A Study to Determine the Relative Bioavailability of Capsule and Tablet Formulations of GDC-0941 and the Effect of Food and Proton Pump Inhibition on GDC-0941 Tablet Pharmacokinetics in Healthy Volunteers

Genentech

Status and phase

Completed

Phase 1

Conditions

Healthy Volunteers

Treatments

Drug: GDC-0941

Drug: rabeprazole

Study type

Interventional

Funder types

Industry

Identifiers

NCT00999128

GDC4740g

Details and patient eligibility

About

This is a Phase I, randomized, two-part, single-center pharmacokinetics (PK) study to assess the relative bioavailability of capsule and tablet formulations of GDC-0941 in the fasted state (Part 1) and to determine the effect of food and proton pump inhibition on the PK of the tablet formulation of GDC-0941 (Part 2). Approximately 18 subjects will be enrolled in Part 1 and up to 32 subjects will be enrolled in Part 2. Subjects who participate in Part 1 are not eligible to participate in Part 2.

Enrollment

50 patients

Sex

All

Ages

18 to 65 years old

Volunteers

Accepts Healthy Volunteers

Inclusion and exclusion criteria

Inclusion Criteria

Male or female, between 18 and 65 years of age, inclusive (Part 1 only)
Male or female, between 18 and 45 years of age, inclusive (Part 2 only)
In good health, as determined by no clinically significant findings from medical history, 12-lead electrocardiogram (ECG), and vital signs assessment
Body Mass Index (BMI) between 18-30 kg/m^2 inclusive, with a body weight >50 kg
Clinical laboratory evaluations within the reference range for the test laboratory
Negative test for selected drugs of abuse at screening (does not include alcohol) and at check-in (does include alcohol)
Negative HIV, hepatitis B surface antigen (HBsAg), and hepatitis C virus antibody screens
Agreement to use an effective form of contraception for the duration of the study

Exclusion Criteria

History or clinical manifestations of significant metabolic (including type 1 and 2 diabetes), hepatic, renal, hematological, pulmonary, cardiovascular, endocrine, gastrointestinal, urological, neurological, psychiatric disorders, or cancer
History of inflammatory arthritis
History of symptomatic hypotension
History of severe physical injury, direct impact trauma, or neurological trauma within a specified timeframe prior to Day 1
History of seizure disorders
History of bipolar or major depressive disorder
History of stomach or intestinal surgery or resection that would potentially alter absorption and/or excretion of orally administered drugs (exceptions: appendectomy, hernia repair, and/or cholecystectomy)
History or presence of an abnormal ECG
Subjects with a history of ventricular dysrhythmias or with risk factors for ventricular dysrhythmias
History of alcoholism, drug abuse, or drug addiction
Use of any nicotine-containing or nicotine-replacement products within a specified timeframe prior to Day 1
Participation in any other investigational study drug trial in which receipt of an investigational study drug occurred within a specified timeframe prior to Day 1
Use of any prescription medications/products within a specified timeframe prior to Day 1 (exceptions: hormone replacement therapy [HRT], oral, implantable, or transdermal contraception)
Receipt of any vaccination or immunization within a specified timeframe prior to Day 1
Use of proton pump inhibitors or H2-receptor antagonists within a specified timeframe prior to Day 1
Known hypersensitivity to rabeprazole or any of its components, or to derived products of benzimidazoles
Use of any over-the-counter (OTC), non-prescription preparations within a specified timeframe prior to Day 1
Use of alcohol-containing, grapefruit-containing, or caffeine-containing foods or beverages within a specified timeframe prior to Day 1
Poor peripheral venous access
Donation of blood or plasma within a specified timeframe prior to Day 1
Receipt of blood products within a specified timeframe prior to Day 1
Vegetarians who are unable to consume a high-fat meal
Women who are pregnant or nursing