Effect of patient genetics on etonogestrel pharmacokinetics when combined with efavirenz or nevirapine ART

J Antimicrob Chemother. 2019 Oct 1;74(10):3003-3010. doi: 10.1093/jac/dkz298.

Abstract

Background: We previously demonstrated that etonogestrel concentrations were 82% lower in women using etonogestrel contraceptive implants plus efavirenz-based ART compared with women not receiving ART.

Objectives: To investigate the genetic contribution to this previously observed drug-drug interaction through studying SNPs in genes known to be involved in efavirenz, nevirapine or etonogestrel metabolism in the same group of women.

Patients and methods: Here, we present a secondary analysis evaluating SNPs involved in efavirenz, nevirapine and etonogestrel metabolism and associated etonogestrel pharmacokinetics among 57 women, 19 not receiving ART (control group), 19 receiving efavirenz- (600 mg daily) based ART and 19 receiving nevirapine- (200 mg twice daily) based ART. Associations between patient genotype and etonogestrel pharmacokinetic parameters were determined through univariate and multivariate linear regression. This study was registered at clinicaltrials.gov (NCT02082652).

Results: Within the control group, CYP2B6 983 T>C was associated with 27% higher etonogestrel Cmax and 28% higher AUC0-24weeks. In the efavirenz group CYP2B6 516 G>T was associated with 43% lower etonogestrel Cmin and 34% lower AUC0-24weeks. For participants receiving nevirapine, NR1I2 63396 C>T was associated with 39% lower etonogestrel Cmin and 37% lower AUC0-24weeks.

Conclusions: This study demonstrates the influence of pharmacogenetics on the extent of drug-drug interactions between etonogestrel and efavirenz- or nevirapine-based ART. Efavirenz plus the etonogestrel contraceptive implant results in a detrimental drug-drug interaction irrespective of patient genetics, which is worsened in women possessing variant alleles for these CYP2B6 SNPs.

Publication types

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

MeSH terms

  • Adult
  • Alkynes
  • Anti-HIV Agents / therapeutic use*
  • Benzoxazines / therapeutic use*
  • Cyclopropanes
  • Cytochrome P-450 CYP2B6 / genetics
  • Desogestrel / pharmacokinetics*
  • Drug Interactions / genetics
  • Female
  • Genotype
  • HIV Infections / drug therapy
  • HIV Infections / genetics
  • Humans
  • Nevirapine / therapeutic use*
  • Polymorphism, Single Nucleotide / genetics
  • Young Adult

Substances

  • Alkynes
  • Anti-HIV Agents
  • Benzoxazines
  • Cyclopropanes
  • etonogestrel
  • Desogestrel
  • Nevirapine
  • Cytochrome P-450 CYP2B6
  • efavirenz

Associated data

  • ClinicalTrials.gov/NCT02082652