Cross-resistance among nonnucleoside reverse transcriptase inhibitors limits recycling efavirenz after nevirapine failure

AIDS Res Hum Retroviruses. 2002 Aug 10;18(12):835-8. doi: 10.1089/08892220260190308.

Abstract

Heterogeneity in genotype mutations associated with resistance of HIV to nonnucleoside reverse transcriptase inhibitors (NNRTIs) should allow identification of patients failing nevirapine (NVP) who might benefit from efavirenz (EFV)-containing salvage regimens. To establish the feasibility of recycling EFV after failure of NVP-containing regimens genotypic data on 103 NVP-failed patients were analyzed to evaluate the prevalence of EFV resistance-conferring mutations. A clinically significant resistance to EFV was found in 50 of 103 (58%) of NVP-failed subjects. Furthermore, the 3-month virological response to salvage regimens containing EFV was assessed in patients previously treated with NVP and carrying single mutations conferring resistance to this drug. A proportion of HIV RNA less than 500 copies/ml at 3 months was obtained only in 2 of 12 (17%) of EFV-treated subjects compared with 35 of 67 (52%) of those without NNRTI mutations (OR, 0.18; 95% CI, 0.03-0.79). The median HIV-1 RNA decrease after 3 months was -0.63 log(10) among patients carrying single NNRTI-associated mutations compared with -1.32 log(10) among those without any NNRTI mutations. No virological response was observed in six patients harboring a single Y181C/I mutation. On the basis of the present data, sequential use of NNRTIs should be avoided in the management of treatment failure.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkynes
  • Benzoxazines
  • Cyclopropanes
  • Drug Resistance, Microbial / genetics
  • HIV Infections / drug therapy*
  • HIV-1 / genetics
  • HIV-1 / isolation & purification
  • Humans
  • Mutation
  • Nevirapine / administration & dosage
  • Nevirapine / therapeutic use*
  • Oxazines / administration & dosage
  • Oxazines / therapeutic use*
  • RNA, Viral / blood
  • Reverse Transcriptase Inhibitors / administration & dosage
  • Reverse Transcriptase Inhibitors / therapeutic use*

Substances

  • Alkynes
  • Benzoxazines
  • Cyclopropanes
  • Oxazines
  • RNA, Viral
  • Reverse Transcriptase Inhibitors
  • Nevirapine
  • efavirenz