Target intelligence / Profile preview

Organic cation transporter type 2 (OCT2)

Target
OCT2
Molecular classification
Transporter, Solute carrier (SLC) family, Major facilitator superfamily (MFS)
01

Overview

Organic cation transporter type 2 (OCT2, SLC22A2) is a polyspecific membrane transporter primarily expressed in the basolateral membrane of renal proximal tubules. It facilitates the renal secretion and clearance of a broad range of endogenous and exogenous organic cations, including many drugs such as metformin and platinum-based chemotherapeutics. OCT2 contains 12 transmembrane domains and functions as part of the solute carrier family, contributing to drug pharmacokinetics and susceptibility to drug interactions. Genetic polymorphisms in SLC22A2 can significantly affect drug distribution, efficacy, and toxicity[2][3][4][5][6]. OCT2 expression is also documented in the pancreas, particularly in β cells, with evidence supporting regulation by glucose and possible functional interaction with the glucose transporter GLUT2[4][6]. OCT2 plays a major role in kidney drug elimination, and its inhibition or genetic variance can result in clinically relevant changes in drug handling and safety[3][4][5].

Other names
SLC22A2renal organic cation transporter 2OCT2solute carrier family 22 member 2
02

Mechanism of action

Facilitated diffusion: transport of organic cations down their electrochemical gradient; Drug uptake into cells via transporter-mediated process; Competition and inhibition by co-administered substances

03

Biological functions

Renal secretion of organic cationsMembrane transport of drugs and xenobioticsUptake of pharmaceuticals (e.g., metformin, platinum-derived chemotherapeutics)Regulation of cellular uptake of organic cations and some weak basesPossible interaction with glucose transporter 2 (GLUT2) in kidney and pancreas
04

Disease associations

Drug response variability (e.g., metformin efficacy)Potential involvement in drug-induced nephrotoxicityAltered transport may be relevant in metabolic diseases (e.g., diabetes)Polymorphisms associated with decreased drug clearance
05

Safety considerations

Drug-drug interactions (competition for transport)Genetic variability leading to altered drug pharmacokinetics and increased adverse effectsNephrotoxicity (especially with drugs like cisplatin, which uses OCT2 for renal uptake)
06

Interacting drugs

Metformin

4 more in the full profile.

07

Biomarkers

SLC22A2 polymorphisms (e.g., c.808G>T, Ala270Ser) may affect drug clearance

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