Preclinical pharmacokinetics of TPN729MA, a novel PDE5 inhibitor, and prediction of its human pharmacokinetics using a PBPK model

Authors: Gao ZW, Zhu YT, Yu MM, Zan B, , Zhang YF, Chen XY, Li XN, Zhong DF
Publication: Acta Pharmacol Sin
Keywords: animals, biological models, blood proteins, Caco-2 cells, dogs, erectile dysfunction, humans, liver microsomes, phosphodiesterase 5, rats
Software: GastroPlus®

Aim

TPN729MA is a novel selective PDE5 inhibitor currently under clinical development in China for the treatment of erectile dysfunction. In this study we characterized its preclinical pharmacokinetics (PK) and predict its human PK using a physiologically based pharmacokinetic (PBPK) model.