Evaluation of HIV-1 integrase resistance emergence and evolution in patients treated with integrase inhibitors

J Glob Antimicrob Resist. 2020 Mar:20:163-169. doi: 10.1016/j.jgar.2019.07.015. Epub 2019 Jul 19.

Abstract

Objectives: This study evaluated the emergence of mutations associated with integrase strand transfer inhibitors (INSTI) resistance (INSTI-RMs) and the integrase evolution in human immunodeficiency virus type 1 (HIV-1) infected patients treated with this drug class.

Methods: The emergence of INSTI-RMs and integrase evolution (estimated as genetic distance between integrase sequences under INSTI treatment and before INSTI treatment) were evaluated in 107 INSTI-naïve patients (19 drug-naïve and 88 drug-experienced) with two plasma genotypic resistance tests: one before INSTI treatment and one under INSTI treatment. A logistic regression analysis was performed to evaluate factors associated with the integrase evolution under INSTI treatment.

Results: The patients were mainly infected by B subtype (72.0%). Eighty-seven patients were treated with raltegravir, 13 with dolutegravir and seven with elvitegravir. Before INSTI treatment one patient harboured the major INSTI-RM R263K and three patients the accessory INSTI-RMs T97A. Under INSTI treatment the emergence of ≥1 INSTI-RM was found in 39 (36.4%) patients. The major INSTI-RMs that more frequently emerged were: N155H (17.8%), G140S (8.4%), Y143R (7.5%), Q148H (6.5%), and Y143C (4.7%). Concerning integrase evolution, a higher genetic distance was found in patients with ≥1 INSTI-RM compared with those without emergence of resistance (0.024 [0.012-0.036] vs. 0.015 [0.009-0.024], P=0.018). This higher integrase evolution was significantly associated with a longer duration of HIV-1 infection, a higher number of past regimens and non-B subtypes.

Conclusions: These findings confirm that major INSTI-RMs very rarely occur in INSTI-naïve patients. Under INSTI treatment, selection of drug-resistance follows the typical drug-resistance pathways; a higher evolution characterises integrase sequences developing drug-resistance compared with those without any resistance.

Keywords: Genetic distance; HIV-1 integrase resistance; Integrase inhibitors; Polymorphisms; Subtype.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Drug Resistance, Viral*
  • Evolution, Molecular
  • Female
  • Genotype
  • HIV Infections / drug therapy*
  • HIV Infections / virology
  • HIV Integrase / genetics*
  • HIV Integrase Inhibitors / pharmacology
  • HIV Integrase Inhibitors / therapeutic use*
  • HIV-1 / drug effects
  • HIV-1 / genetics*
  • Heterocyclic Compounds, 3-Ring / pharmacology
  • Heterocyclic Compounds, 3-Ring / therapeutic use
  • Humans
  • Logistic Models
  • Male
  • Middle Aged
  • Mutation
  • Oxazines / pharmacology
  • Oxazines / therapeutic use
  • Piperazines / pharmacology
  • Piperazines / therapeutic use
  • Pyridones / pharmacology
  • Pyridones / therapeutic use
  • Quinolones / pharmacology
  • Quinolones / therapeutic use
  • Raltegravir Potassium / pharmacology
  • Raltegravir Potassium / therapeutic use

Substances

  • HIV Integrase Inhibitors
  • Heterocyclic Compounds, 3-Ring
  • Oxazines
  • Piperazines
  • Pyridones
  • Quinolones
  • Raltegravir Potassium
  • elvitegravir
  • dolutegravir
  • HIV Integrase