Lolamicin(Lolamicin) - 药物靶点：Lp(a)_在研适应症：革兰氏阴性菌感染_专利_临床

概要

基本信息

药物类型

激素

别名-

靶点

Lp(a)

作用机制

脂蛋白（a）抑制剂

治疗领域

感染

在研适应症

革兰氏阴性菌感染

非在研适应症-

原研机构

University of Illinois At UrbanaChampaign

在研机构

University of Illinois At UrbanaChampaign

非在研机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构

分子式C24H20N4O

InChIKeyCIXIQLLJOWEAKU-UHFFFAOYSA-N

CAS号2930690-12-1

关联

100 项与 Lolamicin 相关的临床结果

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100 项与 Lolamicin 相关的转化医学

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100 项与 Lolamicin 相关的专利（医药）

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1

项与 Lolamicin 相关的文献（医药）

2024-06-13·Nature

A Gram-negative-selective antibiotic that spares the gut microbiome

Article

作者: Muñoz, Kristen A ; Wen, Po-Chao ; Ulrich, Rebecca J ; Lee, Hyang Yeon ; Lau, Gee W ; Hung, Chien-Che ; Holmes, Jessica R ; Tajkhorshid, Emad ; Sinclair, Matt ; Hergenrother, Paul J ; Vasan, Archit K ; Fields, Christopher J

Infections caused by Gram-negative pathogens are increasingly prevalent and are typically treated with broad-spectrum antibiotics, resulting in disruption of the gut microbiome and susceptibility to secondary infections^1-3. There is a critical need for antibiotics that are selective both for Gram-negative bacteria over Gram-positive bacteria, as well as for pathogenic bacteria over commensal bacteria. Here we report the design and discovery of lolamicin, a Gram-negative-specific antibiotic targeting the lipoprotein transport system. Lolamicin has activity against a panel of more than 130 multidrug-resistant clinical isolates, shows efficacy in multiple mouse models of acute pneumonia and septicaemia infection, and spares the gut microbiome in mice, preventing secondary infection with Clostridioides difficile. The selective killing of pathogenic Gram-negative bacteria by lolamicin is a consequence of low sequence homology for the target in pathogenic bacteria versus commensals; this doubly selective strategy can be a blueprint for the development of other microbiome-sparing antibiotics.

100 项与 Lolamicin 相关的药物交易

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