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

Genentech

Status and phase

Completed

Phase 1

Conditions

Healthy Volunteer

Treatments

Drug: ketoconazole

Drug: GDC-0941

Study type

Interventional

Funder types

Industry

Identifiers

NCT01240226

GDC4931g

Details and patient eligibility

About

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.

Enrollment

22 patients

Sex

All

Ages

18 to 50 years old

Volunteers

Accepts Healthy Volunteers

Inclusion and exclusion 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