Evaluation of Generic Methods to Predict Human Pharmacokinetics Using Physiologically Based Pharmacokinetic Model for Early Drug Discovery of Tyrosine Kinase Inhibitors

Authors: Ren HC, Sai Y, Chen T
Publication: Eur J Drug Metab Pharmacokinet
Keywords: drug discovery, FIHSimulator, first-in-human, In vitro in vivo extrapolation (IVIVE), mechanistic absorption model, PBPK, Physiologically based pharmacokinetic (PBPK) modeling
Software: ADMET Predictor®, GastroPlus®

Background

Requirements for predicting human pharmacokinetics in drug discovery are increasing. Developing different methods of human pharmacokinetic prediction will facilitate lead optimization, candidate nomination, and dosing regimens before clinical trials at various early drug discovery stages.