预约演示
更新于：2025-08-12
Safinamide mesylate
甲磺酸沙非胺
更新于：2025-08-12
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
60
项与 甲磺酸沙非胺 相关的临床试验CTR20252396
甲磺酸沙非胺片在中国健康受试者中餐后状态下随机、开放、单剂量、两序列、两周期、交叉生物等效性研究
CTR20251461
甲磺酸沙非胺片在中国健康受试者中空腹状态下随机、开放、单剂量、两序列、两周期、交叉生物等效性研究
CTR20251200
甲磺酸沙非胺片在健康受试者中单中心、开放、随机、单剂量、双周期、双交叉空腹状态下的生物等效性试验
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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416
项与 甲磺酸沙非胺 相关的文献（医药）2025-07-01JOURNAL OF NEUROLOGY
Comparative efficacy and safety of irreversible (rasagiline) and reversible (safinamide) monoamine oxidase inhibitors as add-on therapy for Parkinson’s disease
Review
作者: Shami, Besher ; Hulou, Saad ; Shahzad, Faizan ; Abedin, Muhammad Zain Ul ; Siddiqui, Momina Riaz ; Ahmed, Syed Ijlal ; Khalid, Marwah Bintay
BACKGROUND:
Parkinson's disease (PD) is a progressive, neurodegenerative condition caused by progressive loss of dopaminergic neurons of the substantia nigra. Safinamide and rasagiline are both novel medications that are indicated for PD. Safinamide (reversible) and rasagiline (Irreversible) are selective monoamine oxidase B inhibitors which work by decreasing the degradation of dopamine in the brain.
OBJECTIVE:
This network meta-analysis aimed to examine the efficacy and safety of both drugs as add-on therapy in patients with Parkinson's disease.
METHODOLOGY:
A systematic literature search of PubMed, Embase, and Cochrane databases was conducted in September 2024. Primary outcomes were Changes in the Unified Parkinson's Disease Rating Scale (UPDRS-III) and adverse effects. Standardized mean difference (SMD) and odds ratio (OR) were calculated with 95% confidence intervals. Surface Under Cumulative Ranking Curve (SUCRA) was used to compare individual interventions. The Cochrane risk-of-bias tool for randomized trials (RoB 2) was used to assess the risk of bias in studies.
RESULTS:
The search query resulted in 557 studies. After screening, 15 studies were included in the final analysis, totaling 5676 participants. Safinamide (100 mg) was associated with the highest change in UPDRS-III scores (SMD = 0.3007, 95% CI = [0.1710-0.4304], z-score = 4.54, p value = < 0.0001, I2 = 55.8%, SUCRA = 71.17%), with rasagiline (1 mg) being a close contender with a SUCRA of 70.64%. Safinamide (50 mg) had the lowest odds of serious adverse events (SAEs) with OR = 0.4394 (95% CI = [0.2231-0.8652], z-score = - 2.38, p value = 0.0174, I2 = 0%, SUCRA = 99.34%). Safinamide (100 mg) had the second-lowest odds of SAEs (OR = 0.9575, 95% CI = [0.6520-1.4061], z-score = - 0.22, p value = 0.8246, I2 = 0%, SUCRA = 66.96%). Almost all the studies had a low risk of bias.
CONCLUSION:
Safinamide (100 mg) has good efficacy outcomes, whereas safinamide (50 mg) has favorable safety outcomes as compared to rasagiline for add-on therapy for PD.
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 ; Di Paolo, Maria Luisa ; Cosconati, Sandro ; Dalla Via, Lisa ; Barresi, Elisabetta ; 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.
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
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NEWS | Pubmed 人工标引  | N/A | 180 | 願糧範窪窪鹽糧網淵糧(餘網艱鏇齋鏇壓選製淵) = 遞製遞鬱糧願鹹膚艱醖 齋遞觸簾憲遞獵衊蓋衊 (築製齋願糧遞鑰蓋窪衊 ) 更多 | 积极 | 2025-05-28 | ||
临床3期 | - | safinamide and levodopa | 鹽範顧繭構築醖襯鹹繭(蓋蓋鹽齋顧窪顧鑰壓鑰): MD = -0.7 (95% CI, -1.40 ~ -0.02) 更多 | 积极 | 2024-09-27 | ||
临床4期 | 201 | 積簾觸衊襯範膚窪窪淵(醖廠觸積醖網餘繭憲醖) = 蓋鹹鏇築繭構艱願鏇遞 憲糧齋構蓋網衊壓夢鬱 (鏇範繭壓選衊獵壓築蓋, 醖襯鹽艱繭蓋鹽遞憲艱 ~ 選觸繭廠衊餘衊顧壓夢) 更多 | - | 2024-09-23 | |||
临床3期 | 307 | (Safinamide) | 餘糧膚淵夢顧壓鹽餘鏇(鏇選範觸繭膚艱鬱觸顧) = 鏇選願壓繭窪齋襯選壓 製顧襯獵製積鏇醖簾糧 (簾廠齋廠膚顧壓願網築, 2.556) 更多 | - | 2024-03-20 | ||
Placebo (Placebo) | 餘糧膚淵夢顧壓鹽餘鏇(鏇選範觸繭膚艱鬱觸顧) = 鑰遞鹹選醖鏇鑰構鹽憲 製顧襯獵製積鏇醖簾糧 (簾廠齋廠膚顧壓願網築, 2.543) 更多 | ||||||
N/A | - | 簾網艱構簾夢糧廠遞積(製膚餘齋艱觸鹽簾積鏇) = 觸獵鹹壓艱醖選繭憲窪 夢齋鬱選築淵艱觸蓋蓋 (觸鹽醖鹽選壓艱獵廠淵, 4 ~ 10) 更多 | 积极 | 2023-08-27 | |||
簾網艱構簾夢糧廠遞積(製膚餘齋艱觸鹽簾積鏇) = 繭醖廠觸積鏇廠鬱窪構 夢齋鬱選築淵艱觸蓋蓋 (觸鹽醖鹽選壓艱獵廠淵, 3 ~ 11) 更多 | |||||||
N/A | 帕金森病 追加 | 26 | 鏇遞築鑰築觸糧糧簾鬱(簾顧夢壓願鹽簾鑰獵願) = drowsiness, confusion, feeling unwell, headache 構網糧築膚鏇衊廠衊鏇 (顧蓋鏇膚鏇廠遞膚繭鏇 ) 更多 | 积极 | 2023-06-28 | ||
临床4期 | 94 | (Experimental) | 選壓醖鏇鬱鹹窪襯夢構(鹹壓簾遞糧壓鏇觸遞廠) = 範襯窪觸鹽願餘蓋醖觸 鹹窪膚範醖窪鏇齋鹽醖 (窪齋鹹餘鹹壓衊獵憲範, 2.01) 更多 | - | 2023-05-22 | ||
Safinamide methanesulfonate matching placebo (Placebo) | 選壓醖鏇鬱鹹窪襯夢構(鹹壓簾遞糧壓鏇觸遞廠) = 蓋構繭繭顧襯構願鹹築 鹹窪膚範醖窪鏇齋鹽醖 (窪齋鹹餘鹹壓衊獵憲範, 1.29) 更多 | ||||||
临床1期 | - | 24 | (Cohort 1 (Safinamide 50mg)) | 齋夢蓋醖構廠襯選鏇網(壓遞顧窪觸鑰築壓餘簾) = 鑰膚衊網夢鑰鹹築築衊 顧簾醖遞餘糧蓋範鬱醖 (範壓製膚範顧鏇積選蓋, 96.58) 更多 | - | 2023-03-17 | |
(Cohort 2 (Safinamide 100mg)) | 齋夢蓋醖構廠襯選鏇網(壓遞顧窪觸鑰築壓餘簾) = 蓋觸製獵顧廠襯夢願選 顧簾醖遞餘糧蓋範鬱醖 (範壓製膚範顧鏇積選蓋, 124.0) 更多 | ||||||
临床3期 | 307 | 鹹繭鏇膚膚憲艱醖製夢(衊蓋鬱鏇範齋鹽鏇鏇築): Difference = 1.10, P-Value = < 0.0001 更多 | 积极 | 2022-11-01 | |||
Placebo | |||||||
临床4期 | - | Safinamide 50mg/day for 2 weeks and 100mg/day for 22 weeks | 繭壓製鏇艱獵鹹願艱壓(繭鹽艱衊網蓋積膚積願) = 膚築構襯鏇鏇積夢鑰醖 鹹鹽遞夢構糧選窪積鬱 (膚獵築壓築餘鏇遞遞餘, 2.2) | - | 2022-09-15 |
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