Pharmacokinetic assessment of multiple ATP-binding cassette transporters: the power of combination knockout mice

Mol Interv. 2009 Jun;9(3):136-45. doi: 10.1124/mi.9.3.7.


A TP-binding cassette (ABC) multidrug transporters are cellular efflux pumps with broad and often widely overlapping substrate specificities. They can have a major impact on the pharmacokinetics and hence overall pharmacological behavior of many drugs. To study their separate roles and functional overlap, or complementarity, a collection of mice deficient in two or more ABC transporters has been generated. This review discusses recent findings obtained with these models, focusing on pharmacokinetic studies with a number of clinically relevant drugs. In addition, the characterization of these mice and some physiological aspects of ABC multidrug transporters are addressed.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • ATP-Binding Cassette Transporters / chemistry*
  • ATP-Binding Cassette Transporters / genetics*
  • ATP-Binding Cassette Transporters / metabolism
  • Animals
  • Biological Transport
  • Humans
  • Mice
  • Mice, Knockout
  • Models, Animal*
  • Pharmaceutical Preparations / metabolism


  • ATP-Binding Cassette Transporters
  • Pharmaceutical Preparations