Pharmacokinetics, mass balance, and metabolism of [¹⁴C]TPN171, a novel PDE5 inhibitor, in humans for the treatment of pulmonary arterial hypertension.

ABSTRACT: TPN171 is a novel phosphodiesterase-5 (PDE5) inhibitor used to treat pulmonary arterial hypertension (PAH) and erectile dysfunction (ED), which currently is undergoing phase II clinical trials in China. In this single-center, single-dose, nonrandomized, and open design study, radiolabeled [¹⁴C]TPN171 was used to investigate the metabolic mechanism, pharmacokinetic characteristics, and clearance pathways of TPN171 in 6 healthy Chinese male volunteers. Each volunteer was administered a single oral suspension of 10 mg (100 μCi) of [¹⁴C]TPN171. We found that TPN171 was absorbed rapidly in humans with a peak time (T_max) of 0.667 h and a half-life (t_1/2) of approximately 9.89 h in plasma. Excretion of radiopharmaceutical-related components was collecte

SUBMITTER: He YF 

PROVIDER: S-EPMC9813128 | biostudies-literature | 2023 Jan

REPOSITORIES: biostudies-literature