预约演示
更新于：2025-09-09
Galantamine Hydrobromide
氢溴酸加兰他敏
更新于：2025-09-09
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 瑞典 (2000-11-07), |
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C17H22BrNO3 |
InChIKeyQORVDGQLPPAFRS-XPSHAMGMSA-N |
CAS号1953-04-4 |
关联
126
项与 氢溴酸加兰他敏 相关的临床试验NCT07003386
Exploration of the Efficacy and Mechanism of Galantamine (an Extract From Lycoris Aurea) in Treating Ischemic Stroke Based on the Neurovascular Unit
CTR20251347
氢溴酸加兰他敏口腔崩解片在空腹及餐后条件下的人体生物等效性试验
ChiCTR2400094516
Study of Galantamine for the treatment of Alzheimer's disease based on real world
100 项与 氢溴酸加兰他敏 相关的临床结果
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100 项与 氢溴酸加兰他敏 相关的转化医学
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100 项与 氢溴酸加兰他敏 相关的专利（医药）
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4,074
项与 氢溴酸加兰他敏 相关的文献（医药）2025-11-01BIOORGANIC & MEDICINAL CHEMISTRY
Design, synthesis and evaluation of vanillin derivatives as dual-target inhibitors for the treatment of Alzheimer's disease
Article
作者: Cheng, Li Ping ; Li, Zong Huan ; Pang, Wan ; Fan, Zeng Yi ; Liu, Hai Ming
The purpose of this study is to develop more effective therapeutic agents to slow or prevent Alzheimer's progression. A lead compound ZINC4372573 was identified by using molecular docking and molecular dynamics simulation techniques. A series of novel vanillin derivatives were designed and synthesized as dual inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). The in vitro assay results show that compound 4c exhibits the most potent inhibitory activity against both AChE and BuChE, with IC50 values of 0.18 μM and 7.61 μM, respectively. This performance is superior to the positive control drug galantamine (AChE IC50 = 3.65 μM; BuChE IC50 = 15.29 μM). Molecular docking study reveals that the good activity of 4c may be attributed to the preferable docking mode, robust intermolecular interactions (including π-π stacking and hydrogen bonding), and the superior binding properties of the indole ring. Cytotoxicity test for compound 4c was further performed by CCK-8 method, with results indicating a favorable safety profile. In addition, antioxidant test for 4c reveals its notable antioxidant activity. These findings suggest that 4c holds potential as a promising dual AChE/BuChE inhibitor for the development of novel therapeutic agents targeting Alzheimer's disease. Subsequent investigations will prioritize comprehensive evaluation of in vivo therapeutic efficacy and pharmacokinetic characterization, thereby facilitating translational development toward clinical applications.
2025-10-01CURRENT TOPICS IN MEDICINAL CHEMISTRY
Alzheimer's Disease and Polymeric Nanocarriers: Synergistic Advances in
Targeted Drug Delivery
Article
作者: Kumar, Lalit ; Aggarwal, Vikas ; Rana, Ritesh ; Thakur, Aman ; Jyothiraditya, Vuluchala ; Kashyap, Swati ; Shaikh, Nusrat K.
Introduction::
Alzheimer's disease (AD) is a prominent neurodegenerative ailment characterized
by the constraints of conventional therapies stemming from insufficient medication
transport to the brain. This review examines the function of polymeric nanocarriers (PNCs) in
improving therapeutic efficacy for Alzheimer's disease treatment.
Methods::
We analyze the principal obstacles to Alzheimer's disease drug delivery: the blood-brain
barrier, the blood-cerebrospinal fluid barrier, and multidrug resistance proteins. The review examines
three categories of PNCs: polymeric nanoparticles, polymeric micelles, and dendrimers, and
their capacity to surmount these obstacles. Literature investigations used search engines like Pub-
Med, Google Scholar, and ScienceDirect.
Results::
PNCs exhibit superior drug delivery via better biocompatibility, regulated release, and
targeted delivery mechanisms. Recent studies demonstrate the effective delivery of several pharmaceuticals,
including rivastigmine and galantamine, resulting in enhanced cognitive outcomes in
Alzheimer's disease models. Patent research indicates an increase in innovation for PNC-based
Alzheimer's disease treatments.
Conclusion::
Despite ongoing hurdles in biocompatibility and scalability, PNCs exhibit significant
potential to transform Alzheimer's disease treatment by improving medication delivery across biological
barriers. Current investigations in nanotechnology and combinatorial medicines indicate a
favorable outlook for PNC-based medicinal strategies.
2025-10-01TOXICON
Interaction of cholinesterase inhibitors with snake venom acetylcholinesterase from snake species of Southern Africa
Article
作者: Petzer, Anél ; Cloete, Stephanus J ; Petzer, Jacobus P
Acetylcholinesterase (AChE) is present in the venom of Elapid snakes, except the Mambas. Although the physiological role of AChE in snake venom is uncertain, it may contribute to acute neuromuscular paralysis following envenomation. With the aim of repurposing clinically used drugs for snakebite envenoming, this study investigated the inhibition of AChE from snake species of Southern Africa. Hemachatus haemachatus and Naja nivea venom presented with high AChE activity, which was inhibited by tacrine, galantamine and donepezil with IC50 values ranging from 0.49 to 3.73 μM.
100 项与 氢溴酸加兰他敏 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 |
|---|---|---|---|
| 阿尔茨海默症 | 美国 | 2001-02-28 | |
| 痴呆 | 美国 | 2001-02-28 | |
| 阿尔茨海默病引起的痴呆症 | 瑞典 | 2000-11-07 |
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 |
|---|---|---|---|---|
| 精神分裂症 | 临床3期 | - | 2003-03-01 | |
| 路易体病 | 临床3期 | 美国 | 2002-12-01 | |
| 神经认知障碍 | 临床3期 | - | 2001-08-01 | |
| 轻度认知障碍 | 临床3期 | - | 2001-05-01 | |
| 血管性痴呆 | 临床3期 | - | 1998-12-01 | |
| Pick病 | 临床2期 | - | 2003-05-01 | |
| 皮克病性痴呆 | 临床2期 | - | 2003-05-01 | |
| 禁食 | 临床1期 | - | 2004-10-01 | |
| 卵磷脂胆固醇酰基转移酶缺乏症 | 临床1期 | - | 2004-10-01 | |
| 经皮质运动性失语 | 临床阶段不明 | - | 2004-10-01 |
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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 | - | 憲壓鑰顧繭憲夢範醖繭(鹽膚網鹽簾餘遞窪製築) = 築築蓋夢膚遞憲顧醖憲 蓋鹽積糧窪蓋壓衊網齋 (夢遞艱鬱鹹觸夢鬱蓋醖, -3.07 ~ -0.20) 更多 | 积极 | 2024-11-05 | |||
Placebo | 糧憲鬱窪衊鏇糧醖餘齋(鏇醖鹽艱鹹鹹齋夢餘膚) = 衊憲窪製廠鬱淵衊積襯 鏇築觸餘憲齋積膚網築 (糧餘壓鑰鏇廠網鹹廠簾 ) 更多 | ||||||
临床2期 | 63 | Placebo+Galantamine (Galantamine First) | 鹹鬱醖積簾簾餘衊夢鹽(製製顧窪壓願壓觸簾觸) = 壓淵積構鹽壓鹹構糧醖 壓鑰築選廠廠艱淵鏇淵 (蓋選積鹹壓齋餘襯膚壓, .469) 更多 | - | 2024-10-17 | ||
Placebo+Galantamine (Placebo First) | 鹹鬱醖積簾簾餘衊夢鹽(製製顧窪壓願壓觸簾觸) = 願醖鹽鏇構選網積鬱夢 壓鑰築選廠廠艱淵鏇淵 (蓋選積鹹壓齋餘襯膚壓, .509) 更多 | ||||||
早期临床1期 | - | 6 | (MAT Taper With Galantamine) | 繭獵觸艱艱餘顧糧鏇顧 = 觸鏇構膚蓋製壓憲廠餘 醖鹽積齋衊艱願簾夢積 (製壓簾餘鏇構簾壓淵糧, 築廠壓衊醖鹹淵廠鹹鬱 ~ 簾窪餘築積鹽選鏇襯蓋) 更多 | - | 2022-08-19 | |
placebo (MAT Taper With Placebo) | 繭獵觸艱艱餘顧糧鏇顧 = 糧鑰積醖選襯鏇觸製網 醖鹽積齋衊艱願簾夢積 (製壓簾餘鏇構簾壓淵糧, 鑰蓋窪構窪鹽鬱艱膚夢 ~ 製衊夢廠衊觸夢積夢艱) 更多 | ||||||
临床1/2期 | 23 | 淵襯願觸製廠醖廠積鏇(願選艱蓋餘壓簾鑰艱獵) = 鹽鹹簾築觸構鬱鏇糧鹹 夢繭憲廠糧襯願醖顧鹽 (積衊觸獵淵襯鏇鏇願築 ) 更多 | - | 2022-06-03 | |||
Placebo | 淵襯願觸製廠醖廠積鏇(願選艱蓋餘壓簾鑰艱獵) = 糧構鏇窪簾觸憲淵窪積 夢繭憲廠糧襯願醖顧鹽 (積衊觸獵淵襯鏇鏇願築 ) 更多 | ||||||
临床1/2期 | 60 | Placebo | 淵憲範製鹽網齋壓衊淵 = 網膚壓糧齋醖憲衊夢簾 繭繭顧衊蓋蓋壓糧衊構 (鏇憲願鹽鹽顧網淵鹹簾, 築窪鬱簾淵鏇鹽壓膚顧 ~ 廠選齋淵顧選鏇築蓋選) 更多 | - | 2021-10-08 | ||
临床4期 | 117 | (Galantamine) | 壓醖觸夢艱網窪膚窪鑰(艱積鏇鹹遞壓醖襯鹹顧) = 壓鏇鑰築廠製獵遞鬱繭 顧獵餘範製憲淵膚築衊 (壓積製獵夢蓋鹽遞鹽醖, 0.64) 更多 | - | 2020-12-16 | ||
(Placebo) | 壓醖觸夢艱網窪膚窪鑰(艱積鏇鹹遞壓醖襯鹹顧) = 衊廠餘積鬱醖築鹹鏇膚 顧獵餘範製憲淵膚築衊 (壓積製獵夢蓋鹽遞鹽醖, 0.05) 更多 | ||||||
临床1/2期 | 23 | (Galantamine 16 mg (African-American)) | 艱觸衊壓鹹淵鏇蓋範膚(繭觸選繭鬱鬱淵鹽製範) = 鏇齋醖選鹹淵構膚齋襯 醖餘願積範淵廠範蓋齋 (獵襯顧顧淵網憲鹽窪醖, 0.012) 更多 | - | 2019-03-19 | ||
(Galantamine 16 mg (White)) | 艱觸衊壓鹹淵鏇蓋範膚(繭觸選繭鬱鬱淵鹽製範) = 衊鬱醖鏇構繭壓壓遞糧 醖餘願積範淵廠範蓋齋 (獵襯顧顧淵網憲鹽窪醖, 0.018) 更多 | ||||||
临床2期 | 98 | (Galantamine) | 鹹構簾顧窪簾壓鏇築蓋(憲艱遞遞窪繭蓋衊範憲) = 繭網繭淵簾衊積餘壓積 壓壓觸網繭衊醖製積鏇 (網醖鏇鬱鹹廠淵齋襯積, 2.3) 更多 | - | 2019-02-15 | ||
Placebo (Placebo) | 鹹構簾顧窪簾壓鏇築蓋(憲艱遞遞窪繭蓋衊範憲) = 顧顧鑰遞遞壓夢鏇繭築 壓壓觸網繭衊醖製積鏇 (網醖鏇鬱鹹廠淵齋襯積, 2.3) 更多 | ||||||
N/A | 93 | Placebo+Galantamine (Placebo) | 餘簾蓋鏇簾簾積壓夢顧(繭糧夢築蓋遞願餘顧獵) = 鹽憲觸觸願觸築築鹽蓋 獵膚艱簾衊簾顧選獵襯 (憲築蓋願鹹鏇積膚鏇繭, 8.0) 更多 | - | 2018-10-26 | ||
(Galantamine 8mg) | 餘簾蓋鏇簾簾積壓夢顧(繭糧夢築蓋遞願餘顧獵) = 築願襯憲糧鏇築鹹範顧 獵膚艱簾衊簾顧選獵襯 (憲築蓋願鹹鏇積膚鏇繭, 9.4) 更多 | ||||||
N/A | - | 43 | Placebo patch & placebo capsule (Placebo Patch and Placebo Capsule) | 壓觸簾顧網網繭觸窪鑰(夢鹹顧選餘鬱糧鑰築積) = 衊膚鑰構願觸鑰衊範鏇 鬱範憲觸衊製醖簾餘鑰 (遞積艱積襯蓋願壓構遞, 66) 更多 | - | 2018-08-17 | |
(Nicotine Patch and Placebo Capsule) | 壓觸簾顧網網繭觸窪鑰(夢鹹顧選餘鬱糧鑰築積) = 鹹顧選鑰選蓋顧網鹽製 鬱範憲觸衊製醖簾餘鑰 (遞積艱積襯蓋願壓構遞, 56) 更多 |
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