HIV-1 antiretroviral drug therapy

Cold Spring Harb Perspect Med. 2012 Apr;2(4):a007161. doi: 10.1101/cshperspect.a007161.

Abstract

The most significant advance in the medical management of HIV-1 infection has been the treatment of patients with antiviral drugs, which can suppress HIV-1 replication to undetectable levels. The discovery of HIV-1 as the causative agent of AIDS together with an ever-increasing understanding of the virus replication cycle have been instrumental in this effort by providing researchers with the knowledge and tools required to prosecute drug discovery efforts focused on targeted inhibition with specific pharmacological agents. To date, an arsenal of 24 Food and Drug Administration (FDA)-approved drugs are available for treatment of HIV-1 infections. These drugs are distributed into six distinct classes based on their molecular mechanism and resistance profiles: (1) nucleoside-analog reverse transcriptase inhibitors (NNRTIs), (2) non-nucleoside reverse transcriptase inhibitors (NNRTIs), (3) integrase inhibitors, (4) protease inhibitors (PIs), (5) fusion inhibitors, and (6) coreceptor antagonists. In this article, we will review the basic principles of antiretroviral drug therapy, the mode of drug action, and the factors leading to treatment failure (i.e., drug resistance).

Publication types

  • Review

MeSH terms

  • Anti-HIV Agents / pharmacology*
  • Anti-HIV Agents / therapeutic use*
  • CCR5 Receptor Antagonists
  • Drug Resistance, Viral
  • HIV Fusion Inhibitors / pharmacology
  • HIV Fusion Inhibitors / therapeutic use
  • HIV Infections / drug therapy*
  • HIV Integrase Inhibitors / pharmacology
  • HIV Integrase Inhibitors / therapeutic use
  • HIV Protease Inhibitors / pharmacology
  • HIV Protease Inhibitors / therapeutic use
  • HIV-1 / physiology*
  • Humans
  • Reverse Transcriptase Inhibitors / pharmacology
  • Reverse Transcriptase Inhibitors / therapeutic use
  • Virus Replication / drug effects*

Substances

  • Anti-HIV Agents
  • CCR5 Receptor Antagonists
  • HIV Fusion Inhibitors
  • HIV Integrase Inhibitors
  • HIV Protease Inhibitors
  • Reverse Transcriptase Inhibitors