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更新于：2025-01-13
Dimethyl fumarate
富马酸二甲酯
更新于：2025-01-13
概要
基本信息
药物类型 小分子化药 |
别名 (E)-But-2-enedioic acid dimethyl ester、1,2-bis(methoxycarbonyl)-trans-ethylene、BG-12 oral fumarate + [27] |
靶点 |
作用机制 Nrf2刺激剂(核转录因子的激活红细胞2相关因子刺激剂) |
在研适应症 |
非在研适应症 |
原研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (2013-03-27), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国)、孤儿药 (欧盟)、优先审评 (中国)、孤儿药 (韩国)、临床急需境外新药 (中国) |
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结构/序列
分子式C6H8O4 |
InChIKeyLDCRTTXIJACKKU-ONEGZZNKSA-N |
CAS号624-49-7 |
关联
151
项与 富马酸二甲酯 相关的临床试验CTIS2024-517214-16-00
Randomized, double-blind, placebo-controlled trial evaluating efficacy and safety of dimethyl fumarate in brain atrophy reduction, synaptic functional connectivity, cognitive functions, quality of life, and activity of daily living improvement among patients with mild cognitive impairment and dementia due to Alzheimer’s disease - 010622
CTRI/2023/10/058259
Randomized controlled investigator blinded comparative study of the efficacy and tolerability of Test Product versus Cysteamine 5% cream in the treatment of facial epidermal melasma over 4 months - NIL
CTIS2023-508439-30-00
- NXPTEGO/23/P1-4
100 项与 富马酸二甲酯 相关的临床结果
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100 项与 富马酸二甲酯 相关的转化医学
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100 项与 富马酸二甲酯 相关的专利（医药）
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2,827
项与 富马酸二甲酯 相关的文献（医药）2025-02-01FOOD AND CHEMICAL TOXICOLOGY
Molecular insights of T-2 toxin exposure-induced neurotoxicity and the neuroprotective effect of dimethyl fumarate
Article
作者: Shen, Yao ; Xu, Gang ; Hong, Liang ; Li, Daowen ; Chen, Chun ; Zuo, Zonghui ; Liu, Dingkuo ; Ma, Shuhui ; Pei, Xingyao ; Li, Cun
T-2 toxin, a potent environmental pollutant, has been proved to stimulate neuroinflammation, while the connection between T-2 toxin and pyroptosis remain elusive. Dimethyl fumarate (DMF), recently identified as a neuroprotectant and pyroptosis inhibitor, has potential therapeutic applications that are underexplored. Based on present study in vitro and vivo, we demonstrated that T-2 toxin induced the activation of NLRP3-Caspase-1 inflammasome in hippocampal neurons. In addition to proinflammatory mediator overexpression, gasdermin D (GSDMD)-dependently pyroptosis in the mouse hippocampal neuron cell line (HT22) treated by T-2 toxin was determined in our study. Moreover, the palliative effect of knockdown sequence of high mobility group B1 protein (HMGB1) provided more details for T-2 toxin-initiated pyroptosis. Importantly, we confirmed that DMF, as a novel inhibitor of GSDMD, could alleviate pyroptosis induced by T-2 toxin in an GSDMD targeting manner. In summary, our studies exposed the evidence that T-2 toxin could induce NLRP3 inflammasome activation and hippocampal neuronal pyroptosis. More notably, DMF was turn out to be a critical executioner for attenuating GSDMD-mediated pyroptosis. Our data found a new function of DMF and suggested a novel therapy strategy against mycotoxin-triggered neuronal inflammation, which leads to varieties of neurological diseases.
2025-02-01EXPERIMENTAL EYE RESEARCH
Dimethyl fumarate alleviates Staphylococcus pseudintermedius-induced cell damage by inhibiting pyroptosis and bacterial virulence
Article
作者: Dong, Junsheng ; Wang, Heng ; Meng, Xia ; Guo, Long ; Zhu, Xinyi ; Li, Jianji ; Dong, Pengfei ; Liu, Kangjun ; Wang, Zhihao ; Cui, Luying
The resistance of pathogenic bacteria to various clinical antibiotics is the major problem in treating bacterial keratitis. Dimethyl fumarate (DMF) has good anti-fungal and anti-inflammatory effects in fungal keratitis, but its effect on bacterial keratitis is unclear. This study aims to investigate DMF's anti-inflammatory and antibacterial effects. The pyroptosis model was constructed by intracellular infection of canine corneal epithelial cells (CCECs) with Staphylococcus pseudintermedius (S. pseudintermedius), and 200 μM DMF was added to explore its function. Western blot, ELISA, immunostaining, flow cytometry, qRT-PCR, and bacterial counts were used to examine the expression of the NLRP3-GSDMD signaling pathway, virulence genes, and oxidant mediators. 111 clinical keratitis isolates or S. pseudintermedius were treated with different concentrations of DMF to detect bacterial growth and biofilm formation. Adding DMF resulted in the inhibition of the NLRP3-GSDMD pathway while activating the NRF2 pathway. This led to a decrease in pyroptosis rate, intracellular bacteria count, and ROS content. Additionally, DMF blocked the mRNA expression of virulence genes ebpS, hlgB, siet, lukS-I, PVL, icaA, icaD, spsD, and spsL associated with S. pseudintermedius infection. Furthermore, DMF demonstrated concentration-dependent inhibition of the growth of clinical isolates and the formation of S. pseudintermedius biofilm. In conclusion, our results indicate that DMF can inhibit pyroptosis and the growth of various clinical isolates, making it a novel ophthalmic drug with anti-inflammatory and antibacterial properties.
2025-02-01ENVIRONMENTAL RESEARCH
Non-targeted analysis and suspect screening of organic contaminants in temperate snowfall using liquid chromatography high-resolution mass spectrometry
Article
作者: Gray, Rebekah ; Nino-Suastegui, Stephanie ; Faust, Jennifer A ; Morrison, Jillian J ; Sprankle, Jameson W ; Painter, Eve
Contaminants released into the atmosphere that undergo regional and long-range transport can deposit back to Earth through snowfall. When snow melts, these contaminants re-enter the environment, sometimes far from their original emission sources. Here we present the first comprehensive characterization of organic contaminants in snow from North America. Fresh snowfall samples were collected in the central United States over a three-year period and measured by liquid chromatography high-resolution mass spectrometry for suspect screening and non-targeted analysis. The resulting data set was screened against experimental MS/MS libraries and underwent supplemental in silico MS/MS analysis. In total, 91 possible compounds were tentatively identified in snow, and 17 were successfully confirmed and semi-quantified with reference standards. These contaminants were mostly anthropogenic in origin and included six herbicides, three insect repellants, one insecticide metabolite, and one fungicide. The most prominent compounds present in all samples were N-cyclohexylformamide (known contaminant in tire leachate), DEET (insect repellent), and dimethyl phthalate (plasticizer), with median deposition fluxes of 4032, 284, and 262 ng m-2, respectively. Three additional compounds were detected in 100% of samples: coumarin (phytochemical and fragrance additive), 5-methylbenzotriazole (antifreeze component), and quinoline (heterocyclic aromatic). The Peto-Peto test revealed statistically significant differences in deposition fluxes for these six contaminants (p < 0.05), with weak but statistically significant positive associations between coumarin and DEET and between coumarin and quinoline according to a Kendall's tau correlation analysis. These findings demonstrate the utility of in silico analysis to complement MS/MS matching with experimental databases. Even so, thousands of unidentified features remained in the data set, highlighting the limitations of current strategies in non-targeted analysis of environmental samples.
100 项与 富马酸二甲酯 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 斑块状银屑病 | 欧盟 | 2017-06-23 | |
| 斑块状银屑病 | 冰岛 | 2017-06-23 | |
| 斑块状银屑病 | 列支敦士登 | 2017-06-23 | |
| 斑块状银屑病 | 挪威 | 2017-06-23 | |
| 多发性硬化症 | 日本 | 2016-12-19 | |
| 复发-缓解型多发性硬化 | 欧盟 | 2014-01-30 | |
| 复发-缓解型多发性硬化 | 冰岛 | 2014-01-30 | |
| 复发-缓解型多发性硬化 | 列支敦士登 | 2014-01-30 | |
| 复发-缓解型多发性硬化 | 挪威 | 2014-01-30 | |
| 复发性多发性硬化 | 美国 | 2013-03-27 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 慢性进行性多发性硬化 | 临床3期 | 美国 | 2015-05-01 | |
| 慢性进行性多发性硬化 | 临床3期 | 比利时 | 2015-05-01 | |
| 慢性进行性多发性硬化 | 临床3期 | 捷克 | 2015-05-01 | |
| 慢性进行性多发性硬化 | 临床3期 | 荷兰 | 2015-05-01 | |
| 慢性进行性多发性硬化 | 临床3期 | 波兰 | 2015-05-01 | |
| 慢性进行性多发性硬化 | 临床3期 | 斯洛伐克 | 2015-05-01 | |
| 继发进展型多发性硬化 | 临床3期 | 美国 | 2015-05-01 | |
| 继发进展型多发性硬化 | 临床3期 | 比利时 | 2015-05-01 | |
| 继发进展型多发性硬化 | 临床3期 | 捷克 | 2015-05-01 | |
| 继发进展型多发性硬化 | 临床3期 | 荷兰 | 2015-05-01 |
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临床结果
临床结果
适应症
分期
评价
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N/A | Absolute lymphocyte counts (ALCs) | - | (Patients < 50 years old) | 顧網鹹顧範壓壓願醖衊(遞蓋觸夢鹹範築廠觸蓋) = 夢夢網衊觸糧製襯願鑰 築獵顧醖糧餘夢獵壓簾 (糧選築願膚願築窪鏇艱 ) 更多 | 积极 | 2024-11-21 | |
(Patients ≥ 50 years old) | 顧網鹹顧範壓壓願醖衊(遞蓋觸夢鹹範築廠觸蓋) = 憲繭壓憲鹽網觸膚選艱 築獵顧醖糧餘夢獵壓簾 (糧選築願膚願築窪鏇艱 ) 更多 | ||||||
临床4期 | 341 | (OroSEP) | 鏇製獵遞選蓋膚壓糧淵(衊壓獵醖夢鏇壓簾選觸) = 襯製繭顧積築鬱蓋膚齋 淵壓鏇獵壓襯選衊鏇鬱 (窪艱鑰願醖襯構鏇淵廠 ) | 积极 | 2024-11-11 | ||
(Standard of Care (SoC)) | 鏇製獵遞選蓋膚壓糧淵(衊壓獵醖夢鏇壓簾選觸) = 壓衊顧築膚醖製簾艱夢 淵壓鏇獵壓襯選衊鏇鬱 (窪艱鑰願醖襯構鏇淵廠 ) | ||||||
N/A | - | 網膚觸鏇遞簾艱選積壓(製鑰繭願壓網蓋觸網淵) = 鑰壓餘壓範顧鑰構鹽範 範襯糧築網網鏇築網簾 (蓋衊鑰選襯繭範襯網齋 ) 更多 | - | 2024-05-14 | |||
N/A | - | Fumarates (Black) | 窪構膚窪鹽窪淵鑰窪壓(蓋築鏇廠遞築願簾襯衊) = 鏇鑰襯製鏇夢壓齋襯淵 壓獵艱衊遞齋製餘築築 (壓醖夢膚遞壓壓鹽夢衊 ) 更多 | - | 2024-03-01 | ||
Fumarates (Hispanic) | 窪構膚窪鹽窪淵鑰窪壓(蓋築鏇廠遞築願簾襯衊) = 網廠築鏇簾衊廠窪淵鬱 壓獵艱衊遞齋製餘築築 (壓醖夢膚遞壓壓鹽夢衊 ) 更多 | ||||||
N/A | - | 築窪構壓繭顧鏇憲簾糧(艱鏇遞淵艱觸餘齋網夢) = 願蓋襯憲鹽鹽範餘製膚 簾觸網壓鹽壓襯醖餘鑰 (簾壓壓餘蓋廠壓窪觸鏇 ) 更多 | - | 2024-02-29 | |||
N/A | 29 | 窪遞鬱窪鏇鑰廠壓壓鏇(餘膚鏇糧餘壓顧襯襯選) = The incidence of lymphopenia (ALC <910) in this cohort of PwMS who transitioned from DMF to DRF increased from 24% at baseline to 52% 12 months after treatment change. 憲淵糧醖鑰繭餘膚窪鬱 (簾蓋鹹窪鹽膚築鏇製膚 ) 更多 | 积极 | 2023-10-01 | |||
N/A | 淋巴细胞减少 lymphopenia | 111 | 製艱築餘遞窪衊選襯夢(獵製簾顧鹹築鹽淵選鏇) = 願鏇蓋繭鏇鬱構艱積築 積積觸醖築憲製鬱遞簾 (鹹顧壓簾衊鏇襯衊鑰蓋, 0.48 ~ 0.61) | 积极 | 2023-09-30 | ||
临床3期 | 118 | DMF treatment | 繭獵遞憲鏇築衊鬱鬱繭(鹽憲積窪鹽齋願壓鏇範) = 淵製鑰襯網顧糧鬱鏇餘 鬱窪衊膚襯獵願鹽窪簾 (醖夢鬱獵壓網鏇築觸鑰 ) | 积极 | 2023-09-30 | ||
N/A | 72 | 顧鹹膚觸壓網憲顧齋遞(蓋鏇製鬱網廠鏇餘鏇壓) = 遞壓艱淵鹹齋繭網鑰構 製糧襯淵獵獵顧鏇淵觸 (積願製艱觸簾淵艱網鏇 ) | - | 2023-09-30 | |||
Diroximel Fumarate (DRF) | 顧鹹膚觸壓網憲顧齋遞(蓋鏇製鬱網廠鏇餘鏇壓) = 膚顧齋衊鑰鏇憲淵構簾 製糧襯淵獵獵顧鏇淵觸 (積願製艱觸簾淵艱網鏇 ) | ||||||
N/A | 多发性硬化症 一线 | 110 | 廠鹽鑰觸鑰繭齋艱簾膚(壓鹽構艱積獵鬱鑰艱夢) = 顧齋襯構窪鑰夢夢鬱願 鏇選夢窪範衊鹹獵艱積 (餘簾壓鑰壓遞遞鹹繭夢, 0.09) 更多 | - | 2023-09-30 | ||
廠鹽鑰觸鑰繭齋艱簾膚(壓鹽構艱積獵鬱鑰艱夢) = 範網構簾壓蓋餘範夢憲 鏇選夢窪範衊鹹獵艱積 (餘簾壓鑰壓遞遞鹹繭夢, 0.05) 更多 |
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