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

Healthy Volunteer Clinical Trial

Official 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

Clinical Trial Details — Status: Completed

Administrative data

• NCT number: NCT02390492
• Other study ID #: GP29067
• Status: Completed
• Phase: Phase 1
• First received: March 11, 2015
• Last updated: November 1, 2016
• Start date: March 2015
• Est. completion date: April 2015

Study information

• Verified date: November 2016
• Source: Genentech, Inc.
• Contact: n/a
• Is FDA regulated: No
• Health authority: United States: Food and Drug Administration
• Study type: Interventional

Clinical Trial 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.

Recruitment information / eligibility

• Status: Completed
• Enrollment: 8
• Est. completion date: April 2015
• Est. primary completion date: April 2015
• Accepts healthy volunteers: Accepts Healthy Volunteers
• Gender: Male
• Age group: 18 Years to 55 Years

Eligibility

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

Study Design

Allocation: Non-Randomized, Endpoint Classification: Bio-availability Study, Intervention Model: Single Group Assignment, Masking: Open Label

Related Conditions & MeSH terms

• Healthy Volunteer

Intervention

Drug:
• Period 1 treatment
200 mg oral ipatasertib followed 1 hour later by 80-mcg/800-nCi intravenous [14C]-ipatasertib on Day 1 of study
• Period 2 treatment
200-mg/100-mcCi oral [14C]-ipatasertib on Day 15 of study

Locations

Country	Name	City	State
n/a

Sponsors (1)

Lead Sponsor	Collaborator
Genentech, Inc.

Country where clinical trial is conducted

United States, 

Outcome

Type	Measure	Description	Time frame	Safety issue
Primary	Pharmacokinetics of [14C]-ipatasertib/ipatasertib (oral): apparent terminal elimination half-life		Period 2: Approximately 2 weeks	No
Primary	Pharmacokinetics of ipatasertib (oral): apparent total clearance (CL/F)		Period 2: Approximately 2 weeks	No
Primary	Pharmacokinetics of ipatasertib (oral): apparent volume of distribution (Vz/F)		Period 2: Approximately 2 weeks	No
Primary	Elimination and pharmacokinetics: Total radioactivity concentration in whole blood, plasma, urine, and feces		Period 2: Approximately 2 weeks	No
Primary	Bioavailability: Absolute bioavailability of ipatasertib (area under the concentration-time curve)		Period 1: Approximately 4 days	No
Primary	Mass balance		Period 2: Approximately 2 weeks	No
Primary	Pharmacokinetics of [14C]-ipatasertib/ipatasertib (oral): maximum observed concentration (Cmax)		Period 2: Approximately 2 weeks	No
Primary	Pharmacokinetics of [14C]-ipatasertib/ipatasertib (oral): time to maximum observed concentration (Tmax)		Period 2: Approximately 2 weeks	No
Primary	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	No
Primary	Pharmacokinetics of [14C]-ipatasertib/ipatasertib (oral): area under the concentration-time curve extrapolated to infinity (AUC0-inf)		Period 2: Approximately 2 weeks	No
Primary	Pharmacokinetics of [14C]-ipatasertib/ipatasertib (oral): apparent terminal elimination rate constant		Period 2: Approximately 2 weeks	No
Secondary	Pharmacokinetics of ipatasertib (oral and IV): terminal elimination rate constant adjusted for oral bioavailability as applicable		Period 1: Approximately 4 days	No
Secondary	Pharmacokinetics of ipatasertib (oral and IV): terminal elimination half-life adjusted for oral bioavailability as applicable		Period 1: Approximately 4 days	No
Secondary	Pharmacokinetics of ipatasertib (oral and IV): total clearance adjusted for oral bioavailability as applicable		Period 1: Approximately 4 days	No
Secondary	Pharmacokinetics of ipatasertib (oral and IV): volume of distribution adjusted for oral bioavailability as applicable		Period 1: Approximately 4 days	No
Secondary	Safety: Incidence of adverse events		Approximately 4 weeks	No
Secondary	Elimination and pharmacokinetics: Metabolite concentration(s) in plasma, urine, and feces		Period 2: Approximately 2 weeks	No
Secondary	Pharmacokinetics of ipatasertib (oral and IV): Cmax		Period 1: Approximately 4 days	No
Secondary	Pharmacokinetics of ipatasertib (oral and IV): Tmax		Period 1: Approximately 4 days	No
Secondary	Pharmacokinetics of ipatasertib (oral and IV): AUC0-t		Period 1: Approximately 4 days	No
Secondary	Pharmacokinetics of ipatasertib (oral and IV): AUC0-inf		Period 1: Approximately 4 days	No