Solute carrier family 22 member 2 (SLC22A2) (OCT2)

Organic cation transporter 2 (OCT2), also known as Solute carrier family 22 member 2 (SLC22A2), is a polyspecific, sodium-independent transporter primarily localized to the basolateral membrane of renal proximal tubule cells [2, 13, 15]. It plays a vital role in the renal elimination of numerous cationic drugs and endogenous compounds, such as metformin, creatinine, and various neurotransmitters, by facilitating their uptake from the blood into the kidney [7, 18, 23]. OCT2 is recognized as a major site for clinically significant drug-drug interactions (DDIs); for instance, inhibitors like cimetidine or dolutegravir can significantly decrease the renal clearance of victim drugs like metformin or dofetilide, increasing the risk of toxicity [1, 20, 23]. Furthermore, OCT2 is the primary gateway for the entry of platinum-based chemotherapeutics, such as cisplatin, into renal cells, making it a critical mediator of drug-induced nephrotoxicity [3, 9, 22]. Genetic polymorphisms in the SLC22A2 gene, such as the rs316019 variant, have been shown to influence transporter activity, thereby affecting both the efficacy and the safety profile of its substrates [11, 14, 16]. Consequently, OCT2 is a key focus in pharmacogenomics and drug development for optimizing therapeutic outcomes and minimizing adverse renal effects [5, 6, 7].

Other names

Organic cation transporter 2SLC22A2OCT2HOCT2Solute carrier family 22 member 2

Drugs typically interact with OCT2 as substrates or inhibitors. Substrate drugs are actively transported from the blood into the renal proximal tubule cells for excretion [2, 18]. Inhibitor drugs compete for the binding sites of OCT2, thereby blocking the uptake of other substrates, which leads to reduced renal clearance and increased systemic exposure of the 'victim' drugs [1, 5, 23].