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

Authors: Boetsch C, Parrott N, Fowler S, Poirier A, Hainzl D, Banken L, Martin-Facklam M, Hofmann C
Publication: Clin Pharmacokinet
Keywords: biological models, cytochrome P-450 CYP3A, drug interactions, erythromycin, humans, ketoconazole, piperazines, Sulfones
Software: GastroPlus®

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.