Dicloxacillin and flucloxacillin inhibit hepatic uptake transporters -in vitro investigations and physiologically based pharmacokinetic modelling.

ABSTRACT: Dicloxacillin and flucloxacillin are β-lactamase-resistant penicillin antibiotics that have been in clinical use for over 50 years. While both antibiotics are known to induce cytochrome P450 enzymes, there is limited information available regarding their interactions with drug transporters. Here, we investigated the in vitro transport and inhibition of hepatic organic anion transporting polypeptides (OATPs) and renal organic anion transporters (OATs) by these antibiotics in recombinant transporter overexpressing HEK293 cells. We also investigated the transport of these antibiotics by efflux transporters, as well as their inhibition of breast cancer resistance protein (BCRP) and P-glycoprotein (P-gp) using a HEK293 membrane vesicle transport assay. Dicloxacillin and flucloxacillin inhibited

SUBMITTER: Sjostedt N 

PROVIDER: S-EPMC12633417 | biostudies-literature | 2025 Oct

REPOSITORIES: biostudies-literature