A Phase I Study to Investigate the Absorption, Metabolism, and Excretion of [14c]-GDC-0941 Following Single Oral Dose Administration in Healthy Male Subjects
Trial Snapshot
- Phase
- Phase 1
- Status
- Completed
- Sponsor
- Genentech, Inc.
- Enrollment
- 5
- Primary Endpoint
- Pharmacokinetic property based on the plasma concentrations of total radioactivity and GDC-0941: area under the concentration-time curve extrapolated to infinity
Study Overview
Brief Summary
This study will be an open-label, non-randomized, absorption, metabolism, and excretion study of [14C]-GDC 0941 administered as an oral dose to 6 healthy male subjects following at least a 10-hour fast from food (not including water).
Study Design
- Study Type
- Interventional
- Allocation
- Randomized
- Intervention Model
- Single Group
- Primary Purpose
- Treatment
- Masking
- None
Eligibility Criteria
- Ages
- 18 Years to 55 Years (Adult)
- Sex
- Male
- Accepts Healthy Volunteers
- Yes
Inclusion Criteria
- •Within BMI range 18.5 to 29.9 kg/m2, inclusive
- •In good health, determined by no clinically significant findings from medical history, 12-lead ECG, and vital signs
- •Clinical laboratory evaluations within the reference range for the test laboratory
- •Negative test for selected drugs of abuse at Screening and at Check-in
- •Negative hepatitis panel (including hepatitis B surface antigen [HBsAg], hepatitis C virus antibody [anti-HCV]) and negative HIV antibody screens
- •Subjects will either be sterile or agree to use an approved form of contraception from Check-in until 45 days following Study Completion/ET
- •Agree not to donate sperm from Screening throughout the study period and for at least 3 months (90 days) after the last dose of study drug
- •A minimum of 1 to 2 bowel movements per day
Exclusion Criteria
- •Significant history or clinical manifestation of any significant metabolic, allergic, dermatological, hepatic, renal, hematological, pulmonary, cardiovascular, gastrointestinal, neurological, or psychiatric disorder
- •History of significant hypersensitivity, intolerance, or allergy to any drug compound, food, or other substance
- •History of stomach or intestinal surgery or resection that would potentially alter absorption and/or excretion of orally administered drugs (except that appendectomy and hernia repair will be allowed)
- •History of Gilbert's Syndrome
- •History of diabetes mellitus and/or elevated fasting glucose at baseline
- •History or presence of an abnormal ECG
- •History of alcoholism or drug addiction within 1 year prior to Check-in
- •Participation in more than one other radiolabeled investigational study drug trial within 12 months prior to Check-in. The previous radiolabeled study drug must have been received more than 6 months prior to Check-in for this study and the total exposure from this study and the previous study will be within the recommended levels considered safe
- •Exposure to significant radiation within 12 months prior to Check-in
- •Use of any tobacco-containing or nicotine-containing products within 6 months prior to Check-in or positive urine drug screen for cotinine
- •Participation in any other investigational study drug trial in which receipt of an investigational study drug occurred within 5 half-lives or 30 days, whichever is longer, prior to Check-in
- •Use of any prescription medications/products within 14 days prior to Check-in, unless deemed acceptable by the Investigator
- •Use of any over-the-counter (OTC), non-prescription preparations (including vitamins, minerals, and phytotherapeutic/herbal/plant derived preparations) within 7 days prior to Check-in
- •Use of alcohol-, grapefruit-, or caffeine-containing foods or beverages within 72 hours prior to Check-in, unless deemed acceptable by the Investigator
- •Poor peripheral venous access
- •Donation of blood from 30 days prior to Screening or of plasma from 2 weeks prior to Screening
- •Receipt of blood products within 2 months prior to Check-in
- •Any acute or chronic condition that, in the opinion of the Investigator, would limit the subject's ability to complete and/or participate in this clinical study
Arms & Interventions
A
Experimental
Intervention: GDC-0941 (Drug)
Outcomes
Primary Outcomes
Pharmacokinetic property based on the plasma concentrations of total radioactivity and GDC-0941: area under the concentration-time curve extrapolated to infinity
Time Frame: up to approximately 6 weeks or early study discontinuation
Pharmacokinetic property based on the plasma concentrations of total radioactivity and GDC-0941: apparent terminal phase elimination rate constant
Time Frame: up to approximately 6 weeks or early study discontinuation
Pharmacokinetic property based on the plasma concentrations of total radioactivity and GDC-0941: apparent volume of distribution
Time Frame: up to approximately 6 weeks or early study discontinuation
Pharmacokinetic property based on the plasma concentrations of total radioactivity and GDC-0941: area under the concentration-time curve from Hour 0 to the last measurable concentration
Time Frame: up to approximately 6 weeks or early study discontinuation
Pharmacokinetic property based on the plasma concentrations of total radioactivity and GDC-0941: apparent total clearance
Time Frame: up to approximately 6 weeks or early study discontinuation
Pharmacokinetic property based on the plasma concentrations of total radioactivity and GDC-0941: apparent terminal elimination half-life
Time Frame: up to approximately 6 weeks or early study discontinuation
Pharmacokinetic property based on the plasma concentrations of total radioactivity and GDC-0941: maximum observed concentration
Time Frame: up to approximately 6 weeks or early study discontinuation
Pharmacokinetic property based on the plasma concentrations of total radioactivity and GDC-0941: time to maximum concentration
Time Frame: up to approximately 6 weeks or early study discontinuation
Secondary Outcomes
- Amount of drug excreted in the feces over the sampling interval(up to approximately 6 weeks or early study discontinuation)
- Percent excreted in feces(up to approximately 6 weeks or early study discontinuation)