The Novel In Vitro Method to Calculate Tissue-to-Plasma Partition Coefficient in Humans for Predicting Pharmacokinetic Profiles by Physiologically-Based Pharmacokinetic Model With High Predictability

Proper prediction of human pharmacokinetic (PK) profiles can accelerate the compound selection in drug discovery. Recently, we reported a robust bottom-up physiologically-based pharmacokinetic (PBPK) approach (J Pharm Sci. 2019 Aug; 108(8):2718–2727), which uses the in vivo rat distribution volume at the steady state (Vss) to determine human tissue-to-plasma partition coefficients (Kptissue). Here, we report on a bottom-up PBPK approach that can...