Analysis of genotypic and phenotypic clinical cut-off levels for ritonavir-boosted saquinavir

HIV Med. 2006 Mar;7(2):67-74. doi: 10.1111/j.1468-1293.2006.00351.x.

Abstract

There is a need for new, clinically relevant interpretation algorithms for genotypic and phenotypic resistance for ritonavir-boosted saquinavir (SQV/r) at the current approved dosage [1000/100 mg twice a day (bid)]. Clinical cut-off levels, which correlate baseline measures of resistance with HIV RNA responses in large cohorts or clinical trials, are the ideal reference for developing such algorithms. Cut-off levels previously developed for unboosted saquinavir may no longer apply, as the plasma drug levels with SQV/r are significantly higher and may be able partially to overcome protease inhibitor-resistant HIV. Clinical cut-off levels for SQV/r, assessed in several cohort studies and clinical trials, also suggest that multiple genotypic mutations are required for complete loss of virological response. For phenotypic analysis of resistance, saquinavir cut-off levels 10-11-fold higher than the wild-type IC50 have best distinguished responders from non-responders in cohort studies. Using Virtual Phenotype, a 12.3-fold upper cut-off level was determined from analysis of large cohort databases. These genotypic and phenotypic algorithms need to be validated in larger prospective studies.

Publication types

  • Review

MeSH terms

  • Algorithms
  • Drug Resistance, Viral / genetics
  • Drug Therapy, Combination
  • Genotype
  • HIV Protease Inhibitors / pharmacology*
  • HIV-1 / drug effects*
  • HIV-1 / genetics
  • Humans
  • Mutation
  • Phenotype
  • Ritonavir / pharmacology*
  • Saquinavir / pharmacology*

Substances

  • HIV Protease Inhibitors
  • Saquinavir
  • Ritonavir