Plasma concentrations of melengestrol acetate in humans extrapolated from the pharmacokinetics established in in vivo experiments with rats and chimeric mice with humanized liver and physiologically based pharmacokinetic modeling

► We developed a simple pharmacokinetic (PBPK) model of melengestrol acetate (MGA). ► Rat or mouse PBPK model of MGA was scaled to human model to predict in humans. ► MGA elimination in humans was estimated to be slow compared with those in rodents. ► Concentrations of MGA were evaluated by chimeric mice with humanized liver. ► The simplified human PBPK modeling is useful for risk evaluation of MGA.