Organic anion transporter 1 (OAT1) and Organic anion transporter 3 (OAT3) (OAT1 / OAT3)

Organic anion transporter 1 (OAT1) and organic anion transporter 3 (OAT3) are closely related renal transporters encoded by the SLC22A6 and SLC22A8 genes, respectively, and widely recognized as therapeutic targets due to their central roles in the renal secretion and excretion of a broad range of drugs, xenobiotics, and endogenous metabolites[1][2][4][6]. These membrane proteins are located on the basolateral surface of proximal tubule epithelial cells in the kidney, where they mediate the uptake of organic anions—including drugs such as antivirals, antibiotics, and anticancer agents—from the blood into the cell, facilitating subsequent excretion into urine[1][2][4]. They function chiefly as exchangers, coupling organic anion import with the export of endogenous dicarboxylates[1]. OAT1 and OAT3 have overlapping and broad substrate specificities, and alterations in their function impact drug pharmacokinetics, risk of nephrotoxicity, and blood pressure regulation (notably by OAT3)[2]. These transporters are implicated in drug-drug interactions and are significant determinants of individual variability in drug response and toxicity[2][4][5].

Other names

Solute carrier family 22 member 6 (SLC22A6) [for OAT1]Solute carrier family 22 member 8 (SLC22A8) [for OAT3]Novel kidney transporter (historical, for OAT1)Renal organic anion transporter

Inhibition or competition at the transporter (drug-drug interaction potential); Facilitation of renal tubular secretion