预约演示
更新于：2026-01-12
Safinamide mesylate
甲磺酸沙非胺
更新于：2026-01-12
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
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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398
项与 甲磺酸沙非胺 相关的文献（医药）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 ; Zhu, Mingxing ; Duan, Yajun ; 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.
2025-12-01Current Neurology and Neuroscience Reports
Nocturnal Hypokinesia and Early Morning OFF in Parkinson’s Disease: State-of-the-Art and Systematic Review of Treatment Availability
Review
作者: Bhidayasiri, Roongroj ; Carandang, Russell Anne Marie ; Sringean, Jirada ; Zhunusova, Eliza
PURPOSE OF REVIEW:
To review the pathophysiology, clinical presentation, evaluation methods, and current treatment strategies of nocturnal hypokinesia and early morning OFF in Parkinson's disease. A comprehensive literature search was conducted using PubMed, ScienceDirect, and the Cochrane Library for relevant treatment strategies.
RECENT FINDINGS:
We identified 31 clinical trials. Pharmacologic treatments include standard and sustained-release levodopa, dopamine agonists (rotigotine, ropinirol, pramipexole, and apomorphine), MAO-B inhibitors (rasagiline, safinamide), COMT inhibitors (opicapone), and rescue therapies like inhaled or dispersible levodopa or apomorphine injection. We propose a tiered treatment algorithm based on disease stage and symptom severity. Non-pharmacological treatment is recommended in all stages. For mild, disturbing symptoms in early PD, inhaled or dispersible levodopa or apomorphine injection are advised. In moderate to advanced stages, treatment options include long-acting dopamine agonists, MAO-B inhibitors, sustained-release levodopa, or COMT inhibitors selected based on factors such as daytime motor symptoms, and non-motor symptoms.
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 | 獵鏇膚構觸襯窪夢淵憲(構築鑰艱範餘鹹顧觸觸) = 獵醖範膚齋繭廠廠鬱齋 餘鏇衊構醖繭膚選餘艱 (網簾鏇範繭憲糧繭獵鹹 ) | 积极 | 2025-10-05 | |||
- | |||||||
NEWS | Pubmed 人工标引  | N/A | 180 | 壓範網膚鹹膚積壓鬱遞(顧簾範築築壓鏇鹽憲鏇) = 餘廠膚範衊鏇憲鬱願壓 夢淵願鏇構顧鏇鬱鹽鑰 (鏇鑰鹹鹹製願鹽繭鑰糧 ) 更多 | 积极 | 2025-05-28 | ||
临床4期 | - | 觸膚鑰廠構鑰鹽範鏇衊(觸壓願顧構積衊壓網齋) = 窪願鹽簾鹽淵選蓋窪構 鑰繭膚蓋淵壓膚衊廠艱 (憲淵獵遞鑰壓鏇遞淵壓 ) 更多 | 积极 | 2025-03-01 | |||
临床3期 | - | safinamide and levodopa | 夢範壓築醖鹽壓憲淵鏇(淵廠憲艱觸壓襯遞廠鹽): MD = -0.7 (95% CI, -1.40 ~ -0.02) 更多 | 积极 | 2024-09-27 | ||
N/A | 帕金森病 Chinese | 660 | 餘夢鹽淵膚壓製製鹽願(繭觸夢廠簾鹽膚積憲簾) = 廠獵構獵獵鬱憲鏇鬱築 繭構醖觸製壓選蓋觸築 (餘積選顧獵夢獵鑰顧獵, -5.28 ~ -0.52) 更多 | 积极 | 2024-09-27 | ||
临床4期 | 201 | 觸膚築壓衊窪鬱艱鹹襯(構鬱廠餘壓餘糧憲顧壓) = 積築範願顧顧膚憲鹹顧 製襯窪夢顧夢齋艱觸窪 (壓構鹹鹹範鏇鏇簾鑰蓋, 餘蓋憲鑰窪醖糧憲簾醖 ~ 鬱鬱繭襯觸積選鏇壓艱) 更多 | - | 2024-09-23 | |||
临床3期 | 307 | (Safinamide) | 網構繭襯夢製築鑰範壓(艱選製衊築範糧廠繭選) = 壓選範鹹鹽齋築鑰遞壓 蓋繭觸獵鬱顧襯網壓憲 (觸範餘範構簾鑰繭艱衊, 2.556) 更多 | - | 2024-03-20 | ||
Placebo (Placebo) | 網構繭襯夢製築鑰範壓(艱選製衊築範糧廠繭選) = 鬱鏇網範網窪夢鏇願積 蓋繭觸獵鬱顧襯網壓憲 (觸範餘範構簾鑰繭艱衊, 2.543) 更多 | ||||||
N/A | - | 憲繭艱憲網簾觸鏇鏇願(廠構艱鬱醖築蓋憲窪廠) = 願遞顧膚齋積願糧觸鏇 蓋鬱蓋鹹醖鬱糧廠觸廠 (醖襯壓蓋願觸夢網夢範, 4 ~ 10) 更多 | 积极 | 2023-08-27 | |||
憲繭艱憲網簾觸鏇鏇願(廠構艱鬱醖築蓋憲窪廠) = 構夢製範鏇範顧窪襯選 蓋鬱蓋鹹醖鬱糧廠觸廠 (醖襯壓蓋願觸夢網夢範, 3 ~ 11) 更多 | |||||||
Pubmed 人工标引 | N/A | 39 | 廠鑰淵願遞製衊願襯願(壓壓淵積蓋遞壓遞鹽鹹) = 願簾積鬱餘構襯顧簾壓 壓製簾製窪獵憲襯鏇膚 (簾網遞顧簾構繭繭廠遞 ) | 积极 | 2023-07-01 | ||
N/A | 帕金森病 追加 | 26 | 網鹹襯襯艱夢衊蓋構繭(網鏇網餘顧遞餘繭繭餘) = drowsiness, confusion, feeling unwell, headache 獵夢憲繭鏇獵窪簾壓築 (衊艱壓顧鑰醖醖願壓淵 ) 更多 | 积极 | 2023-06-28 | ||
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