Modulation of K65R selection by zidovudine inclusion: analysis of HIV resistance selection in subjects with virologic failure receiving once-daily abacavir/lamivudine/zidovudine and tenofovir DF (study COL40263)

AIDS Res Hum Retroviruses. 2009 Jul;25(7):665-72. doi: 10.1089/aid.2008.0302.

Abstract

COL40263 was a pilot 48-week, open-label, multicenter study evaluating the efficacy and safety of once-daily coformulated abacavir/lamivudine/zidovudine plus tenofovir in ART-naive, HIV-infected subjects. We examined the patterns of resistance that were selected on-therapy through 48 weeks in subjects with virologic nonresponse (VF). A total of 123 antiretroviral-naive HIV-1-infected subjects with plasma HIV-1 RNA > or = 30,000copies/ml were enrolled. For subjects with confirmed VF (HIV-1 RNA > or = 400 copies/ml at week 24 or later), HIV population genotypic and phenotypic analysis was performed. Of the 123 enrolled subjects, 14 (11%) had confirmed plasma HIV-1 RNA > or = 400 copies/ml through week 48. Of these subjects, 3/14 had evidence of drug resistance at baseline: 2/14 had HIV with K103N, Y188F/H/L/Y, and/or T215A and 1/14 had reduced zidovudine susceptibility. At the last time point analyzed, 4/14 subjects had wild-type HIV, while 10/14 subjects had HIV with either thymidine analogue mutations (TAMS) alone (3/10), TAMS + M184V (4/10), M184V only (1/10), or K65R/K (2/10). Matched phenotype was obtained for 13/14 subjects and 8/13 (62%) subjects had reduced susceptibility to one or more study drugs: 2/13 tenofovir, 3/13 abacavir, 4/13 zidovudine, and 7/13 lamivudine. The resistance pattern in COL40263 subjects with VF differs significantly from that reported for tenofovir-containing triple-nucleoside regimens. TAMs were detected in the majority (7/10) of samples from subjects with VF who selected any resistance mutation. These data suggest that TAMs selection is a preferred resistance route of this combination, with zidovudine modulating the resistance pathway against selection for K65R.

Publication types

  • Clinical Trial
  • Multicenter Study

MeSH terms

  • Adenine / administration & dosage
  • Adenine / analogs & derivatives*
  • Adult
  • Amino Acid Substitution
  • Anti-HIV Agents / administration & dosage*
  • Dideoxynucleosides / administration & dosage*
  • Drug Administration Schedule
  • Drug Resistance, Multiple, Viral / genetics*
  • Female
  • HIV Infections / blood
  • HIV Infections / drug therapy*
  • HIV-1* / drug effects
  • HIV-1* / genetics
  • Humans
  • Lamivudine / administration & dosage*
  • Male
  • Middle Aged
  • Organophosphonates / administration & dosage*
  • Pilot Projects
  • RNA, Viral / blood
  • RNA, Viral / drug effects
  • RNA, Viral / genetics
  • Tenofovir
  • Treatment Failure
  • Zidovudine / administration & dosage*

Substances

  • Anti-HIV Agents
  • Dideoxynucleosides
  • Organophosphonates
  • RNA, Viral
  • Lamivudine
  • Zidovudine
  • Tenofovir
  • Adenine
  • abacavir