Doravirine: A new non-nucleoside reverse transcriptase inhibitor for the treatment of HIV infection

R. Talwani, Z. Temesgen

Research output: Contribution to journalArticle

1 Scopus citations

Abstract

Doravirine is a new non-nucleoside reverse transcriptase inhibitor (NNRTI) that was approved by the United States Food and Drug Administration (FDA) on August 30, 2018, for the treatment of HIV infection in adult patients. The product was also approved in the E.U. and Japan in November 2018 and January 2020, respectively. It is currently available as a single stand-alone tablet as well as part of a single-tablet regimen in a fixed-dose combination with tenofovir disoproxil and lamivudine. Similarly to other NNRTIs, doravirine exerts its antiviral effect through a noncompetitive inhibition of HIV-1 reverse transcriptase. It has a novel resistance pathway so that it retains in vitro activity against clinically relevant NNRTI viral mutations K103N, Y181C and G190A. In randomized clinical trials, doravirine was noninferior to efavirenz- and darunavir-based regimens, with fewer adverse events. Doravirine has a more favorable drug interaction profile compared with earlier NNRTIs as it neither inhibits nor induces the cytochrome P450 3A4 (CYP3A4) enzyme. Doravirine has been added to the category of Recommended Initial Regimens in Certain Clinical Situations in the United States Department of Health and Human Services Antiretroviral Guidelines for Adults and Adolescents.

Original languageEnglish (US)
Pages (from-to)113-124
Number of pages12
JournalDrugs of Today
Volume56
Issue number2
DOIs
StatePublished - Jan 1 2020

Keywords

  • AIDS/HIV
  • Anti-HIV agents
  • Antiretroviral therapies
  • Doravirine
  • HIV infection
  • MK-1439
  • Non-nucleoside reverse transcriptase inhibitors

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)

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