CUO246(CUO246) - 药物靶点：Bacterial DNA gyrase x Topoisomerase IV_在研适应症：新型冠状病毒感染，诊断试剂，精神分裂症_专利_临床

概要

基本信息

药物类型

小分子化药

别名-

靶点

Bacterial DNA gyrase x Topoisomerase IV

作用机制

细菌DNA旋转酶复合体调节剂、Topoisomerase IV modulators(拓扑异构酶 IV调节剂)

治疗领域

感染呼吸系统疾病其他疾病

在研适应症

新型冠状病毒感染诊断试剂精神分裂症

非在研适应症-

原研机构

Novartis AG

在研机构

陕西盘龙药业集团股份有限公司

UCSI UniversityInflamed Pharma GmbH

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-

关联

100 项与 CUO246 相关的临床结果

登录后查看更多信息

100 项与 CUO246 相关的转化医学

登录后查看更多信息

100 项与 CUO246 相关的专利（医药）

登录后查看更多信息

1

项与 CUO246 相关的文献（医药）

2022-12-20·Antimicrobial agents and chemotherapy

In Vitro and In Vivo Properties of CUO246, a Novel Bacterial DNA Gyrase/Topoisomerase IV Inhibitor.

Article

作者: Yue, Qin ; Leeds, Jennifer A ; Vo, Jason ; Morris, Laura ; Ma, Sylvia ; Skepper, Colin ; Thompson, Katherine ; Dean, Charles R ; Prosen, Katherine R ; Lapointe, Guillaume ; Blais, Johanne ; Richie, Daryl ; Moser, Heinz E ; Osborne, Colin S ; Rivkin, Alexey

CUO246, a novel DNA gyrase/topoisomerase IV inhibitor, is active in vitro against a broad range of Gram-positive, fastidious Gram-negative, and atypical bacterial pathogens and retains activity against quinolone-resistant strains in circulation. The frequency of selection for single step mutants of wild-type S. aureus with reduced susceptibility to CUO246 was <4.64 × 10^-9 at 4× and 8× MIC and remained low when using an isogenic QRDR mutant (<5.24 × 10^-9 at 4× and 8× MIC). Biochemical assays indicated that CUO246 had potent inhibitory activity against both DNA gyrase (GyrAB) and topoisomerase IV (ParCE). Furthermore, CUO246 showed rapid bactericidal activity in time-kill assays and potent in vivo efficacy against S. aureus in a neutropenic murine thigh infection model. These results suggest that CUO246 may be useful in treating infections by various causative agents of acute skin and skin structure infections, respiratory tract infections, and sexually transmitted infections.

100 项与 CUO246 相关的药物交易

登录后查看更多信息

研发状态

10 条进展最快的记录,

登录

后查看更多信息

适应症	最高研发状态	国家/地区	公司	日期
新型冠状病毒感染	临床前	-	陕西盘龙药业集团股份有限公司	2022-12-21
诊断试剂	临床前	-	Inflamed Pharma GmbH	2022-12-01
精神分裂症	临床前	-	UCSI University	2022-12-01