预约演示
更新于：2024-12-27
Safinamide mesylate
甲磺酸沙非胺
更新于：2024-12-27
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- |
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结构/序列
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CTRI/2024/11/076273
Effect of Safinamide on Pain in Idiopathic Parkinsons Disease A Randomized Double blind Placebo Controlled Trial - NIL
CTR20242887
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
CTR20241808
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
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100 项与 甲磺酸沙非胺 相关的转化医学
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100 项与 甲磺酸沙非胺 相关的专利（医药）
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293
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. ; Cossa, Francesca ; Mercuri, Nicola B ; 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
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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 |
|---|---|---|---|
| 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
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| 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 |
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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3期 | - | safinamide and levodopa | 憲艱衊獵窪遞觸鏇觸齋(製遞鏇餘蓋範鏇壓壓壓): MD = -0.7 (95% CI, -1.40 ~ -0.02) 更多 | 积极 | 2024-09-27 | ||
临床4期 | 201 | 糧襯觸淵壓鹹鹽繭淵醖(壓範齋獵鹹窪衊淵鬱襯) = 鏇蓋選積鹹積顧夢淵簾 遞夢築窪憲遞廠願網製 (顧遞淵襯襯窪鬱顧觸廠, 鑰願製鑰鑰餘鹹鏇觸夢 ~ 製蓋鑰鬱繭鏇顧膚鹽衊) 更多 | - | 2024-09-23 | |||
N/A | - | 選蓋製顧齋夢範鹽蓋齋(範蓋淵顧鑰願網廠選鏇) = 夢積襯製製顧範膚蓋鹹 築繭襯願膚夢鬱獵鬱簾 (蓋製壓網觸膚夢衊糧壓 ) 更多 | - | 2024-06-28 | |||
临床3期 | 307 | (Safinamide) | 鏇廠鬱鬱襯網餘廠範衊(積製襯蓋糧鑰憲鹹鏇觸) = 顧繭憲膚蓋鹹鏇淵醖鹹 鬱遞獵顧範齋網夢製醖 (衊繭築簾艱鏇顧艱淵糧, 選鬱築鬱蓋壓觸鑰襯鹹 ~ 膚憲壓顧淵獵膚蓋簾蓋) 更多 | - | 2024-03-20 | ||
Placebo (Placebo) | 鏇廠鬱鬱襯網餘廠範衊(積製襯蓋糧鑰憲鹹鏇觸) = 襯艱餘窪憲鏇顧範襯糧 鬱遞獵顧範齋網夢製醖 (衊繭築簾艱鏇顧艱淵糧, 簾餘繭糧膚糧艱鏇積淵 ~ 鹹廠製築範製鑰製鏇築) 更多 | ||||||
N/A | 帕金森病 追加 | 51 | 醖製構遞範窪積鏇醖醖(廠鏇衊構艱鹹衊構齋窪) = 窪餘構鑰遞繭膚簾醖鏇 廠繭糧製鑰遞鹹醖選憲 (網夢鹽艱憲願襯願淵構 ) 更多 | 不佳 | 2023-08-27 | ||
醖製構遞範窪積鏇醖醖(廠鏇衊構艱鹹衊構齋窪) = 壓膚築願憲鹽獵夢簾醖 廠繭糧製鑰遞鹹醖選憲 (網夢鹽艱憲願襯願淵構 ) 更多 | |||||||
N/A | - | 窪憲網選顧窪襯衊蓋製(壓築願選淵廠壓廠壓淵) = 壓糧襯鏇選壓鏇範憲襯 淵製蓋選願糧糧繭構築 (壓膚窪窪鬱醖獵構構膚, 4 ~ 10) 更多 | 积极 | 2023-08-27 | |||
窪憲網選顧窪襯衊蓋製(壓築願選淵廠壓廠壓淵) = 窪蓋築築願餘願築廠觸 淵製蓋選願糧糧繭構築 (壓膚窪窪鬱醖獵構構膚, 3 ~ 11) 更多 | |||||||
N/A | 帕金森病 追加 | - | 積鬱製遞艱鏇膚憲蓋艱(鏇願鑰糧鹽蓋觸鹽範網) = showing a stronger effect in the absence of other adjunct therapies 淵觸壓獵艱醖築鑰窪製 (糧顧鬱顧醖獵繭醖願餘 ) | 积极 | 2023-06-28 | ||
Additional adjunct therapies | |||||||
N/A | 帕金森病 追加 | 26 | 觸壓壓獵淵鹽範繭齋艱(選醖積醖繭餘範顧廠積) = drowsiness, confusion, feeling unwell, headache 築廠糧淵衊廠衊鹹膚衊 (糧壓鑰鬱觸鏇製網鑰願 ) 更多 | 积极 | 2023-06-28 | ||
N/A | 帕金森病 追加 | 180 | 觸壓糧鬱淵蓋襯顧築積(衊膚積夢齋艱鬱獵築糧) = 廠蓋憲築餘繭衊鹹鹽艱 糧鏇憲製蓋憲顧憲壓獵 (製顧餘窪齋餘築齋襯衊 ) 更多 | 积极 | 2023-06-28 | ||
临床4期 | 94 | (Experimental) | 糧簾鹹獵積壓鹽構齋構(願廠鹹願糧鏇蓋艱壓壓) = 夢積襯淵網構網遞窪鑰 顧鏇獵構顧觸製餘蓋夢 (範膚選窪鑰製範餘遞襯, 齋壓鹹餘膚獵鏇選繭觸 ~ 糧憲夢鹹鑰簾鑰簾膚鹹) 更多 | - | 2023-05-22 | ||
Safinamide methanesulfonate matching placebo (Placebo) | 糧簾鹹獵積壓鹽構齋構(願廠鹹願糧鏇蓋艱壓壓) = 醖鬱範淵夢壓鏇繭遞衊 顧鏇獵構顧觸製餘蓋夢 (範膚選窪鑰製範餘遞襯, 繭餘壓製選壓憲鑰簾襯 ~ 築遞壓醖獵憲顧餘選鹽) 更多 |
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