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.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Masking
NONE
Enrollment
8
200 mg oral ipatasertib followed 1 hour later by 80-mcg/800-nCi intravenous \[14C\]-ipatasertib on Day 1 of study
200-mg/100-mcCi oral \[14C\]-ipatasertib on Day 15 of study
Unnamed facility
Madison, Wisconsin, United States
Pharmacokinetics of [14C]-ipatasertib/ipatasertib (oral): apparent terminal elimination half-life
Time frame: Period 2: Approximately 2 weeks
Pharmacokinetics of ipatasertib (oral): apparent total clearance (CL/F)
Time frame: Period 2: Approximately 2 weeks
Pharmacokinetics of ipatasertib (oral): apparent volume of distribution (Vz/F)
Time frame: Period 2: Approximately 2 weeks
Elimination and pharmacokinetics: Total radioactivity concentration in whole blood, plasma, urine, and feces
Time frame: Period 2: Approximately 2 weeks
Bioavailability: Absolute bioavailability of ipatasertib (area under the concentration-time curve)
Time frame: Period 1: Approximately 4 days
Mass balance
Time frame: Period 2: Approximately 2 weeks
Pharmacokinetics of [14C]-ipatasertib/ipatasertib (oral): maximum observed concentration (Cmax)
Time frame: Period 2: Approximately 2 weeks
Pharmacokinetics of [14C]-ipatasertib/ipatasertib (oral): time to maximum observed concentration (Tmax)
Time frame: 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)
Time frame: Period 2: Approximately 2 weeks
Pharmacokinetics of [14C]-ipatasertib/ipatasertib (oral): area under the concentration-time curve extrapolated to infinity (AUC0-inf)
Time frame: Period 2: Approximately 2 weeks
Pharmacokinetics of [14C]-ipatasertib/ipatasertib (oral): apparent terminal elimination rate constant
Time frame: Period 2: Approximately 2 weeks
Pharmacokinetics of ipatasertib (oral and IV): terminal elimination rate constant adjusted for oral bioavailability as applicable
Time frame: Period 1: Approximately 4 days
Pharmacokinetics of ipatasertib (oral and IV): terminal elimination half-life adjusted for oral bioavailability as applicable
Time frame: Period 1: Approximately 4 days
Pharmacokinetics of ipatasertib (oral and IV): total clearance adjusted for oral bioavailability as applicable
Time frame: Period 1: Approximately 4 days
Pharmacokinetics of ipatasertib (oral and IV): volume of distribution adjusted for oral bioavailability as applicable
Time frame: Period 1: Approximately 4 days
Safety: Incidence of adverse events
Time frame: Approximately 4 weeks
Elimination and pharmacokinetics: Metabolite concentration(s) in plasma, urine, and feces
Time frame: Period 2: Approximately 2 weeks
Pharmacokinetics of ipatasertib (oral and IV): Cmax
Time frame: Period 1: Approximately 4 days
Pharmacokinetics of ipatasertib (oral and IV): Tmax
Time frame: Period 1: Approximately 4 days
Pharmacokinetics of ipatasertib (oral and IV): AUC0-t
Time frame: Period 1: Approximately 4 days
Pharmacokinetics of ipatasertib (oral and IV): AUC0-inf
Time frame: Period 1: Approximately 4 days
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