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 - Full Text View

Purpose

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.

Condition	Intervention	Phase
Healthy Volunteers	Drug: GDC-0941 Drug: rabeprazole	Phase 1

Study Type:	Interventional
Study Design:	Intervention Model: Crossover Assignment Masking: Open Label Primary Purpose: Treatment
Official Title:	An Open-Label, Two-Part 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

Resource links provided by NLM:

Drug Information available for: Rabeprazole Rabeprazole sodium

U.S. FDA Resources

Further study details as provided by Genentech:

Primary Outcome Measures:

Incidence, nature, and severity of adverse events [ Time Frame: Through study completion or early study discontinuation ]
PK parameters of GDC-0941 (total exposure, maximum and minimum plasma concentration) [ Time Frame: Following administration of study drug ]

Enrollment:	50
Study Start Date:	October 2009
Primary Completion Date:	February 2010 (Final data collection date for primary outcome measure)

Arms	Assigned Interventions
Experimental: Part 1	Drug: GDC-0941 Oral repeating dose
Experimental: Part 2	Drug: GDC-0941 Oral repeating dose Drug: rabeprazole Oral repeating dose

Eligibility

Ages Eligible for Study:	18 Years to 65 Years
Genders Eligible for Study:	Both
Accepts Healthy Volunteers:	Yes

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

Contacts and Locations

Please refer to this study by its ClinicalTrials.gov identifier: NCT00999128

Locations

United States, California
Genentech Trial Information Support
South San Francisco, California, United States, 94080

Sponsors and Collaborators

Genentech

Investigators

Study Director:

Scott Holden, M.D.

Genentech

More Information

No publications provided

Responsible Party:	Clinical Trials Posting Group, Genentech, Inc.
ClinicalTrials.gov Identifier:	NCT00999128 History of Changes
Other Study ID Numbers:	GDC4740g
Study First Received:	October 19, 2009
Last Updated:	February 25, 2010
Health Authority:	France: Afssaps - Agence française de sécurité sanitaire des produits de santé (Saint-Denis)

Keywords provided by Genentech:

PI3K inhibitor
PI3 kinase
PI3 kinase inhibitor

Additional relevant MeSH terms:

Rabeprazole
Enzyme Inhibitors
Molecular Mechanisms of Pharmacological Action
Pharmacologic Actions

Anti-Ulcer Agents
Gastrointestinal Agents
Therapeutic Uses

ClinicalTrials.gov processed this record on May 19, 2013