雷得唑来(Radezolid) - 药物靶点：23S rRNA x 50S subunit_在研适应症：耐甲氧西林金黄色葡萄球菌感染，耐万古霉素肠球菌感染_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Radezolid (USAN/INN)、Radezolid Hydrochloride

+ [7]

靶点

23S rRNA x 50S subunit

作用机制

23S rRNA modulators(23S Ribosomal RNA modulators)、50S subunit抑制剂(50S核糖体亚基抑制剂)

治疗领域

感染

在研适应症

耐甲氧西林金黄色葡萄球菌感染耐万古霉素肠球菌感染

非在研适应症

脓肿社区获得性肺炎复杂皮肤和皮肤结构感染+ [2]

原研机构

Melinta Therapeutics, Inc.

在研机构

Melinta Subsidiary Corp.

非在研机构

Melinta Therapeutics, Inc.

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-

登录后查看时间轴

结构/序列

分子式C22H23FN6O3

InChIKeyBTTNOGHPGJANSW-IBGZPJMESA-N

CAS号869884-78-6

关联

2

项与雷得唑来相关的临床试验

NCT00646958

/ Completed临床2期

A Phase 2, Multicenter, Randomized, Open-Label, Comparative Study to Evaluate the Safety and Efficacy of RX-1741 Versus Linezolid in the Outpatient Treatment of Adult Patients With Uncomplicated Skin and Skin Structure Infection

The purpose of this study is to assess the efficacy, safety and tolerability of RX-1741, an oxazolidinone, versus linezolid, another oxazolidinone, in the treatment of uncomplicated skin and skin structure infections

开始日期2007-12-01

申办/合作机构

Melinta Therapeutics, Inc.

NCT00640926

/ Completed临床2期

A Phase 2, Multicenter, Randomized, Double-Blind Study to Evaluate the Safety and Efficacy of RX-1741 in the Treatment of Adult Patients With Mild to Moderate Severity of Community-Acquired Pneumonia (CAP)

The purpose of this study is to determine whether RX-1741, an oxazolidinone antibiotic, is safe and effective in the treatment of mild to moderate community acquired pneumonia (CAP).

开始日期2007-10-01

申办/合作机构

Melinta Therapeutics, Inc.

100 项与雷得唑来相关的临床结果

登录后查看更多信息

100 项与雷得唑来相关的转化医学

登录后查看更多信息

100 项与雷得唑来相关的专利（医药）

登录后查看更多信息

36

项与雷得唑来相关的文献（医药）

2024-11-16·Critical Reviews in Analytical Chemistry

Analytical Methodologies for the Estimation of Oxazolidinone Antibiotics as Key Members of anti-MRSA Arsenal: A Decade in Review

Review

作者: Khafagy, El-Sayed ; El-Kimary, Eman I. ; Hegazy, Wael A. H. ; Allam, Ahmed N.

Gram-positive bacterial infections are among the most serious diseases related with high mortality rates and huge healthcare costs especially with the rise of antibiotic-resistant strains that limits treatment options. Thus, development of new antibiotics combating these multi-drug resistant bacteria is crucial. Oxazolidinone antibiotics are the only totally synthetic group of antibiotics that showed activity against multi-drug resistant Gram positive bacteria including MRSA because of their unique mechanism of action in targeting protein synthesis. This group include approved marketed members (tedizolid, linezolid and contezolid) or those under development (delpazlolid, radezolid and sutezolid). Due to the significant impact of this class, larger number of analytical methods were required to meet the needs of both clinical and industrial studies. Analyzing these drugs either alone or with other antimicrobial agents commonly used in ICU, in the presence of pharmaceutical or endogenous biological interferences, or in the presence of matrix impurities as metabolites and degradation products poses a big analytical challenge. This review highlights current analytical approaches published in the last decade (2012-2022) that dealt with the determination of these drugs in different matrices and discusses their advantages and disadvantages. Various techniques have been described for their determination including chromatographic, spectroscopic, capillary electrophoretic and electroanalytical methods. The review comprises six sections (one for each drug) with their related tables that depict critical figures of merit and some experimental conditions for the reviewed methods. Furthermore, future perspectives about the analytical methodologies that can be developed in the near future for determination of these drugs are suggested.

2023-01-01·Frontiers in microbiology

Antibacterial and anti-biofilm activity of radezolid against Staphylococcus aureus clinical isolates from China.

Article

作者: Deng, Qiwen ; Yu, Zhijian ; Wei, Ying ; Deng, Xiangbing ; Wang, Cong ; Wen, Zewen ; Cao, Xinyi ; Li, Guiqiu ; Xiong, Yanpeng ; Bao, Chai

Although the potent antibacterial ability of radezolid against Staphylococcus aureus has been widely reported worldwide, its antibacterial and anti-biofilm activity against the S. aureus clinical isolates from China remains elusive. In this study, the minimum inhibitory concentration (MIC) of radezolid was determined in S. aureus clinical isolates from China using the agar dilution method, and the relationship between radezolid susceptibility and ST distribution was also investigated. The anti-biofilm activity of radezolid against S. aureus was determined by a crystal violet assay and compared with that of linezolid and contezolid. The quantitative proteomics of S. aureus treated with radezolid was analyzed, and the genetic mutations in radezolid-induced resistant S. aureus were determined by whole-genome sequencing. The dynamic changes in transcriptional expression levels of several biofilm-related genes were analyzed by quantitative RT-PCR. Our data showed that radezolid MIC ranged from ≤0.125 to 0.5 mg/L, which was almost 1/4 × MIC of linezolid against S. aureus, indicating the greater antibacterial activity of radezolid than linezolid. The S. aureus clinical isolates with radezolid MICs of 0.5 mg/L were most widely distributed in ST239 of MRSA and ST7 of MSSA. Moreover, the more robust anti-biofilm activity of radezolid with subinhibitory concentrations (1/8 × MIC and 1/16 × MIC) was demonstrated against S. aureus when compared with that of contezolid and linezolid. Genetic mutations were found in glmS, 23S rRNA, and DUF1542 domain-containing protein in radezolid-induced resistant S. aureus selected by in vitro induction of drug exposure. Quantitative proteomic analysis of S. aureus indicated that the global expression of some biofilm-related and virulence-related proteins was downregulated. Quantitative RT-PCR further confirmed that the expressions of some downregulated biofilm-related proteins, including sdrD, carA, sraP, hlgC, sasG, spa, sspP, fnbA, and oatA, were decreased after 12 h and 24 h of exposure to radezolid. Conclusively, radezolid shows robust antibacterial and anti-biofilm activity against S. aureus clinical isolates from China when compared with contezolid and linezolid.

2022-12-01·European Journal of Medicinal Chemistry

1,2,3-Triazole-containing hybrids with potential antibacterial activity against ESKAPE pathogens

Review

作者: Wang, Jun ; Yan, Heng ; Liu, Bao-Shan ; Liu, Kai ; Shi, Yu-Min ; Deng, Cui

ESKAPE pathogens, as priority 1 and 2 pathogens, are prevalent infectious agents associated with high morbidity and mortality. ESKAPE can cause broad-spectrum diseases with increasing tendency of resistance acquisition to antibiotics and have enhanced the urge for the development of alternate therapeutics. 1,2,3-Triazole, a highly privileged moiety for the discovery of novel drugs, not only can act as a linker to tether different pharmacophores, but also can serve as a pharmacophore. Notably, several 1,2,3-triazole-containing hybrids which are exemplified by cefatrizine, radezolid and tazobactam have already approved as antibiotics to treat infections caused by various organisms including ESKAPE pathogens and their drug-resistant forms, revealing that 1,2,3-triazole-containing hybrids are useful prototypes for clinical deployment in the control of bacterial infections. The purpose of the present review article is to provide an emphasis on the current scenario (2018-2022) of 1,2,3-triazole-containing hybrids with potential antibacterial activity against ESKAPE pathogens to facilitate further rational design of more effective candidates.

100 项与雷得唑来相关的药物交易

登录后查看更多信息

外链

KEGG	Wiki	ATC	Drug Bank
D09369	雷得唑来	-	DB12339

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
耐甲氧西林金黄色葡萄球菌感染	临床前	美国	Melinta Subsidiary Corp.	2008-07-05
耐万古霉素肠球菌感染	临床前	美国	Melinta Subsidiary Corp.	2008-07-05
脓肿	药物发现	美国	Melinta Therapeutics, Inc.	2007-12-01
复杂皮肤和皮肤结构感染	药物发现	美国	Melinta Therapeutics, Inc.	2007-12-01
葡萄球菌皮肤感染	药物发现	美国	Melinta Therapeutics, Inc.	2007-12-01
链球菌感染	药物发现	美国	Melinta Therapeutics, Inc.	2007-12-01
社区获得性肺炎	药物发现	加拿大	Melinta Therapeutics, Inc.	2007-10-01
社区获得性肺炎	药物发现	美国	Melinta Therapeutics, Inc.	2007-10-01
社区获得性肺炎	药物发现	俄罗斯	Melinta Therapeutics, Inc.	2007-10-01

登录后查看更多信息

临床结果

适应症

分期

评价

查看全部结果

研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT00640926 (CTgov)	临床2期	社区获得性肺炎	158	Radezolid (Radezolid 300 mg PO Daily (QD))	獵衊窪憲簾選襯選獵醖(鹽構積膚夢鏇窪衊製餘) = 鏇繭壓鏇範鑰壓鹹築鏇範憲願淵鬱網艱鏇顧鏇 (廠鬱襯襯齋願範鏇鏇繭, 醖淵鹽餘築築積襯鬱艱 ~ 窪憲膚糧廠繭廠網鹹積) 更多	-	2010-02-04
				Radezolid (Radezolid 450 mg PO Daily (QD))	獵衊窪憲簾選襯選獵醖(鹽構積膚夢鏇窪衊製餘) = 廠醖衊蓋衊選襯積餘衊範憲願淵鬱網艱鏇顧鏇 (廠鬱襯襯齋願範鏇鏇繭, 製襯鑰鹽獵製鹽蓋製遞 ~ 積鏇淵鏇積選壓膚襯艱) 更多
NCT00646958 (CTgov)	临床2期	复杂皮肤和皮肤结构感染 \| 脓肿 \| 链球菌感染 \| 葡萄球菌皮肤感染	150	Radezolid (Radezolid QD)	網齋艱獵獵齋範繭鹽簾(窪顧蓋蓋製鬱蓋簾憲鑰) = 製網構夢窪淵衊願鹽鏇廠顧鑰獵壓觸醖鹹簾鬱 (醖遞製衊繭構淵糧鹹夢, 簾鑰窪蓋網艱醖蓋鬱鏇 ~ 夢窪觸鬱膚鏇鹽製遞醖) 更多	-	2009-06-26
				Radezolid (Radezolid BID)	網齋艱獵獵齋範繭鹽簾(窪顧蓋蓋製鬱蓋簾憲鑰) = 壓範繭齋廠憲淵糧網製廠顧鑰獵壓觸醖鹹簾鬱 (醖遞製衊繭構淵糧鹹夢, 獵觸襯蓋醖憲醖鑰築淵 ~ 顧憲襯壓鏇齋醖窪襯鑰) 更多