Healthy Volunteer
Conditions
Brief summary
This 2-period, open-label, nonrandomized study will be conducted to determine the absolute bioavailability as well as the absorption, metabolism, and excretion of ipatasertib and its metabolite(s). Healthy male participants will receive a single 200-mg oral dose of ipatasertib followed 1 hour later by an 80-mcg/800-nCi intravenous dose of \[14C\]-ipatasertib. After a 4-day observation period and 10-day washout, participants will receive a single 200-mg/100-mcCi oral dose of \[14C\]-ipatasertib with subsequent data collection for an additional 7 to 14 days until discharge criteria are met.
Interventions
DRUGPeriod 1 treatment
200 mg oral ipatasertib followed 1 hour later by 80-mcg/800-nCi intravenous \[14C\]-ipatasertib on Day 1 of study
DRUGPeriod 2 treatment
200-mg/100-mcCi oral \[14C\]-ipatasertib on Day 15 of study
Sponsors
Genentech, Inc.
Study design
Allocation
NON_RANDOMIZED
Intervention model
SINGLE_GROUP
Masking
NONE
Eligibility
Sex/Gender
MALE
Age
18 Years to 55 Years
Healthy volunteers
Yes
Inclusion criteria
* Healthy male volunteers 18 to 55 years of age, inclusive * Body mass index (BMI) 18 to 32 kg/m2, inclusive
Exclusion criteria
* Females * Clinically significant findings from medical history or screening evaluations * Recent participation in any other investigational drug study or biologic agent study, or receipt of a previous radiolabeled investigational drug within 6 months prior to check-in * Significant radiation exposure within 12 months prior to check-in
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| Pharmacokinetics of [14C]-ipatasertib/ipatasertib (oral): apparent terminal elimination rate constant | Period 2: Approximately 2 weeks |
| Pharmacokinetics of [14C]-ipatasertib/ipatasertib (oral): maximum observed concentration (Cmax) | Period 2: Approximately 2 weeks |
| Elimination and pharmacokinetics: Total radioactivity concentration in whole blood, plasma, urine, and feces | Period 2: Approximately 2 weeks |
| Bioavailability: Absolute bioavailability of ipatasertib (area under the concentration-time curve) | Period 1: Approximately 4 days |
| Mass balance | Period 2: Approximately 2 weeks |
| Pharmacokinetics of [14C]-ipatasertib/ipatasertib (oral): apparent terminal elimination half-life | Period 2: Approximately 2 weeks |
| Pharmacokinetics of ipatasertib (oral): apparent total clearance (CL/F) | Period 2: Approximately 2 weeks |
| Pharmacokinetics of ipatasertib (oral): apparent volume of distribution (Vz/F) | Period 2: Approximately 2 weeks |
| Pharmacokinetics of [14C]-ipatasertib/ipatasertib (oral): time to maximum observed concentration (Tmax) | Period 2: Approximately 2 weeks |
| Pharmacokinetics of [14C]-ipatasertib/ipatasertib (oral): area under the concentration-time curve from Hour 0 to the last measurable concentration (AUC0-t) | Period 2: Approximately 2 weeks |
| Pharmacokinetics of [14C]-ipatasertib/ipatasertib (oral): area under the concentration-time curve extrapolated to infinity (AUC0-inf) | Period 2: Approximately 2 weeks |
Secondary
| Measure | Time frame |
|---|---|
| Pharmacokinetics of ipatasertib (oral and IV): Cmax | Period 1: Approximately 4 days |
| Pharmacokinetics of ipatasertib (oral and IV): Tmax | Period 1: Approximately 4 days |
| Pharmacokinetics of ipatasertib (oral and IV): AUC0-t | Period 1: Approximately 4 days |
| Pharmacokinetics of ipatasertib (oral and IV): AUC0-inf | Period 1: Approximately 4 days |
| Pharmacokinetics of ipatasertib (oral and IV): terminal elimination rate constant adjusted for oral bioavailability as applicable | Period 1: Approximately 4 days |
| Pharmacokinetics of ipatasertib (oral and IV): terminal elimination half-life adjusted for oral bioavailability as applicable | Period 1: Approximately 4 days |
| Pharmacokinetics of ipatasertib (oral and IV): total clearance adjusted for oral bioavailability as applicable | Period 1: Approximately 4 days |
| Pharmacokinetics of ipatasertib (oral and IV): volume of distribution adjusted for oral bioavailability as applicable | Period 1: Approximately 4 days |
| Safety: Incidence of adverse events | Approximately 4 weeks |
| Elimination and pharmacokinetics: Metabolite concentration(s) in plasma, urine, and feces | Period 2: Approximately 2 weeks |
Countries
United States
Outcome results
None listed