Accumulation of Multiple Mutations In Vivo Confers Cross-Resistance to New and Existing Integrase Inhibitors

J Infect Dis. 2018 Oct 20;218(11):1773-1776. doi: 10.1093/infdis/jiy428.

Abstract

Bictegravir (BIC) and cabotegravir (CAB) are the latest available HIV integrase inhibitors in clinical trials. The combination of major integrase inhibitor substitutions G140S/Q148H has been shown to confer high-level resistance to the approved integrase inhibitors raltegravir (RAL) and elvitegravir (EVG) but not necessarily dolutegravir (DTG). We assayed recombinant viruses made from patient-derived RNA extracts for resistance phenotype for a panel of viruses containing G140S/Q148H with additional accessory substitutions. The accumulation of multiple integrase substitutions confers high-level resistance to all 5 integrase inhibitors. There is extensive cross-resistance between DTG, BIC, and CAB (r = 0.96-0.97).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amides
  • Cell Line
  • Drug Resistance, Viral* / drug effects
  • Drug Resistance, Viral* / genetics
  • HIV Infections / virology
  • HIV Integrase Inhibitors / pharmacology*
  • HIV-1* / drug effects
  • HIV-1* / genetics
  • Heterocyclic Compounds, 3-Ring / pharmacology
  • Heterocyclic Compounds, 4 or More Rings / pharmacology
  • Humans
  • Oxazines
  • Piperazines
  • Pyridones / pharmacology

Substances

  • Amides
  • HIV Integrase Inhibitors
  • Heterocyclic Compounds, 3-Ring
  • Heterocyclic Compounds, 4 or More Rings
  • Oxazines
  • Piperazines
  • Pyridones
  • bictegravir
  • dolutegravir
  • cabotegravir

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