Remdesivir: Review of Pharmacology, Pre-clinical Data, and Emerging Clinical Experience for COVID-19

Pharmacotherapy. 2020 Jul;40(7):659-671. doi: 10.1002/phar.2429. Epub 2020 Jun 28.

Abstract

The global pandemic of novel coronavirus disease 2019 (COVID-19) caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has created an urgent need for effective antivirals. Remdesivir (formerly GS-5734) is a nucleoside analogue pro-drug currently being evaluated in COVID-19 clinical trials. Its unique structural features allow high concentrations of the active triphosphate metabolite to be delivered intracellularly and it evades proofreading to successfully inhibit viral RNA synthesis. In pre-clinical models, remdesivir has demonstrated potent antiviral activity against diverse human and zoonotic β-coronaviruses, including SARS-CoV-2. In this article, we critically review available data on remdesivir with an emphasis on biochemistry, pharmacology, pharmacokinetics, and in vitro activity against coronaviruses as well as clinical experience and current progress in COVID-19 clinical trials.

Keywords: COVID-19; GS-5734; Remdesivir; SARS-CoV-2; coronavirus; severe acute respiratory syndrome.

Publication types

  • Review

MeSH terms

  • Adenosine Monophosphate / administration & dosage
  • Adenosine Monophosphate / analogs & derivatives*
  • Adenosine Monophosphate / pharmacokinetics
  • Adenosine Monophosphate / pharmacology
  • Alanine / administration & dosage
  • Alanine / analogs & derivatives*
  • Alanine / pharmacokinetics
  • Alanine / pharmacology
  • Animals
  • Antiviral Agents / administration & dosage*
  • Antiviral Agents / pharmacokinetics
  • Antiviral Agents / pharmacology
  • Betacoronavirus / drug effects
  • Betacoronavirus / isolation & purification
  • COVID-19
  • Coronavirus Infections / drug therapy*
  • Coronavirus Infections / virology
  • Humans
  • Pandemics
  • Pneumonia, Viral / drug therapy*
  • Pneumonia, Viral / virology
  • SARS-CoV-2

Substances

  • Antiviral Agents
  • remdesivir
  • Adenosine Monophosphate
  • Alanine

Supplementary concepts

  • COVID-19 drug treatment