Human Mass Balance and Metabolite Profiling of [¹⁴ C]-Pamiparib, a Poly (ADP-Ribose) Polymerase Inhibitor, in Patients With Advanced Cancer.

ABSTRACT: Pamiparib, a selective poly (ADP-ribose) polymerase 1/2 inhibitor, demonstrated tolerability and antitumor activity in patients with solid tumors at 60 mg orally twice daily. This phase 1 open-label study (NCT03991494; BGB-290-106) investigated the absorption, metabolism, and excretion (AME) of 60 mg [¹⁴ C]-pamiparib in 4 patients with solid tumors. The mass balance in excreta, blood, and plasma radioactivity and plasma pamiparib concentration were determined along with metabolite profiles in plasma, urine, and feces. Unchanged pamiparib accounted for the most plasma radioactivity (67.2% ± 10.2%). Pamiparib was rapidly absorbed with a median time to maximum plasma concentration (C_max ) of 2.00 hours (range, 1.00-3.05 hours). After reaching C_max , pamiparib

SUBMITTER: Mu S 

PROVIDER: S-EPMC8453745 | biostudies-literature | 2021 Sep

REPOSITORIES: biostudies-literature