Effect of baseline protease genotype and phenotype on HIV response to atazanavir/ritonavir in treatment-experienced patients

AIDS. 2006 Apr 4;20(6):847-53. doi: 10.1097/01.aids.0000218548.77457.76.

Abstract

Objectives: To assess the virologic response rates of atazanavir/ritonavir and lopinavir/ritonavir based on baseline genotype and phenotype.

Methods: Resistance analyses were performed on a Bristol-Myers Squibb-sponsored study comparing the safety and efficacy of atazanavir/ritonavir to lopinavir/ritonavir in treatment-experienced subjects at 48 weeks. Analyses evaluated virologic response based on the presence of baseline primary protease inhibitor mutations and baseline susceptibility.

Results: Less than 30% of atazanavir/ritonavir-treated patients were responders if substitutions at positions M46, G73, I84 or L90 were present in their HIV at baseline. In comparison, lopinavir/ritonavir response rates were less than 30% when protease substitutions at M46, I54, or I84 were present at baseline. The response rates were similar between atazanavir/ritonavir and lopinavir/ritonavir-treated subjects with zero to four baseline protease inhibitor mutations, but response rates were reduced if five or more baseline mutations were present: 0% for atazanavir/ritonavir compared with 28% for lopinavir/ritonavir. Baseline phenotype results showed that response rates were similar between atazanavir/ritonavir and lopinavir/ritonavir if shifts in susceptibility were zero to five, but response rates were lower if shifts were greater than five; 11% for atazanavir/ritonavir compared with 27% for lopinavir/ritonavir.

Conclusions: Both type and number of baseline protease inhibitor mutations affected virologic response to atazanavir/ritonavir and lopinavir/ritonavir in treatment-experienced subjects. In addition, baseline phenotypic susceptibility could differentiate virologic response rates to the two drugs. These resistance analyses provide information on the likelihood of a virologic response to antiretroviral drugs based on baseline genotypic and phenotypic data, which is valuable to physicians and patients when choosing antiretroviral regimens.

Publication types

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

MeSH terms

  • Adult
  • Antiretroviral Therapy, Highly Active
  • Atazanavir Sulfate
  • Drug Approval / methods
  • Drug Resistance, Viral / genetics
  • Female
  • Genotype
  • HIV Infections / drug therapy*
  • HIV Infections / virology
  • HIV Protease / genetics*
  • HIV Protease Inhibitors / therapeutic use*
  • HIV-1 / drug effects
  • HIV-1 / genetics*
  • Humans
  • Male
  • Middle Aged
  • Mutation
  • Oligopeptides / therapeutic use
  • Phenotype
  • Pyridines / therapeutic use
  • Ritonavir / therapeutic use
  • Treatment Outcome
  • Viral Load

Substances

  • HIV Protease Inhibitors
  • Oligopeptides
  • Pyridines
  • Atazanavir Sulfate
  • HIV Protease
  • Ritonavir