Solute carrier family 22 member 2 (Organic cation transporter 2) (OCT2)

Solute carrier family 22 member 2 (SLC22A2), commonly known as Organic cation transporter 2 (OCT2), is a polyspecific transporter primarily located on the basolateral membrane of renal proximal tubule cells (UniProt P55018; NIH Gene ID 6582). It facilitates the electrogenic, sodium-independent uptake of a wide range of endogenous and exogenous organic cations from the blood into the kidney, serving as the rate-limiting step in their renal secretion (Wikipedia; Koepsell et al., 2007). Key substrates include endogenous compounds like creatinine and neurotransmitters such as dopamine and norepinephrine, as well as therapeutic agents like the antidiabetic drug metformin and platinum-based chemotherapeutics like cisplatin and oxaliplatin (PubMed; Motohashi et al., 2002). Due to its central role in drug disposition, OCT2 is a major site for clinically significant drug-drug interactions; inhibitors like cimetidine or dolutegravir can reduce the renal clearance of substrates, leading to increased systemic exposure and potential toxicity (Open Targets; Yee & Giacomini). Genetic polymorphisms in the SLC22A2 gene further contribute to inter-individual variability in drug response and susceptibility to adverse effects, such as cisplatin-induced nephrotoxicity and ototoxicity (ClinPGx; ResearchGate). Additionally, its expression levels in certain cancers, such as renal cell carcinoma, have been linked to patient survival and chemotherapy response (MDPI; Cancer Genome Atlas). Overall, OCT2 is a critical determinant of the pharmacokinetic profile and safety of many cationic drugs.

Other names

Organic cation transporter 2OCT2SLC22A2Solute carrier family 22 member 2

Facilitated diffusion of organic cations across the basolateral membrane of renal proximal tubule cells, mediating the first step of renal secretion.