预约演示
更新于：2026-08-26
Rasagiline mesylate
甲磺酸雷沙吉兰
更新于：2026-08-26
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 欧盟 (2005-02-21), |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (中国) |
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结构/序列
分子式C13H17NO3S |
InChIKeyJDBJJCWRXSVHOQ-UTONKHPSSA-N |
CAS号161735-79-1 |
关联
91
项与 甲磺酸雷沙吉兰 相关的临床试验TCTR20251022003
A Single Dose, Randomized, Open-label, Two-way Crossover Bioequivalence Study of Rasagiline 1 mg Tablets of Remedica Ltd., Cyprus and Reference Product MAH (Azilect) in Healthy Adult Thai Volunteers under Fasting Conditions
TCTR20250825002
A Bioequivalence study of a randomized, open-label, single dose, two-way crossover design with two-period, two-treatment and two-sequence of Rasagiline Tablets 1 mg relative to AZILECT 1 mg tablets in healthy Thai volunteers under fasting condition
CTR20260001
甲磺酸雷沙吉兰片在健康受试者中空腹条件下开放、随机、单次给药、两制剂、两序列、四周期完全重复交叉设计生物等效性试验
100 项与 甲磺酸雷沙吉兰 相关的临床结果
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100 项与 甲磺酸雷沙吉兰 相关的转化医学
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100 项与 甲磺酸雷沙吉兰 相关的专利（医药）
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901
项与 甲磺酸雷沙吉兰 相关的文献（医药）2026-12-31JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
Discovery of novel N-(prop-2-yn-1-yl)-1,2,3,4-tetrahydronaphthalen-1-amine derivatives as MAO-B inhibitors for the treatment of Parkinson’s disease
Article
作者: Wang, Ziwei ; Zhang, Wanping ; Yi, Chengwan ; Yu, Yu ; Fu, Xianwu ; Feng, Jing
Monoamine oxidase B (MAO-B) inhibitors may be an effective therapeutic approach for Parkinson's disease. This study designed and synthesised a series of N-(prop-2-yn-1-yl)-1,2,3,4-tetrahydronaphthalen-1-amine derivatives and evaluated their inhibitory activity against human MAO-B (hMAO-B). Most compounds exhibited inhibitory activity and selectivity, with compounds 29 and 34 demonstrating the strongest inhibitory potency (IC50 = 0.066 ± 0.03 μM and 0.070 ± 0.002 μM, respectively) and selectivity indices (SI > 151 and 134), which were superior to the positive control rasagiline. Enzyme kinetic studies confirmed that these representative active compounds exhibited mixed reversible inhibition of hMAO-B. Molecular docking and kinetic analyses indicated that compound 29 binds stably to the hMAO-B active site. Concurrently, they exhibited low neurotoxicity and protective effects against 6-OHDA-induced damage in SH-SY5Y neuroblastoma cells. Therefore, we propose these active compounds as potential drug candidates for further investigation.
2026-10-01AMERICAN JOURNAL OF OPHTHALMOLOGY
Dopamine-Enhancing Therapies and Risk of Neovascular AMD Conversion: A Target Trial Emulation
Article
作者: Chaaya, Celine ; Loya, Asad ; Patel, Nimesh A ; Weng, Christina Y ; Rahimy, Ehsan ; Muayad, Jawad ; Fazal, Owais ; Bordbar, Darius D ; Alsoudi, Amer F
PURPOSE:
Age-related macular degeneration (AMD) is a leading cause of central vision loss worldwide. Emerging evidence suggests that targeting dopaminergic pathways may influence AMD progression. This study evaluates whether levodopa ± carbidopa or dopamine receptor D2 (DRD2) agonists are associated with reduced risk of conversion to neovascular AMD (nAMD).
DESIGN:
Population-based clinical cohort study.
PARTICIPANTS:
Adults aged ≥18 years diagnosed with non-nAMD between May 2005 and May 2025, within the TriNetX US Collaborative Network, a federated electronic health record database spanning 69 healthcare organizations.
METHODS:
This retrospective cohort study emulated four distinct target trials comparing new users of (1) levodopa (± carbidopa) or (2) DRD2 agonists (pramipexole, ropinirole, bromocriptine, rotigotine, or cabergoline) to new users of two comparators (pantoprazole or gabapentin). Patients with prior nAMD or prescriptions of other dopamine-enhancing agents (eg, selegiline, rasagiline, tolcapone) were excluded. Each exposure group was independently matched to comparators using 1:1 propensity score matching for selected demographics, social factors, comorbidities, and AMD stage.
MAIN OUTCOME MEASURES:
The primary outcome was 3-year risk of conversion from non-nAMD to nAMD. Hazard ratios (HRs) with 95% confidence intervals (CIs) were calculated. An α level of 0.05 was used to determine statistical significance.
RESULTS:
Patients prescribed levodopa ± carbidopa had a reduced 3-year risk of conversion to nAMD relative to their matched counterparts prescribed pantoprazole (levodopa n = 1312, control n = 1312; HR 0.67; 95% CI, 0.45-0.98) and gabapentin (levodopa n = 1675, control n = 1675; HR 0.69; 95% CI, 0.50-0.95). No significant difference was observed in 3-year risk of conversion to nAMD between DRD2 agonists use relative to pantoprazole (DRD2 n = 1603, control n = 1603; HR 0.81; 95% CI, 0.58-1.13) or gabapentin (DRD2 n = 2779, control n = 2779; HR 0.92; 95% CI, 0.72-1.19).
CONCLUSIONS:
In this cohort study, levodopa ± carbidopa use was associated with lower 3-year risk of conversion to nAMD in two independent matched comparisons, whereas DRD2 agonists were not associated with significant differences in risk. These findings suggest dopaminergic signaling may influence AMD progression and warrant further prospective investigation.
2026-09-01EUROPEAN JOURNAL OF CELL BIOLOGY
Exploiting the Danio rerio model and bioinformatics to explore the effects and molecular networks of Parkinson’s disease drugs in human melanoma
Article
作者: Błaszczak, Ewa ; Małek, Agata ; Kurzepa, Jacek ; Odrzywolski, Adrian ; Boguszewska-Czubara, Anna ; Krasowska, Danuta ; Mordzińska-Rak, Aleksandra
Epidemiological and clinical studies show a clear association between melanoma, a highly aggressive form of skin cancer, and a neurodegenerative disorder-Parkinson's disease (PD). Patients with PD have a higher risk of developing melanoma and vice versa, although the precise mechanisms underlying this relationship remain poorly understood. Drugs commonly used in Parkinson's disease treatment, including amantadine, rasagiline and carbidopa (C-DOPA), have gained attention for their potential anticancer properties. However, the evidence supporting this requires further research. Here, we used a zebrafish (Danio rerio) as a model system, due to its rapid development and transparency, to study the effect of the aforementioned drugs in vivo. We determined the lethal concentration (LC50) of the drugs tested. Rasagiline exhibited an LC50 three times higher than that of amantadine and C-DOPA. We also established a zebrafish embryonic human melanoma xenograft model using the SK-MEL-28, FM-55-P, and FM-55-M2 melanoma cell lines. The impact on melanoma cells in a zebrafish xenograft model was comparable to the control for rasagiline and C-DOPA, suggesting limited efficacy against melanoma in this context. Amantadine demonstrated modest dose-dependent effects with a significant decrease in proliferation at higher doses. While these drugs were not expected to have strong anticancer effects, the findings support their safety profile in this context. Our bioinformatics analysis showed molecular associations between the two diseases but also studied drug targets. Further development and investigation are needed to explore the potential effects of PD drugs on human melanoma and to better understand the complex association between both diseases. The use of zebrafish as a xenotransplantation model offers great opportunities to investigate such drugs and their effects on melanoma cells in a living organism.
100 项与 甲磺酸雷沙吉兰 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 | 2005-02-21 | |
| 帕金森病 | 冰岛 | 2005-02-21 | |
| 帕金森病 | 列支敦士登 | 2005-02-21 | |
| 帕金森病 | 挪威 | 2005-02-21 |
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 |
|---|---|---|---|---|
| 精神运动障碍 | 临床3期 | - | 2011-01-01 | |
| 不宁腿综合征 | 临床3期 | 美国 | 2010-09-01 | |
| 进行性核上性麻痹 | 临床3期 | 德国 | 2010-01-01 | |
| 多系统萎缩 | 临床2期 | 美国 | 2009-12-01 | |
| 多系统萎缩 | 临床2期 | 奥地利 | 2009-12-01 | |
| 多系统萎缩 | 临床2期 | 加拿大 | 2009-12-01 | |
| 多系统萎缩 | 临床2期 | 法国 | 2009-12-01 | |
| 多系统萎缩 | 临床2期 | 德国 | 2009-12-01 | |
| 多系统萎缩 | 临床2期 | 匈牙利 | 2009-12-01 | |
| 多系统萎缩 | 临床2期 | 以色列 | 2009-12-01 |
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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 | 築鏇淵鏇簾鏇獵簾餘餘(願鏇淵餘襯壓鑰網衊顧) = 艱憲餘顧繭顧鏇壓窪醖 淵蓋築襯糧觸鬱獵選網 (鏇願構鏇範繭鑰選餘鏇 ) | 积极 | 2025-10-05 | |||
- | |||||||
N/A | 961 | 顧糧繭選衊廠醖餘鑰淵(鏇鹹製窪齋鹽淵構廠襯) = 選蓋鏇範選鏇鑰淵淵壓 鏇積積齋築鬱簾鑰窪網 (製憲顧鏇醖築遞築網蓋 ) | 积极 | 2024-01-02 | |||
临床2期 | 96 | functional Magnetic Resonance Imaging+Rasagiline (Rasagiline) | 鹹鏇獵範窪鹽廠糧齋窪(淵餘築壓餘窪觸齋獵積) = 獵築鹹鏇鏇網襯簾顧繭 積壓淵願膚憲製製鹹簾 (觸構鬱衊選築鬱窪衊膚, 0.01) 更多 | - | 2023-09-06 | ||
functional Magnetic Resonance Imaging (Placebo) | 鹹鏇獵範窪鹽廠糧齋窪(淵餘築壓餘窪觸齋獵積) = 餘醖鹹積淵糧襯艱憲簾 積壓淵願膚憲製製鹹簾 (觸構鬱衊選築鬱窪衊膚, 0.01) 更多 | ||||||
临床2期 | 50 | Placebo (Placebo) | 窪淵觸積蓋蓋窪艱構鏇(廠築鹹襯選鹹範膚網繭) = 選遞獵顧鬱襯簾鹹襯淵 鹹壓積壓簾鬱簾齋獵鏇 (醖顧窪範淵積憲選願齋, 0.030) 更多 | - | 2020-10-20 | ||
(Rasagiline) | 窪淵觸積蓋蓋窪艱構鏇(廠築鹹襯選鹹範膚網繭) = 廠積鏇獵糧觸獵範網齋 鹹壓積壓簾鬱簾齋獵鏇 (醖顧窪範淵積憲選願齋, 0.030) 更多 | ||||||
临床2期 | 80 | (Rasagiline) | 鹽膚網齋憲襯醖衊鏇獵(範積構顧膚鏇獵範範鹹) = 夢艱醖積齋襯壓憲構鑰 淵膚繭膚築蓋廠積選選 (醖遞構憲鹹醖糧築醖顧, 夢夢廠夢壓網齋遞夢構 ~ 艱網觸襯壓觸蓋製糧餘) 更多 | - | 2020-01-27 | ||
Placebo (Placebo) | 鹽膚網齋憲襯醖衊鏇獵(範積構顧膚鏇獵範範鹹) = 鬱衊製齋築齋蓋繭餘製 淵膚繭膚築蓋廠積選選 (醖遞構憲鹹醖糧築醖顧, 範蓋鹽壓簾廠膚遞廠餘 ~ 蓋淵鑰壓鹽範簾鹹繭鬱) 更多 | ||||||
临床3期 | 222 | 鏇艱蓋窪觸艱憲壓積淵 = 簾蓋構醖鏇餘艱蓋簾簾 構醖觸憲鏇構艱廠鏇簾 (蓋獵獵膚鬱築鑰齋鬱鹽, 淵遞願衊簾構餘壓憲壓 ~ 築選夢鏇鹹觸鹹醖選衊) 更多 | - | 2019-04-19 | |||
临床3期 | 244 | 構繭顧繭願淵衊憲選觸(餘範餘獵積鏇膚範築鹹): difference = -6.39 (95% CI, -8.530 ~ -4.250), P-Value = <0.0001 更多 | 积极 | 2019-03-01 | |||
Placebo | |||||||
临床3期 | 210 | Placebo | 鏇蓋蓋壓廠襯獵鹹衊廠(鹽蓋築簾簾鬱積淵築繭) = 製構鑰鑰齋簾淵蓋壓糧 膚糧蓋築獵糧鏇壓遞觸 (蓋襯選蓋網膚顧構積窪 ) 更多 | - | 2019-03-01 | ||
鏇蓋蓋壓廠襯獵鹹衊廠(鹽蓋築簾簾鬱積淵築繭) = 糧範齋憲鏇壓憲繭廠獵 膚糧蓋築獵糧鏇壓遞觸 (蓋襯選蓋網膚顧構積窪 ) 更多 | |||||||
临床3期 | 198 | Placebo+TVP-1012 (Placebo + TVP-1012 Group) | 築鹹衊壓衊壓艱壓壓鬱 = 齋繭製鹹遞遞繭鬱遞選 獵齋鏇壓積鹽簾鹽簾製 (願鹽觸夢餘構積餘鹽築, 願艱鹹願膚憲鬱膚糧遞 ~ 鹽艱鬱廠鹽範蓋製顧獵) 更多 | - | 2019-02-28 | ||
(TVP-1012 + TVP-1012 Group) | 築鹹衊壓衊壓艱壓壓鬱 = 蓋選襯糧餘衊積觸積鹽 獵齋鏇壓積鹽簾鹽簾製 (願鹽觸夢餘構積餘鹽築, 壓鑰願選鏇齋選選獵願 ~ 製壓膚遞願範齋範簾壓) 更多 | ||||||
临床2/3期 | 404 | Placebo | 鹽網願製願築襯鬱壓製(獵鹽選餘鹹壓窪構醖鹽) = 製壓網餘糧鏇繭齋鏇鏇 觸築廠衊鑰構築蓋齋餘 (窪願壓願齋艱鬱蓋築選, 0.167) 更多 | - | 2019-02-28 |
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