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

Solute carrier family 22 member 2 (OCT2) is a polyspecific transporter protein primarily expressed on the basolateral membrane of renal proximal tubule cells (UniProt: O15244). It plays a pivotal role in the renal clearance of many endogenous and exogenous organic cations by facilitating their uptake from the blood into the tubular cells. Imagabalin (PD-0332334), a gabapentinoid ligand for the alpha2-delta subunit of voltage-gated calcium channels, has been identified as a substrate for OCT2, as well as the apical efflux transporters MATE1 and MATE2-K (PubMed: 22407615). The interaction between imagabalin and these renal transporters is a key determinant of the drug's pharmacokinetic profile, as its excretion is predominantly renal. Inhibition of OCT2 by other drugs, such as cimetidine, can lead to reduced renal secretion and significantly elevated plasma levels of imagabalin, increasing the risk of adverse effects (PubMed: 23633525). Consequently, OCT2 is a critical focus for evaluating potential drug-drug interactions during the development of renally cleared cationic medications. Understanding the activity of this transporter system is essential for predicting patient-specific clearance and avoiding toxicity in clinical settings.

Other names

Organic cation transporter 2OCT2SLC22A2Renal organic cation transporter 2

Mediates the electrogenic, sodium-independent uptake of organic cations from the blood into renal proximal tubule cells across the basolateral membrane.