PF-07328948 + cyclosporine

PF-07328948 + cyclosporine is a drug combination primarily utilized in clinical pharmacology studies to evaluate drug-drug interactions (DDI). PF-07328948 is a potent, selective, and reversible small-molecule inhibitor of the organic anion transporting polypeptides 1B1 and 1B3 (OATP1B1 and OATP1B3), developed by Pfizer. It was designed as a clinical "probe" inhibitor to specifically isolate the role of OATP1B transporters in drug clearance without the confounding effects on Cytochrome P450 enzymes or other transporters. Cyclosporine, a well-established immunosuppressant and calcineurin inhibitor, is used in these studies as a non-selective comparator due to its broad inhibitory profile against OATP1B1, OATP1B3, P-glycoprotein (P-gp), and CYP3A4. The combination is typically administered to healthy volunteers to characterize the pharmacokinetic impact of OATP1B inhibition on various substrates (such as rosuvastatin) and to validate PF-07328948 as a selective tool for DDI prediction in drug development.

Other names

PF-07328948 plus cyclosporinePF07328948 plus cyclosporinePF 07328948 plus cyclosporine