Darunavir is a synthetic nonpeptidic inhibitor of protease and was developed to increase interaction with HIV-1 protease and to be more resistant against HIV-1 protease mutations. It was initially considered as a promising antiviral treatment for COVID-19. However, in two recent in vitro studies (De Meyer 2020, Touret 2020), darunavir showed low to no antiviral activity against SARS-CoV-2, the virus that caused COVID-19, at clinically relevant concentrations.
Johnson and Johnson released a position statement that did not support the use of darunavir in COVID-19.
Specifically, Janssen has no clinical nor pharmacological evidence to support the inclusion of DRV/cobicistat in treatment guidelines for COVID-19, nor are there published data on the safety and efficacy profile of DRV/cobicistat in treatment of COVID-19. There are no published clinical studies that have evaluated the efficacy and safety of DRV, DRV/cobicistat or DRV/cobicistat/emtricitabine/tenofovir alafenamide for the treatment of novel coronavirus. Many Janssen compounds, including darunavir, are in the process of being evaluated in-vitro for potential antiviral activity against SARS-CoV-2. The in-vitro antiviral activity of DRV against SARS-CoV-2 was assessed. DRV showed no activity against SARS-CoV-2 at clinically relevant concentrations (EC50 >100 μM). These data do not support the use of DRV for treatment of COVID-19. Results from a single center, open label, randomized, and controlled trial conducted at Shanghai Public Health Clinical Center (SPHCC) of darunavir and cobicistat (DRV/c) in treating laboratory-confirmed 30 COVID-19 patients showed that DRV/c was not effective. Additionally, structural analyses show very few interactions of DRV with the active site of the SARS-CoV-2 protease.
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