Update on drug-drug interaction at organic cation transporters: mechanisms, clinical impact, and proposal for advanced<i>in vitro</i>testing

Introduction: Organic cation transporters collectively called OCTs belong to three gene families (SLC22A1 OCT1, SLC22A2 OCT2, SLC22A3 OCT3, SLC22A4 OCTN1, SLC22A5 OCTN2, SLC29A4 PMAT, SLC47A1 MATE1, and MATE2-K). transport structurally diverse drugs with overlapping selectivity. Some were shown be critically involved in pharmacokinetics therapeutic efficacy of cationic drugs. Drug-drug interactions at individual result clinical effects. Procedures for vitro testing interaction MATE2-K have been recommended.Areas covered: An overview functional properties, selectivity, location, impact is provided. In addition, clinically relevant drug-drug are compiled. Because it was observed that the half maximal concentration inhibit by (IC50) dependent on transported its concentration, an advanced protocol proposed. suggested include OCT3 PMAT testing.Expert opinion: Research roles should reinforced including more improvement considering recent data imperative benefit patients.