Gidari Anna, Sabbatini Samuele, Pallotto Carlo, Bastianelli Sabrina, Pierucci Sara, Busti Chiara, Schiaroli Elisabetta, Francisci Daniela
Department of Medicine and Surgery, Clinic of Infectious Diseases, "Santa Maria della Misericordia" Hospital, University of Perugia, 06123 Perugia, Italy.
Department of Medicine and Surgery, Medical Microbiology Section, University of Perugia, 06123 Perugia, Italy.
Microorganisms. 2022 Dec 14;10(12):2471. doi: 10.3390/microorganisms10122471.
After almost three years of the pandemic, Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) is still spreading around the world, causing notable sanitary and social issues. New antiviral therapies are constantly under investigation. However, few options have been approved for the treatment of COVID-19. Clinical trials are currently ongoing to evaluate the efficacy of nelfinavir on mild−moderate COVID-19. This study aims to investigate the activity of this compound on SARS-CoV-2 “Variants of Concern” (VOCs), comparing its effectiveness with the approved drugs remdesivir and molnupiravir. The experiments were conducted in a biosafety level 3 facility. In this study, we used a Vero-E6-cell-based infection assay to investigate the in vitro activity of nelfinavir, molnupiravir, and remdesivir. Four strains of SARS-CoV-2 were tested: 20A.EU1, B.1.1.7, P.1, and B.1.617.2. All compounds reached micromolar/submicromolar EC50, EC90, and EC99. Furthermore, the Cmax/EC50 and Cmax/EC90 ratios were >1 for all compounds and all variants tested. Our study demonstrated that nelfinavir, as molnupiravir, and remdesivir are effective in vitro on SARS-CoV-2 variants.
在经历了近三年的疫情之后，严重急性呼吸综合征冠状病毒2（SARS-CoV-2）仍在全球传播，引发了显著的卫生和社会问题。新的抗病毒疗法一直在研究中。然而，用于治疗新冠肺炎的获批药物很少。目前正在进行临床试验以评估奈非那韦对轻至中度新冠肺炎的疗效。本研究旨在调查该化合物对SARS-CoV-2“关注变体”（VOCs）的活性，并将其有效性与获批药物瑞德西韦和莫努匹韦进行比较。实验在生物安全3级设施中进行。在本研究中，我们使用基于Vero-E6细胞的感染试验来研究奈非那韦、莫努匹韦和瑞德西韦的体外活性。测试了四种SARS-CoV-2毒株：20A.EU1、B.1.1.7、P.1和B.1.617.2。所有化合物的半数有效浓度（EC50）、90%有效浓度（EC90）和99%有效浓度（EC99）均达到微摩尔/亚微摩尔水平。此外，所有测试化合物和变体的最大血药浓度（Cmax）与EC50和Cmax与EC90的比值均>1。我们的研究表明，奈非那韦与莫努匹韦和瑞德西韦一样，在体外对SARS-CoV-2变体有效。
