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Study to Investigate the Absorption, Metabolism, and Excretion of [14C]-GDC-0980 Following Single Oral Dose Administration in Healthy Postmenopausal Female Subjects

Phase 1
Completed
Conditions
Healthy Volunteer
Interventions
Drug: [14C]-GDC-0980
Registration Number
NCT01487239
Lead Sponsor
Genentech, Inc.
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).

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
Female
Target Recruitment
4
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
  • Exposure to significant radiation 12 months prior to Check-in
  • Use of any tobacco-containing or nicotine-containing products within 3 months/approximately 90 days prior to Check-in or positive urine screening 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 within 7 days prior to Check-in
  • Use of alcohol-, grapefruit-, or caffeine-containing foods or beverages within 72 hours
  • 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

Study & Design

Study Type
INTERVENTIONAL
Study Design
SINGLE_GROUP
Arm && Interventions
GroupInterventionDescription
A[14C]-GDC-0980\[14C\]-GDC-0980 administered as a 10-mg oral dose
Primary Outcome Measures
NameTimeMethod
Pharmacokinetic based on the plasma concentrations of total radioactivity and GDC-0980: maximum observed concentration (Cmax)up to approximately 5 weeks
Pharmacokinetic based on the plasma concentrations of total radioactivity and GDC-0980: time to maximum concentration (tmax)up to approximately 5 weeks
Pharmacokinetic based on the plasma concentrations of total radioactivity and GDC-0980: apparent total clearanceup to approximately 5 weeks
Pharmacokinetic based on the plasma concentrations of total radioactivity and GDC-0980: apparent terminal elimination half-life (t1/2)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)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 infinityup to approximately 5 weeks
Pharmacokinetic based on the plasma concentrations of total radioactivity and GDC-0980: apparent terminal phase elimination rate constantup to approximately 5 weeks
Pharmacokinetic based on the plasma concentrations of total radioactivity and GDC-0980: apparent volume of distributionup to approximately 5 weeks
Secondary Outcome Measures
NameTimeMethod
Pharmacokinetic based on the urine radioactivity concentrations: percent excreted in urineup 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 intervalup to approximately 5 weeks
Pharmacokinetic based on the urine radioactivity concentrations: renal clearanceup to approximately 5 weeks
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