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

This study has been completed.
Sponsor:
Information provided by:
Genentech
ClinicalTrials.gov Identifier:
NCT00999128
First received: October 19, 2009
Last updated: February 25, 2010
Last verified: February 2010
  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:


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 April 17, 2014