Organic Cation Transporter 2 Inhibitors

Organic cation transporter 2 (OCT2/SLC22A2) is an electrogenic, sodium-independent uniporter sitting on the basolateral membrane of renal proximal tubule cells and hepatocytes, where it takes up bioactive amines and cationic drugs down their electrochemical gradient as the first step in their excretion. Drugs in this class inhibit that uptake, so a cationic drug that depends on OCT2 for renal secretion is cleared more slowly. FDA lists cimetidine and clonidine as in vitro OCT2 inhibitors.