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

Genentech, Inc.13 enrolled

Overview

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.

Study Type

INTERVENTIONAL

Allocation

RANDOMIZED

Purpose

BASIC_SCIENCE

Masking

NONE

Enrollment

Conditions

Healthy Volunteers

Interventions

GDC-0973 IV InfusionDRUG

IV infusion.

GDC-0973 Oral CapsulesDRUG

Oral dose.

Eligibility

Sex: ALLMin age: 18 YearsMax age: 55 YearsHealthy volunteers:

Medical Language ↔ Plain English

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)

Outcomes

Primary Outcomes

Maximum Observed Plasma Concentration (Cmax) of IV and Oral GDC-0973

Time frame: Part 2: 0 hours (Hrs) (pre-dose), 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 144, and 192 Hrs post-dose on Day 1

Dose Normalized Cmax [Cmax(dn)] of IV and Oral GDC-0973

Cmax(dn) is Cmax divided by dose.