预约演示
更新于：2026-01-27
Safinamide mesylate
甲磺酸沙非胺
更新于：2026-01-27
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CTIS2025-521512-20-00
EFFECTS OF SAFINAMIDE VERSUS PLACEBO ON PAIN IN PATIENTS WITH PARKINSON’S DISEASE WITH MOTOR FLUCTUATIONS: A RANDOMIZED, CONTROLLED, DOUBLE-BLIND CLINICAL TRIAL. Protocol code: SAVE PAIN 2025
CTR20252464
甲磺酸沙非胺片（100mg）在中国健康受试者中餐后给药条件下随机、开放、单剂量、两序列、两周期、双交叉生物等效性试验
CTR20253904
中国健康参与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
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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402
项与 甲磺酸沙非胺 相关的文献（医药）2026-04-01SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
An hMAO-B-activatable mitochondrial binding fluorescent probe in live-cell via enzyme-anchored and charge-driven dual targeting
Article
作者: Hu, Yufei ; Yao, Xinyi ; Mi, Pengbing ; Li, Xiongwang ; Ma, Lin ; Yuan, Zhonghua ; Lin, Rong ; Li, Siqi ; Lang, Jia-Jia
Enzyme-responsive (ER) probes trageting human monoamine oxidase B (hMAO-B) represent pivotal tools for investigating a variety of diseases, including neurodegenerative pathologies, liver diseases, heart failure, metabolic disorders and cancers. Herein, we report THT-MTP-a thiochromone-based fluorescent probe exhibiting highly sensitivity and specificity for hMAO-B that undergoes hMAO-B-catalyzed oxidative conversion of its MTP moiety to MPy+, along with >100-fold fluorescence enhancement. Its activation mechanism was validated through safinamide-inhibition assays in both enzyme and cellular models. The hMAO-B-activatable imaging capability demonstrates intensity proportionality to enzyme levels across cell lines with differential MAO-B expression (HepG2 > SH-SY5Y ≫ NIH-3T3). THT-MTP exhibited excellent mitochondrial accumulation via enzyme-anchored and charge-driven dual targeting. This work establishes a design paradigm for hMAO-B-selectvie probes combining high-precision subcellular targeting, activatable imaging capability and wash-free operation, offering a robust molecular tool for investigating hMAO-B-associated diseases.
2026-01-01JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
Evaluation of novel selective MAO-B inhibitors using immobilized enzymes on magnetic beads
Article
作者: da Silva, Matheus Müller Pereira ; Dos Reis, Vitor Eduardo Narciso ; Viegas, Claudio ; Franco, Graziella Dos Reis Rosa ; Dardenne, Laurent Emmanuel ; de Souza, Mikaela Lucinda ; Alvim Guedes, Isabella ; Cardoso, Carmen Lúcia
Monoamine oxidase A (MAO-A) and B (MAO-B) are critical enzymes involved in regulating neurotransmitters such as dopamine, serotonin, and norepinephrine. Dysregulated MAO activity is associated with neurological disorders, including Parkinson's disease, depression, and cardiovascular diseases, making MAO-A and MAO-B important therapeutic targets. Here, we present a novel assay using MAOs immobilized on magnetic beads (MB) in an immobilized enzyme reactor configuration (MAO-MB) to screen for selective MAO-A and MAO-B inhibitors. The immobilization of both enzymes proved efficient, as no protein was detected in the supernatant after the process by the Bradford assay. Enzyme activity was quantified using HPLC-MS, and kinetic parameters were evaluated, with apparent Michaelis-Menten constants (Kmapp) of 19.36 ± 0.71 µM for MAO-A-MB and 38.85 ± 1.70 µM for MAO-B-MB. The assay was qualified with toloxatone and safinamide as reference inhibitors, yielding IC50 values of 3.42 ± 0.11 µM and 33.38 ± 1.38 nM, respectively. Additionally, a collection of terpenyl-benzohydrazides was screened, identifying PQM-244 (5c) as a selective MAO-B inhibitor (IC50 = 4.17 ± 0.082 µM) with a non-competitive inhibition mechanism (Ki = 2.28 ± 0.38 µM). These findings suggest that 5c (PQM-244) has significant potential to contribute to developing selective MAO-B inhibitors for Parkinson's disease therapy.
2025-12-01EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Design, synthesis, and biological evaluation of highly potent and selective hMAO-B inhibitors featuring a tetrahydrobenzo[f][1,4]oxazepine core
Article
作者: Liao, Chenzhong ; Xie, Xiang-Peng ; Wang, Suqiang ; Xie, Zhouling ; Duan, Yajun ; Zhu, Mingxing ; Zhao, Zhiwei ; Zhang, Xing Xing
The advancement of human monoamine oxidase B (hMAO-B) inhibitors for the management of Parkinson's disease (PD) has seen notable progress, however, the clinical application of existing hMAO-B inhibitors is hindered by their limited efficacy and associated adverse effects. This article presents highly potent and selective hMAO-B inhibitors characterized by either a 2,3,4,5-tetrahydrobenzo[f][1,4]oxazepine core or a 2,3,4,5-tetrahydro-1H-benzo[c]azepine core. These compounds were designed through the cyclization of the amine group with the phenyl ring of safinamide, a second-generation hMAO-B inhibitor that has received approval for PD treatment. Among the synthesized compounds, ZM24 and ZM26, which possess the 2,3,4,5-tetrahydrobenzo[f][1,4]oxazepane core structure, exhibited a significant increase in both efficacy and isoform selectivity relative to safinamide. Subsequent biological assessments revealed that these two compounds act as reversible hMAO-B inhibitors, demonstrate substantial neuroprotective properties, and significantly improve motor dysfunction in MPTP-induced mouse models of PD, thereby reinforcing their potential therapeutic applications in 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 | - | |
| 肝损伤 | 临床1期 | 德国 | 2009-04-01 |
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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
N/A | 160 | 願襯獵鹹獵顧鬱鑰積淵(醖襯願遞選衊顧淵繭衊) = 艱鏇糧蓋鹹構齋鏇壓選 艱遞淵願壓願淵蓋廠範 (夢鬱壓夢願齋範鬱鬱築 ) | 积极 | 2025-10-05 | |||
- | |||||||
NEWS | Pubmed 人工标引  | N/A | 180 | 繭遞願繭願壓夢鬱網醖(糧鹽襯膚顧繭簾鬱齋鬱) = 淵選夢鑰顧廠壓醖範積 鑰鑰網膚簾鹹襯遞夢顧 (壓衊顧壓範餘鹽願膚網 ) 更多 | 积极 | 2025-05-28 | ||
临床4期 | - | 壓憲餘鹽構範襯鏇鏇鬱(簾鹹願鹹襯糧簾糧顧廠) = 網夢糧膚廠網顧簾餘築 製鹽構齋醖鏇廠築簾積 (網蓋築鹹憲廠遞窪遞願 ) 更多 | 积极 | 2025-03-01 | |||
临床3期 | - | safinamide and levodopa | 鏇餘鬱範餘鏇鏇願蓋艱(鬱鹽獵蓋鑰衊襯範鬱醖): MD = -0.7 (95% CI, -1.40 ~ -0.02) 更多 | 积极 | 2024-09-27 | ||
N/A | 帕金森病 Chinese | 660 | 窪鹽蓋艱襯壓繭製艱繭(遞願鑰膚齋網壓鑰選簾) = 壓醖蓋憲壓鹹糧觸鹽鑰 網鹹鏇窪廠鹽築蓋糧憲 (遞壓憲糧觸網襯願觸齋, -5.28 ~ -0.52) 更多 | 积极 | 2024-09-27 | ||
临床4期 | 201 | 願簾壓鏇淵餘窪範襯鏇(製艱廠衊廠構艱鹽淵鑰) = 淵醖窪淵餘憲夢鏇襯膚 鹹憲廠廠鏇製窪蓋網夢 (餘憲壓齋廠顧壓選選鑰, 齋構選鹽艱範鹹鑰衊艱 ~ 壓襯艱繭壓窪膚鑰築鹽) 更多 | - | 2024-09-23 | |||
临床3期 | 307 | (Safinamide) | 醖窪繭鑰顧蓋繭獵衊願(廠鏇製餘遞鏇構襯糧遞) = 顧艱製膚築鏇顧築鏇選 鑰構鏇憲積簾獵壓構淵 (觸網夢鏇鏇襯鏇窪醖築, 2.556) 更多 | - | 2024-03-20 | ||
Placebo (Placebo) | 醖窪繭鑰顧蓋繭獵衊願(廠鏇製餘遞鏇構襯糧遞) = 鏇憲蓋鏇淵鏇鹹艱顧築 鑰構鏇憲積簾獵壓構淵 (觸網夢鏇鏇襯鏇窪醖築, 2.543) 更多 | ||||||
N/A | - | 廠簾遞壓鑰鬱憲積齋齋(衊餘製鏇遞餘顧蓋廠糧) = 艱築糧糧壓顧膚糧夢淵 顧築願繭築窪衊窪積選 (鹹糧顧窪選襯艱範製壓, 4 ~ 10) 更多 | 积极 | 2023-08-27 | |||
廠簾遞壓鑰鬱憲積齋齋(衊餘製鏇遞餘顧蓋廠糧) = 簾夢齋獵淵憲鹹淵窪窪 顧築願繭築窪衊窪積選 (鹹糧顧窪選襯艱範製壓, 3 ~ 11) 更多 | |||||||
Pubmed 人工标引 | N/A | 39 | 遞蓋餘壓範製壓醖鑰壓(鹹簾糧齋醖範襯願醖構) = 構顧鹽憲夢積窪衊淵築 鑰願廠製構廠餘遞夢觸 (遞襯夢窪醖願艱繭餘憲 ) | 积极 | 2023-07-01 | ||
N/A | 帕金森病 追加 | 26 | 蓋構廠壓網繭醖鑰鏇醖(簾築網構鹹築選糧艱膚) = drowsiness, confusion, feeling unwell, headache 鏇製夢夢獵憲顧積襯窪 (糧選夢製願積蓋積襯艱 ) 更多 | 积极 | 2023-06-28 | ||
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