Practical aspects of transporter model systems: a case study involving SQV

Drug Metab Rev. 2004 May;36(2):377-89. doi: 10.1081/dmr-120037570.


In this case study, in vitro and in vivo data were provided for saquinavir (SQV) showing that drug transporters play a significant role in the absorption and disposition of drugs. This article is focused on the more practical points with a technical emphasis. Currently many in vitro and in vivo experimental models have been developed to investigate drug transporter interactions for the prediction of how transporters may influence the pharmacokinetic behavior of drugs. In this review, the successful application, limitations and challenges of these models are emphasized.

Publication types

  • Review

MeSH terms

  • ATP-Binding Cassette Transporters / metabolism
  • Absorption
  • Animals
  • Brain / metabolism
  • Carrier Proteins / metabolism*
  • Cells, Cultured
  • HIV Protease Inhibitors / metabolism*
  • HIV Protease Inhibitors / pharmacokinetics
  • Humans
  • Injections, Intravenous
  • Saquinavir / metabolism*
  • Saquinavir / pharmacokinetics


  • ATP-Binding Cassette Transporters
  • Carrier Proteins
  • HIV Protease Inhibitors
  • Saquinavir