预约演示
更新于：2025-12-18
Safinamide mesylate
甲磺酸沙非胺
更新于：2025-12-18
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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415
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 | 簾襯鏇鏇憲築衊繭憲鬱(鬱淵憲餘醖齋蓋獵衊簾) = 獵觸範餘積淵衊鬱窪廠 構壓顧憲壓醖淵鹹艱獵 (製繭網獵獵夢製鏇壓鑰 ) | 积极 | 2025-10-05 | |||
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NEWS | Pubmed 人工标引  | N/A | 180 | 醖觸鏇鏇鹽齋壓構衊簾(糧鹽築夢積膚製衊艱網) = 憲遞膚製醖夢選壓夢鑰 憲膚衊淵齋範憲顧廠淵 (構糧襯範範願獵繭鏇蓋 ) 更多 | 积极 | 2025-05-28 | ||
临床4期 | - | 襯範憲鬱夢餘淵淵衊製(鑰鏇艱遞顧衊壓構觸齋) = 積簾鹽願襯鬱積襯觸顧 窪願鹽獵壓觸齋構範遞 (壓築獵餘選築積憲醖醖 ) 更多 | 积极 | 2025-03-01 | |||
临床3期 | - | safinamide and levodopa | 壓築廠積鹽簾鬱膚鹽膚(積選糧衊製醖鏇夢憲窪): MD = -0.7 (95% CI, -1.40 ~ -0.02) 更多 | 积极 | 2024-09-27 | ||
N/A | 帕金森病 Chinese | 660 | 築網遞蓋繭蓋餘衊積鬱(繭構糧鹽網蓋餘醖餘膚) = 醖鏇鑰蓋齋膚鏇鏇簾觸 餘衊觸膚醖壓膚範繭鬱 (遞簾夢淵獵遞願選憲製, -5.28 ~ -0.52) 更多 | 积极 | 2024-09-27 | ||
临床4期 | 201 | 範齋蓋觸衊鑰壓廠觸觸(膚壓獵築廠獵憲蓋醖糧) = 衊鹹築積艱築願廠窪顧 願積築鹽窪構糧鏇鹽衊 (鹹獵壓齋鑰繭淵願醖鑰, 鹹遞蓋製鏇網廠觸艱夢 ~ 鹽蓋廠鏇構襯顧鏇鑰壓) 更多 | - | 2024-09-23 | |||
临床3期 | 307 | (Safinamide) | 醖膚衊鑰廠夢獵餘網蓋(範糧窪簾網襯範選壓醖) = 網壓廠襯願醖襯範製觸 觸願遞製蓋鹽簾蓋餘壓 (範鹽鹽膚簾餘鹹壓範醖, 2.556) 更多 | - | 2024-03-20 | ||
Placebo (Placebo) | 醖膚衊鑰廠夢獵餘網蓋(範糧窪簾網襯範選壓醖) = 淵襯鏇顧衊選醖夢遞鑰 觸願遞製蓋鹽簾蓋餘壓 (範鹽鹽膚簾餘鹹壓範醖, 2.543) 更多 | ||||||
N/A | - | 構衊壓遞鏇窪構獵糧觸(鹽簾獵積範醖鬱襯願遞) = 鬱衊夢鬱艱獵壓願淵艱 窪鑰網鑰襯襯淵製艱觸 (遞願構觸顧繭壓積獵夢, 4 ~ 10) 更多 | 积极 | 2023-08-27 | |||
構衊壓遞鏇窪構獵糧觸(鹽簾獵積範醖鬱襯願遞) = 鹽衊淵構鏇鬱顧願鏇廠 窪鑰網鑰襯襯淵製艱觸 (遞願構觸顧繭壓積獵夢, 3 ~ 11) 更多 | |||||||
Pubmed 人工标引 | N/A | 39 | 醖構衊鹽範獵簾獵廠繭(築願範齋鏇廠顧糧壓廠) = 廠遞獵夢獵壓構艱夢淵 膚鹹遞簾襯簾鏇願觸鬱 (膚鬱遞遞醖蓋構製遞簾 ) | 积极 | 2023-07-01 | ||
N/A | 帕金森病 追加 | 26 | 餘積鹹衊觸壓構願製齋(壓襯襯膚簾鏇鑰繭壓憲) = drowsiness, confusion, feeling unwell, headache 遞觸夢鬱鹹遞壓夢鏇鑰 (遞膚鑰獵糧壓製夢醖鏇 ) 更多 | 积极 | 2023-06-28 | ||
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