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Remdesivir: Review of Pharmacology, Pre-clinical Data, and Emerging Clinical Experience for COVID-19.
Pharmacotherapy ( IF 4.1 ) Pub Date : 2020-05-23 , DOI: 10.1002/phar.2429
Sarah C J Jorgensen 1 , Razieh Kebriaei 2 , Linda D Dresser 3, 4
Affiliation  

The global pandemic of novel coronavirus disease 2019 (COVID‐19) caused by severe acute respiratory syndrome coronavirus 2 (SARS‐CoV‐2) has created an urgent need for effective antivirals. Remdesivir (formerly GS‐5734) is a nucleoside analogue pro‐drug currently being evaluated in COVID‐19 clinical trials. Its unique structural features allow high concentrations of the active triphosphate metabolite to be delivered intracellularly and it evades proofreading to successfully inhibit viral RNA synthesis. In pre‐clinical models, remdesivir has demonstrated potent antiviral activity against diverse human and zoonotic β‐coronaviruses, including SARS‐CoV‐2. In this article, we critically review available data on remdesivir with an emphasis on biochemistry, pharmacology, pharmacokinetics, and in vitro activity against coronaviruses as well as clinical experience and current progress in COVID‐19 clinical trials.

中文翻译:

瑞德西韦:对 COVID-19 的药理学、临床前数据和新兴临床经验的回顾。

由严重急性呼吸综合征冠状病毒 2 (SARS-CoV-2) 引起的 2019 年新型冠状病毒病 (COVID-19) 在全球大流行,迫切需要有效的抗病毒药物。Remdesivir(以前称为 GS-5734)是一种核苷类似物前药,目前正在 COVID-19 临床试验中进行评估。其独特的结构特征允许高浓度的活性三磷酸代谢物在细胞内传递,并且它可以逃避校对,成功抑制病毒RNA合成。在临床前模型中,瑞德西韦已证明对多种人类和人畜共患 β-冠状病毒(包括 SARS-CoV-2)具有有效的抗病毒活性。在本文中,我们批判性地回顾了瑞德西韦的现有数据,重点是生物化学、药理学、药代动力学和针对冠状病毒的体外活性,以及​​ COVID-19 临床试验的临床经验和当前进展。
更新日期:2020-07-20
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