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

NCT00999128 | Completed Phase 1

• 1 other identifier: GDC4740g
• Study Type: interventional
• Target: 50
• Locations: 1 country
• Sites: 1

Brief Summary

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.

Conditions

Healthy Volunteers

Keywords

PI3K inhibitor; PI3 kinase; PI3 kinase inhibitor

Outcome Measures

Primary Outcomes (2)

• Incidence, nature, and severity of adverse events

  Through study completion or early study discontinuation

• PK parameters of GDC-0941 (total exposure, maximum and minimum plasma concentration)

  Following administration of study drug

Study Arms (2)

Part 1

EXPERIMENTAL

Drug: GDC-0941

Part 2

EXPERIMENTAL

Drug: GDC-0941; Drug: rabeprazole

Interventions

GDC-0941 DRUG

Oral repeating dose

Part 1; Part 2

rabeprazole DRUG

Oral repeating dose

Part 2

Eligibility Criteria

• Age: 18 Years - 65 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• 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

You may not qualify if:

• 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

Sponsors & Collaborators

• Genentech, Inc.: lead

Study Sites (1)

Genentech Trial Information Support

South San Francisco, California, 94080, United States

Location

MeSH Terms

Conditions

Hereditary Sensory and Autonomic Neuropathies

Interventions

2-(1H-indazol-4-yl)-6-(4-methanesulfonylpiperazin-1-ylmethyl)-4-morpholin-4-ylthieno(3,2-d)pyrimidine; Rabeprazole

Condition Hierarchy (Ancestors)

Nervous System Malformations; Nervous System Diseases; Heredodegenerative Disorders, Nervous System; Neurodegenerative Diseases; Polyneuropathies; Peripheral Nervous System Diseases; Neuromuscular Diseases; Congenital Abnormalities; Congenital, Hereditary, and Neonatal Diseases and Abnormalities; Genetic Diseases, Inborn

Intervention Hierarchy (Ancestors)

2-Pyridinylmethylsulfinylbenzimidazoles; Sulfoxides; Sulfur Compounds; Organic Chemicals; Pyridines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds; Benzimidazoles; Heterocyclic Compounds, 2-Ring; Heterocyclic Compounds, Fused-Ring

Study Officials

• Scott Holden, M.D.

  Genentech, Inc.

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: October 19, 2009
• First Posted: October 21, 2009
• Study Start: October 26, 2009
• Primary Completion: February 26, 2010
• Study Completion: February 26, 2010
• Last Updated: February 9, 2017

Record last verified: 2010-02

Locations

US (1)