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

This study has been completed.
Sponsor:
Information provided by (Responsible Party):
Genentech
ClinicalTrials.gov Identifier:
NCT01240226
First received: November 10, 2010
Last updated: July 19, 2012
Last verified: July 2012
  Purpose

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.


Condition Intervention Phase
Healthy Volunteer
Drug: GDC-0941
Drug: ketoconazole
Phase 1

Study Type: Interventional
Study Design: Allocation: Randomized
Intervention Model: Crossover Assignment
Masking: Open Label
Primary Purpose: Treatment
Official Title: 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

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 ] [ Designated as safety issue: No ]
  • Pharmacokinetic parameters of GDC-0941 (total exposure, maximum and minimum plasma concentration) [ Time Frame: Prior to and after GDC-0941 dosing ] [ Designated as safety issue: No ]

Enrollment: 22
Study Start Date: November 2010
Study Completion Date: December 2010
Primary Completion Date: December 2010 (Final data collection date for primary outcome measure)
Arms Assigned Interventions
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

  Eligibility

Ages Eligible for Study:   18 Years to 50 Years
Genders Eligible for Study:   Both
Accepts Healthy Volunteers:   Yes
Criteria

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
  Contacts and Locations
Please refer to this study by its ClinicalTrials.gov identifier: NCT01240226

Locations
United States, Texas
Investigational Site
Austin, Texas, United States, 78744
Sponsors and Collaborators
Genentech
Investigators
Study Director: Scott Holden, M.D. Genentech
  More Information

No publications provided

Responsible Party: Genentech
ClinicalTrials.gov Identifier: NCT01240226     History of Changes
Other Study ID Numbers: GDC4931g
Study First Received: November 10, 2010
Last Updated: July 19, 2012
Health Authority: United States: Food and Drug Administration

Additional relevant MeSH terms:
Ketoconazole
14-alpha Demethylase Inhibitors
Enzyme Inhibitors
Molecular Mechanisms of Pharmacological Action
Pharmacologic Actions
Antifungal Agents
Anti-Infective Agents
Therapeutic Uses

ClinicalTrials.gov processed this record on April 16, 2014