GW433908/ritonavir once daily in antiretroviral therapy-naive HIV-infected patients: absence of protease resistance at 48 weeks

AIDS. 2004 Mar 5;18(4):651-5. doi: 10.1097/00002030-200403050-00009.

Abstract

Objectives: To investigate the emergence of resistance to GW433908 (908), a protease inhibitor (PI) with demonstrated antiviral efficacy, safety and tolerability, when administered once daily (q.d.) with low dose ritonavir (908/r).

Design: A 48-week Phase III open-label study (SOLO, APV30002) in which antiretroviral therapy-naive patients (n = 649) were treated with 908/r, (1400 mg/200 mg, q.d.) or nelfinavir [1250 mg, twice daily (b.i.d.)] with two nucleoside reverse transcriptase inhibitors (NRTI), abacavir (300 mg, b.i.d.) and lamivudine (150 mg, b.i.d.).

Methods: Viral genotype and phenotype were analysed at baseline and on treatment up to 48 weeks and beyond.

Results: Emergence of genotypic resistance was significantly different between the 908/r q.d. and the nelfinavir b.i.d. treatment arms for both PIs (0 versus 50%; P < 0.001) and the NRTI (13% versus 69%; P < 0.001) received. In the nelfinavir arm the key protease mutations D30N and/or L90M were frequently observed. The absence of protease resistance mutations and reduced incidence of NRTI resistance mutations in the 908/r q.d. arm was confirmed by phenotyping, which showed a lack of PI cross-resistance.

Conclusions: The absence of resistance to 908 or cross-resistance to other PIs, and reduced NRTI resistance, following a 908/r q.d. regimen supports the use of this boosted PI early in therapy.

Publication types

  • Clinical Trial
  • Clinical Trial, Phase III
  • Multicenter Study
  • Randomized Controlled Trial

MeSH terms

  • Antiretroviral Therapy, Highly Active
  • Carbamates
  • Drug Resistance
  • Drug Resistance, Multiple, Viral / genetics
  • Drug Resistance, Viral / genetics
  • Follow-Up Studies
  • Furans
  • Genotype
  • HIV Infections / drug therapy*
  • HIV Infections / virology
  • HIV Protease Inhibitors / therapeutic use*
  • HIV-1 / drug effects*
  • HIV-1 / genetics
  • Humans
  • Mutation
  • Organophosphates / therapeutic use*
  • Phenotype
  • Ritonavir / therapeutic use*
  • Sulfonamides / therapeutic use*

Substances

  • Carbamates
  • Furans
  • HIV Protease Inhibitors
  • Organophosphates
  • Sulfonamides
  • Ritonavir
  • fosamprenavir