A Phase I Study to Investigate the Absorption, Metabolism, and Excretion of [14C]-GDC-0980 Following Single Oral Dose Administration in Healthy Postmenopausal Female Subjects
Overview
- Phase
- Phase 1
- Intervention
- [14C]-GDC-0980
- Conditions
- Healthy Volunteer
- Sponsor
- Genentech, Inc.
- Enrollment
- 4
- Primary Endpoint
- Pharmacokinetic based on the plasma concentrations of total radioactivity and GDC-0980: maximum observed concentration (Cmax)
- Status
- Completed
- Last Updated
- 9 years ago
Overview
Brief Summary
This study will be an open-label, non-randomized, absorption, metabolism, and excretion study of [14C]-GDC-0980 administered as a 10-mg oral dose to 6 healthy postmenopausal and/or surgically sterile female subjects following at least a 10-hour fast from food (not including water).
Investigators
Eligibility Criteria
Inclusion Criteria
- •Medically healthy as determined by the absence of clinically significant findings in the medical history, physical examination, vital signs, 12-lead ECG, and clinical laboratory evaluations within the reference range for the test laboratory, unless deemed not clinically significant by the Investigator
- •Female subjects of non-childbearing potential, as defined as either: postmenopausal and without recent history of menorrhea as documented either by physician note or confirmed by serum follicle-stimulating hormone level consistent with postmenopausal status, or surgically sterile
- •BMI range within 18.5 to 29.9 kg/m2, inclusive
- •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
- •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
- •History or presence of inflammatory diseases, including those with small or large intestine inflammation such as Crohn's disease or ulcerative colitis, which required immunosuppressants
- •Use of potent proton-pump inhibitors such as omeprazole, lansoprazole, dexlansoprazole, esomeprazole, pantoprazole, and rabeprazole
- •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
Arms & Interventions
A
\[14C\]-GDC-0980 administered as a 10-mg oral dose
Intervention: [14C]-GDC-0980
Outcomes
Primary Outcomes
Pharmacokinetic based on the plasma concentrations of total radioactivity and GDC-0980: maximum observed concentration (Cmax)
Time Frame: up to approximately 5 weeks
Pharmacokinetic based on the plasma concentrations of total radioactivity and GDC-0980: time to maximum concentration (tmax)
Time Frame: up to approximately 5 weeks
Pharmacokinetic based on the plasma concentrations of total radioactivity and GDC-0980: apparent total clearance
Time Frame: up to approximately 5 weeks
Pharmacokinetic based on the plasma concentrations of total radioactivity and GDC-0980: apparent terminal elimination half-life (t1/2)
Time Frame: up to approximately 5 weeks
Pharmacokinetic based on the plasma concentrations of total radioactivity and GDC-0980: area under the concentration-time curve from Hour 0 to the last measurable concentration (AUC0-t)
Time Frame: up to approximately 5 weeks
Pharmacokinetic based on the plasma concentrations of total radioactivity and GDC-0980: area under the concentration-time curve extrapolated to infinity
Time Frame: up to approximately 5 weeks
Pharmacokinetic based on the plasma concentrations of total radioactivity and GDC-0980: apparent terminal phase elimination rate constant
Time Frame: up to approximately 5 weeks
Pharmacokinetic based on the plasma concentrations of total radioactivity and GDC-0980: apparent volume of distribution
Time Frame: up to approximately 5 weeks
Secondary Outcomes
- Pharmacokinetic based on the urine radioactivity concentrations: percent excreted in urine(up to approximately 5 weeks)
- Pharmacokinetic parameters for the metabolites of [14C]-GDC-0980 calculated based on plasma, urine, and fecal concentration levels.(up to approximately 5 weeks)
- Pharmacokinetic based on the urine radioactivity concentrations: amount of drug excreted in the urine over sampling interval(up to approximately 5 weeks)
- Pharmacokinetic based on the urine radioactivity concentrations: renal clearance(up to approximately 5 weeks)