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



Status:Completed
Conditions:Healthy Studies
Therapuetic Areas:Other
Healthy:No
Age Range:18 - 50
Updated:3/4/2017
Start Date:November 2010
End Date:December 2010

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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.


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
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