UNIT 23.3 Renal Transporters in Drug Disposition, Drug-Drug Interactions, and Nephrotoxicity

  1. Bo Feng1,
  2. Ayman F. El-Kattan1,
  3. Zaher A. Radi2

Published Online: 1 AUG 2012

DOI: 10.1002/0471140856.tx2303s53

Current Protocols in Toxicology

Current Protocols in Toxicology

How to Cite

Feng, B., El-Kattan, A. F. and Radi, Z. A. 2012. Renal Transporters in Drug Disposition, Drug-Drug Interactions, and Nephrotoxicity. Current Protocols in Toxicology. 53:23.3:23.3.1–23.3.15.

Author Information

  1. 1

    Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research and Development, Groton, Connecticut

  2. 2

    Drug Safety Research and Development, Pfizer Worldwide Research and Development, Cambridge, Massachusetts

Publication History

  1. Published Online: 1 AUG 2012


This unit describes in detail the in vitro methods for measuring the interaction of new chemical entities (NCEs) with human renal transporters (hOAT1, hOAT2, and hOCT2) as both a substrate and inhibitor. Renal transporter substrate assays help in the identification of renal secretion mechanisms and assessment of the potential renal drug-drug interactions (DDIs) for NCE as a target, as well as to predict its renal clearance in humans. Human renal transporter (hOAT1, hOAT2, and hOCT2) inhibition assays characterize the inhibition potency of NCE and predict the potential for renal DDIs as a perpetrator with xenobiotics and drugs that are mainly renally cleared. In addition, such inhibition assays enable a better assessment of the potential for renal transporter-mediated nephrotoxicity and pathology. Therefore, renal transporter substrate and inhibition assays are pivotal in drug discovery and development for renally cleared drugs and those that are co-administered with marketed compounds mainly eliminated via the kidney. Curr. Protoc. Toxicol. 53:23.3.1-23.3.15. © 2012 by John Wiley & Sons, Inc.


  • renal transporters;
  • nephrotoxicity;
  • drug-drug interaction