Pharmacokinetics of the Multi-kinase Inhibitor Pexidartinib: Mass Balance and Dose Proportionality.

ABSTRACT: Pexidartinib is an oral small-molecule tyrosine kinase inhibitor that selectively targets colony-stimulating factor 1 receptor. Two phase 1 single-center trials were conducted in healthy subjects to determine the absorption, distribution, metabolism, and excretion of pexidartinib using radiolabeled drug and to assess the dose proportionality of pexidartinib following single oral doses. In the mass balance study, eight male subjects received a single oral dose of [¹⁴ C]-pexidartinib 400 mg with radioactivity assessed in plasma, urine, and feces samples taken at various timepoints postdose. In the dose-proportionality study, 18 subjects received single doses of pexidartinib 200, 400, and 600 mg using randomization sequences. Peak pexidartinib and total radioactivity were observed

SUBMITTER: Zahir H 

PROVIDER: S-EPMC10099993 | biostudies-literature | 2023 Feb

REPOSITORIES: biostudies-literature