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对瑞德西韦进行广泛的分析,以确定其广谱抗病毒活性和体外与其他药物相互作用的低潜力。

Expanded profiling of Remdesivir as a broad-spectrum antiviral and low potential for interaction with other medications in vitro.

机构信息

The Geneva Foundation, United States Army Medical Research Institute of Infectious Diseases (USAMRIID), Fort Detrick, Frederick, MD, USA.

Division of Antivirals, Office of Infectious Diseases, Center for Drug Evaluation and Research, Food and Drug Administration, Silver Spring, MD, USA.

出版信息

Sci Rep. 2023 Feb 23;13(1):3131. doi: 10.1038/s41598-023-29517-9.

Abstract

Remdesivir (GS-5734; VEKLURY) is a single diastereomer monophosphoramidate prodrug of an adenosine analog (GS-441524). Remdesivir is taken up by target cells and metabolized in multiple steps to form the active nucleoside triphosphate (GS-443902), which acts as a potent inhibitor of viral RNA-dependent RNA polymerases. Remdesivir and GS-441524 have antiviral activity against multiple RNA viruses. Here, we expand the evaluation of remdesivir's antiviral activity to members of the families Flaviviridae, Picornaviridae, Filoviridae, Orthomyxoviridae, and Hepadnaviridae. Using cell-based assays, we show that remdesivir can inhibit infection of flaviviruses (such as dengue 1-4, West Nile, yellow fever, Zika viruses), picornaviruses (such as enterovirus and rhinovirus), and filoviruses (such as various Ebola, Marburg, and Sudan virus isolates, including novel geographic isolates), but is ineffective or is significantly less effective against orthomyxoviruses (influenza A and B viruses), or hepadnaviruses B, D, and E. In addition, remdesivir shows no antagonistic effect when combined with favipiravir, another broadly acting antiviral nucleoside analog, and has minimal interaction with a panel of concomitant medications. Our data further support remdesivir as a broad-spectrum antiviral agent that has the potential to address multiple unmet medical needs, including those related to antiviral pandemic preparedness.

摘要

瑞德西韦(GS-5734;Veklury)是一种单非对映体单磷酰胺前药,是一种腺苷类似物(GS-441524)。瑞德西韦被靶细胞摄取,并通过多个步骤代谢为活性核苷三磷酸(GS-443902),后者作为一种有效的病毒 RNA 依赖性 RNA 聚合酶抑制剂。瑞德西韦和 GS-441524 对多种 RNA 病毒具有抗病毒活性。在这里,我们将瑞德西韦的抗病毒活性评估扩展到黄病毒科、小核糖核酸病毒科、丝状病毒科、正粘病毒科和嗜肝 DNA 病毒科的成员。我们通过细胞测定表明,瑞德西韦可以抑制黄病毒(如登革热 1-4 型、西尼罗河、黄热病、寨卡病毒)、小核糖核酸病毒(如肠道病毒和鼻病毒)和丝状病毒(如各种埃博拉、马尔堡和苏丹病毒分离株,包括新型地理分离株)的感染,但对正粘病毒(甲型和乙型流感病毒)或嗜肝 DNA 病毒 B、D 和 E 无效或效果明显降低。此外,瑞德西韦与另一种广泛作用的抗病毒核苷类似物法匹拉韦联合使用时没有拮抗作用,并且与一组伴随药物的相互作用最小。我们的数据进一步支持瑞德西韦作为一种广谱抗病毒药物,具有解决多种未满足的医疗需求的潜力,包括与抗病毒大流行防范相关的需求。

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