Effects of Cytochrome P450 3A4 Inhibitors—Ketoconazole and Erythromycin—on Bitopertin Pharmacokinetics and Comparison with Physiologically Based Modelling Predictions

Objective To assess the effect of strong and moderate cytochrome P450 (CYP) 3A4 inhibition on exposure of bitopertin, a glycine reuptake inhibitor primarily metabolized by CYP3A4, and to compare the results with predictions based on physiologically based pharmacokinetic (PBPK) modelling.