SLC22A2, more commonly referred to as OCT2 (Organic Cation Transporter 2), is a renal uptake transporter that plays a key role in disposition and renal clearance of drugs and endogenous compounds. OCT2 substrate drugs have the potential for drug drug interactions with co-administered therapeutics that are inhibitors of this transporter. The FDA and EMA require in vitro testing for OCT2 liability with drug candidates that are eliminated at least in part via the kidneys.

Genes:
SLC22A2

Human Protein:
UniProt O15244

Tissue:
kidney, small intestine, lung, skin, placenta, brain and choroid plexus

Function/ Application:
In the basolateral membrane of the distal tubule in the kidney, OCT2 transporter mediates uptake from the blood to the proximal tubular cells during the renal secretion of organic cations. OCT2 transports many organic cations and play an important role on the pharmacological, pharmacokinetic and toxicological properties of therapeutics. OCT2 transports monoamine neurotransmitters, thereby participating in the regulation of interstitial and intracellular concentrations of monoamine neurotransmitters and cationic drugs.

Pathology:
OCT2 transporter contributes to renal drug uptake, clearance and transporter – mediated drug interactions.

Substrates:
choline, metformin, TEA

Assays:
SURFE2R transporter assays

Recommended Reviews:
Koepsell, H. and H. Endou, The SLC22 drug transporter family. Pflugers Arch, 2004. 447(5): p. 666-76; Jonker, J.W. and A.H. Schinkel, Pharmacological and physiological functions of the polyspecific organic cation transporters: OCT1, 2, and 3 (SLC22A1-3). J Pharmacol Exp Ther, 2004. 308(1): p. 2-9; Koepsell, H., Polyspecific organic cation transporters: their functions and interactions with drugs. Trends Pharmacol Sci, 2004. 25(7): p. 375-81.