An Absolute Bioavailability Study in Healthy Participants Comparing Oral to Intravenous Administration of GDC-0973 (Cobimetinib)

NCT ID: NCT01249118

Last Updated: 2017-05-10

Basic Information

• Recruitment Status: COMPLETED
• Clinical Phase: PHASE1
• Total Enrollment: 13 participants
• Study Classification: INTERVENTIONAL
• Study Start Date: 2010-11-30
• Study Completion Date: 2011-01-31

Brief Summary

The primary objective of Part 1 of this study is to evaluate the safety and tolerability of the intravenous (IV) dose of GDC-0973. The primary objectives of Part 2 of this study are to evaluate the absolute bioavailability of GDC-0973 and to evaluate the pharmacokinetic (PK) of GDC-0973 following IV and oral administration. The secondary objective of Part 2 of this study is to evaluate the safety of GDC-0973 administered orally and intravenously.

Conditions

Healthy Volunteers

Study Design

• Allocation Method: RANDOMIZED
• Intervention Model: CROSSOVER
• Primary Study Purpose: BASIC_SCIENCE
• Blinding Strategy: NONE

Study Groups

Part 1: GDC-0973 IV Infusion First, Then GDC-0973 Capsules

Participants will receive single dose of GDC-0973 2 milligrams (mg) IV infusion in first intervention period followed by single dose of GDC-0973 20 mg oral capsules (four 5-mg capsules) in second intervention period. The washout period between each period will be a minimum of 10 days.

Group Type: EXPERIMENTAL

GDC-0973 IV Infusion

Intervention Type: DRUG

IV infusion.

GDC-0973 Oral Capsules

Intervention Type: DRUG

Oral dose.

Part 2: GDC-0973 IV Infusion First, Then GDC-0973 Capsules

Participants will receive single dose of GDC-0973 2 mg IV infusion in first intervention period followed by single dose of GDC-0973 20 mg oral capsules (four 5-mg capsules) in second intervention period. The washout period between each period will be a minimum of 10 days.

Group Type: EXPERIMENTAL

GDC-0973 IV Infusion

Intervention Type: DRUG

IV infusion.

GDC-0973 Oral Capsules

Intervention Type: DRUG

Oral dose.

Part 2: GDC-0973 Capsules First, Then GDC-0973 IV Infusion

Participants will receive single dose of GDC-0973 20 mg oral capsules (four 5-mg capsules) in first intervention period followed by single dose of GDC-0973 2 mg IV infusion in second intervention period. The washout period between each period will be a minimum of 10 days.

Group Type: EXPERIMENTAL

GDC-0973 IV Infusion

Intervention Type: DRUG

IV infusion.

GDC-0973 Oral Capsules

Intervention Type: DRUG

Oral dose.

Interventions

GDC-0973 IV Infusion

IV infusion.

Intervention Type: DRUG

GDC-0973 Oral Capsules

Oral dose.

Intervention Type: DRUG

Other Intervention Names

XL518; XL518

Eligibility Criteria

Inclusion Criteria

• Within body mass index range 18.5 to 29.9 kilograms per square meter (kg/m^2)
• In good health, determined by no clinically significant findings from medical history, 12-lead electrocardiogram (ECG), and vital signs
• Clinical laboratory evaluations within the reference range for the test laboratory
• Negative test for selected drugs of abuse at Screening and at each Check-in
• Negative hepatitis panel and anti-hepatitis C virus and negative human immunodeficiency virus (HIV) antibody screens
• Healthy males and females of non-child-bearing potential or who agree to use effective contraception

Exclusion Criteria

• Significant history or clinical manifestation of any significant metabolic, allergic, dermatological, hepatic, renal, hematological, pulmonary, cardiovascular, gastrointestinal, neurological, or psychiatric disorder
• History of significant hypersensitivity, intolerance, or allergy to any drug compound, food, or other substance
• History of stomach or intestinal surgery or resection that would potentially alter absorption and/or excretion of orally administered drugs except that appendectomy, hernia repair, and cholecystectomy will be allowed
• History or presence of an abnormal ECG
• History of alcoholism or drug addiction prior to period 1 check-in
• Use of any tobacco-containing or nicotine-containing products prior to period 1 check-in
• Participation in any other investigational study drug trial in which receipt of an investigational study drug occurred within 28 days or 5 half-lives, whichever is longer, prior to period 1 check-in
• Use of any prescription medications/products, including proton pump inhibitors, within 14 days prior to period 1 check-in
• Poor peripheral venous access
• Any acute or chronic condition that would limit the participants ability to complete and/or participate in this clinical study
• Female participant is pregnant, lactating, or breastfeeding
• Predisposing factors to retinal vein occlusion (RVO)

• Minimum Eligible Age: 18 Years
• Maximum Eligible Age: 55 Years
• Eligible Sex: ALL
• Accepts Healthy Volunteers: Yes

Sponsors

Genentech, Inc.

INDUSTRY

Sponsor Role: lead

Responsible Party

Responsibility Role: SPONSOR

Principal Investigators

Isabelle Rooney, M.D., PhD

Role: STUDY_DIRECTOR

Genentech, Inc.

Other Identifiers

MEK4952g

Identifier Type: -

Identifier Source: org_study_id