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NCT Number: NCT02390492

A Phase I Bioavailability and Pharmacokinetic Study of [14C]-Ipatasertib Single Oral and Intravenous Doses in Healthy Male Subjects

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.

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Key information

Conditions

Healthy Volunteer

Age range

18 year–55 year

Sex eligibility

Male

Study type

Interventional

Phase

Phase 1

Primary location

Madison, Wisconsin, 53704, United States

Who can participate

Healthy volunteers accepted: Yes

Only the study team can determine whether someone qualifies for participation.

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

Treatment and study plan

Period 1 treatment

Drug

200 mg oral ipatasertib followed 1 hour later by 80-mcg/800-nCi intravenous [14C]-ipatasertib on Day 1 of study

Period 2 treatment

Drug

200-mg/100-mcCi oral [14C]-ipatasertib on Day 15 of study

Primary outcomes

  1. Pharmacokinetics of [14C]-ipatasertib/ipatasertib (oral): apparent terminal elimination half-life

    Time frame: Period 2: Approximately 2 weeks

  2. Pharmacokinetics of ipatasertib (oral): apparent total clearance (CL/F)

    Time frame: Period 2: Approximately 2 weeks

  3. Pharmacokinetics of ipatasertib (oral): apparent volume of distribution (Vz/F)

    Time frame: Period 2: Approximately 2 weeks

  4. Elimination and pharmacokinetics: Total radioactivity concentration in whole blood, plasma, urine, and feces

    Time frame: Period 2: Approximately 2 weeks

  5. Bioavailability: Absolute bioavailability of ipatasertib (area under the concentration-time curve)

    Time frame: Period 1: Approximately 4 days

  6. Mass balance

    Time frame: Period 2: Approximately 2 weeks

  7. Pharmacokinetics of [14C]-ipatasertib/ipatasertib (oral): maximum observed concentration (Cmax)

    Time frame: Period 2: Approximately 2 weeks

  8. Pharmacokinetics of [14C]-ipatasertib/ipatasertib (oral): time to maximum observed concentration (Tmax)

    Time frame: Period 2: Approximately 2 weeks

  9. 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

  10. Pharmacokinetics of [14C]-ipatasertib/ipatasertib (oral): area under the concentration-time curve extrapolated to infinity (AUC0-inf)

    Time frame: Period 2: Approximately 2 weeks

  11. Pharmacokinetics of [14C]-ipatasertib/ipatasertib (oral): apparent terminal elimination rate constant

    Time frame: Period 2: Approximately 2 weeks

Secondary outcomes

  1. Pharmacokinetics of ipatasertib (oral and IV): terminal elimination rate constant adjusted for oral bioavailability as applicable

    Time frame: Period 1: Approximately 4 days

  2. Pharmacokinetics of ipatasertib (oral and IV): terminal elimination half-life adjusted for oral bioavailability as applicable

    Time frame: Period 1: Approximately 4 days

  3. Pharmacokinetics of ipatasertib (oral and IV): total clearance adjusted for oral bioavailability as applicable

    Time frame: Period 1: Approximately 4 days

  4. Pharmacokinetics of ipatasertib (oral and IV): volume of distribution adjusted for oral bioavailability as applicable

    Time frame: Period 1: Approximately 4 days

  5. Safety: Incidence of adverse events

    Time frame: Approximately 4 weeks

  6. Elimination and pharmacokinetics: Metabolite concentration(s) in plasma, urine, and feces

    Time frame: Period 2: Approximately 2 weeks

  7. Pharmacokinetics of ipatasertib (oral and IV): Cmax

    Time frame: Period 1: Approximately 4 days

  8. Pharmacokinetics of ipatasertib (oral and IV): Tmax

    Time frame: Period 1: Approximately 4 days

  9. Pharmacokinetics of ipatasertib (oral and IV): AUC0-t

    Time frame: Period 1: Approximately 4 days

  10. Pharmacokinetics of ipatasertib (oral and IV): AUC0-inf

    Time frame: Period 1: Approximately 4 days

Sponsors and collaborators

Lead sponsor

Genentech, Inc.

Industry

Registry information

Official study title

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

Important dates

Study start
2015
Primary completion
2015
Study completion
2015
First posted
Mar 17, 2015
Registry last updated
Nov 2, 2016

OpenTrials presents study information sourced from ClinicalTrials.gov. The official registry record should be consulted for the latest information.

View the official ClinicalTrials.gov record (opens in a new tab)

This listing is for discovery and informational purposes only. It is not medical advice, does not guarantee that a study is recruiting, and does not determine eligibility. Contact the study team and a qualified healthcare professional when considering participation.

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