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瑞德西韦综述:一种有望用于治疗新冠肺炎的药物

A Review on Remdesivir: A Possible Promising Agent for the Treatment of COVID-19.

作者信息

Hashemian Seyed MohammadReza, Farhadi Tayebeh, Velayati Ali Akbar

机构信息

Clinical Tuberculosis and Epidemiology Research Center, National Research Institute of Tuberculosis and Lung Disease (NRITLD), Shahid Beheshti University of Medical Sciences, Tehran, Iran.

Chronic Respiratory Diseases Research Center (CRDRC), National Research Institute of Tuberculosis and Lung Diseases (NRITLD), Shahid Beheshti University of Medical Sciences, Tehran, Iran.

出版信息

Drug Des Devel Ther. 2020 Aug 6;14:3215-3222. doi: 10.2147/DDDT.S261154. eCollection 2020.

Abstract

The novel coronavirus 2019 (2019-nCoV), formally named severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), is a novel human infectious coronavirus. The disease caused by SARS-CoV-2 is named COVID-19. Development and manufacturing of specific therapeutics and vaccines to treat COVID-19 are time-consuming processes. At this time, using available conventional therapeutics along with other treatment options may be useful to fight COVID-19. In different clinical trials, efficacy of remdesivir (GS-5734) against Ebola virus has been demonstrated. Moreover, remdesivir may be an effective therapy in vitro and in animal models infected by SARS and MERS coronaviruses. Hence, the drug may be theoretically effective against SARS-CoV-2. Remdesivir is a phosphoramidate prodrug of an adenosine C-nucleoside. By entrance into respiratory epithelial cells in human, the prodrug is metabolized to a nucleoside triphosphate as the active form. The nucleoside analog inhibits the viral RNA-dependent RNA polymerase (RdRp) by competing with the usual counterpart adenosine triphosphate (ATP). The nucleoside analog is incorporated into the generating RNA strand and causes a delayed stop in the viral replication process. Knowledge about the potential efficacy of remdesivir against coronaviruses has been restricted to in vitro studies and animal models. However, information related to COVID-19 is rapidly growing. Several clinical trials are ongoing for the management of COVID-19 using remdesivir. In this study, characteristics of remdesivir and its usage for treatment of COVID-19 are reviewed based on an electronic search using PubMed and Google Scholar.

摘要

2019年新型冠状病毒(2019-nCoV),正式名称为严重急性呼吸综合征冠状病毒2(SARS-CoV-2),是一种新型人类感染性冠状病毒。由SARS-CoV-2引起的疾病名为COVID-19。开发和制造用于治疗COVID-19的特定疗法和疫苗是耗时的过程。此时,使用现有的传统疗法以及其他治疗选择可能有助于对抗COVID-19。在不同的临床试验中,已证明瑞德西韦(GS-5734)对埃博拉病毒有效。此外,瑞德西韦在体外以及感染SARS和MERS冠状病毒的动物模型中可能是一种有效的疗法。因此,该药物理论上可能对SARS-CoV-2有效。瑞德西韦是一种腺苷C-核苷的磷酸酰胺前药。通过进入人体呼吸道上皮细胞,前药代谢为活性形式的核苷三磷酸。核苷类似物通过与通常的对应物三磷酸腺苷(ATP)竞争来抑制病毒RNA依赖性RNA聚合酶(RdRp)。核苷类似物被掺入正在生成的RNA链中,并导致病毒复制过程延迟终止。关于瑞德西韦对冠状病毒潜在疗效的知识仅限于体外研究和动物模型。然而,与COVID-19相关的信息正在迅速增加。正在进行几项使用瑞德西韦治疗COVID-19的临床试验。在本研究中,基于使用PubMed和谷歌学术进行的电子检索,对瑞德西韦的特性及其用于治疗COVID-19的情况进行了综述。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ea18/7425093/4ab80db8e4a5/DDDT-14-3215-g0001.jpg

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