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

A PHASE 1, OPEN-LABEL, SINGLE-DOSE, RANDOMIZED, 2-PERIOD, 2-TREATMENT SEQUENCE CROSS-OVER STUDY TO ASSESS THE RELATIVE BIOAVAILABILITY OF COBIMETINIB ADMINISTERED AS A TABLET FORMULATION COMPARED TO A CAPSULE FORMULATION IN HEALTHY SUBJECTS

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT02136524

Enrollment

Registered

2014-05-13

Start date

2014-04-30

Completion date

2014-05-31

Last updated

2016-11-02

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Healthy Volunteer

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.

Interventions

DRUGcobimetinib

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

Study design

Allocation

RANDOMIZED

Intervention model

CROSSOVER

Masking

NONE

Eligibility

Sex/Gender

ALL

Age

18 Years to 55 Years

Healthy volunteers

Yes

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)

Design outcomes

Primary

Measure	Time frame
Relative bioavailability (Frel)	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)
Maximum observed concentration (Cmax)	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)

Secondary

Measure	Time frame
Incidence of adverse events	Up to 4 weeks

Countries

United States

Outcome results

None listed

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026