达芦那韦对 SARS-CoV-2 无抗病毒活性。
Lack of antiviral activity of darunavir against SARS-CoV-2.
机构信息
Janssen Pharmaceutica NV, Beerse, Belgium.
Institute of Medical Virology, University Hospital Frankfurt, Goethe University, Frankfurt am Main, Germany.
出版信息
Int J Infect Dis. 2020 Aug;97:7-10. doi: 10.1016/j.ijid.2020.05.085. Epub 2020 May 29.
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 (EC > 100 μM). Remdesivir, used as a positive control, demonstrated potent antiviral activity (EC = 0.38 μM).
CONCLUSIONS
Overall, the data do not support the use of DRV for the treatment of COVID-19.
目的
鉴于对治疗 COVID-19（由严重急性呼吸系统综合征相关冠状病毒-2 [SARS-CoV-2] 引起的疾病）的高度需求和缺乏特定抗病毒药物，人类免疫缺陷病毒（HIV）蛋白酶抑制剂正被考虑作为治疗的替代药物。
方法
Prezcobix/Rezolsta 是一种固定剂量组合，包含 800 毫克 HIV 蛋白酶抑制剂达芦那韦（DRV）和 150 毫克考比司他，一种 CYP3A4 抑制剂，与其他抗逆转录病毒药物联合用于治疗 HIV 感染。目前尚无关于 DRV/cobicistat 治疗 COVID-19 的安全性和疗效的明确数据。评估了达芦那韦对来自 SARS-CoV-2 感染患者的临床分离株的体外抗病毒活性。
结果
在临床相关浓度（EC > 100 μM）下，DRV 对 SARS-CoV-2 没有抗病毒活性。瑞德西韦作为阳性对照，显示出强大的抗病毒活性（EC = 0.38 μM）。
结论
总体而言，数据不支持使用 DRV 治疗 COVID-19。
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