A perspective on efflux transport proteins in the liver

Clin Pharmacol Ther. 2012 Nov;92(5):599-612. doi: 10.1038/clpt.2012.79. Epub 2012 Sep 5.


Detailed knowledge regarding the influence of hepatic transport proteins on drug disposition has advanced at a rapid pace over the past decade. Efflux transport proteins located in the basolateral and apical (canalicular) membranes of hepatocytes play an important role in the hepatic elimination of many endogenous and exogenous compounds, including drugs and metabolites. This review focuses on the role of these efflux transporters in hepatic drug excretion. The impact of these proteins as underlying factors for disease is highlighted, and the importance of hepatic efflux proteins in the efficacy and toxicity of drugs is discussed. In addition, a brief overview of methodology to evaluate the function of hepatic efflux transport proteins is provided. Current challenges in predicting the impact of altered efflux protein function on systemic, intestinal, and hepatocyte exposure to drugs and metabolites are highlighted.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Biological Transport
  • Drug-Related Side Effects and Adverse Reactions
  • Hepatocytes / metabolism
  • Humans
  • Intestinal Mucosa / metabolism
  • Liver / metabolism*
  • Membrane Transport Proteins / metabolism*
  • Pharmaceutical Preparations / metabolism*


  • Membrane Transport Proteins
  • Pharmaceutical Preparations