Human immunodeficiency virus type 1 protease inhibitors

Arch Intern Med. 1997 May 12;157(9):951-9.


Until recently, treatment for human immunodeficiency virus type 1 (HIV-1) infection was limited to the use of nucleoside inhibitors of the viral enzyme reverse transcriptase. While these agents initially offered promise, they have only modest antiviral activity and the benefits of treatment are limited by the emergence of drug resistance and dose-limiting toxic effects. Development of more potent drugs that target different stages of the virus life cycle has thus been aggressively pursued. Efforts to develop inhibitors of HIV-1 protease have yielded a potent new class of compounds that suppress HIV-1 replication to an extent far greater than was previously attainable. Four protease inhibitors, saquinavir mesylate, ritonavir, nelfinavir, and indinavir sulfate, have been approved by the Food and Drug Administration. Other agents are undergoing active investigation. The purpose of this article is to review the currently available data on those agents that have been approved for clinical use.

Publication types

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

MeSH terms

  • Acquired Immunodeficiency Syndrome / drug therapy*
  • Animals
  • Anti-HIV Agents / adverse effects
  • Anti-HIV Agents / pharmacokinetics
  • Anti-HIV Agents / pharmacology*
  • CD4 Lymphocyte Count / drug effects
  • Clinical Trials as Topic
  • Drug Interactions
  • Drug Resistance
  • HIV Protease Inhibitors / adverse effects
  • HIV Protease Inhibitors / pharmacokinetics
  • HIV Protease Inhibitors / pharmacology*
  • HIV-1 / enzymology*
  • Humans
  • Indinavir / pharmacology
  • Isoquinolines / pharmacology
  • Nelfinavir
  • RNA, Viral / drug effects
  • Ritonavir / pharmacology
  • Saquinavir / pharmacology
  • Sulfonic Acids / pharmacology


  • Anti-HIV Agents
  • HIV Protease Inhibitors
  • Isoquinolines
  • RNA, Viral
  • Sulfonic Acids
  • Indinavir
  • Nelfinavir
  • Saquinavir
  • Ritonavir