Clinical trial NCT01474668: Study to Investigate the Absorption, Metabolism, and Excretion of [14C]-GDC-0941 Following Single Oral Dose Administration in Healthy Male Subjects
Official title: A Phase I Study to Investigate the Absorption, Metabolism, and Excretion of [14c]-GDC-0941 Following Single Oral Dose Administration in Healthy Male Subjects
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Healthy Volunteer
Lead sponsor: Genentech, Inc.
Sponsor class: INDUSTRY
First posted: 2011-11-18
Enrollment: 5
Sex: MALE
Minimum age (years): 18
Maximum age (years): 55
Standard ages: ADULT
Accepts healthy volunteers: yes
Allocation: RANDOMIZED
Intervention model: SINGLE_GROUP
Primary purpose: TREATMENT

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).


Eligibility criteria: 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

Primary outcomes:
measure: Pharmacokinetic property based on the plasma concentrations of total radioactivity and GDC-0941: apparent terminal elimination half-life
timeFrame: up to approximately 6 weeks or early study discontinuation
measure: Pharmacokinetic property based on the plasma concentrations of total radioactivity and GDC-0941: apparent terminal phase elimination rate constant
timeFrame: up to approximately 6 weeks or early study discontinuation
measure: Pharmacokinetic property based on the plasma concentrations of total radioactivity and GDC-0941: apparent total clearance
timeFrame: up to approximately 6 weeks or early study discontinuation
measure: Pharmacokinetic property based on the plasma concentrations of total radioactivity and GDC-0941: apparent volume of distribution
timeFrame: up to approximately 6 weeks or early study discontinuation
measure: Pharmacokinetic property based on the plasma concentrations of total radioactivity and GDC-0941: area under the concentration-time curve extrapolated to infinity
timeFrame: up to approximately 6 weeks or early study discontinuation
measure: 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
timeFrame: up to approximately 6 weeks or early study discontinuation
measure: Pharmacokinetic property based on the plasma concentrations of total radioactivity and GDC-0941: maximum observed concentration
timeFrame: up to approximately 6 weeks or early study discontinuation
measure: Pharmacokinetic property based on the plasma concentrations of total radioactivity and GDC-0941: time to maximum concentration
timeFrame: up to approximately 6 weeks or early study discontinuation
Secondary outcomes:
measure: Amount of drug excreted in the feces over the sampling interval
timeFrame: up to approximately 6 weeks or early study discontinuation
measure: Percent excreted in feces
timeFrame: up to approximately 6 weeks or early study discontinuation
Other outcomes:
Locations:
city: Madison
country: United States
state: Wisconsin
Study officials:
affiliation: Genentech, Inc.
name: Scott Holden, M.D.
role: STUDY_DIRECTOR
References: