更新于：2024-12-24
Safinamide mesylate
甲磺酸沙非胺
更新于：2024-12-24
概要
基本信息
非在研机构 |
最高研发阶段批准上市 |
首次获批日期 欧盟 (2015-02-23), |
最高研发阶段(中国)批准上市 |
特殊审评- |
登录后查看时间轴
结构
分子式C18H23FN2O5S |
InChIKeyYKOCHIUQOBQIAC-YDALLXLXSA-N |
CAS号202825-46-5 |
关联
63
项与 甲磺酸沙非胺 相关的临床试验Effect of Safinamide on Pain in Idiopathic Parkinsons Disease A Randomized Double blind Placebo Controlled Trial - NIL
中国健康受试者空腹和餐后状态下口服甲磺酸沙非胺片单中心、随机、开放、单剂量、两周期、两序列、双交叉设计的生物等效性试验
甲磺酸沙芬酰胺片在中国健康受试者中进行的单中心、随机、开放、单次（空腹/餐后）口服给药、两制剂、两序列、两周期、交叉的人体生物等效性试验。
100 项与 甲磺酸沙非胺 相关的临床结果
登录后查看更多信息
100 项与 甲磺酸沙非胺 相关的转化医学
登录后查看更多信息
100 项与 甲磺酸沙非胺 相关的专利（医药）
登录后查看更多信息
290
项与 甲磺酸沙非胺 相关的文献（医药）2024-12-01EPILEPSY & BEHAVIOR
Drug repurposing in status epilepticus
Article
作者: Walker, Matthew C
The treatment of status epilepticus (SE) has changed little in the last 20 years, largely because of the high risks and costs of new drug development for SE. Moreover, SE poses specific challenges to drug development, such as patient diversity, logistical hurdles, and the need for acute treatment strategies that differ from chronic seizure prevention. This has reduced the appetite of industry to develop new drugs in this area. Drug repurposing is an attractive approach to address this unmet need. It offers significant advantages, including reduced development time, lower costs, and higher success rates, compared to novel drug development. Here I demonstrate how novel methods integrating biological knowledge and computational methods can be applied to drug repurposing in status epilepticus. Biological approaches focus on addressing mechanisms underlying drug resistance in SE (using for example ketamine, tacrolimus and safinamide) and longer-term consequences (using for example omaveloxolone, celecoxib and losartan). Additionally, artificial intelligence platforms, such as ChatGPT, can rapidly generate promising drug lists, while in silico methods can analyze gene expression changes to predict molecular targets. Combining AI and in silico approaches has identified several candidate drugs, including metformin, sirolimus and riluzole, for SE treatment. Despite the promise of repurposing, challenges remain, such as intellectual property issues and regulatory barriers. Nonetheless, drug repurposing presents a viable solution to the high costs and slow progress of traditional drug development for SE. This paper is based on a presentation made at the 9th London-Innsbruck Colloquium on Status Epilepticus and Acute Seizures, in April 2024.
2024-12-01European Journal of Nuclear Medicine and Molecular Imaging
PET imaging of synaptic vesicle glycoprotein 2 subtype A for neurological recovery in ischemic stroke
Article
作者: Zhang, Hong ; Jin, Chentao ; Niu, Jiaqi ; Wen, Junjie ; Yu, Congcong ; Wang, Jing ; Luo, Xiaoyun ; Chen, Hetian ; Tian, Mei ; Dou, Xiaofeng ; Zhong, Yan
PURPOSE:
[18F]SynVesT-1 is a novel radiopharmaceutical for assessing synaptic density in vivo. This study aims to investigate the potential of [18F]SynVesT-1 positron emission tomography (PET) in evaluating neurological recovery in the rat model of ischemic stroke, and to compare its performance with [18F]FDG PET.
METHODS:
Sprague-Dawley rats were subjected to photothrombotic cerebral infarction, and safinamide was administered intraperitoneally from day 3 to day 14 post-stroke to alleviate neurological deficits. Cylinder test and forelimb placing test were performed to assess the neurological function. MRI, [18F]SynVesT-1 PET/CT and [18F]FDG PET/CT imaging were used to evaluate infarct volume, synaptic density, and cerebral glucose metabolism pre- and post-treatment. [18F]SynVesT-1 and [18F]FDG PET images were compared using Statistical Parametric Mapping (SPM) and region of interest (ROI)-based analysis. Post-mortem histological analysis was performed to validate PET images.
RESULTS:
Safinamide treatment improved behavioral outcomes in stroke-damaged rats. Both [18F]SynVesT-1 and [18F]FDG PET detected stroke-induced injury, with the injured region being significantly larger in [18F]FDG PET than in [18F]SynVesT-1 PET. Compared with the saline group, radiotracer uptake in the injured area significantly increased in [18F]SynVesT-1 PET after safinamide treatment, whereas no notable change was observed in [18F]FDG PET. Additionally, [18F]SynVesT-1 PET imaging showed a better correlation with neurological function recovery than [18F]FDG PET. Post-mortem analysis revealed increased neuronal numbers, synaptic density, and synaptic neuroplasticity, as well as decreased glia activation in the stroke-injured area after treatment.
CONCLUSION:
[18F]SynVesT-1 PET effectively quantified spatiotemporal dynamics of synaptic density in the rat model of stroke, and showed different capabilities in detecting stroke injury and neurological recovery compared with [18F]FDG PET. The utilization of [18F]SynVesT-1 PET holds promise as a potential non-invasive biomarker for evaluating ischemic stroke in conjunction with [18F]FDG PET.
2024-11-01PARKINSONISM & RELATED DISORDERS
Functional efficacy of the MAO-B inhibitor safinamide in murine substantia nigra pars compacta dopaminergic neurons in vitro: A comparative study with tranylcypromine
Article
作者: Federici, Mauro ; Mercuri, Nicola B. ; Mercuri, Nicola B ; Cossa, Francesca ; Giacomet, Cecilia ; Berretta, Nicola ; Zarrilli, Beatrice
Safinamide (SAF) is currently used to treat Parkinson's disease (PD) symptoms based on its theoretical ability to potentiate the dopamine (DA) signal, blocking monoamine oxidase (MAO) B. The present work aims to highlight the functional relevance of SAF as an enhancer of the DA signal, by evaluating its ability to prolong recovery from DA-mediated firing inhibition of DAergic neurons of the substantia nigra pars compacta (SNpc), compared to another MAO antagonist, tranylcypromine (TCP). Using multielectrode array (MEA) and single electrode extracellular recordings of spontaneous spikes from presumed SNpc DAergic cells in vitro, we show that SAF (30 μM) mildly prolongs the DA-mediated firing inhibition, as opposed to the profound effect of TCP (10 μM). In patch-clamp recordings, we found that SAF (30 μM) significantly reduced the number of spikes evoked by depolarizing currents in SNpc DAergic neurons, in a sulpiride (1 μM) independent manner. According to our results, SAF marginally potentiates the DA signal in SNpc DAergic neurons, while exerting an inhibitory effect on the postsynaptic excitability acting on membrane conductances. Thus, we propose that the therapeutic effects of SAF in PD patients partially depends on MAO inhibition, while other MAO-independent sites of action could be more relevant.
100 项与 甲磺酸沙非胺 相关的药物交易
登录后查看更多信息
研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
登录
| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 帕金森病 | 欧盟 | 2015-02-23 | |
| 帕金森病 | 冰岛 | 2015-02-23 | |
| 帕金森病 | 列支敦士登 | 2015-02-23 | |
| 帕金森病 | 挪威 | 2015-02-23 |
未上市
10 条进展最快的记录, 后查看更多信息
登录
| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 药物性运动障碍 | 临床3期 | - | 2019-10-01 | |
| 帕金森病（青年型、早发型） | 临床3期 | 瑞士 | 2009-10-01 | |
| 精神运动障碍 | 临床3期 | - | 2007-08-01 | |
| 多系统萎缩（MSA）性体位性低血压 | 临床2期 | 意大利 | 2019-10-29 | |
| 多系统萎缩（MSA）性体位性低血压 | 临床2期 | 西班牙 | 2019-10-29 | |
| 多系统萎缩，帕金森变异 | 临床2期 | 意大利 | 2019-10-29 | |
| 多系统萎缩，帕金森变异 | 临床2期 | 西班牙 | 2019-10-29 | |
| 认知功能障碍 | 临床2期 | 美国 | 2010-09-01 | |
| 认知功能障碍 | 临床2期 | 西班牙 | 2010-09-01 | |
| 帕金森病所致痴呆 | 临床2期 | 美国 | 2010-09-01 |
登录后查看更多信息
临床结果
临床结果
适应症
分期
评价
查看全部结果
临床3期 | - | safinamide and levodopa | 繭淵淵壓餘鬱齋積鹽簾(鹽鑰醖鹹築網夢簾鑰醖): MD = -0.7 (95% CI, -1.40 ~ -0.02) 更多 | 积极 | 2024-09-27 | ||
临床4期 | 201 | 齋觸簾齋顧糧齋蓋製餘(製願鑰壓選夢鏇廠夢遞) = 遞製窪積醖範齋遞選遞 齋築鬱窪範鏇廠艱憲壓 (觸齋淵糧襯獵遞鑰壓構, 築蓋醖鬱顧廠齋餘鬱鏇 ~ 願蓋鬱衊繭鹹窪遞鬱艱) 更多 | - | 2024-09-23 | |||
N/A | - | 鏇餘簾選糧壓膚範襯鬱(壓願範觸膚鏇醖鏇鏇鏇) = 簾遞構繭齋艱鑰鬱遞壓 築遞鬱淵廠衊窪淵遞壓 (積鏇繭壓壓襯齋糧壓繭 ) 更多 | - | 2024-06-28 | |||
临床3期 | 307 | (Safinamide) | 憲繭艱鬱網鹽獵選構願(簾壓選襯淵夢齋鏇蓋醖) = 選製淵鹽鑰壓壓鹹獵製 願鑰窪簾築願壓憲夢鏇 (築獵選蓋築衊網製夢構, 築膚壓鏇艱顧淵網壓憲 ~ 餘觸餘糧繭壓鏇築衊網) 更多 | - | 2024-03-20 | ||
Placebo (Placebo) | 憲繭艱鬱網鹽獵選構願(簾壓選襯淵夢齋鏇蓋醖) = 夢壓鑰鑰網淵築選範衊 願鑰窪簾築願壓憲夢鏇 (築獵選蓋築衊網製夢構, 憲鑰觸築醖獵鬱壓鹹鑰 ~ 齋憲繭憲遞積鏇壓製簾) 更多 | ||||||
N/A | - | 窪積獵鬱繭鑰繭遞鏇廠(鏇憲衊襯鑰蓋構壓網艱) = 醖網膚遞壓憲蓋膚襯衊 憲廠顧餘鹽製範選憲齋 (餘繭蓋顧鬱構衊築網膚, 4 ~ 10) 更多 | 积极 | 2023-08-27 | |||
窪積獵鬱繭鑰繭遞鏇廠(鏇憲衊襯鑰蓋構壓網艱) = 糧網鹽糧窪構醖壓構艱 憲廠顧餘鹽製範選憲齋 (餘繭蓋顧鬱構衊築網膚, 3 ~ 11) 更多 | |||||||
N/A | 帕金森病 追加 | 51 | 構襯鬱憲鬱蓋製衊艱鑰(鬱糧衊醖範襯鬱廠遞簾) = 遞鏇餘淵築鬱憲範構醖 艱醖鏇壓顧壓醖窪簾網 (壓網觸觸獵觸餘願鏇鹽 ) 更多 | 不佳 | 2023-08-27 | ||
構襯鬱憲鬱蓋製衊艱鑰(鬱糧衊醖範襯鬱廠遞簾) = 糧鑰願齋艱壓餘觸鹹鹽 艱醖鏇壓顧壓醖窪簾網 (壓網觸觸獵觸餘願鏇鹽 ) 更多 | |||||||
N/A | 帕金森病 追加 | 26 | 繭壓鑰選衊淵鑰醖廠製(膚鹹廠壓壓襯夢繭遞遞) = drowsiness, confusion, feeling unwell, headache 鑰蓋範顧憲網製顧襯壓 (鏇艱鬱憲構築醖觸願鹽 ) 更多 | 积极 | 2023-06-28 | ||
N/A | 帕金森病 追加 | - | 鏇築窪鹹膚襯選繭網觸(淵鏇鹹憲鹹齋醖網願艱) = showing a stronger effect in the absence of other adjunct therapies 遞窪鹹遞襯繭齋鹽糧憲 (夢獵製齋範醖憲蓋鏇憲 ) | 积极 | 2023-06-28 | ||
Additional adjunct therapies | |||||||
N/A | 帕金森病 追加 | 180 | 獵遞簾觸遞鹽築簾築鹹(鏇願鹹窪齋構鏇鹹艱繭) = 襯膚鏇願襯繭願夢網淵 願鑰鏇積憲製艱範積齋 (鏇鏇範艱顧壓餘網襯鏇 ) 更多 | 积极 | 2023-06-28 | ||
临床4期 | 94 | (Experimental) | 鏇願襯襯構鏇鹽鬱艱構(範繭繭選夢築願衊蓋選) = 選淵襯鹹窪鑰顧艱顧鑰 積衊襯願醖鏇觸積構鹹 (構願憲廠鏇齋繭網願鬱, 憲襯鑰淵顧繭餘積積簾 ~ 夢壓夢衊夢壓遞艱範廠) 更多 | - | 2023-05-22 | ||
Safinamide methanesulfonate matching placebo (Placebo) | 鏇願襯襯構鏇鹽鬱艱構(範繭繭選夢築願衊蓋選) = 築鏇齋壓衊淵獵糧顧衊 積衊襯願醖鏇觸積構鹹 (構願憲廠鏇齋繭網願鬱, 膚糧製鬱壓淵夢衊繭餘 ~ 糧衊艱繭夢獵膚鑰鑰觸) 更多 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
来和芽仔聊天吧
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用