Lack of antiviral activity of darunavir against SARS-CoV-2

Int J Infect Dis. 2020 Aug:97:7-10. doi: 10.1016/j.ijid.2020.05.085. Epub 2020 May 29.

Abstract

Objectives: Given the high need and the absence of specific antivirals for treatment of COVID-19 (the disease caused by severe acute respiratory syndrome-associated coronavirus-2 [SARS-CoV-2]), human immunodeficiency virus (HIV) protease inhibitors are being considered as therapeutic alternatives.

Methods: Prezcobix/Rezolsta is a fixed-dose combination of 800 mg of the HIV protease inhibitor darunavir (DRV) and 150 mg cobicistat, a CYP3A4 inhibitor, which is indicated in combination with other antiretroviral agents for the treatment of HIV infection. There are currently no definitive data on the safety and efficacy of DRV/cobicistat for the treatment of COVID-19. The in vitro antiviral activity of darunavir against a clinical isolate from a patient infected with SARS-CoV-2 was assessed.

Results: DRV showed no antiviral activity against SARS-CoV-2 at clinically relevant concentrations (EC50 > 100 μM). Remdesivir, used as a positive control, demonstrated potent antiviral activity (EC50 = 0.38 μM).

Conclusions: Overall, the data do not support the use of DRV for the treatment of COVID-19.

Keywords: COVID-19; Darunavir; In vitro; SARS-CoV-2.

MeSH terms

  • Antiviral Agents / therapeutic use
  • Betacoronavirus / drug effects*
  • COVID-19
  • Cell Line
  • Cell Survival / drug effects
  • Coronavirus Infections* / drug therapy
  • Darunavir / therapeutic use*
  • Humans
  • Pandemics*
  • Pneumonia, Viral* / drug therapy
  • SARS-CoV-2

Substances

  • Antiviral Agents
  • Darunavir