Renal tubular transport inhibitor

Renal tubular transport inhibitor
Drug class
Class identifiers
UseTreatment of gout, reduced clearance of co-administered drugs
Mechanism of actionTransporter inhibitor
Biological targetOAT1, OAT3, OCT2, MATE1 and MATE2
Legal status

Renal tubular transport inhibitors are a class of drugs that interfere with the function of specific transporters in the renal proximal tubules, affecting the excretion and reabsorption of various substances, including drugs and endogenous compounds. These inhibitors target membrane transport proteins expressed in kidney tubule epithelial cells, which play a crucial role in drug elimination and can significantly influence drug pharmacokinetics.[1] By modulating the activity of transporters such as organic anion transporters (OATs), organic cation transporters (OCTs), and multidrug and toxin extrusion proteins (MATEs), these inhibitors can alter the renal clearance of drugs, potentially leading to clinically significant drug-drug interactions (DDIs) and changes in drug efficacy or toxicity.[2][3] Renal tubular transport inhibitors have both therapeutic applications, such as enhancing the efficacy of certain medications or reducing drug-induced nephrotoxicity, and potential risks, including unwanted drug accumulation and altered pharmacokinetics of co-administered drugs.[1][3]

  1. ^ a b Łapczuk-Romańska J, Droździk M, Oswald S, Droździk M (February 2023). "Kidney Drug Transporters in Pharmacotherapy". Review. International Journal of Molecular Sciences. 24 (3): 2856. doi:10.3390/ijms24032856. PMC 9917665. PMID 36769175.
  2. ^ Yin J, Wang J (September 2016). "Renal drug transporters and their significance in drug-drug interactions". Acta Pharmaceutica Sinica. B. 6 (5): 363–373. doi:10.1016/j.apsb.2016.07.013. PMC 5045553. PMID 27709005.
  3. ^ a b Launay-Vacher V, Izzedine H, Karie S, Hulot JS, Baumelou A, Deray G (2006). "Renal tubular drug transporters". Nephron. Physiology. 103 (3): 97–106. doi:10.1159/000092212. PMID 16554667.