Tipranavir-ritonavir genotypic resistance score in protease inhibitor-experienced patients

Antimicrob Agents Chemother. 2008 Sep;52(9):3237-43. doi: 10.1128/AAC.00133-08. Epub 2008 Jul 14.

Abstract

To identify mutations associated with the virological response (VR) to a tipranavir-ritonavir (TPV/r)-based regimen, 143 patients previously treated with protease inhibitor (PI) were studied. VR was defined by a decrease of at least 1 log(10) in, or undetectable, human immunodeficiency virus (HIV) RNA at month 3. The effect of each mutation in the protease, considering all variants at a residue as a single variable, on the VR to TPV/r was investigated. Mutations at six residues were associated with a lower VR (E35D/G/K/N, M36I/L/V, Q58E, Q61D/E/G/H/N/R, H69I/K/N/Q/R/Y, and L89I/M/R/T/V), and one mutation was associated with a higher VR (F53L/W/Y). The genotypic score M36I/L/V-53L/W/Y + Q58E + H69I/K/N/Q/R/Y + L89I/M/R/T/V was selected as providing a strong association with VR. For the seven patients with a genotypic score of -1 (viruses with only mutation at codon 53), the percentage of responders was 100% and the percentages were 79%, 56%, 33%, 21%, and 0% for those with scores of 0, 1, 2, 3, and 4, respectively. The percentage of patients showing a response to TPV/r was lower for patients infected with non-clade B viruses (n = 16, all non-B subtypes considered together) than for those infected with clade B viruses (n = 127) (25% and 59%, respectively; P = 0.015). Most mutations associated with VR to TPV/r had not previously been associated with PI resistance. This is consistent with phenotypic analysis showing that TPV has a unique resistance profile. Mutations at five positions (35, 36, 61, 69, and 89) were observed significantly more frequently in patients infected with a non-B subtype than in those infected with the B subtype, probably explaining the lower VR observed in these patients.

MeSH terms

  • Anti-HIV Agents / therapeutic use
  • Drug Resistance, Viral / genetics*
  • Drug Therapy, Combination
  • Female
  • Genotype
  • HIV Infections / drug therapy*
  • HIV Infections / virology
  • HIV Protease / drug effects
  • HIV Protease / genetics*
  • HIV Protease Inhibitors / pharmacology*
  • HIV Protease Inhibitors / therapeutic use
  • HIV-1 / classification
  • HIV-1 / drug effects*
  • HIV-1 / enzymology
  • HIV-1 / genetics
  • Humans
  • Male
  • Mutation
  • Pyridines / pharmacology*
  • Pyrones / pharmacology*
  • Reverse Transcriptase Inhibitors / therapeutic use
  • Ritonavir / pharmacology*
  • Sulfonamides

Substances

  • Anti-HIV Agents
  • HIV Protease Inhibitors
  • Pyridines
  • Pyrones
  • Reverse Transcriptase Inhibitors
  • Sulfonamides
  • HIV Protease
  • Ritonavir
  • tipranavir