Drug uptake transporters in antiretroviral therapy

Pharmacol Ther. 2011 Dec;132(3):268-79. doi: 10.1016/j.pharmthera.2011.06.007. Epub 2011 Jul 23.


Current treatment of human immunodeficiency virus-1 (HIV-1) infection is effective, although it does not permanently suppress viral replication in all patients. Viral persistence, drug toxicity, and antiretroviral resistance are challenging barriers to successful treatment of HIV-1 infection. It has become increasingly apparent that the balance between drug influx and efflux transporter activity plays a critical role in the overall disposition of anti-HIV drugs in both cells and tissues. Thus, drug transporters directly influence the appearance of drug resistance and toxicity, and could also be related to persistence of HIV-1. We review the role of drug uptake transporters from the solute carrier (SLC) superfamily, their relation with specific antiretroviral drug disposition, and their efficacy in the tissues that absorb, metabolize, and eliminate anti-HIV drugs. Recent studies focusing on the role of drug uptake transporters in immune cells, key sites in the action of antiviral therapy, are highlighted.

Publication types

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

MeSH terms

  • Animals
  • Anti-HIV Agents / pharmacokinetics*
  • Antiretroviral Therapy, Highly Active / methods
  • Biological Transport
  • HIV Infections / drug therapy*
  • HIV Infections / metabolism*
  • HIV-1*
  • Humans


  • Anti-HIV Agents