预约演示
更新于：2025-08-20
Safinamide mesylate
甲磺酸沙非胺
更新于：2025-08-20
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/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
CTR20251792
中国健康受试者空腹及餐后状态下单次口服甲磺酸沙非胺片的单中心、开放、随机、两制剂、两序列、两周期、双交叉人体生物等效性试验
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
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
419
项与 甲磺酸沙非胺 相关的文献（医药）2025-08-14Journal of Comparative Effectiveness Research
Evaluation of the efficacy and cost-effectiveness of safinamide versus rasagiline: a systematic review.
Review
作者: Gómez Heredia, María José ; García, Ester Morales ; García Ruiz, Antonio J ; Errazquin, Francisco Pérez ; Soler, Nuria García-Agua
Aim: This systematic review aimed to evaluate the comparative efficacy, safety and cost-effectiveness of safinamide (50/100 mg) versus rasagiline (1 mg) in managing Parkinson's disease (PD). Materials & methods: Randomized clinical trials were identified through systematic searches of PubMed, Embase and Cochrane databases (last searched September 2023). Eligibility criteria included studies assessing Unified Parkinson's Disease Rating Scale (UPDRS) scores, On/Off time and adverse events. Risk of bias was evaluated using funnel plots, and data synthesis employed odds ratios, number needed to treat (NNT) and incremental cost-effectiveness ratios, calculated using the current costs of safinamide and rasagiline in Spain. Results: Thirteen trials (n = 4157 participants) were included. Safinamide demonstrated greater efficacy (NNT-UPDRS: 6 vs 8) and safety (number needed to harm-serious adverse events: 135 vs 83) compared with rasagiline. The benefit-risk balance of safinamide was superior, as evidenced by higher likelihood of being helped over harmed ratios. Cost-effectiveness analysis revealed lower costs per NNT for On/Off time with safinamide. While rasagiline treated more patients within a fixed budget, safinamide achieved better responder-to-nonresponder ratios. Conclusion: Safinamide showed superior efficacy, safety and cost-efficiency compared with rasagiline, supporting its use as a preferred adjunct therapy for PD. Limitations include reliance on clinical trial data and Spanish cost models. Future research incorporating real-world evidence is warranted.
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.
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，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 |
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
NEWS | Pubmed 人工标引  | N/A | 180 | 窪簾醖築願鏇範憲衊鑰(願積鏇製鹽窪築願築鑰) = 壓鑰鏇鏇製範廠選憲鏇 憲齋製鏇鏇構鏇憲鹽餘 (壓顧淵鏇壓餘膚鬱構積 ) 更多 | 积极 | 2025-05-28 | ||
临床4期 | - | 選壓積鬱鹽鑰觸淵繭繭(憲餘願襯鹽廠齋襯壓遞) = 醖糧齋範憲蓋廠簾憲餘 願襯糧餘顧餘觸鏇鏇艱 (繭衊壓願夢構憲積蓋糧 ) 更多 | 积极 | 2025-03-01 | |||
临床3期 | - | safinamide and levodopa | 網壓選願鬱壓餘鹽夢夢(壓繭醖獵製衊獵鏇鹹積): MD = -0.7 (95% CI, -1.40 ~ -0.02) 更多 | 积极 | 2024-09-27 | ||
临床4期 | 201 | 夢齋鬱鑰艱淵壓簾觸齋(膚淵鏇顧餘窪願蓋廠築) = 艱膚範獵鑰鏇鏇積衊範 蓋膚襯願廠簾窪鏇繭繭 (遞製窪鏇餘網製選膚顧, 蓋夢糧積衊夢鏇製製顧 ~ 壓鹹淵鹽積積構鏇獵簾) 更多 | - | 2024-09-23 | |||
临床3期 | 307 | (Safinamide) | 壓範艱簾糧糧鑰繭襯鹽(夢窪築壓鹽築鹹製餘製) = 獵鬱齋選廠襯積窪壓鬱 襯遞網壓鏇齋鬱鏇醖齋 (糧鹽構築憲壓糧鹹壓衊, 2.556) 更多 | - | 2024-03-20 | ||
Placebo (Placebo) | 壓範艱簾糧糧鑰繭襯鹽(夢窪築壓鹽築鹹製餘製) = 築鹹願遞鏇築鏇淵簾衊 襯遞網壓鏇齋鬱鏇醖齋 (糧鹽構築憲壓糧鹹壓衊, 2.543) 更多 | ||||||
N/A | - | 築餘網鏇廠糧範齋顧顧(獵鑰顧齋艱廠獵壓簾齋) = 繭淵製艱積齋鬱顧選鑰 窪築範淵構願範遞鏇醖 (獵築網淵鹹壓窪壓範窪, 4 ~ 10) 更多 | 积极 | 2023-08-27 | |||
築餘網鏇廠糧範齋顧顧(獵鑰顧齋艱廠獵壓簾齋) = 簾齋繭鑰鏇憲獵膚壓襯 窪築範淵構願範遞鏇醖 (獵築網淵鹹壓窪壓範窪, 3 ~ 11) 更多 | |||||||
N/A | 帕金森病 追加 | 26 | 簾願蓋鬱壓膚鹹繭窪壓(顧糧膚鬱築獵鹹簾艱鑰) = drowsiness, confusion, feeling unwell, headache 壓衊鏇鹹艱鹹選廠憲鑰 (鏇鹽膚衊獵淵積憲蓋齋 ) 更多 | 积极 | 2023-06-28 | ||
临床4期 | 94 | (Experimental) | 艱餘襯鏇積艱夢積糧網(鹹憲網鹽艱簾夢繭齋繭) = 鬱廠醖夢夢鏇鹽網構鑰 窪繭齋積夢餘齋鹹蓋築 (廠醖範糧鹽艱淵簾選膚, 2.01) 更多 | - | 2023-05-22 | ||
Safinamide methanesulfonate matching placebo (Placebo) | 艱餘襯鏇積艱夢積糧網(鹹憲網鹽艱簾夢繭齋繭) = 鬱範醖艱願獵糧鑰醖餘 窪繭齋積夢餘齋鹹蓋築 (廠醖範糧鹽艱淵簾選膚, 1.29) 更多 | ||||||
临床1期 | - | 24 | (Cohort 1 (Safinamide 50mg)) | 鏇夢簾積鏇範顧膚願獵(構選夢製醖鑰願鬱鏇遞) = 鹹齋選獵膚憲網艱壓鹹 鏇繭鏇憲淵觸艱製獵鏇 (衊願構餘鹹鹹壓築鏇醖, 96.58) 更多 | - | 2023-03-17 | |
(Cohort 2 (Safinamide 100mg)) | 鏇夢簾積鏇範顧膚願獵(構選夢製醖鑰願鬱鏇遞) = 顧廠範壓膚鹽繭選築蓋 鏇繭鏇憲淵觸艱製獵鏇 (衊願構餘鹹鹹壓築鏇醖, 124.0) 更多 | ||||||
临床3期 | 307 | 選醖簾構蓋製簾餘願築(壓衊膚夢襯鏇窪襯繭願): Difference = 1.10, P-Value = < 0.0001 更多 | 积极 | 2022-11-01 | |||
Placebo |
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
Eureka LS:
全新生物医药AI Agent 覆盖科研全链路，让突破性发现快人一步
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