NCT03811834

A Study to Assess Absolute Bioavailability (ABA) of Mobocertinib (TAK-788) and to Characterize Mass Balance, Pharmacokinetics (PK), Metabolism, and Excretion of Carbon-14 ([14C])-Mobocertinib in Male Healthy Participants

A Phase 1 Study to Assess Absolute Bioavailability of TAK-788 and to Characterize Mass Balance, Pharmacokinetics, Metabolism, and Excretion of [14C]-TAK-788 in Male Healthy Subjects

• Status: Completed
• Phase: Phase 1
• Study type: Interventional
• Enrollment: 7 (actual)
• Sponsor: Millennium Pharmaceuticals, Inc. · Industry
• Sex: Male
• Age: 19 Years – 55 Years
• Healthy volunteers: Accepted

Summary

The purpose of this study is to determine: Period 1 (ABA): ABA of mobocertinib following single microdose intravenous administration of 50 microgram (mcg) (approximately 2 microcurie \[mcCi\]) \[14 C\]-\]-mobocertinib and single oral administration of 160 milligram (mg) mobocertinib. Period 2 (absorption, distribution, metabolism, and elimination \[ADME\]): the mass balance and metabolic profile of mobocertinib in plasma, urine, and feces, to characterize the PK of mobocertinib and its metabolites (AP32960 and AP32914) in plasma, whole blood, and urine, and total radioactivity concentration equivalents in plasma and whole blood following a single oral administration of 160 mg (approximately 100 mcCi) \[14C\]-mobocertinib solution.

Detailed description

The drug being tested in this study is called mobocertinib. The study will determine ABA of mobocertinib following single microdose of 50 mcg \[14C\]-mobocertinib and single oral administration of 160 mg mobocertinib and will assess the mass balance and metabolic profile of mobocertinib in plasma, urine, and feces following a single oral administration of 160 mg \[14C\]-mobocertinib solution, and will characterize the PK of mobocertinib and its metabolites in plasma, whole blood, and urine, and total radioactivity concentration equivalents in plasma and whole blood following a single dose of 160 mg \[14C\]-mobocertinib. The study will enroll approximately 6 participants. The study is designed to consist of 2 periods: Period 1 (ABA study period) and Period 2 (ADME study period). In Period 1, all participants will receive single unlabeled oral 160 mg dose of mobocertinib as capsules. At 3.75 hours post oral dosing, participants will receive 15-minute intravenous infusion of a microdose of 50 mcg (approximately 2mcCi) \[14C\]-mobocertinib. In Period 2, participants will receive single dose of 160 mg (approximately 100 mcCi) \[14C\]-mobocertinib as an oral solution. This single center trial will be conducted in the United States. The overall time to participate in this study is approximately 65 days including screening period. Participants will be contacted approximately 30 days after the last dose of study drug for a follow-up assessment.

Conditions

• Healthy Volunteers

Interventions

Type	Name	Description
DRUG	Mobocertinib	Mobocertinib capsule, \[14C\]-Mobocertinib intravenous infusion, \[14C\]-Mobocertinib oral solution.

Timeline

• Start date: 2019-01-22
• Primary completion: 2019-03-11
• Completion: 2019-03-11
• First posted: 2019-01-22
• Last updated: 2024-02-12
• Results posted: 2021-07-30

Locations

1 site across 1 country: United States

Regulatory

• FDA-regulated drug study