HIV protease inhibitors: recent clinical trials and recommendations on use

Expert Opin Pharmacother. 2009 Jul;10(10):1615-29. doi: 10.1517/14656560902980202.


Background: HIV protease inhibitors (PIs) are potent antiretroviral drugs that represent a pivotal component of highly active antiretroviral therapy (HAART). PIs have evolved over the years to gain in potency, convenience, tolerability and genetic barrier to resistance.

Objective: Updated summary of evidence-based information about the efficacy and safety of PIs on initial, simplification and rescue interventions in HIV patients.

Methods: Review of available data reported in peer-reviewed journals, medical conferences and treatment guidelines.

Results: Due to their characteristics, PIs are, and will remain, a cornerstone component in most lines of antiretroviral therapy. The antiviral activity, tolerability and convenience of PIs have improved significantly in recent years. Differences between compounds within this class may favour their use in specific situations, such as the friendly metabolic profile of atazanavir in patients with cardiovascular disease or the high genetic barrier of darunavir or tipranavir in heavily pretreated individuals with HIV.

Publication types

  • Review

MeSH terms

  • Anti-HIV Agents / therapeutic use*
  • Antiretroviral Therapy, Highly Active
  • Antiviral Agents / therapeutic use
  • Atazanavir Sulfate
  • Clinical Trials as Topic
  • Darunavir
  • Drug Interactions
  • Drug Resistance, Viral
  • HIV Fusion Inhibitors / therapeutic use
  • HIV Infections / drug therapy*
  • HIV Protease Inhibitors / administration & dosage
  • HIV Protease Inhibitors / therapeutic use*
  • HIV-1 / drug effects
  • Humans
  • Metabolome
  • Oligopeptides / therapeutic use
  • Pyridines / therapeutic use
  • Pyrones / therapeutic use
  • Sulfonamides / therapeutic use
  • Treatment Outcome


  • Anti-HIV Agents
  • Antiviral Agents
  • HIV Fusion Inhibitors
  • HIV Protease Inhibitors
  • Oligopeptides
  • Pyridines
  • Pyrones
  • Sulfonamides
  • Atazanavir Sulfate
  • Darunavir
  • tipranavir