Implications of Efavirenz Pharmacogenetics When Switching From Efavirenz- to Dolutegravir-containing Antiretroviral Regimens

Clin Infect Dis. 2021 May 18;72(10):1820-1822. doi: 10.1093/cid/ciaa975.

Abstract

Many patients switch from efavirenz- to dolutegravir-based regimens. In a phase 1 dolutegravir-efavirenz interaction study, mean dolutegravir minimum concentration decreased by 60% and 85% among CYP2B6 normal and slow/intermediate metabolizers, respectively. Mean efavirenz half-life was 2.7 times greater in slow vs normal metabolizers. Slow metabolizers will experience more prolonged subtherapeutic dolutegravir concentrations.

Keywords: dolutegravir; efavirenz; pharmacogenetics.

Publication types

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

MeSH terms

  • Alkynes
  • Anti-HIV Agents* / therapeutic use
  • Benzoxazines / therapeutic use
  • Cyclopropanes / therapeutic use
  • Cytochrome P-450 CYP2B6 / genetics
  • HIV Infections* / drug therapy
  • Heterocyclic Compounds, 3-Ring
  • Humans
  • Oxazines
  • Pharmacogenetics
  • Piperazines
  • Pyridones

Substances

  • Alkynes
  • Anti-HIV Agents
  • Benzoxazines
  • Cyclopropanes
  • Heterocyclic Compounds, 3-Ring
  • Oxazines
  • Piperazines
  • Pyridones
  • dolutegravir
  • Cytochrome P-450 CYP2B6
  • efavirenz