A Study to Determine the Relative Bioavailability of a Tablet Formulation of GDC-0941 and the Effect of Ketoconazole on the Pharmacokinetics of the GDC-0941 Tablet

An Open-Label, 2-Part Study to Determine the Relative Bioavailability of a Tablet Formulation of GDC-0941 and the Effect of Ketoconazole on the Pharmacokinetics of the GDC-0941 Tablet

This will be a single-center, open-label, randomized, 2-part study to determine the relative bioavailability of GDC-0941 capsule and market-image tablet formulations and the effect of ketoconazole on the pharmacokinetics of the GDC-0941 market-image tablet formulation.

Study Overview

• Status: Completed
• Conditions: Healthy Volunteer
• Intervention / Treatment: Drug: GDC-0941; Drug: ketoconazole

• Study Type: Interventional
• Enrollment (Actual): 22
• Phase: Phase 1

Contacts and Locations

Study Locations

• United States
  • Texas
    • Austin, Texas, United States, 78744
      • Investigational Site

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 50 years (Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: All

Description

Inclusion Criteria

• Medically healthy as determined by the absence of clinically significant findings in the physical examination, medical history, vital sign measurements, clinical laboratory tests, or 12-lead electrocardiograms (ECGs)
• For female subjects: postmenopausal and without recent history of menorrhea, surgically sterile or using an effective method of contraception such as oral or transdermal contraceptives, double-barrier contraception, intrauterine device, depot progesterone, or implanted contraceptive devices, from Day -1 until 45 days after study drug completion/discharge; female subjects must have a negative pregnancy test at Screening and on Day -1
• For male subjects: sterile or a sterile sexual partner, or agreement to use 2 forms of medically acceptable methods of contraception, one of which is a barrier, and agreement not to donate sperm from Screening throughout the study period and for at least 3 months after the last dose of study drug.

Exclusion Criteria

• History of clinical manifestations of significant metabolic (including type 1 and 2 diabetes), hepatic, renal, hematological, pulmonary, cardiovascular, endocrine, gastrointestinal (including gastric or duodenal ulcers), urological, neurological, or psychiatric disease, 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 initiation of study treatment
• History of seizure disorders
• History of bipolar or major depressive disorder
• History of stomach or intestinal surgery or resection (except appendectomy, hernia repair, and cholecystectomy)
• History or presence of an abnormal ECG
• History of ventricular dysrhythmias or 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 initiation of study treatment
• Use of medications capable of inhibiting hepatic enzymes within a specified timeframe prior to initiation of study treatment
• Participation in any other investigational drug study in which receipt of an investigational study drug occurred within a specified timeframe prior to initiation of study treatment
• Use of any prescription medications/products including monoamine oxidase inhibitors, thioridazine, pimozide, or antidepressants within a specified timeframe prior to initiation of study treatment (2 weeks for antibiotics) (except hormone-replacement therapy or 2 weeks use of narcotics for pain)
• Any vaccination or immunization within a specified timeframe prior to initiation of study treatment
• Routine use of PPIs or histamine H2-receptor antagonists, or any use of these drugs within a specified timeframe prior to initiation of study treatment
• Known hypersensitivity to ketoconazole or other azole antifungals
• Use of any over-the-counter, nonprescription preparations (including supplements, vitamins, minerals, phytotherapeutic/herbal/plant-derived preparations, tryptophans, and St. John's wort) within a specified timeframe prior to initiation of study treatment
• Use of alcohol-containing, grapefruit-containing, or caffeine-containing foods or beverages within a specified timeframe prior to initiation of study treatment
• Donated blood within within a specified timeframe prior to initiation of study treatment
• Received blood products within a specified timeframe prior to initiation of study treatment

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: None (Open Label)

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: A	Drug: GDC-0941; Oral repeating dose; Drug: ketoconazole; Oral repeating dose
Experimental: B	Drug: GDC-0941; Oral repeating dose; Drug: ketoconazole; Oral repeating dose

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Incidence, nature, and severity of adverse events	Through study completion or early study discontinuation
Pharmacokinetic parameters of GDC-0941 (total exposure, maximum and minimum plasma concentration)	Prior to and after GDC-0941 dosing

Collaborators and Investigators

• Sponsor: Genentech, Inc.

Study record dates

Study Major Dates

• Study Start: November 1, 2010
• Primary Completion (Actual): December 1, 2010
• Study Completion (Actual): December 1, 2010

Study Registration Dates

• First Submitted: November 10, 2010
• First Submitted That Met QC Criteria: November 10, 2010
• First Posted (Estimate): November 15, 2010

Study Record Updates

• Last Update Posted (Actual): March 3, 2017
• Last Update Submitted That Met QC Criteria: March 2, 2017
• Last Verified: July 1, 2012

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Physiological Effects of Drugs; Molecular Mechanisms of Pharmacological Action; Anti-Infective Agents; Enzyme Inhibitors; Hormones, Hormone Substitutes, and Hormone Antagonists; Cytochrome P-450 CYP3A Inhibitors; Cytochrome P-450 Enzyme Inhibitors; Hormone Antagonists; Antifungal Agents; Steroid Synthesis Inhibitors; 14-alpha Demethylase Inhibitors; Ketoconazole
• Other Study ID Numbers: GDC4931g