Analysis of drug resistance during HIV RNA viraemia in the MONET trial of darunavir/ritonavir monotherapy

Antivir Ther. 2011;16(1):59-65. doi: 10.3851/IMP1710.

Abstract

Background: When patients have HIV RNA suppressed to <50 copies/ml on current treatment, switching to darunavir (DRV)/ritonavir (DRV/r) monotherapy could prevent the development of resistance to other drug classes.

Methods: In the MONET trial, 256 patients with HIV RNA<50 copies/ml on current highly active antiretroviral therapy (57% with protease inhibitors [PIs] and 43% with non-nucleoside reverse transcriptase inhibitors) and no history of virological failure were randomized to DRV/r 800/100 mg once daily, either as monotherapy (monotherapy arm) or with two nucleoside reverse transcriptase inhibitors (NRTIs; triple therapy arm). All samples with HIV RNA ≥ 50 copies/ml were genotyped, and a virtual phenotype was calculated (VircoType HIV-1 assays; Virco BVBA, Mechelen, Belgium).

Results: A total of 63 patients had ≥ 1 HIV RNA result ≥ 50 copies/ml, of whom 38 were successfully genotyped. Most HIV RNA increases were transient and in the range of 50-200 copies/ml. Overall, 36 of the 38 (95%) successfully genotyped patients showed no International AIDS Society-USA major PI mutations, DRV mutations or NRTI mutations. Two patients showed some evidence of PI resistance during transient HIV RNA elevations: one patient in the monotherapy arm had a single DRV mutation (L33F) when HIV RNA was 63 copies/ml (the virus was phenotypically sensitive to DRV [fold change 0.8]) and one PI pretreated patient taking tenofovir disoproxil fumarate/emtricitabine/DRV/r had re-emergence of pre-existing NRTI (M184V) and PI (V82I and L90M) mutations after a short treatment interruption (this virus remained phenotypically sensitive to DRV/r). Both patients showed sustained HIV RNA suppression to week 48 remaining with the same treatment.

Conclusions: Emergence of drug resistance after changing a suppressive triple antiretroviral therapy to DRV/r with or without nucleoside analogues is uncommon.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenine / administration & dosage
  • Adenine / analogs & derivatives
  • Adenine / therapeutic use
  • Adult
  • Anti-HIV Agents / administration & dosage
  • Anti-HIV Agents / therapeutic use
  • Clinical Trials as Topic
  • Darunavir
  • Deoxycytidine / administration & dosage
  • Deoxycytidine / analogs & derivatives
  • Deoxycytidine / therapeutic use
  • Drug Administration Schedule
  • Drug Resistance, Viral / drug effects*
  • Drug Resistance, Viral / genetics*
  • Drug Therapy, Combination
  • Emtricitabine
  • Female
  • HIV Infections / drug therapy*
  • HIV Infections / epidemiology
  • HIV Infections / genetics*
  • HIV Infections / virology
  • HIV Protease Inhibitors / administration & dosage
  • HIV Protease Inhibitors / therapeutic use
  • HIV-1 / genetics*
  • Humans
  • Male
  • Molecular Typing
  • Mutation
  • Organophosphonates / administration & dosage
  • Organophosphonates / therapeutic use
  • RNA, Viral / analysis
  • Ritonavir / administration & dosage
  • Ritonavir / therapeutic use
  • Sulfonamides / administration & dosage
  • Sulfonamides / therapeutic use
  • Tenofovir
  • Treatment Outcome
  • Virus Replication / drug effects
  • Virus Replication / genetics

Substances

  • Anti-HIV Agents
  • HIV Protease Inhibitors
  • Organophosphonates
  • RNA, Viral
  • Sulfonamides
  • Deoxycytidine
  • Tenofovir
  • Emtricitabine
  • Adenine
  • Ritonavir
  • Darunavir