雷得唑来(Radezolid) - 药物靶点：23S rRNA x 50S subunit_在研适应症：脓肿分枝杆菌感染，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

+ [8]

靶点

23S rRNA x 50S subunit

作用方式

调节剂、抑制剂

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

脓肿分枝杆菌感染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

Gyeongsang National UniversityMelinta Subsidiary Corp.

非在研机构

Melinta Therapeutics, Inc.

权益机构-

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-

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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

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100 项与雷得唑来相关的转化医学

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100 项与雷得唑来相关的专利（医药）

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55

项与雷得唑来相关的文献（医药）

2025-04-01·Journal of Molecular Structure

Design, synthesis, and computational docking techniques of novel 1,2,3‒triazole‒tetrazole hybrids as potential leads in the development of anticancer agents

作者: Allaka, Tejeswara Rao ; Vudari, Balaraju ; Vellaiyan, Venkatesan ; Nagarajaiah, Honnappa ; Chepuri, Kalyani ; Bhoomandla, Srinu

New flurbiprofen linked 1,2,3-triazole and tetrazole scaffolds have been designed and synthesized using a Cu(I)-catalyzed azide-alkyne cycloaddition (CuAAC).All the synthesized compounds were examined for the growth inhibition of HepG2, HuH7, MCF-7, and T-47D tumor cells and binding with focusing on the human cytochrome P 450 2C9 active site was investigated using mol. modeling.There was a strong correlation between the data from the docking studies and the biol. screening results.The cell lines that responded to the novel compound′s effects the best were HepG2 and MCF-7.Compound 5j was the most efficacious derivative among the four cancer cells (HepG2, HuH7, MCF-7, and T-47D) having IC₅₀ values of 1.89 ± 0.103, 2.86 ± 0.167, 1.66 ± 0.056, and 3.55 ± 0.045 μM, resp. and it had greater activity than doxorubicin.In addition, an in silico docking anal. was carried out to confirm the results of the experimentThe results highlight the potential of our triazole-bridged tetrazoles when combined with flurbiprofen (PDB: 1R9O) to enter the active site of human cytochrome P 450 2C9.The proposed binding mode of ligand 5 g was shown three hydrogen bonding via tetrazole with Glu427 (N24...OE1), triazole with Ala280 (N17...O) and fluoro group with Arg80 (F28...NH2) residues their internuclear distances are 2.89 Å, 2.71 Å, and 3.19 Å resp.Furthermore, the ADMET profile was assessed for each mol., and the findings of the in vitro and in silico investigations indicate that the triazoles incorporating tetrazole provide important new information for the creation of innovative anti-cancer treatments.

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.

2023-12-31·Journal of Enzyme Inhibition and Medicinal Chemistry

Investigating the potential anticancer activities of antibiotics as topoisomerase II inhibitors and DNA intercalators: in vitro , molecular docking, molecular dynamics, and SAR studies

Article

作者: Al‐Karmalawy, Ahmed A. ; Farouk, Faten ; Abourehab, Mohammed A. S. ; Elmaaty, Ayman Abo ; Saleh, Mohamed A. ; Elkamhawy, Ahmed ; Alnajjar, Radwan ; Tawfik, Haytham O. ; Eldehna, Wagdy M.

Topoisomerase II (TOP-2) is a promising molecular target for cancer therapy. Numerous antibiotics could interact with biologically relevant macromolecules and provoke antitumor potential. Herein, molecular docking studies were used to investigate the binding interactions of 138 antibiotics against the human topoisomerase II-DNA complex. Followed by the MD simulations for 200 ns and MM-GBSA calculations. On the other hand, the antitumor activities of the most promising candidates were investigated against three cancer cell lines using doxorubicin (DOX) as a reference drug. Notably, spiramycin (SP) and clarithromycin (CL) showed promising anticancer potentials on the MCF-7 cell line. Moreover, azithromycin (AZ) and CL exhibited good anticancer potentials against the HCT-116 cell line. Finally, the TOP-2 enzyme inhibition assay was carried out to confirm the proposed rationale. Briefly, potent TOP-2 inhibitory potentials were recorded for erythromycin (ER) and roxithromycin (RO). Additionally, a SAR study opened eyes to promising anticancer pharmacophores encountered by these antibiotics.HighlightsMolecular docking studies of 139 antibiotics against the topoisomerase II-DNA complex.SP, RO, AZ, CL, and ER were the most promising and commercially available candidates.Molecular dynamics simulations for 200 ns for the most promising five complexes.MM-GBSA calculations for the frontier five complexes.SP and CL showed promising anticancer potentials on the MCF-7 cell line, besides, AZ and CL exhibited good anticancer potentials against the HCT-116 cell line.Potent TOP-2 inhibitory potentials were recorded for ER and RO.

100 项与雷得唑来相关的药物交易

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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,

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适应症	最高研发状态	国家/地区	公司	日期
脓肿分枝杆菌感染	临床前	韩国	Gyeongsang National University	2018-04-26
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	俄罗斯	Melinta Therapeutics, Inc.	2007-10-01
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

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临床结果

适应症

分期

评价

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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))	觸顧築鑰糧繭醖願繭壓(觸齋鏇餘繭鑰淵選憲齋) = 選壓襯蓋選鑰膚觸選衊範壓膚餘憲襯鹽齋鬱夢 (襯膚鏇膚鏇積遞膚簾壓, 構憲築鑰繭觸糧繭夢壓 ~ 壓製製艱觸窪衊蓋鬱衊) 更多	-	2010-02-04
				Radezolid (Radezolid 450 mg PO Daily (QD))	觸顧築鑰糧繭醖願繭壓(觸齋鏇餘繭鑰淵選憲齋) = 觸窪鏇簾範鏇鹹鹽衊壓範壓膚餘憲襯鹽齋鬱夢 (襯膚鏇膚鏇積遞膚簾壓, 網蓋築簾鹹簾鑰願鬱窪 ~ 夢襯窪鹽構蓋遞獵糧顧) 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)	繭糧廠齋鬱網艱構簾鹽(廠網遞醖觸襯醖憲夢積) = 鑰餘範衊衊觸壓廠範鹽顧餘壓蓋壓齋願壓廠選 (蓋壓鏇簾醖窪衊築餘構, 構糧糧範艱觸簾選壓鹹 ~ 淵願築簾淵鏇壓襯窪製) 更多	-	2009-06-26
				Radezolid (Radezolid BID)	繭糧廠齋鬱網艱構簾鹽(廠網遞醖觸襯醖憲夢積) = 糧繭窪鹹網網憲選窪積顧餘壓蓋壓齋願壓廠選 (蓋壓鏇簾醖窪衊築餘構, 膚糧鑰淵鹽壓壓夢膚糧 ~ 夢衊鬱鹽鑰願範齋遞鬱) 更多