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

NCT02136524 | Completed Phase 1

• 1 other identifier: GP28370
• Study Type: interventional
• Target: 28
• Locations: 1 country
• Sites: 1

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.

Conditions

Healthy Volunteer

Outcome Measures

Primary Outcomes (8)

• 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 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)

• 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 Outcomes (1)

• Incidence of adverse events

  Up to 4 weeks

Study Arms (2)

Capsule formulation

EXPERIMENTAL

Drug: cobimetinib

Tablet formulation

EXPERIMENTAL

Drug: cobimetinib

Interventions

cobimetinib DRUG

Single, oral dose given as a tablet on Day 1 after a minimum 8 h fast

Also known as: GDC-0973, XL-518

Tablet formulation

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• 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

You may not qualify if:

• 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)

Sponsors & Collaborators

• Genentech, Inc.: lead

Study Sites (1)

Unknown Facility

Dallas, Texas, 75247, United States

Location

MeSH Terms

Interventions

cobimetinib

Study Officials

• Clinical Trials

  Hoffmann-La Roche

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: May 9, 2014
• First Posted: May 13, 2014
• Study Start: April 1, 2014
• Primary Completion: May 1, 2014
• Study Completion: May 1, 2014
• Last Updated: November 2, 2016

Record last verified: 2016-11

Locations

US (1)