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

NCT01240226 | Completed Phase 1

• 1 other identifier: GDC4931g
• Study Type: interventional
• Target: 22
• Locations: 1 country
• Sites: 1

Brief Summary

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.

Conditions

Healthy Volunteer

Outcome Measures

Primary Outcomes (2)

• 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

Study Arms (2)

A

EXPERIMENTAL

Drug: GDC-0941; Drug: ketoconazole

B

EXPERIMENTAL

Drug: GDC-0941; Drug: ketoconazole

Interventions

GDC-0941 DRUG

Oral repeating dose

A

ketoconazole DRUG

Oral repeating dose

A; B

Eligibility Criteria

• Age: 18 Years - 50 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• 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.

You may not qualify if:

• 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

Sponsors & Collaborators

• Genentech, Inc.: lead

Study Sites (1)

Investigational Site

Austin, Texas, 78744, United States

Location

MeSH Terms

Interventions

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

Intervention Hierarchy (Ancestors)

Piperazines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds

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: November 10, 2010
• First Posted: November 15, 2010
• Study Start: November 1, 2010
• Primary Completion: December 1, 2010
• Study Completion: December 1, 2010
• Last Updated: March 3, 2017

Record last verified: 2012-07

Locations

US (1)