Functional CYP2B6 variants and virologic response to an efavirenz-containing regimen in Port-au-Prince, Haiti

J Antimicrob Chemother. 2014 Aug;69(8):2187-90. doi: 10.1093/jac/dku088. Epub 2014 Apr 2.

Abstract

Objectives: Efavirenz is widely prescribed for HIV-1 infection. Three polymorphisms in CYP2B6 define plasma efavirenz trough concentration strata that vary across an ∼10-fold range. We characterized associations between human genetic polymorphisms and virologic response among participants who received efavirenz-containing regimens in a prospective clinical trial.

Methods: We genotyped 76 polymorphisms in CYP2B6 (including those that define efavirenz concentration strata), CYP2A6, CYP3A4, CYP3A5 and ABCB1 and week 48 virologic responses in 360 Haitians who initiated efavirenz-containing regimens in protocol HT 001. Associations were characterized by logistic regression analysis and Fisher's exact test.

Results: Proportions with HIV-1 RNA <50 or <200 copies/mL did not differ across 10 CYP2B6 metabolizer strata. In analyses that combined strata into three metabolizer levels (extensive, intermediate and slow), the respective proportions were 0.79, 0.79 and 0.81 (<50 copies/mL cut-off) and 0.84, 0.86 and 0.87 (<200 copies/mL cut-off). Genetic associations were not identified after controlling for baseline variables or with other polymorphisms after adjusting for multiple comparisons.

Conclusions: Virologic failures in HT 001 were not explained by genetic polymorphisms known to define the lowest plasma efavirenz concentration stratum.

Trial registration: ClinicalTrials.gov NCT00120510.

Keywords: AIDS; HIV; antiretroviral therapy; pharmacogenomics.

Publication types

  • Clinical Trial
  • Randomized Controlled Trial
  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • ATP Binding Cassette Transporter, Subfamily B / genetics
  • Adult
  • Alkynes
  • Anti-HIV Agents / therapeutic use
  • Benzoxazines / blood*
  • Benzoxazines / therapeutic use*
  • Cyclopropanes
  • Cytochrome P-450 CYP2A6 / genetics
  • Cytochrome P-450 CYP2B6 / genetics*
  • Cytochrome P-450 CYP2B6 Inducers / therapeutic use
  • Cytochrome P-450 CYP3A / genetics
  • Female
  • Genetic Association Studies
  • HIV Infections / drug therapy*
  • HIV-1 / drug effects*
  • Haiti
  • Humans
  • Male
  • Middle Aged
  • Polymorphism, Single Nucleotide
  • Prospective Studies
  • RNA, Viral / blood
  • Reverse Transcriptase Inhibitors / therapeutic use
  • Secondary Metabolism
  • Treatment Outcome

Substances

  • ABCB1 protein, human
  • ATP Binding Cassette Transporter, Subfamily B
  • Alkynes
  • Anti-HIV Agents
  • Benzoxazines
  • Cyclopropanes
  • Cytochrome P-450 CYP2B6 Inducers
  • RNA, Viral
  • Reverse Transcriptase Inhibitors
  • CYP2A6 protein, human
  • CYP3A5 protein, human
  • Cytochrome P-450 CYP2A6
  • Cytochrome P-450 CYP2B6
  • Cytochrome P-450 CYP3A
  • efavirenz

Associated data

  • ClinicalTrials.gov/NCT00120510