In vitro and in vivo models for assessing drug efflux transporter activity

Adv Drug Deliv Rev. 2003 Jan 21;55(1):31-51. doi: 10.1016/s0169-409x(02)00170-9.

Abstract

Determining the activity of drug efflux transport proteins has important implications in the identification of substrates and/or inhibitors of the various transport systems, as well as mechanistic determination of localization, and functional role of the transporters in absorption, distribution and elimination of compounds in the body. This review examines both in vitro and in vivo approaches used to determine drug efflux transporter activity, their applications, and advantages and potential limitations.

Publication types

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

MeSH terms

  • ATP-Binding Cassette Transporters / metabolism*
  • Animals
  • Animals, Genetically Modified
  • Biological Transport, Active
  • Humans
  • Mice
  • Mice, Mutant Strains
  • Models, Biological
  • Pharmaceutical Preparations / metabolism*
  • Rats
  • Rats, Mutant Strains

Substances

  • ATP-Binding Cassette Transporters
  • Pharmaceutical Preparations