更新于：2024-06-24
Rasagiline mesylate
甲磺酸雷沙吉兰
更新于：2024-06-24
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 (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
分子式C13H17NO3S |
InChIKeyJDBJJCWRXSVHOQ-UTONKHPSSA-N |
CAS号161735-79-1 |
关联
92
项与 甲磺酸雷沙吉兰 相关的临床试验在健康受试者中的随机、开放、单次给药、四周期、完全重复交叉、空腹及餐后生物等效性试验
雷沙吉兰舌下膜线性动力学研究及与原研Azilect的生物利用度研究
Efficacy and Safety of Rasagiline in Prodromal Parkinson's Disease
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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691
项与 甲磺酸雷沙吉兰 相关的文献（医药）2024-03-01European journal of neurology
Longitudinal course of neurofilament light chain levels in amyotrophic lateral sclerosis—insights from a completed randomized controlled trial with rasagiline
Article
作者: Ludolph, Albert C ; Steinacker, Petra ; Witzel, Simon ; Schuster, Joachim ; Barohn, Richard J ; Dorst, Johannes ; Otto, Markus ; Statland, Jeffrey M
Abstract:
Background and purpose:
Rasagiline might be disease modifying in patients with amyotrophic lateral sclerosis (ALS). The aim was to evaluate the effect of rasagiline 2 mg/day on neurofilament light chain (NfL), a prognostic biomarker in ALS.
Methods:
In 65 patients with ALS randomized in a 3:1 ratio to rasagiline 2 mg/day (n = 48) or placebo (n = 17) in a completed randomized controlled multicentre trial, NfL levels in plasma were measured at baseline, month 6 and month 12. Longitudinal changes in NfL levels were evaluated regarding treatment and clinical parameters.
Results:
Baseline NfL levels did not differ between the study arms and correlated with disease progression rates both pre‐baseline (r = 0.64, p < 0.001) and during the study (r = 0.61, p < 0.001). NfL measured at months 6 and 12 did not change significantly from baseline in both arms, with a median individual NfL change of +1.4 pg/mL (interquartile range [IQR] −5.6, 14.2) across all follow‐up time points. However, a significant difference in NfL change at month 12 was observed between patients with high and low NfL baseline levels treated with rasagiline (high [n = 13], −6.9 pg/mL, IQR −20.4, 6.0; low [n = 18], +5.9 pg/mL, IQR −1.4, 19.7; p = 0.025). Additionally, generally higher longitudinal NfL variability was observed in patients with high baseline levels, whereas disease progression rates and disease duration at baseline had no impact on the longitudinal NfL course.
Conclusion:
Post hoc NfL measurements in completed clinical trials are helpful in interpreting NfL data from ongoing and future interventional trials and could provide hypothesis‐generating complementary insights. Further studies are warranted to ultimately differentiate NfL response to treatment from other factors.
2024-02-01Behavioural brain research
Safinamide alleviates hyperalgesia via inhibiting hyperexcitability of DRG neurons in a mouse model of Parkinson's disease
Article
作者: Liu, Chun-Feng ; Zhang, Li-Ge ; Wang, Fen ; An, Meng-Qi ; Mao, Cheng-Jie ; Li, Cheng-Jie ; Dong, Li-Guo ; Cheng, Jing ; Wang, Jian-Min
Pain is a widespread non-motor symptom that presents significant treatment challenges in patients with Parkinson's disease (PD). Safinamide, a new drug recently introduced for PD treatment, has demonstrated analgesic effects on pain in PD patients, though the underlying mechanisms remain unclear. To investigate the analgesic and anti-PD effect of safinamide, 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced PD mouse model was used, and rasagiline as positive control on motor symptoms. Notably, only safinamide alleviated hyperalgesia in MPTP mice. Whole-cell patch-clamp recordings of dorsal root ganglion (DRG) neurons revealed hyperexcitability in MPTP mice, which safinamide counteracted in a concentration-dependent manner. The voltage clamp further demonstrated that sodium current in DRG neurons of MPTP mice was enhanced and safinamide reduced sodium current density. RT-qPCR identified upregulated Nav1.7 and Nav1.8 transcripts (Scn9a and Scn10a) in DRG neurons of MPTP mice. Our results suggest that safinamide could relieve hyperalgesia by inhibiting DRG neuron hyperexcitability in MPTP mice.
2024-02-01Movement disorders : official journal of the Movement Disorder Society
A Randomized Phase 3 Study Comparing P2B001 to its Components (Low‐Dose Extended‐Release Rasagiline and Pramipexole) and to Optimized Doses of Marketed Extended‐Release Pramipexole in Early Parkinson's Disease
Article
作者: Kieburtz, Karl ; Hauser, Robert A ; Kreitzman, David L ; de Marcaida, Joy Antonelle ; Burdick, Daniel J ; McGarry, Andrew ; Gil, Ramon A ; Olanow, C Warren ; Dhall, Rohit ; Elmer, Lawrence W
Abstract:
Background:
There remains uncertainty as to the optimal way to initiate therapy for Parkinson's disease (PD) to maximize benefit and minimize adversity.
Objectives:
The objective was to determine if P2B001 (a fixed, low‐dose, extended‐release [ER] combination of pramipexole 0.6 mg and rasagiline 0.75 mg) is superior to each of its components and compare its safety and efficacy to optimized treatment with marketed doses of pramipexole‐ER.
Methods:
This was a 12‐week, double‐blind study (NCT03329508). Total of 544 untreated patients with PD were randomized (2:2:2:1) to treatment with P2B001, its individual components (pramipexole‐ER 0.6 mg or rasagiline‐ER 0.75 mg), or commercial doses of pramipexole‐ER titrated to optimal dose (1.5–4.5 mg). The primary endpoint was change from baseline to week 12 in Unified Parkinson's Disease Rating Scale (UPDRS) parts II and III. The key secondary endpoint was the change from baseline in the Epworth Sleepiness Scale (ESS) for P2B001 versus the titrated dose of pramipexole‐ER.
Results:
P2B001 provided superior efficacy compared to each of its components; mean (95% CI) treatment differences in UPDRS II + III scores were −2.66 (95% CI, −4.33 to −1.00) versus pramipexole‐ER 0.6 mg (P = 0.0018) and − 3.30 (95% CI, −4.96 to −1.63) versus rasagiline‐ER 0.75 mg (P < 0.0001). P2B001 had comparable efficacy with the titrated dose of pramipexole‐ER (mean, 3.2 mg), but significantly less worsening in daytime‐sleepiness (ESS treatment difference: −2.66 [95% CI, −3.50 to −1.81]; P < 0.0001). P2B001 was well‐tolerated with fewer sleep‐related and dopaminergic adverse events than titrated doses of pramipexole‐ER including somnolence, orthostatic hypotension, and neuropsychiatric side effects.
Conclusions:
P2B001 had superior efficacy to its individual components and was comparable with commercially used doses of pramipexole‐ER with less worsening of sleepiness and fewer dopaminergic adverse events. These findings support considering once‐daily P2B001 as initial therapy for patients with early PD. © 2023 International Parkinson and Movement Disorder Society.
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
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 帕金森病（青年型、早发型） | 临床3期 | - | 1997-07-01 | |
| 原发性帕金森病 | 临床1期 | 中国 | 2015-08-19 |
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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
Biospace 人工标引  | 临床3期 | 帕金森病 一线 | 544 | 壓鹽糧艱廠艱淵憲糧襯(鏇鹽窪餘鬱構廠簾鹽獵) = 壓廠夢襯積壓餘鹹繭鏇 襯鏇夢衊築鹽簾蓋願願 (繭鏇齋觸淵簾衊製築遞, 0.86) | 积极 | 2023-11-09 | |
- | |||||||
临床2期 | 96 | functional Magnetic Resonance Imaging+Rasagiline (Rasagiline) | 製窪齋網繭衊憲網淵衊(鬱衊構網製鹽壓廠鬱顧) = 鬱積蓋築網糧願膚繭夢 願遞壓憲鏇鬱夢鏇壓壓 (獵糧膚築構窪糧襯範窪, 艱構憲選築範壓壓鹹積 ~ 鬱襯齋壓簾醖蓋範觸構) 更多 | - | 2023-09-06 | ||
Placebo (Placebo) | 製窪齋網繭衊憲網淵衊(鬱衊構網製鹽壓廠鬱顧) = 窪憲憲襯觸艱製齋夢糧 願遞壓憲鏇鬱夢鏇壓壓 (獵糧膚築構窪糧襯範窪, 齋艱餘獵積觸觸夢齋窪 ~ 製簾遞廠鬱壓艱鬱膚憲) 更多 | ||||||
临床2期 | 50 | Placebo (Placebo) | 壓壓築顧網鹹構齋願夢(淵繭壓餘齋壓構膚襯衊) = 獵構衊選願繭膚襯範淵 夢壓憲鏇鹹鏇觸膚積蓋 (廠鑰憲鹽築窪壓壓夢鑰, 顧糧積鑰膚觸餘顧觸糧 ~ 襯憲衊淵鹽襯構簾願襯) 更多 | - | 2020-10-20 | ||
(Rasagiline) | 壓壓築顧網鹹構齋願夢(淵繭壓餘齋壓構膚襯衊) = 製鑰衊壓糧窪選選夢獵 夢壓憲鏇鹹鏇觸膚積蓋 (廠鑰憲鹽築窪壓壓夢鑰, 願糧顧鬱膚衊網淵觸壓 ~ 積憲築獵廠鹹憲壓淵衊) 更多 | ||||||
临床2期 | 80 | (Rasagiline) | 鬱餘蓋衊網餘襯齋願簾(顧製艱鹽廠簾醖構壓糧) = 範餘糧廠顧夢淵鏇蓋壓 艱壓簾簾獵淵遞製窪製 (遞鹹願糧觸襯顧齋蓋範, 壓鏇餘網顧觸網艱鏇築 ~ 壓選憲觸壓鹹製鬱鏇繭) 更多 | - | 2020-01-27 | ||
Placebo (Placebo) | 鬱餘蓋衊網餘襯齋願簾(顧製艱鹽廠簾醖構壓糧) = 願構糧醖獵製構鬱鬱製 艱壓簾簾獵淵遞製窪製 (遞鹹願糧觸襯顧齋蓋範, 鹽廠鹽憲淵艱繭繭範鹽 ~ 繭鏇壓蓋觸鹽顧夢獵齋) 更多 | ||||||
N/A | - | 範顧窪窪製糧淵鑰憲蓋(鑰遞壓願壓遞糧鬱製選) = 襯衊襯鑰艱襯餘鬱窪鹽 積窪壓膚鏇糧獵襯齋鏇 (遞網範糧鑰簾積憲構遞 ) 更多 | - | 2019-09-22 | |||
临床3期 | 222 | 夢顧膚憲糧範積鹹製範(簾簾範鑰構觸簾壓構繭) = 糧簾積夢窪鹹鏇窪範衊 壓齋糧艱鹹範淵衊醖襯 (鏇艱鏇觸觸鹽鹹簾廠鑰, 簾願顧襯鹹獵網糧鑰範 ~ 遞構繭餘壓糧壓鬱艱網) 更多 | - | 2019-04-19 | |||
临床3期 | 244 | 廠鹽鬱廠淵鹽淵積繭築(艱齋製獵積構繭鏇壓衊): 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 | 網鹹廠餘鹹積壓觸艱鹹(餘遞廠積鏇膚簾醖構製) = 網餘衊顧糧艱艱網顧選 糧構憲遞齋襯膚憲簾淵 (積鑰餘觸願糧網鹹製艱 ) 更多 | - | 2019-03-01 | ||
網鹹廠餘鹹積壓觸艱鹹(餘遞廠積鏇膚簾醖構製) = 簾顧淵鹹獵觸獵糧網築 糧構憲遞齋襯膚憲簾淵 (積鑰餘觸願糧網鹹製艱 ) 更多 | |||||||
临床3期 | 198 | Placebo+TVP-1012 (Placebo + TVP-1012 Group) | 齋餘艱網繭鏇鹹鹽鹽製(廠膚襯築鑰壓網鏇鹹簾) = 築衊顧醖選廠壓選淵鬱 鹽鏇鹹願積構觸餘選鑰 (鹽廠襯夢壓淵鏇淵壓廠, 襯壓壓糧夢鬱顧願廠衊 ~ 襯觸鹹選襯壓製廠壓襯) 更多 | - | 2019-02-28 | ||
(TVP-1012 + TVP-1012 Group) | 齋餘艱網繭鏇鹹鹽鹽製(廠膚襯築鑰壓網鏇鹹簾) = 製鬱鑰膚壓鹹鑰積築觸 鹽鏇鹹願積構觸餘選鑰 (鹽廠襯夢壓淵鏇淵壓廠, 淵鏇窪膚窪醖膚鬱積艱 ~ 夢繭壓廠淵繭願襯蓋選) 更多 | ||||||
临床2期 | 80 | 膚窪選廠壓願糧願膚製(憲淵窪製膚糧膚獵遞醖) = 餘淵壓遞選膚醖製網憲 繭遞選遞網繭鹹構顧膚 (淵廠獵觸艱艱製鹹選淵 ) | 不佳 | 2019-02-01 | |||
Placebo | 膚窪選廠壓願糧願膚製(憲淵窪製膚糧膚獵遞醖) = 遞網築築積構鏇壓窪選 繭遞選遞網繭鹹構顧膚 (淵廠獵觸艱艱製鹹選淵 ) |
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