Metabolic disposition of the EGFR covalent inhibitor furmonertinib in humans.

ABSTRACT: Furmonertinib was designed for the treatment of non-small cell lung cancer (NSCLC) patients with EGFR T790M mutation. In this study, we investigated the metabolic disposition and mass balance in humans and tissue distribution in rats. After a single oral administration of 97.9 μCi/81.5 mg [¹⁴C]-furmonertinib mesylate to six healthy male volunteers, the absorption process of furmonertinib was fast with a t_max of total plasma radioactivity at 0.75 h. Afterward, furmonertinib was extensively metabolized, with the parent drug and active metabolite AST5902 accounting for 1.68% and 0.97% of total radioactivity in plasma. The terminal t_1/2 of total radioactivity in plasma was as long as 333 h, suggesting that the covalent binding of drug-related substances to plas

SUBMITTER: Meng J 

PROVIDER: S-EPMC8791928 | biostudies-literature | 2022 Feb

REPOSITORIES: biostudies-literature