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

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.

Timeline

Start

2019-01-22

Primary completion

2019-03-11

Completion

2019-03-11

Publications

• Hanley MJ, Zhang S, Griffin R, Zhu SX, Fram RJ, Lin J, Venkatakrishnan K, Gupta N. A phase 1 study to assess the absolute bioavailability, mass balance, pharmacokinetics, metabolism, and excretion of [14C]-mobocertinib, an oral inhibitor of EGFR exon 20 insertion mutations, in healthy participants. Invest New Drugs. 2024 Aug;42(4):343-352. doi: 10.1007/s10637-024-01446-y. Epub 2024 May 24.

Drugs

Indications

No indication recorded.