Predicting OCT2 / MATEs ‐Mediated Drug Interactions in Healthy Volunteers and Patients with Chronic Kidney Disease: Insights from Extended Clearance Concept, Endogenous Biomarkers, and In Vitro Inhibition Studies (Perspectives from the International Transporter Consortium)

Abstract excerpt

Organic cation transporter (OCT) 2 and multidrug and toxin extrusion (MATE) transporters play significant roles in the renal secretion of organic cations and drug–drug interactions (DDIs). Recent in vitro studies indicate that the K i values for OCT2 exhibit substrate dependency and increase in potency with pre‐incubation. However, consensus is lacking on whether these factors should be considered in predicting...

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