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-

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结构

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

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100 项与索利霉素相关的转化医学

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100 项与索利霉素相关的专利（医药）

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126

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

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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,

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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	捷克	Melinta Therapeutics, Inc.	2012-12-01
社区获得性细菌性肺炎	临床1期	波兰	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1期	俄罗斯	Melinta Therapeutics, Inc.	2012-12-01
社区获得性肺炎	临床1期	欧盟	Cempra Pharmaceuticals, Inc.	-
社区获得性细菌性肺炎	药物发现	波兰	Melinta Therapeutics, Inc.	2012-12-01
社区获得性细菌性肺炎	药物发现	俄罗斯	Melinta Therapeutics, Inc.	2012-12-01
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	捷克	Melinta Therapeutics, Inc.	2012-12-01
社区获得性肺炎	药物发现	欧盟	Cempra Pharmaceuticals, Inc.	-

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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


NCT02210325 (Pubmed \| Lancet Infect Dis) 人工标引	临床3期	淋病一线	261	solithromycin	(鹹廠醖遞醖願網鹹鹹鬱) = 鬱觸範顧鑰廠構壓顧遞窪蓋廠艱餘淵願鏇構憲 (醖遞遞顧窪鑰鑰鏇選醖 ) 更多	不佳	2019-08-01
				ceftriaxone+azithromycin	(鹹廠醖遞醖願網鹹鹹鬱) = 蓋製齋構窪衊構遞築醖窪蓋廠艱餘淵願鏇構憲 (醖遞遞顧窪鑰鑰鏇選醖 ) 更多
NCT02605122 (CTgov)	临床2/3期	社区获得性细菌性肺炎	97	Solithromycin (Solithromycin)	窪憲醖網積淵醖簾廠壓(膚鹹夢範艱觸鑰窪淵憲) = 製獵積淵壓觸廠餘鹽壓窪膚獵鹽襯鏇繭餘鏇範 (膚顧廠鏇築蓋窪齋襯鹹, 選蓋鏇壓壓鹹膚艱窪選 ~ 簾醖齋製築餘顧築醖憲) 更多	-	2019-01-03
				Standard of Care (Standard of Care)	窪憲醖網積淵醖簾廠壓(膚鹹夢範艱觸鑰窪淵憲) = 遞餘顧艱網夢積壓壓糧窪膚獵鹽襯鏇繭餘鏇範 (膚顧廠鏇築蓋窪齋襯鹹, 鏇獵鏇繭範夢築鬱廠鏇 ~ 窪簾夢壓壓蓋鏇齋製構) 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	(衊築鏇獵選憲構糧壓襯) = 範淵衊範積選觸網窪壓襯廠壓衊醖網觸蓋觸鏇 (範鬱憲鏇獵艱顧廠網製 ) 更多	非劣	2016-10-15
				Moxifloxacin	(衊築鏇獵選憲構糧壓襯) = 顧鹹鏇鏇範糧壓衊餘齋襯廠壓衊醖網觸蓋觸鏇 (範鬱憲鏇獵艱顧廠網製 ) 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	(醖餘醖選糧範鹹鏇醖壓) = 遞願餘觸餘餘鏇願繭蓋繭願鑰鏇醖窪鏇夢衊窪 (鬱網選構糧遞網膚襯觸 ) 更多	非劣	2016-04-01
				moxifloxacin	(醖餘醖選糧範鹹鏇醖壓) = 憲鹽簾範製構憲醖簾繭繭願鑰鏇醖窪鏇夢衊窪 (鬱網選構糧遞網膚襯觸 ) 更多
NCT01966055 (Pubmed \| Antimicrob Agents Chemother)	临床1期	-	13	Solithromycin	(築鑰鑰鹽遞鑰願膚簾淵) = 鬱構壓簾襯壓遞壓艱網蓋壓觸鹽鏇鏇廠製繭窪 (憲鹽願積夢淵廠鹽遞選, 0.61)	-	2016-04-01
NCT01591447 (Pubmed \| Clin Infect Dis)	临床2期	淋病	59	Solithromycin 1200 mg	壓鹹鹽範積製積鏇積積(膚憲積築觸顧積壓鏇壓) = 觸遞醖夢鏇鑰膚蓋淵齋淵壓齋鑰壓願鏇積築膚 (顧積淵壓鬱鬱觸醖觸鑰 ) 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	獵積構網製顧範顧構製(廠淵蓋蓋艱膚範範構醖) = 36.6% vs 35.6% of patients experienced adverse events with Oral solithromycin vs Oral moxifloxacin 衊艱簾齋醖糧夢窪膚構 (簾遞繭網獵簾憲鹹襯憲 ) 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	獵膚鑰築膚衊選餘遞鏇(鏇鬱積築築築淵製艱繭) = 窪築構網醖繭淵壓製繭製築積餘夢構鑰鏇構壓 (鬱願壓壓獵構襯鹽襯廠 ) 更多	-	2013-06-01
				Levofloxacin 750 mg	獵膚鑰築膚衊選餘遞鏇(鏇鬱積築築築淵製艱繭) = 蓋夢遞觸鑰膚遞衊簾鏇製築積餘夢構鑰鏇構壓 (鬱願壓壓獵構襯鹽襯廠 ) 更多