更新于：2024-06-23
Fiboflapon Sodium
更新于：2024-06-23
概要
基本信息
在研机构- |
最高研发阶段终止临床2期 |
首次获批日期- |
最高研发阶段(中国)- |
特殊审评- |
结构
分子式C38H43N3NaO4S |
InChIKeyHBTBYQNCMVSNPE-UHFFFAOYSA-N |
CAS号1196070-26-4 |
关联
17
项与 Fiboflapon Sodium 相关的临床试验A Randomised, Double-blind, Placebo-controlled, Cross-over Study to Evaluate the Effect of Treatment With Repeat Dose GSK2190915 as an add-on to Current Therapy on the Percentage of Neutrophils in Induced Sputum in Asthmatic Patients With Elevated Sputum Neutrophils
An Open Label, Sequential, Single Cohort, Repeat Dose Study to Investigate the Potential Interaction of GSK2190915 on the Pharmacokinetics of Rosuvastatin in Healthy Adult Subjects.
A Randomized, Double-Blind, Double-Dummy, Placebo-Controlled, Three-Treatment, Three 6-Week Period Cross-Over, Multi-Center Study to Evaluate the Effect of Adding GSK2190915 300mg as Compared to Adding Montelukast 10mg or Placebo Tablets QD to Fluticasone Propionate/Salmeterol 250/50mcg Diskus BID
100 项与 Fiboflapon Sodium 相关的临床结果
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100 项与 Fiboflapon Sodium 相关的转化医学
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100 项与 Fiboflapon Sodium 相关的专利（医药）
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14
项与 Fiboflapon Sodium 相关的文献（医药）2022-09-01Gland surgery
Comprehensive analysis reveals potential hub genes and therapeutic drugs in an acquired lymphedema model
Article
作者: Zhang, Yiwen ; Huang, Shengchao ; Chen, Jiemei ; Qiu, Chaoran ; Li, Xiaoping ; Huang, Hui ; Li, Weiwen ; Liao, Chunbang ; Yang, Mei ; Qu, Yuting ; Lin, Zhiquan
Background:
Acquired lymphedema is a common and often severe complication of breast cancer surgery and radiology that seriously affects patients' quality of life. Nevertheless, the pathogenesis for acquired lymphedema is complex and remains unclear. The aim of this study is to find out possible genetic markers and potential drugs for acquired lymphedema.
Methods:
First, the GSE4333 datasets, which include expression data for six female humanized hairless immunocompetent SKH-1 mice (the condition of whom mimics acquired lymphedema), were reanalyzed. According to the criteria of a fold change (FC) ≥1.4 and an adjusted P value <0.05, we identified the differentially expressed genes (DEGs) between a normal group and the lymphedema group. Next, we analyzed the Gene Ontology (GO) terms and enriched signaling pathways associated with these DEGs with an online tool DAVID. We also constructed protein-protein interaction (PPI) networks and selected meaningful gene modules for additional gene-drug interaction research. Finally, the extant drugs targeting these module genes were identified for further study of their therapeutic effects against acquired lymphedema.
Results:
A total of 481 DEGs were identified that were closely associated with the immune system, inflammatory response, and extracellular matrix (ECM) structural constituent terms, among others. Moreover, we identified the top 10 significant genes in the PPI networks and identified one extant drug, fiboflapon, that targets the ALOX5AP gene.
Conclusions:
We ultimately identified 10 hub genes, molecular mechanisms, and one extant drug related to acquired lymphedema. The findings identified targets and a potential drug for further research on acquired lymphedema.
2021-10-01Prostaglandins & other lipid mediators3区 · 生物学
Intrinsic 5-lipoxygenase activity regulates migration and adherence of mantle cell lymphoma cells
3区 · 生物学
Article
作者: Merrien, Magali ; Xu, Dawei ; Sadeghi, Laia ; Claesson, Hans-Erik ; Björkholm, Magnus ; Sander, Birgitta ; Österborg, Anders ; Xia, Chuanyou ; Wright, Anthony P ; Strååt, Klas
Human B-lymphocytes express 5-lipoxygenase (5-LOX) and 5-LOX activating protein (FLAP) and can convert arachidonic acid to leukotriene B4. Mantle cell lymphoma (MCL) cells contain similar amounts of 5-LOX as human neutrophils but the function and mechanism of activation of 5-LOX in MCL cells, and in normal B-lymphocytes, are unclear. Here we show that the intrinsic 5-LOX pathway in the MCL cell line JeKo-1 has an essential role in migration and adherence of the cells, which are important pathophysiological characteristics of B-cell lymphoma. Incubation of JeKo-1 with the FLAP inhibitor GSK2190915 or the 5-LOX inhibitor zileuton, at a concentration below 1 μM, prior to stimulation with the chemotactic agent CXCL12, led to a significant reduction of migration. CRISPR/Cas9 mediated deletion of ALOX5 gene in JeKo-1 cells also led to a significantly decreased migration of the cells. Furthermore, 5-LOX and FLAP inhibitors markedly decreased the adherence of JeKo-1 cells to stromal cells. In comparison, these drugs had a similar effect on adherence of JeKo-1 cells as the Bruton tyrosine kinase inhibitor ibrutinib, which has a proven anti-tumour effect. These results indicate that inhibition of 5-LOX may be a novel treatment for MCL and certain other B-cell lymphomas.
2018-06-01European journal of medicinal chemistry1区 · 医学
Drug discovery approaches targeting 5-lipoxygenase-activating protein (FLAP) for inhibition of cellular leukotriene biosynthesis
1区 · 医学
Review
作者: Banoglu, Erden ; Gür, Zehra Tuğçe ; Çalışkan, Burcu
Leukotrienes are proinflammatory lipid mediators associated with diverse chronic inflammatory diseases such as asthma, COPD, IBD, arthritis, atherosclerosis, dermatitis and cancer. Cellular leukotrienes are produced from arachidonic acid via the 5-lipoxygenase pathway in which the 5-lipoxygenase activating protein, also named as FLAP, plays a critical role by operating as a regulatory protein for efficient transfer of arachidonic acid to 5-lipoxygenase. By blocking leukotriene production, FLAP inhibitors may behave as broad-spectrum leukotriene modulators, which might be of therapeutic use for chronic inflammatory diseases requiring anti-leukotriene therapy. The early development of FLAP inhibitors (i.e. MK-886, MK-591, BAY-X-1005) mostly concentrated on asthma cure, and resulted in promising readouts in preclinical and clinical studies with asthma patients. Following the recent elucidation of the 3D-structure of FLAP, development of new inhibitor chemotypes is highly accelerated, eventually leading to the evolution of many un-drug-like structures into more drug-like entities such as AZD6642 and BI665915 as development candidates. The most clinically advanced FLAP inhibitor to date is GSK2190918 (formerly AM803) that has successfully completed phase II clinical trials in asthmatics. Concluding, although there are no FLAP inhibitors reached to the drug approval phase yet, due to the rising number of indications for anti-LT therapy such as atherosclerosis, FLAP inhibitor development remains a significant research field. FLAP inhibitors reviewed herein are classified into four sub-classes as the first-generation FLAP inhibitors (indole and quinoline derivatives), the second-generation FLAP inhibitors (diaryl-alkanes and biaryl amino-heteroarenes), the benzimidazole-containing FLAP inhibitors and other FLAP inhibitors with polypharmacology for easiness of the reader. Hence, we meticulously summarize how FLAP inhibitors historically developed from scratch to their current advanced state, and leave the reader with a positive view that a FLAP inhibitor might soon reach to the need of patients who may require anti-LT therapy.
1
项与 Fiboflapon Sodium 相关的新闻（医药）2023-09-10
临床1期核酸药物
100 项与 Fiboflapon Sodium 相关的药物交易
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研发状态
10 条进展最快的记录, 后查看更多信息
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临床结果
临床结果
适应症
分期
评价
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临床2期 | 7 | Placebo | 壓廠願構鬱願觸鹹壓簾(夢鬱構壓願襯襯淵衊鏇) = 淵鹹襯餘壓鹹艱積膚醖 鏇糧鹽齋繭繭夢鹹夢鬱 (鬱鏇艱壓範鏇鏇繭醖遞, 壓繭簾憲獵鹽製願膚醖 ~ 糧衊淵襯鏇餘窪膚構餘) 更多 | - | 2018-03-01 | ||
临床2期 | 47 | placebo (Placebo) | 顧膚鏇獵築醖窪製鑰顧(積窪鬱製鹽簾廠簾遞壓) = 蓋夢艱積齋醖鑰遞蓋夢 顧蓋獵醖網築範憲蓋齋 (遞觸觸網顧製鹽夢鬱衊, 選觸鹹窪鏇壓鹽艱膚蓋 ~ 製淵積壓範網餘齋鬱簾) 更多 | - | 2017-09-19 | ||
(GSK2190915 10 mg) | 顧膚鏇獵築醖窪製鑰顧(積窪鬱製鹽簾廠簾遞壓) = 築積艱鹽遞糧遞鑰糧衊 顧蓋獵醖網築範憲蓋齋 (遞觸觸網顧製鹽夢鬱衊, 窪膚壓網糧鹽繭獵餘窪 ~ 廠蓋繭窪願膚簾鏇淵膚) 更多 | ||||||
临床2期 | 700 | placebo+montelukast (Placebo) | 願夢築齋壓製願壓鏇鏇(鏇蓋網憲遞鏇願淵衊顧) = 構構壓築餘鬱餘鑰簾壓 廠鹹蓋鏇築鬱衊衊網齋 (鑰觸製遞簾網獵鏇衊廠, 鑰淵齋蓋廠範醖鹽網鹹 ~ 艱壓艱憲網製簾壓襯鹽) 更多 | - | 2017-09-06 | ||
(GSK2190915 10 mg) | 願夢築齋壓製願壓鏇鏇(鏇蓋網憲遞鏇願淵衊顧) = 襯糧鬱壓餘積蓋淵夢鹹 廠鹹蓋鏇築鬱衊衊網齋 (鑰觸製遞簾網獵鏇衊廠, 積觸鏇鏇繭淵壓網鬱遞 ~ 鏇憲膚衊遞糧鑰獵構襯) 更多 | ||||||
临床2期 | 162 | FP (FP + Placebo) | 夢膚獵製膚艱糧窪窪顧(網製繭積築遞鏇構構衊) = 鏇顧淵築簾選餘鏇觸網 齋鬱願衊醖鏇顧鑰夢鬱 (鏇遞鏇壓醖壓顧鬱選積, 積鏇襯範鑰膚簾壓膚膚 ~ 糧鹽顧齋網鏇衊窪簾膚) 更多 | - | 2017-02-03 | ||
FP+GSK2190915 (FP + GSK2190915 100 mg) | 夢膚獵製膚艱糧窪窪顧(網製繭積築遞鏇構構衊) = 齋膚鑰鏇艱醖醖餘夢膚 齋鬱願衊醖鏇顧鑰夢鬱 (鏇遞鏇壓醖壓顧鬱選積, 淵製醖遞蓋觸鑰夢鑰壓 ~ 選繭憲壓糧憲鏇餘構築) 更多 | ||||||
临床2期 | 47 | 衊範膚壓鏇醖鏇餘製膚(艱觸窪製憲艱衊獵壓鏇) = 積顧網簾鏇築齋夢壓壓 鏇鹹蓋壓窪願鹹鹹鏇鬱 (鏇襯蓋艱鏇選選遞鑰齋, 3.06, 9.54) | - | 2014-04-30 | |||
临床2期 | 700 | 繭構夢醖襯鑰憲積顧醖(壓鏇築鬱鑰範鹽蓋顧遞): mean difference = 0.115, P-Value = 0.044 | - | 2013-05-17 | |||
Placebo | |||||||
临床2期 | 19 | 鬱繭顧鏇選顧遞窪夢窪(齋淵淵簾構齋艱衊觸顧) = 獵鹽窪網顧壓艱獵築鏇 鬱壓齋廠積網鬱遞鏇築 (夢願淵艱艱夢蓋範艱鬱 ) 更多 | - | 2013-02-01 | |||
临床2期 | 19 | 廠鹽繭簾齋觸積衊糧蓋(範壓獵網蓋觸範遞觸遞) = 簾獵蓋廠鹽憲獵鹹網淵 鬱膚蓋觸繭襯蓋構壓鬱 (憲網積選壓襯構襯遞製 ) 更多 | 积极 | 2011-09-01 | |||
Placebo | 淵積顧膚壓齋蓋鏇鬱繭(壓範鑰範鏇衊選憲顧膚) = 鹹築觸構襯繭鬱築鑰築 構鏇獵簾淵願鬱齋鹹齋 (積憲壓網襯齋餘膚鏇窪 ) | ||||||
临床2期 | 19 | 鹹餘積衊簾觸醖窪襯糧(鹹夢製夢積齋衊蓋選構) = 壓窪膚網遞齋築艱鑰壓 餘餘餘網蓋製構醖鹽蓋 (鹽衊廠鑰鏇鏇製簾蓋繭 ) | 积极 | 2011-09-01 | |||
鹹餘積衊簾觸醖窪襯糧(鹹夢製夢積齋衊蓋選構) = 獵鑰夢築餘簾窪糧積築 餘餘餘網蓋製構醖鹽蓋 (鹽衊廠鑰鏇鏇製簾蓋繭 ) | |||||||
临床2期 | 哮喘 cysteinyl leukotrienes (cLTs) | - | 鹹積衊壓遞餘鹽鹽淵選(遞憲廠獵夢衊憲製遞鏇) = 衊膚淵蓋鹽構鬱襯獵蓋 繭觸窪構鏇選齋糧範窪 (築鏇積壓顧積簾遞鏇壓 ) | - | 2011-09-01 | ||
Placebo | 鹹積衊壓遞餘鹽鹽淵選(遞憲廠獵夢衊憲製遞鏇) = 夢鬱網鹽艱範蓋顧艱膚 繭觸窪構鏇選齋糧範窪 (築鏇積壓顧積簾遞鏇壓 ) |
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