Emerging mutations at virological failure of HAART combinations containing tenofovir and lamivudine or emtricitabine

AIDS. 2010 Apr 24;24(7):1013-8. doi: 10.1097/QAD.0b013e328336e962.

Abstract

Objective: To compare the emergence of drug-resistant HIV variants at failure of lamivudine (3TC)/tenofovir (TDF)-containing or emtricitabine (FTC)/TDF-containing HAART as a consequence of the different 3TC and FTC intracellular half-lives.

Design: Retrospective evaluation of 859 patients selected from an Italian HIV resistance database (Antiretroviral Resistance Cohort Analysis).

Methods: Patients were selected for analysis if treated with a HAART whose nucleoside/nucleotide reverse transcriptase inhibitor backbone was either 3TC/TDF or FTC/TDF; if they experienced a virological failure after at least 6 months of plasma HIV-RNA undetectability; and if HIV genotypes before treatment and at failure were available. Univariate and multivariate logistic regression analyses were done to detect predictors of resistance mutations emerging at failure.

Results: Of 714 patients failing with 3TC/TDF and 145 with FTC/TDF, 35.8 and 21.1% were in Centers for Disease Control and Prevention stage C, and 8.8 and 15.2% were on first-line HAART, respectively. At multivariate analysis, the emergence of K70R (P = 0.002), M184V (P = 0.031), T215F (P = 0.020) and Y181C (P = 0.005) was significantly more common in 3TC-treated than in FTC-treated patients, with an odds ratio of 4, 1.56, 1.89 and 3.84, respectively.

Conclusion: Despite their close structural similarity, 3TC and FTC are associated with a significantly different rate of drug resistance at treatment failure when combined with TDF in HAART regimens independently of the third drug used.

MeSH terms

  • Adenine / analogs & derivatives*
  • Adenine / therapeutic use
  • Adult
  • Analysis of Variance
  • Anti-HIV Agents / therapeutic use
  • Antiretroviral Therapy, Highly Active / methods*
  • Deoxycytidine / analogs & derivatives*
  • Deoxycytidine / therapeutic use
  • Drug Resistance, Viral / genetics*
  • Emtricitabine
  • Female
  • HIV Infections / drug therapy*
  • HIV Infections / genetics
  • HIV Infections / virology
  • HIV-1 / drug effects*
  • HIV-1 / genetics
  • Humans
  • Lamivudine / therapeutic use*
  • Male
  • Mutation / genetics
  • Organophosphonates / therapeutic use*
  • RNA, Viral / genetics
  • Retrospective Studies
  • Tenofovir
  • Treatment Failure
  • Viral Load

Substances

  • Anti-HIV Agents
  • Organophosphonates
  • RNA, Viral
  • Deoxycytidine
  • Lamivudine
  • Tenofovir
  • Emtricitabine
  • Adenine