Evaluation of absorption, distribution, metabolism, and excretion of [¹⁴C]-rucaparib, a poly(ADP-ribose) polymerase inhibitor, in patients with advanced solid tumors.

ABSTRACT: Rucaparib, a poly(ADP-ribose) polymerase inhibitor, is licensed for use in recurrent ovarian, fallopian tube, or primary peritoneal cancer. We characterized the absorption, distribution, metabolism, and elimination of rucaparib in 6 patients with advanced solid tumors following a single oral dose of [¹⁴C]-rucaparib 600 mg (≈140 μCi). Total radioactivity (TRA) in blood, plasma, urine, and feces was measured using liquid scintillation counting. Unchanged rucaparib concentrations in plasma were determined using validated liquid chromatography with tandem mass spectrometry. Maximum concentration (C_max) of TRA and unchanged rucaparib in plasma was 880 ng Eq/mL and 428 ng/mL, respectively, at approximately 4 h post dose; terminal half-life was >25 h for both TRA and rucapar

SUBMITTER: Liao M 

PROVIDER: S-EPMC7211193 | biostudies-literature | 2020 Jun

REPOSITORIES: biostudies-literature