The role of ABC transporters in drug absorption, distribution, metabolism, excretion and toxicity (ADME-Tox)

Drug Discov Today. 2008 May;13(9-10):379-93. doi: 10.1016/j.drudis.2007.12.010. Epub 2008 Feb 20.


ATP binding cassette (ABC) drug transporters play an important role in cancer drug resistance, protection against xenobiotics, and in general in the passage of drugs through cellular and tissue barriers. This review explores how human ABC transporters modulate the pharmacological effects of various drugs, and how this predictable ADME-TOX modulation can be used during the process of drug discovery and development. We provide a description of the relevant human ABC drug transporters and review the models and assay systems that can be applied for the analysis of their expected drug interactions. The use of the in vitro, in vivo, in silico models, their combination, and the emerging clinical information are evaluated with respect to their potential application in early drug screening.

Publication types

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

MeSH terms

  • ATP-Binding Cassette Transporters / metabolism*
  • Animals
  • Drug Design*
  • Drug-Related Side Effects and Adverse Reactions*
  • Humans
  • Pharmacokinetics*


  • ATP-Binding Cassette Transporters