Single genome sequencing of HIV-1 gag and protease resistance mutations at virologic failure during the OK04 trial of simplified versus standard maintenance therapy

Antivir Ther. 2011;16(5):725-32. doi: 10.3851/IMP1812.

Abstract

Background: Ritonavir-boosted lopinavir (LPV/RTV) alone has been evaluated as simplified maintenance therapy for HIV-1 infection, but there are concerns about greater potential for emergence of protease inhibitor (PI) resistance. The OK04 trial evaluated maintenance therapy with LPV/RTV alone versus standard therapy (ST) with two NRTIs plus LPV/RTV in 205 patients, of whom 15 had virological rebound by week 48 (11 versus 4 patients, respectively). We developed a single genome sequencing (SGS) assay of HIV-1 gag and protease to assess the emergence of low frequency drug-resistant variants during virological rebound.

Methods: Plasma samples from 15 subjects at virological rebound were analysed by SGS of HIV-1 gag and protease genes. A total of 45 SGS sequences were planned per sample, providing 90% power to detect variants comprising >5% of the virus population.

Results: Overall, 521 single sequences obtained from 13 patients (range 4-48 sequences/patient) revealed similar frequencies of major protease resistance mutations in samples from the LPV/RTV alone (3/11) and ST (3/4) arms (P=0.10), with a median number of minor protease resistance mutations of 3.0 versus 3.5, respectively (P=0.23). Median number of gag PI resistance mutations were similar between the LPV/RTV alone and ST arms at cleavage sites (3.0 versus 2.5; P=0.83), non-cleavage sites (21 versus 16.5; P=0.71) and the transframe protein-p6 pol region cleavage sites (4.0 versus 3.0; P=0.6).

Conclusions: Although more subjects with simplified maintenance therapy with LPV/RTV alone had virological rebound compared to the ST arm, this was not associated with more frequent emergence of variants encoding PI resistance mutations in gag or protease detected by SGS.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Clinical Trials as Topic
  • Drug Resistance, Viral / genetics*
  • Genes, pol
  • HIV Infections / drug therapy
  • HIV Infections / genetics
  • HIV Infections / virology
  • HIV Protease / genetics
  • HIV Protease Inhibitors / metabolism*
  • HIV Protease Inhibitors / therapeutic use
  • HIV-1 / drug effects
  • HIV-1 / genetics
  • Humans
  • Lipoproteins / genetics
  • Lipoproteins / metabolism
  • Mutation*
  • Standard of Care
  • Treatment Failure*
  • Viral Load*
  • gag Gene Products, Human Immunodeficiency Virus / metabolism*

Substances

  • HIV Protease Inhibitors
  • Lipoproteins
  • gag Gene Products, Human Immunodeficiency Virus
  • lipoprotein-associated coagulation inhibitor
  • HIV Protease