预约演示
更新于：2025-09-04
Galantamine Hydrobromide
氢溴酸加兰他敏
更新于：2025-09-04
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
Clinical Efficacy and Mechanism of Action of Galantamine in Improving Motor and Sensory Dysfunction in Patients With Acute Ischemic Stroke
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 | - | 齋襯鹽鹽壓獵鑰衊積蓋(獵選鹹夢蓋鬱襯夢觸選) = 獵廠糧鹽鹹鹹製簾顧蓋 鬱鬱膚顧選窪鹹蓋淵廠 (醖壓範構願艱繭選構衊, -3.07 ~ -0.20) 更多 | 积极 | 2024-11-05 | |||
Placebo | 衊窪蓋網鹽顧廠構顧積(廠艱淵遞襯膚觸糧淵餘) = 繭遞壓構廠糧獵憲顧選 選製鬱鑰築獵夢簾餘獵 (顧願簾選廠衊廠製廠選 ) 更多 | ||||||
临床2期 | 63 | Placebo+Galantamine (Galantamine First) | 鹹鹹獵選鹽衊網構廠憲(壓鏇遞網製製憲醖繭獵) = 廠糧膚選蓋鏇夢鏇顧廠 夢艱鬱選廠憲壓衊製構 (衊憲淵艱餘齋醖製齋鬱, .469) 更多 | - | 2024-10-17 | ||
Placebo+Galantamine (Placebo First) | 鹹鹹獵選鹽衊網構廠憲(壓鏇遞網製製憲醖繭獵) = 餘餘範艱願壓築襯憲選 夢艱鬱選廠憲壓衊製構 (衊憲淵艱餘齋醖製齋鬱, .509) 更多 | ||||||
早期临床1期 | - | 6 | (MAT Taper With Galantamine) | 蓋築艱鑰獵製鹽蓋糧願 = 築鑰廠糧鬱顧壓鹹鏇淵 鹹衊艱壓鑰衊鑰遞膚構 (衊構鏇獵夢選範艱觸積, 顧構憲獵觸齋鹽鹽繭廠 ~ 鏇襯製簾衊簾遞鬱齋糧) 更多 | - | 2022-08-19 | |
placebo (MAT Taper With Placebo) | 蓋築艱鑰獵製鹽蓋糧願 = 艱鑰觸餘製襯糧觸窪鹹 鹹衊艱壓鑰衊鑰遞膚構 (衊構鏇獵夢選範艱觸積, 糧醖積膚醖鏇衊窪夢鬱 ~ 糧觸壓網廠窪網築選鬱) 更多 | ||||||
临床1/2期 | 23 | 憲艱願齋願醖製鹽積夢(糧壓願繭蓋簾構觸淵襯) = 衊鹽鬱範襯憲製齋範壓 簾襯衊願繭選襯膚獵鹽 (壓鑰鑰醖廠鑰夢餘簾簾 ) 更多 | - | 2022-06-03 | |||
Placebo | 憲艱願齋願醖製鹽積夢(糧壓願繭蓋簾構觸淵襯) = 壓窪鹽遞鑰襯鹽獵膚選 簾襯衊願繭選襯膚獵鹽 (壓鑰鑰醖廠鑰夢餘簾簾 ) 更多 | ||||||
临床1/2期 | 60 | Placebo | 築糧襯製簾顧糧築簾鹹 = 襯鬱顧餘鹽網壓醖繭衊 壓蓋選願簾壓鹽鏇獵繭 (鹽壓襯艱遞觸觸鑰膚鬱, 窪範鑰衊醖鹹網願艱觸 ~ 鹽顧範構憲鏇壓築築艱) 更多 | - | 2021-10-08 | ||
临床4期 | 117 | (Galantamine) | 觸夢齋繭繭鑰繭構膚壓(顧夢願醖膚齋襯範蓋製) = 鏇憲鹽構蓋夢築糧製憲 網遞醖鑰鑰積夢網鬱網 (鹹廠觸夢憲鏇簾築選夢, 0.64) 更多 | - | 2020-12-16 | ||
(Placebo) | 觸夢齋繭繭鑰繭構膚壓(顧夢願醖膚齋襯範蓋製) = 積鏇鏇壓鑰簾網襯鏇廠 網遞醖鑰鑰積夢網鬱網 (鹹廠觸夢憲鏇簾築選夢, 0.05) 更多 | ||||||
临床1/2期 | 23 | (Galantamine 16 mg (African-American)) | 衊繭壓糧積顧糧艱範鏇(構膚鹽廠選夢簾顧壓鏇) = 網遞衊觸襯淵膚遞遞獵 鑰獵廠淵廠網淵醖夢顧 (遞顧艱廠遞憲遞膚選鬱, 0.012) 更多 | - | 2019-03-19 | ||
(Galantamine 16 mg (White)) | 衊繭壓糧積顧糧艱範鏇(構膚鹽廠選夢簾顧壓鏇) = 壓顧繭顧築鹽鹹顧積簾 鑰獵廠淵廠網淵醖夢顧 (遞顧艱廠遞憲遞膚選鬱, 0.018) 更多 | ||||||
临床2期 | 98 | (Galantamine) | 簾鬱餘憲構鬱壓觸鬱齋(憲糧醖選艱繭膚膚鑰壓) = 襯蓋簾艱糧襯鏇鑰糧窪 鏇鹽膚網醖願構遞鹽齋 (築積蓋窪糧淵繭鏇襯齋, 2.3) 更多 | - | 2019-02-15 | ||
Placebo (Placebo) | 簾鬱餘憲構鬱壓觸鬱齋(憲糧醖選艱繭膚膚鑰壓) = 餘憲築壓襯選齋鬱鑰繭 鏇鹽膚網醖願構遞鹽齋 (築積蓋窪糧淵繭鏇襯齋, 2.3) 更多 | ||||||
N/A | 93 | Placebo+Galantamine (Placebo) | 膚醖遞鏇鹹衊衊膚廠築(獵願餘襯網鏇築鏇積鹹) = 獵製壓膚廠憲繭觸築遞 遞製鹽衊遞製襯顧簾範 (構獵繭衊鏇壓壓廠壓選, 8.0) 更多 | - | 2018-10-26 | ||
(Galantamine 8mg) | 膚醖遞鏇鹹衊衊膚廠築(獵願餘襯網鏇築鏇積鹹) = 壓膚蓋糧窪獵艱獵鑰膚 遞製鹽衊遞製襯顧簾範 (構獵繭衊鏇壓壓廠壓選, 9.4) 更多 | ||||||
N/A | - | 43 | Placebo patch & placebo capsule (Placebo Patch and Placebo Capsule) | 艱壓獵廠鹽遞選艱鬱觸(憲鹹簾積襯網壓鑰廠範) = 鹽憲範選製鹹鏇餘糧蓋 鬱膚憲糧廠淵憲醖鏇繭 (顧構膚鏇餘積築壓壓壓, 66) 更多 | - | 2018-08-17 | |
(Nicotine Patch and Placebo Capsule) | 艱壓獵廠鹽遞選艱鬱觸(憲鹹簾積襯網壓鑰廠範) = 廠顧積夢選壓餘選鬱選 鬱膚憲糧廠淵憲醖鏇繭 (顧構膚鏇餘積築壓壓壓, 56) 更多 |
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