[EDP-938, a new antiviral with inhibitory activity against the nucleoprotein of the respiratory syncytial virus].

IF 16.4 1区 化学 Q1 CHEMISTRY, MULTIDISCIPLINARY
J Reina, C Iglesias
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引用次数: 1

Abstract

The absence of an effective vaccine against respiratory syncytial virus (RSV) has led to the development of various drugs with the ability to inhibit or block its replicative activity. The first generation, called fusion inhibitors, bind to the protein on the viral surface and prevent the virus from binding and entering the cell. However, its low efficacy has determined the start of studies with second-generation compounds capable of binding or blocking the nucleoprotein (N); most of these compounds are analogs of 1,4-benzodiazepines. EDP-938 has shown high efficacy against RSV. The first trials in humans have shown that this antiviral is rapidly absorbed after oral administration and has a half-life of between 11-18 hours Administration for seven days of multiple oral doses of up to 600 mg/day or 300 mg/day/twice a day, there were hardly any significant adverse effects and the viral load in the lower respiratory tract decreased significantly.

Abstract Image

Abstract Image

[EDP-938,一种对呼吸道合胞病毒核蛋白具有抑制活性的新型抗病毒药物]。
由于缺乏针对呼吸道合胞病毒(RSV)的有效疫苗,因此开发了各种能够抑制或阻断其复制活性的药物。第一代称为融合抑制剂,与病毒表面的蛋白质结合,阻止病毒结合并进入细胞。然而,其低功效决定了能够结合或阻断核蛋白(N)的第二代化合物的研究开始;这些化合物大多是1,4-苯二氮卓类药物的类似物。EDP-938对RSV有较高的抗病毒效果。第一次人体试验表明,这种抗病毒药物在口服后被迅速吸收,半衰期在11-18小时之间。连续7天,多次口服剂量高达600毫克/天或300毫克/天/每天两次,几乎没有任何明显的不良反应,下呼吸道的病毒载量显著下降。
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来源期刊
Accounts of Chemical Research
Accounts of Chemical Research 化学-化学综合
CiteScore
31.40
自引率
1.10%
发文量
312
审稿时长
2 months
期刊介绍: Accounts of Chemical Research presents short, concise and critical articles offering easy-to-read overviews of basic research and applications in all areas of chemistry and biochemistry. These short reviews focus on research from the author’s own laboratory and are designed to teach the reader about a research project. In addition, Accounts of Chemical Research publishes commentaries that give an informed opinion on a current research problem. Special Issues online are devoted to a single topic of unusual activity and significance. Accounts of Chemical Research replaces the traditional article abstract with an article "Conspectus." These entries synopsize the research affording the reader a closer look at the content and significance of an article. Through this provision of a more detailed description of the article contents, the Conspectus enhances the article's discoverability by search engines and the exposure for the research.
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