 to 10 of the second crossover sequence)
Area under the concentration-time curve (AUC)	Days 1 to 10 and 15 to 25 (1 to 10 of the second crossover sequence)
Apparent volume of distribution (Vz/F)	Days 1 to 10 and 15 to 25 (1 to 10 of the second crossover sequence)
Relative bioavailability (Frel)	Days 1 to 10 and 15 to 25 (1 to 10 of the second crossover sequence)

Secondary Outcome Measures

Name	Time	Method
Incidence of adverse events	Up to 4 weeks