Influence of drug transport proteins on the pharmacokinetics and drug interactions of HIV protease inhibitors

J Pharm Sci. 2011 Sep;100(9):3636-54. doi: 10.1002/jps.22655. Epub 2011 Jun 22.


Protease inhibitors, a class of antiretroviral agents frequently used in the treatment of HIV infection, interact with numerous transport proteins resulting in clinically significant drug-drug interactions (DDIs). This review focuses on the proteins that transport protease inhibitors and directly influence the pharmacokinetics of these drugs, as well as the transport proteins that are inhibited or induced by protease inhibitors. Clinically relevant DDIs involving drug transporters and protease inhibitors, either as "victim" drugs or as "perpetrator" drugs, and the pharmacokinetic consequences of such interactions are highlighted. A summary of transporter-mediated processes underlying the toxicity of protease inhibitors is provided. Finally, the effect of HIV infection or co-infection on drug transport proteins, and the implications for protease inhibitor pharmacokinetics is discussed. Transport proteins significantly influence the pharmacokinetics, efficacy and toxicity profiles of this important class of drugs.

Publication types

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

MeSH terms

  • Carrier Proteins / metabolism*
  • Drug Interactions*
  • HIV Protease Inhibitors / pharmacokinetics
  • HIV Protease Inhibitors / pharmacology*
  • Humans
  • Pharmacokinetics*


  • Carrier Proteins
  • HIV Protease Inhibitors