Mass balance and pharmacokinetics of an oral dose of ¹⁴ C-napabucasin in healthy adult male subjects.

ABSTRACT: This phase 1, open-label study assessed¹⁴ C-napabucasin absorption, metabolism, and excretion, napabucasin pharmacokinetics, and napabucasin metabolites (primary objectives); safety/tolerability were also evaluated. Eight healthy males (18-45 years) received a single oral 240-mg napabucasin dose containing ~100 μCi¹⁴ C-napabucasin. Napabucasin was absorbed and metabolized to dihydro-napabucasin (M1; an active metabolite [12.57-fold less activity than napabucasin]), the sole major circulating metabolite (median time to peak concentration: 2.75 and 2.25 h, respectively). M1 plasma concentration versus time profiles generally mirrored napabucasin; similar arithmetic mean half-lives (7.14 and 7.92 h, respectively) suggest M1 formation was rate limiting. Napabucasin system

SUBMITTER: Dai X 

PROVIDER: S-EPMC7878185 | biostudies-literature | 2021 Feb

REPOSITORIES: biostudies-literature