Integrase Strand Transfer Inhibitors Are Effective Anti-HIV Drugs

Viruses. 2021 Jan 29;13(2):205. doi: 10.3390/v13020205.


Integrase strand transfer inhibitors (INSTIs) are currently recommended for the first line treatment of human immunodeficiency virus type one (HIV-1) infection. The first-generation INSTIs are effective but can select for resistant viruses. Recent advances have led to several potent second-generation INSTIs that are effective against both wild-type (WT) HIV-1 integrase and many of the first-generation INSTI-resistant mutants. The emergence of resistance to these new second-generation INSTIs has been minimal, which has resulted in alternative treatment strategies for HIV-1 patients. Moreover, because of their high antiviral potencies and, in some cases, their bioavailability profiles, INSTIs will probably have prominent roles in pre-exposure prophylaxis (PrEP). Herein, we review the current state of the clinically relevant INSTIs and discuss the future outlook for this class of antiretrovirals.

Keywords: HIV; INSTIs; antiviral therapy; drug resistance; integration.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • DNA, Viral / metabolism
  • Drug Resistance, Viral
  • HIV Infections / drug therapy
  • HIV Integrase / chemistry
  • HIV Integrase / genetics
  • HIV Integrase / metabolism
  • HIV Integrase Inhibitors / chemistry
  • HIV Integrase Inhibitors / pharmacology*
  • HIV Integrase Inhibitors / therapeutic use
  • HIV-1 / drug effects*
  • HIV-1 / enzymology
  • HIV-1 / genetics
  • Humans
  • Mutation
  • Pre-Exposure Prophylaxis
  • Virus Replication


  • DNA, Viral
  • HIV Integrase Inhibitors
  • HIV Integrase