Rovafovir etalafenamide Nucleotide reverse transcriptase inhibitor Treatment of HIV-1 infection

M. Berg, Z. Temesgen

Research output: Contribution to journalArticlepeer-review

Abstract

Rovafovir, formerly GS-9131, is a novel nucleotide-analogue reverse transcriptase inhibitor in clinical development. It is a phosphonoamidate prodrug of GS-9148 and has demonstrated potent antiviral activity against viruses containing major mutations associated with resistance to nucleoside-analogue reverse transcriptase inhibitors, such as mK65R, L74V and M184V. In early preclinical studies, rovafovir showed a favorable toxicity, resistance and pharmacokinetic profile including potential for once-daily dosing; low potential for mitochondrial and renal toxicity; and low potential for drug–drug interactions. A phase II functional monotherapy clinical study evaluating the short-term safety and efficacy of rovafovir when added to a failing antiretroviral regimen is currently underway.

Original languageEnglish (US)
Pages (from-to)459-469
Number of pages11
JournalDrugs of the Future
Volume45
Issue number7
DOIs
StatePublished - Jul 2020

Keywords

  • GS-9131
  • HIV-1
  • NRTI resistance
  • Nucleotide reverse transcriptase inhibitor
  • Rovafovir

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)

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