A Phase I Study to Investigate the Absorption, Metabolism, and Excretion of [14C]-Ipatasertib (GDC-0068) Following a Single Oral Dose and to Investigate the Absolute Bioavailability Following Single Oral and Intravenous Doses in a Single Cohort of Healthy Male Subjects
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 8
- 主要终点
- Pharmacokinetics of [14C]-ipatasertib/ipatasertib (oral): apparent terminal elimination rate constant
研究概览
简要总结
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.
研究设计
- 研究类型
- Interventional
- 分配方式
- Non Randomized
- 干预模型
- Single Group
- 盲法
- None
入排标准
- 年龄范围
- 18 Years 至 55 Years（Adult）
- 性别
- Male
- 接受健康志愿者
- 是
入选标准
- •Healthy male volunteers 18 to 55 years of age, inclusive
- •Body mass index (BMI) 18 to 32 kg/m2, inclusive
排除标准
- •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
研究组 & 干预措施
Ipatasertib/[14C]-ipatasertib
干预措施: Period 1 treatment (Drug)
Ipatasertib/[14C]-ipatasertib
干预措施: Period 2 treatment (Drug)
结局指标
主要结局
Pharmacokinetics of [14C]-ipatasertib/ipatasertib (oral): apparent terminal elimination rate constant
时间窗: Period 2: Approximately 2 weeks
Pharmacokinetics of [14C]-ipatasertib/ipatasertib (oral): maximum observed concentration (Cmax)
时间窗: 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)
时间窗: Period 2: Approximately 2 weeks
Pharmacokinetics of [14C]-ipatasertib/ipatasertib (oral): area under the concentration-time curve extrapolated to infinity (AUC0-inf)
时间窗: Period 2: Approximately 2 weeks
Pharmacokinetics of [14C]-ipatasertib/ipatasertib (oral): apparent terminal elimination half-life
时间窗: Period 2: Approximately 2 weeks
Pharmacokinetics of ipatasertib (oral): apparent total clearance (CL/F)
时间窗: Period 2: Approximately 2 weeks
Pharmacokinetics of ipatasertib (oral): apparent volume of distribution (Vz/F)
时间窗: Period 2: Approximately 2 weeks
Elimination and pharmacokinetics: Total radioactivity concentration in whole blood, plasma, urine, and feces
时间窗: Period 2: Approximately 2 weeks
Bioavailability: Absolute bioavailability of ipatasertib (area under the concentration-time curve)
时间窗: Period 1: Approximately 4 days
Mass balance
时间窗: Period 2: Approximately 2 weeks
Pharmacokinetics of [14C]-ipatasertib/ipatasertib (oral): time to maximum observed concentration (Tmax)
时间窗: Period 2: Approximately 2 weeks
次要结局
- 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)
- Pharmacokinetics of ipatasertib (oral and IV): AUC0-inf(Period 1: Approximately 4 days)
- Elimination and pharmacokinetics: Metabolite concentration(s) in plasma, urine, and feces(Period 2: Approximately 2 weeks)
- Pharmacokinetics of ipatasertib (oral and IV): Cmax(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): Tmax(Period 1: Approximately 4 days)
- Safety: Incidence of adverse events(Approximately 4 weeks)
- Pharmacokinetics of ipatasertib (oral and IV): AUC0-t(Period 1: Approximately 4 days)