Lack of antiviral activity of darunavir against SARS-CoV-2
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. M...
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| Format: | Article |
| Language: | English |
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Elsevier
2020-08-01
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| Series: | International Journal of Infectious Diseases |
| Subjects: | |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S1201971220303921 |
| _version_ | 1828836191544279040 |
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| author | Sandra De Meyer Denisa Bojkova Jindrich Cinatl Ellen Van Damme Christophe Buyck Marnix Van Loock Brian Woodfall Sandra Ciesek |
| author_facet | Sandra De Meyer Denisa Bojkova Jindrich Cinatl Ellen Van Damme Christophe Buyck Marnix Van Loock Brian Woodfall Sandra Ciesek |
| author_sort | Sandra De Meyer |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-12-12T18:17:31Z |
| format | Article |
| id | doaj.art-90d3b12b6ba74d96bc31c99b569501e3 |
| institution | Directory Open Access Journal |
| issn | 1201-9712 |
| language | English |
| last_indexed | 2024-12-12T18:17:31Z |
| publishDate | 2020-08-01 |
| publisher | Elsevier |
| record_format | Article |
| series | International Journal of Infectious Diseases |
| spelling | doaj.art-90d3b12b6ba74d96bc31c99b569501e32022-12-22T00:16:14ZengElsevierInternational Journal of Infectious Diseases1201-97122020-08-0197710Lack of antiviral activity of darunavir against SARS-CoV-2Sandra De Meyer0Denisa Bojkova1Jindrich Cinatl2Ellen Van Damme3Christophe Buyck4Marnix Van Loock5Brian Woodfall6Sandra Ciesek7Janssen Pharmaceutica NV, Beerse, Belgium; Corresponding author at: Turnhoutseweg 30, 2340 Beerse, Belgium.Institute of Medical Virology, University Hospital Frankfurt, Goethe University, Frankfurt am Main, GermanyInstitute of Medical Virology, University Hospital Frankfurt, Goethe University, Frankfurt am Main, GermanyJanssen Pharmaceutica NV, Beerse, BelgiumJanssen Pharmaceutica NV, Beerse, BelgiumJanssen Pharmaceutica NV, Beerse, BelgiumJanssen Biopharma Inc, South San Francisco, CA, USAInstitute of Medical Virology, University Hospital Frankfurt, Goethe University, Frankfurt am Main, Germany; German Center for Infection Research (DZIF), Frankfurt, GermanyObjectives: 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.http://www.sciencedirect.com/science/article/pii/S1201971220303921DarunavirSARS-CoV-2COVID-19In vitro |
| spellingShingle | Sandra De Meyer Denisa Bojkova Jindrich Cinatl Ellen Van Damme Christophe Buyck Marnix Van Loock Brian Woodfall Sandra Ciesek Lack of antiviral activity of darunavir against SARS-CoV-2 International Journal of Infectious Diseases Darunavir SARS-CoV-2 COVID-19 In vitro |
| title | Lack of antiviral activity of darunavir against SARS-CoV-2 |
| title_full | Lack of antiviral activity of darunavir against SARS-CoV-2 |
| title_fullStr | Lack of antiviral activity of darunavir against SARS-CoV-2 |
| title_full_unstemmed | Lack of antiviral activity of darunavir against SARS-CoV-2 |
| title_short | Lack of antiviral activity of darunavir against SARS-CoV-2 |
| title_sort | lack of antiviral activity of darunavir against sars cov 2 |
| topic | Darunavir SARS-CoV-2 COVID-19 In vitro |
| url | http://www.sciencedirect.com/science/article/pii/S1201971220303921 |
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