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2015年末处于临床研发阶段的抗生素

Antibiotics in the clinical pipeline at the end of 2015.

作者信息

Butler Mark S, Blaskovich Mark At, Cooper Matthew A

机构信息

Institute for Molecular Bioscience, The University of Queensland, St Lucia, Brisbane, Australia.

出版信息

J Antibiot (Tokyo). 2017 Jan;70(1):3-24. doi: 10.1038/ja.2016.72. Epub 2016 Jun 29.

Abstract

There is growing global recognition that the continued emergence of multidrug-resistant bacteria poses a serious threat to human health. Action plans released by the World Health Organization and governments of the UK and USA in particular recognize that discovering new antibiotics, particularly those with new modes of action, is one essential element required to avert future catastrophic pandemics. This review lists the 30 antibiotics and two β-lactamase/β-lactam combinations first launched since 2000, and analyzes in depth seven new antibiotics and two new β-lactam/β-lactamase inhibitor combinations launched since 2013. The development status, mode of action, spectra of activity and genesis (natural product, natural product-derived, synthetic or protein/mammalian peptide) of the 37 compounds and six β-lactamase/β-lactam combinations being evaluated in clinical trials between 2013 and 2015 are discussed. Compounds discontinued from clinical development since 2013 and new antibacterial pharmacophores are also reviewed.

摘要

全球越来越认识到,多重耐药菌的不断出现对人类健康构成严重威胁。世界卫生组织以及英国和美国政府发布的行动计划尤其认识到,发现新的抗生素,特别是那些具有新作用方式的抗生素,是避免未来灾难性大流行所需的一个关键要素。本综述列出了自2000年以来首次推出的30种抗生素和两种β-内酰胺酶/β-内酰胺组合,并深入分析了自2013年以来推出的7种新抗生素和两种新的β-内酰胺/β-内酰胺酶抑制剂组合。讨论了2013年至2015年期间在临床试验中评估的37种化合物和6种β-内酰胺酶/β-内酰胺组合的开发状态、作用方式、活性谱和起源(天然产物、天然产物衍生、合成或蛋白质/哺乳动物肽)。还综述了自2013年以来停止临床开发的化合物和新的抗菌药效基团。

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