环孢素抑制剂阿利匹韦（Debio 025）抑制 SARS-CoV-2 感染。
Inhibition of SARS-CoV-2 Infection by the Cyclophilin Inhibitor Alisporivir (Debio 025).
机构信息
Research Team "Viruses, Hepatology, Cancer," Institut Mondor de Recherche Biomédicale, INSERM U955, Créteil, France.
Department of Virology, Hôpital Henri Mondor, Université Paris-Est, Créteil, France.
出版信息
Antimicrob Agents Chemother. 2020 Jun 23;64(7). doi: 10.1128/AAC.00876-20.
Cyclophilins play a key role in the life cycle of coronaviruses. Alisporivir (Debio 025) is a nonimmunosuppressive analogue of cyclosporine with potent cyclophilin inhibition properties. Alisporivir reduced SARS-CoV-2 RNA production in a dose-dependent manner in Vero E6 cells, with a 50% effective concentration (EC) of 0.46 ± 0.04 μM. Alisporivir inhibited a postentry step of the SARS-CoV-2 life cycle. These results justify rapidly conducting a proof-of-concept phase 2 trial with alisporivir in patients with SARS-CoV-2 infection.
亲环素在冠状病毒的生命周期中发挥着关键作用。阿利司匹韦（Debio 025）是一种非免疫抑制性环孢素类似物，具有很强的亲环素抑制特性。阿利司匹韦以剂量依赖的方式降低了 Vero E6 细胞中的 SARS-CoV-2 RNA 产生，其 50%有效浓度（EC）为 0.46±0.04 μM。阿利司匹韦抑制了 SARS-CoV-2 生命周期的进入后步骤。这些结果证明，在 SARS-CoV-2 感染患者中快速进行阿利司匹韦的概念验证阶段 2 试验是合理的。
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