HIV-1 drug resistance in the iPrEx preexposure prophylaxis trial

J Infect Dis. 2014 Oct 15;210(8):1217-27. doi: 10.1093/infdis/jiu233. Epub 2014 Apr 16.

Abstract

Background: The iPrEx study demonstrated that combination oral emtricitabine and tenofovir disoproxil fumarate (FTC/TDF) as preexposure prophylaxis (PrEP) protects against HIV acquisition in men who have sex with men and transgender women. Selection for drug resistance could offset PrEP benefits.

Methods: Phenotypic and genotypic clinical resistance assays characterized major drug resistant mutations. Minor variants with FTC/TDF mutations K65R, K70E, M184V/I were measured using 454 deep sequencing and a novel allele-specific polymerase chain reaction (AS-PCR) diagnostic tolerant to sequence heterogeneity.

Results: Control of primer-binding site heterogeneity resulted in improved accuracy of minor variant measurements by AS-PCR. Of the 48 on-study infections randomized to FTC/TDF, none showed FTC/TDF mutations by clinical assays despite detectable drug levels in 8 participants. Two randomized to FTC/TDF had minor variant M184I detected at 0.53% by AS-PCR or 0.75% by deep sequencing, only 1 of which had low but detectable drug levels. Among those with acute infection at randomization to FTC/TDF, M184V or I mutations that were predominant at seroconversion waned to background levels within 24 weeks after discontinuing drug.

Conclusions: Drug resistance was rare in iPrEx on-study FTC/TDF-randomized seroconverters, and only as low-frequency minor variants. FTC resistance among those initiating PrEP with acute infection waned rapidly after drug discontinuation. Clinical Trials Registration.NCT00458393.

Keywords: 454 deep sequencing; AS-PCR; FTC/TDF; HIV-1; PrEP; drug resistance; minor variant; preexposure prophylaxis.

Publication types

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

MeSH terms

  • Adenine / administration & dosage
  • Adenine / analogs & derivatives
  • Adenine / therapeutic use
  • Anti-HIV Agents / administration & dosage
  • Anti-HIV Agents / pharmacology*
  • Deoxycytidine / administration & dosage
  • Deoxycytidine / analogs & derivatives
  • Deoxycytidine / therapeutic use
  • Drug Resistance, Viral*
  • Emtricitabine
  • Female
  • Genotype
  • HIV Infections / prevention & control*
  • HIV Infections / virology*
  • HIV-1 / drug effects*
  • HIV-1 / genetics
  • Homosexuality, Male
  • Humans
  • Male
  • Mutation
  • Organophosphonates / administration & dosage
  • Organophosphonates / therapeutic use
  • RNA, Viral / genetics
  • Tenofovir
  • Transgender Persons
  • Viral Load

Substances

  • Anti-HIV Agents
  • Organophosphonates
  • RNA, Viral
  • Deoxycytidine
  • Tenofovir
  • Emtricitabine
  • Adenine

Associated data

  • ClinicalTrials.gov/NCT00458393