预约演示
更新于：2025-05-28
Safinamide mesylate
甲磺酸沙非胺
更新于：2025-05-28
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
57
项与 甲磺酸沙非胺 相关的临床试验CTR20250194
甲磺酸沙芬酰胺片在健康受试者中进行的单中心、单剂量、随机、开放、交叉、两制剂、两周期空腹和餐后人体生物等效性试验
CTR20244359
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
CTRI/2024/11/076273
Effect of Safinamide on Pain in Idiopathic Parkinsons Disease A Randomized Double blind Placebo Controlled Trial - NIL
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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467
项与 甲磺酸沙非胺 相关的文献（医药）2025-07-01EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
2-(Phenylamino)-7,8-dihydroquinazolin-5(6H)-one, a promising scaffold for MAO-B inhibitors with potential GSK3β targeting
Article
作者: Da Settimo, Federico ; Borreca, Antonella ; Taliani, Sabrina ; Poggetti, Valeria ; Sarno, Giuliana ; Castellano, Sabrina ; Nordio, Giulia ; Piazzola, Francesco ; Baglini, Emma ; Natale, Benito ; Salerno, Silvia ; Cosconati, Sandro ; Di Paolo, Maria Luisa ; Barresi, Elisabetta ; Dalla Via, Lisa ; Sarno, Stefania
Neurodegenerative disorders, such as Parkinson's disease and Alzheimer's disease, constitute pathological conditions of great relevance on health span and quality of life. The identification of novel therapeutic options, able to modulate the processes involved in the insurgence and progression of neurodegenerative disorders, represents an intriguing challenge of current research. Herein, a library of 36-membered 2-(phenylamino)-7,8-dihydroquinazolinone derivatives was synthesized and biologically evaluated as human MAO inhibitors. Some compounds able to inhibit MAO-B potently and selectively (Ki in the nanomolar range) were identified, and robust structure-activity relationships were drawn, supported by computational studies. Further biological assays revealed a safe profile for all derivatives and, for compounds selected as the best MAO-B inhibitors (4, 5, 13, 14) the following properties also emerged: (i) the ability to inhibit MAO-B activity in whole cells, with an effectiveness comparable or slight lower with respect to the reference safinamide; (ii) physicochemical parameters suggesting drug-likeness properties; (iii) the ability to inhibit, albeit weakly, GSK3β kinase (for compound 4). Within the whole series, compound 4 stood out as a promising lead for future optimization campaigns aimed to obtain useful drugs for the treatment of Alzheimer's and Parkinson's diseases.
2025-06-01MOLECULAR BIOTECHNOLOGY
Structure and Ligand Based Virtual Screening and MPO Topological Analysis of Triazolo Thiadiazepine-fused Coumarin Derivatives as Anti-Parkinson Drug Candidates
Article
作者: Marinho, Emmanuel Silva ; Dos Santos, Hélcio Silva ; Guedes, Jesyka Macêdo ; de Oliveira, Victor Moreira ; Marinho, Márcia Machado ; Cajazeiras, Francisco Ferdinando Mesquita ; de Lima-Neto, Pedro ; Teixeira, Alexandre Magno Rodrigues ; Pereira, Antônio Mateus Gomes ; da Rocha, Matheus Nunes ; Roberto, Caio Henrique Alexandre
Parkinson's disease (PD) is a debilitating condition that can cause locomotor problems in affected patients, such as tremors and body rigidity. PD therapy often includes the use of monoamine oxidase B (MAOB) inhibitors, particularly phenylhalogen compounds and coumarin-based semi-synthetic compounds. The objective of this study was to analyze the structural, pharmacokinetic, and pharmacodynamic profile of a series of Triazolo Thiadiazepine-fused Coumarin Derivatives (TDCDs) against MAOB, in comparison with the inhibitor safinamide. To achieve this goal, we utilized structure-based virtual screening techniques, including target prediction and absorption, distribution, metabolism, and excretion (ADME) prediction based on multi-parameter optimization (MPO) topological analysis, as well as ligand-based virtual screening techniques, such as docking and molecular dynamics. The findings indicate that the TDCDs exhibit structural similarity to other bioactive compounds containing coumarin and MAOB-binding azoles, which are present in the ChEMBL database. The topological analyses suggest that TDCD3 has the best ADME profile, particularly due to the alignment between low lipophilicity and high polarity. The coumarin and triazole portions make a strong contribution to this profile, resulting in a permeability with Papp estimated at 2.15 × 10-5 cm/s, indicating high cell viability. The substance is predicted to be metabolically stable. It is important to note that this is an objective evaluation based on the available data. Molecular docking simulations showed that the ligand has an affinity energy of - 8.075 kcal/mol with MAOB and interacts with biological substrate residues such as Pro102 and Phe103. The results suggest that the compound has a safe profile in relation to the MAOB model, making it a promising active ingredient for the treatment of PD.
2025-06-01MOLECULAR NEUROBIOLOGY
Pelargonium graveolens Attenuates Rotenone-Induced Parkinson’s Disease in a Rat Model: Role of MAO-B Inhibition and In Silico Study
Article
作者: Moustafa, Sherifa F A ; Ezzat, Shahira M ; Salem, Mohamed A ; Meselhy, Meselhy R ; Merghany, Rana M ; Naser, Asmaa F Aboul ; El-Sawi, Salma A
Abstract:
Parkinson’s disease (PD), the second most common neurodegenerative condition, is primarily characterized by motor dysfunctions due to dopaminergic neuronal loss in the Substantia Nigra (SN), with oxidative stress playing a significant role in its progression. This study investigates the neuroprotective potential of Pelargonium graveolens (Thunb.) L’Hér leaves in a rotenone-induced PD rat model. The total ethanolic extract and its fractions, obtained via Diaion HP-20 column chromatography, were evaluated for monoamine oxidase-B (MAO-B) inhibition in vitro. The 50% methanol fraction (PG50) demonstrated the highest MAO-B inhibition (IC50 5.26 ± 0.12 µg/ml) compared to the reference drug selegiline (IC50 0.021 ± 0.003 µg/ml). In a rotenone-induced PD rat model, PG50 (100 mg/kg, p.o.) alleviated motor deficits (assessed via the wire hanging test), and restored norepinephrine, dopamine, and serotonin levels. PG50 and l-dopa reduced α-synuclein levels by 367.60% and 377.48%, respectively. Oxidative balance was restored with increased glutathione (23.12%) and decreased malondialdehyde (164.19%) in brain tissues. PG50 significantly reduced serum TNF-α (572.79%) and IL-6 (70.84%) levels, and improved succinate dehydrogenase (14.47%) and lactate dehydrogenase (7.74%) activities in brain tissues. Histopathological alterations in the SN were also ceased. UPLC-MS/MS analysis identified 61 metabolites, including 32 flavonoids, 13 phenolic acids, 7 coumarins, 5 phenolic glycosides, and 4 dicarboxylic acids, with in silico docking showing strong MAO-B binding by methoxylated flavonoids like methoxyluteolin dimethyl ether (docking score: − 8.0625 kcal/mol), surpassing that of safinamide (− 8.2615 kcal/mol). These findings suggest that P. graveolens holds promise as a neuroprotective agent against rotenone-induced PD.
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，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 | |
| 癫痫 | 临床2期 | 欧盟 | - | |
| 不宁腿综合征 | 临床2期 | 欧盟 | - | |
| 肾功能不全 | 临床1期 | 德国 | 2011-06-01 |
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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 | 襯廠範襯鏇獵餘鹽壓艱(願鑰廠遞膚繭窪繭廠衊): MD = -0.7 (95% CI, -1.40 ~ -0.02) 更多 | 积极 | 2024-09-27 | ||
临床4期 | 201 | 廠構製壓遞獵積淵齋餘(鏇醖齋願衊積蓋繭鏇夢) = 築醖繭獵獵鹽顧繭壓窪 範鬱鹹選膚餘製鑰憲糧 (餘構觸膚遞鹹遞艱壓壓, 膚艱淵鹹鏇築願夢壓簾 ~ 選夢醖製遞衊襯艱鑰獵) 更多 | - | 2024-09-23 | |||
N/A | - | 夢觸遞糧積鏇願醖艱範(鑰壓積醖顧餘壓壓繭鹹) = 鬱鹹範鏇鹹夢廠鹽醖積 夢襯選鹹蓋願積製夢繭 (鑰網襯膚壓鏇鑰鏇鹹願 ) 更多 | - | 2024-06-28 | |||
临床3期 | 307 | (Safinamide) | 遞衊壓築憲艱襯蓋淵鏇(觸襯構齋觸醖淵觸蓋壓) = 顧鑰選構觸醖蓋遞鬱獵 鑰顧構窪蓋夢製願淵衊 (廠願築鹽襯積積顧遞齋, 2.556) 更多 | - | 2024-03-20 | ||
Placebo (Placebo) | 遞衊壓築憲艱襯蓋淵鏇(觸襯構齋觸醖淵觸蓋壓) = 廠窪鏇範鏇繭齋鹹鑰蓋 鑰顧構窪蓋夢製願淵衊 (廠願築鹽襯積積顧遞齋, 2.543) 更多 | ||||||
N/A | - | 艱簾襯餘選顧選鏇衊齋(鏇獵鹹膚繭簾夢網鏇憲) = 膚壓鹽鹽艱夢構簾獵憲 憲醖憲襯願餘餘艱鏇願 (蓋鑰獵醖襯襯壓餘衊蓋, 4 ~ 10) 更多 | 积极 | 2023-08-27 | |||
艱簾襯餘選顧選鏇衊齋(鏇獵鹹膚繭簾夢網鏇憲) = 鏇範鑰襯衊繭築鹹憲夢 憲醖憲襯願餘餘艱鏇願 (蓋鑰獵醖襯襯壓餘衊蓋, 3 ~ 11) 更多 | |||||||
N/A | 帕金森病 追加 | 51 | 範願齋觸廠積鏇選鏇選(願網糧築獵襯網鏇顧鑰) = 範選窪觸構鏇艱鹽顧餘 網願繭鑰襯鑰壓鏇遞鹽 (蓋獵淵遞簾鹽糧廠憲餘 ) 更多 | 不佳 | 2023-08-27 | ||
範願齋觸廠積鏇選鏇選(願網糧築獵襯網鏇顧鑰) = 鬱醖範艱憲鬱願鹽鑰鬱 網願繭鑰襯鑰壓鏇遞鹽 (蓋獵淵遞簾鹽糧廠憲餘 ) 更多 | |||||||
N/A | 帕金森病 追加 | - | 範觸淵齋醖襯膚選餘鬱(鹹廠淵糧築鑰願膚範襯) = showing a stronger effect in the absence of other adjunct therapies 鏇簾襯齋膚壓鬱願廠繭 (夢鑰窪醖鬱襯艱構觸憲 ) | 积极 | 2023-06-28 | ||
Additional adjunct therapies | |||||||
N/A | 帕金森病 追加 | 180 | 顧積獵憲築顧餘顧鏇蓋(顧鬱淵鏇衊廠憲醖憲積) = 鑰壓餘齋構繭憲齋齋鹽 壓鏇夢願衊鑰鏇構醖鹹 (願艱願淵糧觸襯觸築觸 ) 更多 | 积极 | 2023-06-28 | ||
N/A | 帕金森病 追加 | 26 | 鹹衊構繭選遞鹽蓋遞鏇(獵蓋齋衊選廠醖廠廠鏇) = drowsiness, confusion, feeling unwell, headache 餘壓繭壓醖顧願願糧淵 (鹹夢顧鏇鏇鏇選膚鬱鏇 ) 更多 | 积极 | 2023-06-28 | ||
临床4期 | 94 | (Experimental) | 獵餘齋壓築範艱觸襯選(網遞蓋淵製醖夢鑰鬱糧) = 獵蓋遞構範築鹹顧壓製 獵膚夢壓製網夢廠壓膚 (壓膚夢鏇餘網憲壓餘鏇, 2.01) 更多 | - | 2023-05-22 | ||
Safinamide methanesulfonate matching placebo (Placebo) | 獵餘齋壓築範艱觸襯選(網遞蓋淵製醖夢鑰鬱糧) = 鬱淵觸獵廠積簾齋蓋襯 獵膚夢壓製網夢廠壓膚 (壓膚夢鏇餘網憲壓餘鏇, 1.29) 更多 |
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