索利霉素(Solithromycin) - 药物靶点：50S subunit_在研适应症：呼吸道感染_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Solithromycin (JAN/USAN)

+ [3]

靶点

50S subunit

作用机制

50S subunit抑制剂(50S核糖体亚基抑制剂)、蛋白质生物合成抑制剂

治疗领域

感染呼吸系统疾病

在研适应症

呼吸道感染

非在研适应症

气道病变社区获得性肺炎社区获得性细菌性肺炎+ [3]

原研机构

Cubist Pharmaceuticals LLC

在研机构

FUJIFILM Pharmaceuticals USA, Inc.

非在研机构

Melinta Therapeutics, Inc.Cempra Pharmaceuticals, Inc.

最高研发阶段临床3期

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C43H65FN6O10

InChIKeyIXXFZUPTQVDPPK-ZAWHAJPISA-N

CAS号760981-83-7

关联

36

项与索利霉素相关的临床试验

JPRN-JapicCTI-195002

/ Recruiting临床3期

A Phase 3, Multicenter, Randomized, Double-Blind Noninferiority Study of Oral Solithromycin Compared to Oral Azithromycin in the Treatment of Patients with Community-Acquired Pneumonia

开始日期2019-10-25

申办/合作机构

FUJIFILM Toyama Chemical Co., Ltd.

JPRN-JapicCTI-194685

/ Suspended临床1期

An Open-label, One-sequence Crossover Study of Solithromycin to Evaluate the Effects on the Pharmacokinetics of Rosuvastatin Calcium in Healthy Adult Subjects

开始日期2019-03-28

申办/合作机构

FUJIFILM Toyama Chemical Co., Ltd.

JPRN-JapicCTI-194686

/ Suspended临床1期

An Open-label, One-sequence Crossover Study of Solithromycin to Evaluate the Effects on the Pharmacokinetics of Metformin Hydrochloride in Healthy Adult Subjects

开始日期2019-03-28

申办/合作机构

FUJIFILM Toyama Chemical Co., Ltd.

100 项与索利霉素相关的临床结果

登录后查看更多信息

100 项与索利霉素相关的转化医学

登录后查看更多信息

100 项与索利霉素相关的专利（医药）

登录后查看更多信息

134

项与索利霉素相关的文献（医药）

2024-11-04·ChemBioChem

Engineering of a Malonyl‐CoA Ligase for Production of Fluorinated Polyketide Extender Units

Article

作者: Williams, Gavin J. ; Paulsel, Thaddeus Q.

AbstractEnzymatic platforms for producing malonyl‐CoA‐based extender units required for polyketide biosynthesis are often based on malonyl‐CoA ligases such as MatB from Rhizobium trifolii and Rhodopseudomonas palustris. However, despite broad interest in the fluorination of polyketides and prior success with engineering MatB homologs, the suitability of MatB for accessing the tertiary substituted fluoromethylmalonyl‐CoA needed to produce flurithromycin and solithromycin has not yet been reported. Herein, we report the structure‐guided engineering of a MatB homolog to optimize the production of fluoromethylmalonyl‐CoA, resulting in a variant with increased conversion and providing a platform to produce a suitable building block mixture for fluorinated macrolide production. Additionally, the mutant demonstrated broad utility for various substituted malonyl‐CoAs. The MatB mutant sets the stage to access fluorinated macrolides by coupling it with altered PKS machinery to install fluorinated malonyl‐CoA into macrolide scaffolds.

2024-07-31·Journal of Clinical and Translational Hepatology

Pipeline of New Drug Treatment for Non-alcoholic Fatty Liver Disease/Metabolic Dysfunction-associated Steatotic Liver Disease

Review

作者: Liu, Yu-Dong ; Hu, Ye ; Sun, Chao ; Chen, Ying ; Fan, Jian-Gao

Given the global prevalence and rising incidence of metabolic dysfunction-associated steatotic liver disease (MASLD), the absence of licensed medications is striking. A deeper understanding of the heterogeneous nature of MASLD has recently contributed to the discovery of novel groups of agents and the potential repurposing of currently available medications. MASLD therapies center on four major pathways. Considering the close relationship between MASLD and type 2 diabetes, the first approach involves antidiabetic medications, including incretins, thiazolidinedione insulin sensitizers, and sodium-glucose cotransporter 2 inhibitors. The second approach targets hepatic lipid accumulation and the resultant metabolic stress. Agents in this group include peroxisome proliferator-activated receptor agonists (e.g., pioglitazone, elafibranor, saroglitazar), bile acid-farnesoid X receptor axis regulators (obeticholic acid), de novo lipogenesis inhibitors (aramchol, NDI-010976), and fibroblast growth factor 21/19 analogs. The third approach focuses on targeting oxidative stress, inflammation, and fibrosis. Agents in this group include antioxidants (vitamin E), tumor necrosis factor α pathway regulators (emricasan, pentoxifylline, ZSP1601), and immune modulators (cenicriviroc, belapectin). The final group targets the gut (IMM-124e, solithromycin). Combination therapies targeting different pathogenetic pathways may provide an alternative to MASLD treatment with higher efficacy and fewer side effects. This review aimed to provide an update on these medications.

2024-06-01·Indian Journal of Microbiology

Solithromycin in Combination with Other Antimicrobial Agents Against the Carbapenem Resistant Klebsiella pneumoniae (CRKP)

Article

作者: Sharma, Shingini ; Samuel Raj, V. ; Sharma, Amit ; Rani, Kusum ; Tripathi, Shyam ; Sheba, Poornima

Klebsiella pneumoniae is considered as the most common pathogen of hospital-acquired pneumonia. K. pneumoniae has emerged as the superbug which had shown multidrug resistance (MDR) as well as extensively drug resistance. Carbapenem resistant K. pneumoniae (CRKP) has become a menace for the treatment with monotherapy of the patients mainly admitted in intensive care units. Hence, in the present study we collected total 187 sputum isolates of K. pneumoniae and performed the antimicrobial susceptibility testing by using the automated Vitek-2 system and broth micro-dilution method (67 CRKP). The combination study of solithromycin with meropenem, colistin, cefotaxime, piperacillin and tazobactam, nitrofurantoin, tetracycline, levofloxacin, curcumin and nalidixic acid was performed by using checkerboard assay. We observed the high rate of resistance towards ampicillin, cefotaxime, ceftriaxone, cefuroxime and aztreonam. The colistin and tigecycline were the most sensitive drugs. The CRKP were 36%, maximum were from the patients of ICUs. The best synergistic effect of solithromycin was with meropenem and cefotaxime (100%), colistin and tetracycline (80%). So, these combinations can be a choice of treatment for the infections caused by MDR CRKP and other Gram-negative bacteria where the monotherapy could not work.

1

项与索利霉素相关的新闻（医药）

2023-03-30

·drugs

Not Enough Antibiotics in Drug Development Pipeline, WHO Says

THURSDAY, March 30, 2023 -- Only 12 new antibiotics entered the market between 2017 and 2021, and too few currently are under development against critical pathogens, according to a World Health Organization presentation at the 33rd European Congress of Clinical Microbiology & Infectious Diseases, held from April 15 to 18 in Copenhagen, Denmark. Valeria Gigante, Ph.D., from the WHO Antimicrobial Resistance Division in Geneva, and colleagues updated the state of the antibiotic landscape. They reported that of the 12 antibiotics approved, only cefiderocol is able to target all the pathogens deemed critical by WHO. Of the 27 antibiotics currently under development, only solithromycin, which is used to treat community-acquired pneumonia and other infections, is awaiting market authorization and seven are in phase 3 trials. Only four of the 27 have new mechanisms of action, and most are not new drug classes. Only six of the 27 are considered innovative enough to overcome antibiotic resistance using WHO criteria, and only two of the six target highly drug-resistant forms of these microbes. "There is a major gap regarding products addressing multidrug resistant pathogens, such as Acinetobacter baumannii and Pseudomonas aeruginosa ," Gigante said in a statement. "Few new innovative antibiotics are expected in the coming years. We have no silver bullets." More Information Posted March 2023

临床3期合格传染病产品

100 项与索利霉素相关的药物交易

登录后查看更多信息

外链

KEGG	Wiki	ATC	Drug Bank
D09965	索利霉素	J01FA16	DB09308

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
社区获得性细菌性肺炎	临床1期	美国	Melinta Therapeutics, Inc.	2012-12-01
社区获得性细菌性肺炎	临床1期	多米尼加共和国	Melinta Therapeutics, Inc.	2012-12-01
社区获得性细菌性肺炎	临床1期	匈牙利	Melinta Therapeutics, Inc.	2012-12-01
社区获得性细菌性肺炎	临床1期	厄瓜多尔	Melinta Therapeutics, Inc.	2012-12-01
社区获得性细菌性肺炎	临床前	匈牙利	Melinta Therapeutics, Inc.	2012-12-01
社区获得性肺炎	临床前	欧盟	Cempra Pharmaceuticals, Inc.	-
社区获得性细菌性肺炎	药物发现	厄瓜多尔	Melinta Therapeutics, Inc.	2012-12-01
社区获得性细菌性肺炎	药物发现	多米尼加共和国	Melinta Therapeutics, Inc.	2012-12-01
社区获得性细菌性肺炎	药物发现	美国	Melinta Therapeutics, Inc.	2012-12-01
社区获得性肺炎	药物发现	欧盟	Cempra Pharmaceuticals, Inc.	-

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


NCT02210325 (Pubmed \| Lancet Infect Dis) 人工标引	临床3期	淋病一线	261	solithromycin	(築衊鬱鹹選獵夢範餘願) = 蓋醖齋廠製憲鹽憲鹹醖淵顧選鹹築構鬱構鹽繭 (鏇觸窪襯製願醖醖淵窪 ) 更多	不佳	2019-08-01
				ceftriaxone+azithromycin	(築衊鬱鹹選獵夢範餘願) = 網鏇簾範鬱鹹衊夢構築淵顧選鹹築構鬱構鹽繭 (鏇觸窪襯製願醖醖淵窪 ) 更多
NCT02605122 (CTgov)	临床2/3期	社区获得性细菌性肺炎	97	Solithromycin (Solithromycin)	(網願簾繭淵網鹽鬱鬱鹹) = 廠糧艱齋製蓋獵餘範憲憲醖膚鬱鏇獵鹹夢襯積 (遞鑰艱夢簾窪簾選築糧, 選遞蓋廠遞窪鑰淵膚衊 ~ 顧簾艱願糧醖選積鹹願) 更多	-	2019-01-03
				Standard of Care (Standard of Care)	(網願簾繭淵網鹽鬱鬱鹹) = 襯淵獵製鑰襯製願範鏇憲醖膚鬱鏇獵鹹夢襯積 (遞鑰艱夢簾窪簾選築糧, 願夢蓋廠願範構選壓憲 ~ 壓鑰範壓夢獵繭顧簾艱) 更多
NCT01968733 (SOLITAIRE-IV, Pubmed \| Clin Infect Dis) 人工标引	临床3期	社区获得性细菌性肺炎	863	Solithromycin	(構齋齋簾顧窪鏇積製簾) = 夢願蓋觸齋衊鹽選鬱蓋顧遞範選淵顧積齋膚範 (製壓繭窪夢範膚觸鏇醖 ) 更多	非劣	2016-10-15
				Moxifloxacin	(構齋齋簾顧窪鏇積製簾) = 膚鬱築艱積網鹽鹽簾窪顧遞範選淵顧積齋膚範 (製壓繭窪夢範膚觸鏇醖 ) 更多
NCT01756339 (SOLITAIRE-ORAL, Pubmed \| Lancet Infect Dis) 人工标引	临床3期	社区获得性细菌性肺炎	860	Placebo+solithromycin	(膚衊襯壓選衊網製廠製) = 膚選繭遞顧襯願選齋襯網鑰顧積觸淵齋製製願 (齋選壓膚餘蓋鹹獵廠膚 ) 更多	非劣	2016-04-01
				moxifloxacin	(膚衊襯壓選衊網製廠製) = 簾鏇鹽餘網網膚願鹽鏇網鑰顧積觸淵齋製製願 (齋選壓膚餘蓋鹹獵廠膚 ) 更多
NCT01966055 (Pubmed \| Antimicrob Agents Chemother)	临床1期	-	13	Solithromycin	(醖糧網獵廠積衊壓醖鑰) = 鬱憲憲壓鑰網醖觸壓齋築夢膚積鹹繭鹹顧願醖 (蓋艱鹽糧艱鹽艱鑰膚簾, 0.61)	-	2016-04-01
NCT01591447 (Pubmed \| Clin Infect Dis)	临床2期	淋病	59	Solithromycin 1200 mg	遞製夢襯衊觸選鏇鬱遞(蓋築夢蓋鹽壓襯窪構積) = 衊襯夢網積鹹顧顧餘鬱蓋鬱鏇糧簾鏇齋蓋窪範 (醖網構範夢醖壓鏇壓衊 ) 更多	积极	2015-10-01
ERS2015	临床3期	慢性阻塞性肺疾病 \| 哮喘 \| 社区获得性肺炎	860	Oral solithromycin	鬱壓憲遞鹽餘繭鬱構艱(構築網淵網製製積壓壓) = 36.6% vs 35.6% of patients experienced adverse events with Oral solithromycin vs Oral moxifloxacin 壓衊鹽網蓋遞網顧壓膚 (衊範選淵積網簾襯構蓋 ) 更多	-	2015-09-01
				Oral moxifloxacin
NCT01168713 (Pubmed \| Antimicrob Agents Chemother)	临床2期	社区获得性细菌性肺炎	132	Solithromycin 800 mg	淵衊網製醖選齋鹹蓋鏇(衊襯醖艱獵夢鬱積願廠) = 夢鏇製壓鹹願繭選選鑰簾鹹鹹積獵艱製鹹製遞 (選餘獵齋襯鏇壓觸鑰繭 ) 更多	-	2013-06-01
				Levofloxacin 750 mg	淵衊網製醖選齋鹹蓋鏇(衊襯醖艱獵夢鬱積願廠) = 糧夢鏇願範餘鹹壓繭窪簾鹹鹹積獵艱製鹹製遞 (選餘獵齋襯鏇壓觸鑰繭 ) 更多