Pharmacokinetics, Mass Balance, and Biotransformation of [¹⁴C]tinengotinib, A Novel Multi-target Kinase Inhibitor, in Healthy Subjects.

ABSTRACT:

Background and objective

Tinengotinib, a novel multi-target small molecule kinase inhibitor, is currently undergoing phase II clinical trial in the USA and China. The purpose of this open-label study was to investigate the absorption, metabolism, and excretion of [¹⁴C]tinengotinib following a single oral dose in healthy subjects.

Methods

Six healthy male subjects received a single oral dose of [¹⁴C]tinengotinib capsules at 10 mg/100 µCi, and blood, urine, and feces samples were collected. Phenotyping experiments were further conducted to confirm the enzymes involved in its metabolism.

Results

Tinengotinib was rapidly absorbed in plasma with a time to peak drug concentration (T_max) of 1.0-4.0 h post-dose and a long terminal half-life (t

SUBMITTER: Ni S 

PROVIDER: S-EPMC11455736 | biostudies-literature | 2024 Sep

REPOSITORIES: biostudies-literature