A Phase I, Open-Label Absorption, Distribution, Metabolism, and Excretion (ADME) Study of the Hedgehog Pathway Inhibitor GDC-0449 in Healthy Female Subjects of Non-Childbearing Potential
Overview
- Phase
- Phase 1
- Intervention
- GDC-0449 oral capsules (non-labeled)
- Conditions
- Healthy
- Sponsor
- Genentech, Inc.
- Enrollment
- 24
- Primary Endpoint
- PK (Max observed and time to max plasma concentrations, area under the plasma concentration-time curve, absolute bioavailability, total plasma clearance, vol of dist, plasma terminal phase half-life, cumulative % excretion in urine and feces [Part B])
- Status
- Completed
- Last Updated
- 8 years ago
Overview
Brief Summary
This is an open-label, Phase I, single-center, single-dose administration study to determine the absolute bioavailability, clearance, and volume of distribution of GDC-0449 (Part A) and to determine the routes of excretion and extent of metabolism of GDC-0449 (Part B). Parts A and B will be conducted sequentially, with ≥ 7 days between dosing the sixth subject in Part A and dosing the first subject in Part B. In each part, 6 healthy female subjects of non-childbearing potential, between 18 and 65 years of age (inclusive), will be dosed.
Investigators
Eligibility Criteria
Inclusion Criteria
- Not provided
Exclusion Criteria
- Not provided
Arms & Interventions
A
On Day 1, subjects received a single oral dose of non-labeled GDC-0449 and a single IV tracer dose of 14C-GDC-0449.
Intervention: GDC-0449 oral capsules (non-labeled)
A
On Day 1, subjects received a single oral dose of non-labeled GDC-0449 and a single IV tracer dose of 14C-GDC-0449.
Intervention: GDC-0449 IV injection (labeled)
B
On Day 1, subjects received a single oral dose of 14C-GDC-0449.
Intervention: CDC-0449 oral suspension (labeled)
C
On Days 1-7, subjects received a single oral dose of non-labeled GDC-0449. On Day 7, subjects also received a single IV tracer dose of 14C-GDC-0449.
Intervention: GDC-0449 oral capsules (non-labeled)
C
On Days 1-7, subjects received a single oral dose of non-labeled GDC-0449. On Day 7, subjects also received a single IV tracer dose of 14C-GDC-0449.
Intervention: GDC-0449 IV injection (labeled)
D
On Days 1-6, subjects received a single oral dose of non-labeled GDC-0449. On Day 7, subjects received a single oral dose of 14C-GDC-0449.
Intervention: GDC-0449 oral capsules (non-labeled)
D
On Days 1-6, subjects received a single oral dose of non-labeled GDC-0449. On Day 7, subjects received a single oral dose of 14C-GDC-0449.
Intervention: CDC-0449 oral suspension (labeled)
Outcomes
Primary Outcomes
PK (Max observed and time to max plasma concentrations, area under the plasma concentration-time curve, absolute bioavailability, total plasma clearance, vol of dist, plasma terminal phase half-life, cumulative % excretion in urine and feces [Part B])
Time Frame: Until study discontinuation
Secondary Outcomes
- Safety outcome measures (incidence, nature, and severity of adverse events; change in clinical laboratory results; change in vital signs; change in electrocardiogram [ECG]; and change in physical examination findings)(Until study discontinuation)