Ipatasertib (GDC-0068) Study to Evaluate Formulation Change and Food Effect on Bioavailability in Healthy Subjects

NCT02536391 | Completed Phase 1

• 1 other identifier: GO29868
• Study Type: interventional
• Target: 18
• Locations: 1 country
• Sites: 1

Brief Summary

This Phase I, open-label, randomized, 3-period crossover study was designed to determine the relative bioavailability of ipatasertib administered as capsule and tablet formulations to healthy volunteers. In addition, the influence of food on ipatasertib exposure will also be determined. Participants will be randomized to one of six treatment sequences to receive three treatments of a single oral administration of ipatasertib in, 1) tablet formulation in the fasted state, 2) capsule formulation in the fasted state or 3) tablet formulation in the fed state. Pharmacokinetics will be assessed, and standard physical and clinical evaluations will be performed throughout the study. Time on study is expected to be 3 weeks.

Conditions

Cancer

Outcome Measures

Primary Outcomes (7)

• Maximum Observed Concentration (Cmax) of Ipatasertib

  Days 1, 8 and 15

• Time to Maximum Concentration (tmax) of Ipatasertib

  Days 1, 8 and 15

• Area Under the Concentration-time Curve (AUC) from Hour 0 to the Last Quantifiable Concentration (AUC0-t) of Ipatasertib

  Days 1, 8 and 15

• Area Under the Concentration-time Curve (AUC) from Hour 0 Extrapolated to Infinity

  Days 1, 8 and 15

• Apparent Terminal Elimination Half-Life (t1/2) of Ipatasertib

  Days 1, 8 and 15

• Apparent Total Clearance (CL/F) of Ipatasertib

  Days 1, 8 and 15

• Apparent Volume of Distribution (Vz/F) of Ipatasertib

  Days 1, 8 and 15

Secondary Outcomes (1)

• Percentage of Participants with Adverse Events

  From check in (Day -1) to 30 days after the last dose of study drug

Study Arms (6)

Sequence 1: Tablet/Capsule/Tablet with food

EXPERIMENTAL

Day 1: ipatasertib tablet administered after fast, Day 8: ipatasertib capsule administered after fast, Day 15: ipatasertib tablet administered after high-fat meal.

Drug: Ipatasertib (capsule); Drug: Ipatasertib (tablet)

Sequence 2: Tablet/Tablet with food/Capsule

EXPERIMENTAL

Day 1: ipatasertib tablet administered after fast, Day 8: ipatasertib tablet administered after high-fat meal, Day 15: ipatasertib capsule administered after fast.

Drug: Ipatasertib (capsule); Drug: Ipatasertib (tablet)

Sequence 3: Capsule/Tablet/Tablet with food

EXPERIMENTAL

Day 1: ipatasertib capsule administered after fast, Day 8: ipatasertib tablet administered after fast, Day 15: ipatasertib tablet administered after high-fat meal.

Drug: Ipatasertib (capsule); Drug: Ipatasertib (tablet)

Sequence 4: Capsule/Tablet with food/Tablet

EXPERIMENTAL

Day 1: ipatasertib capsule administered after fast, Day 8: ipatasertib tablet administered after high-fat meal, Day 15: ipatasertib tablet administered after fast.

Drug: Ipatasertib (capsule); Drug: Ipatasertib (tablet)

Sequence 5: Tablet with food/Tablet/Capsule

EXPERIMENTAL

Day 1: ipatasertib tablet administered after high-fat meal, Day 8: ipatasertib tablet administered after fast, Day 15: ipatasertib capsule administered after fast.

Drug: Ipatasertib (capsule); Drug: Ipatasertib (tablet)

Sequence 6: Tablet with food/Capsule/Tablet

EXPERIMENTAL

Day 1: ipatasertib tablet administered after high-fat meal, Day 8: ipatasertib capsule administered after fast, Day 15: ipatasertib tablet administered after fast.

Drug: Ipatasertib (capsule); Drug: Ipatasertib (tablet)

Interventions

Ipatasertib (capsule) DRUG

Orally administered single dose of Ipatasertib formulated as a capsule.

Also known as: GDC-0068 (capsule)

Sequence 1: Tablet/Capsule/Tablet with food; Sequence 2: Tablet/Tablet with food/Capsule; Sequence 3: Capsule/Tablet/Tablet with food; Sequence 4: Capsule/Tablet with food/Tablet; Sequence 5: Tablet with food/Tablet/Capsule; Sequence 6: Tablet with food/Capsule/Tablet

Ipatasertib (tablet) DRUG

Orally administered single dose of Ipatasertib formulated as a tablet.

Also known as: GDC-0068 (tablet)

Sequence 1: Tablet/Capsule/Tablet with food; Sequence 2: Tablet/Tablet with food/Capsule; Sequence 3: Capsule/Tablet/Tablet with food; Sequence 4: Capsule/Tablet with food/Tablet; Sequence 5: Tablet with food/Tablet/Capsule; Sequence 6: Tablet with food/Capsule/Tablet

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Healthy males or females, between 18 and 55 years of age, inclusive
• Body mass index between 18.5 and 29.9 kg/m\^2, inclusive

You may not qualify if:

• \- Clinically significant findings from medical history or screening evaluations.

Sponsors & Collaborators

• Genentech, Inc.: lead

Study Sites (1)

Unknown Facility

Madison, Wisconsin, 53704, United States

Location

Related Publications (1)

• Malhi V, Budha N, Sane R, Huang J, Liederer B, Meng R, Patel P, Deng Y, Cervantes A, Tabernero J, Musib L. Single- and multiple-dose pharmacokinetics, potential for CYP3A inhibition, and food effect in patients with cancer and healthy subjects receiving ipatasertib. Cancer Chemother Pharmacol. 2021 Dec;88(6):921-930. doi: 10.1007/s00280-021-04344-9. Epub 2021 Sep 1.

  PMID: 34471960 DERIVED

MeSH Terms

Conditions

Neoplasms

Interventions

ipatasertib; Capsules; Tablets

Intervention Hierarchy (Ancestors)

Dosage Forms; Pharmaceutical Preparations

Study Officials

• Clinical Trials

  Hoffmann-La Roche

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: August 27, 2015
• First Posted: August 31, 2015
• Study Start: October 1, 2015
• Primary Completion: November 1, 2015
• Study Completion: November 1, 2015
• Last Updated: November 2, 2016

Record last verified: 2016-11

Locations

US (1)