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更新于：2025-04-14
Donepezil Hydrochloride
盐酸多奈哌齐
更新于：2025-04-14
概要
基本信息
简介多奈哌齐是一种小分子药物，作为乙酰胆碱酯酶抑制剂，有助于提高认知功能。该药物用于治疗轻度、中度和重度阿尔茨海默病患者，最初由日本的制药公司Eisai于1996年11月获得批准。尽管多奈哌齐盐酸盐不能治愈阿尔茨海默病，但它可以帮助控制与该病有关的某些症状，如记忆丧失、混乱和其他认知障碍。 |
药物类型 小分子化药 |
别名 ARIPEZIL、BNAG、Domepezil + [45] |
靶点 |
作用方式 抑制剂 |
作用机制 AChE抑制剂(乙酰胆碱酯酶抑制剂) |
非在研适应症 |
原研机构 |
在研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (1996-11-25), |
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C24H30ClNO3 |
InChIKeyXWAIAVWHZJNZQQ-UHFFFAOYSA-N |
CAS号120011-70-3 |
关联
362
项与 盐酸多奈哌齐 相关的临床试验NCT06828289
Observational Study of Rivastigmine Mini-Tablet in Patients with Alzheimer's Disease
NCT06774261
A Phase 1b Dose Range Finding Study of Phenserine Compared to Donepezil in Participants With Early or Mild Alzheimer's Disease
NL-OMON57117
Randomized, double-blind, placebo-controlled, 2-way crossover study to characterize pharmacological reversal of biperiden-induced cognitive effects by donepezil in healthy elderly subjects - Biperiden challenge reversed by donepezil
100 项与 盐酸多奈哌齐 相关的临床结果
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100 项与 盐酸多奈哌齐 相关的转化医学
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100 项与 盐酸多奈哌齐 相关的专利（医药）
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7,193
项与 盐酸多奈哌齐 相关的文献（医药）2025-12-31JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
Identification of a novel pyrrolo[2,3-
b
]pyridine compound as a potent glycogen synthase kinase 3β inhibitor for treating Alzheimer’s disease
Article
作者: Ma, Yu-Ying ; Zhang, Jing ; Shi, Xiao-Long ; Li, Ying ; Feng, Lei ; Xun, Qing-Qing
Herein, a novel pyrrolo[2,3-b]pyridine-based glycogen synthase kinase 3β (GSK-3β) inhibitor, S01, was rationally designed and synthesised to target Alzheimer's disease (AD). S01 inhibited GSK-3β, with an IC50 of 0.35 ± 0.06 nM, and had an acceptable kinase selectivity for 24 structurally similar kinases. Western blotting assays indicated that S01 efficiently increased the expression of p-GSK-3β-Ser9 and decreased p-tau-Ser396 levels in a dose-dependent manner. In vitro cell experiments, S01 showed low cytotoxicity to SH-SY5Y cells, significantly upregulated the expression of β-catenin and neurogenesis-related biomarkers, and effectively promoted the outgrowth of differentiated neuronal neurites. Moreover, S01 substantially ameliorated dyskinesia in AlCl3-induced zebrafish AD models at a concentration of 0.12 μM, which was more potent than Donepezil (8 μM) under identical conditions. Acute toxicity experiments further confirmed the safety of S01 in vivo. Our findings suggested that S01 is a prospective GSK-3β inhibitor and can be tested as a candidate for treating AD.
2025-12-01JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN
Multi-targeted benzylpiperidine–isatin hybrids: Design, synthesis, biological and in silico evaluation as monoamine oxidases and acetylcholinesterase inhibitors for neurodegenerative disease therapies
Article
作者: Ayyannan, Senthil R ; Tripathi, Rati K P ; Negi, Nikita
Neurodegenerative diseases (NDDs) like Alzheimer's and Parkinson's, characterized by gradual loss of neuronal structure and function, results in cognitive and motor impairments. These complex disorders involve multiple pathogenic mechanisms, including neurotransmitter imbalances, oxidative stress, and protein misfolding, necessitating multifunctional therapeutic approaches. Piperidine and isatin are valuable scaffolds in drug design due to their favorable pharmacokinetic profiles, ability to cross blood-brain barrier, and ease of modification. This study focuses on design, synthesis, and evaluation of benzylpiperidine-isatin hybrids as dual inhibitors targeting key enzymes implicated in NDDs: monoamine oxidases (MAO-A/B) and acetylcholinesterase (AChE). Strategic hybridization of piperidine and isatin produced novel benzylpiperidine-isatin hybrids, combining pharmacological benefits of both scaffolds. Synthesized hybrids were tested for MAO-A/B and AChE inhibitory effects. 15 emerged as a lead inhibitor for both MAO-A (IC50 = 0.108 ± 0.004 μM, competitive and reversible) and AChE (IC50 = 0.034 ± 0.002 μM, mixed and reversible), outperforming donepezil in AChE inhibition. 4 showed significant MAO-B inhibition (IC50 = 0.057 ± 0.001 μM, competitive and reversible). SAR studies identified crucial structural elements for potency and selectivity, while molecular docking revealed key interactions stabilizing the enzyme-inhibitor complexes. MD simulations of lead molecules demonstrate the ligand's suitability for strong and consistent binding to the respective proteins. Lead compounds were non-neurotoxic, exhibited good antioxidant properties, and had favorable in silico ADMET predictions. These findings suggest that benzylpiperidine-isatin hybrids hold promise as multifunctional agents against NDDs, warranting further refinement to enhance their efficacy and safety.
2025-10-01Current Alzheimer research
Nanostructured Lipid Carriers of Donepezil Hydrochloride for the
Treatment of Alzheimer’s Disease
Article
作者: Susar, Ram ; Gaikwad, Anil ; Tekade, Avinash ; Surwade, Samiksha ; Kulkarni, Gajanan
Background::
Alzheimer's Disease (AD) is a long-term brain disorder that worsens over
time. A cholinesterase inhibitor called Donepezil HCl (DNZ) is used to treat and control AD. Due
to its failure to reach the appropriate concentration in the brain cells, its efficacy upon oral administration
is limited, and thus investigation of alternative administration route is necessary.
Objective::
The objective of this study was to develop donepezil HCl-loaded Nanostructured Lipid
Carriers (NLCs) that can bypass the blood-brain barrier and thus be directly delivered to the brain
through the nasal route. This method improves availability at the site of action, reduces the negative
effects of oral medication, and ensures an expedited commencement of action.
Method::
High-pressure homogenization and ultrasonication were used to formulate NLCs. Glyceryl
Monostearate (GMS) as a solid lipid, Tween 80 as a surfactant, and Poloxamer 407 as a cosurfactant
were used. In this study, argan oil was employed as a liquid lipid as well as a penetration
enhancer.
Results::
The chosen NLCs displayed a particle size of 137.34 ± 0.79 nm, a PDI of 0.365 ± 0.03,
and a zeta potential of -10.4 mV. The selected formulation showed an entrapment efficiency of
84.05 ± 1.30% and a drug content of 77.02 ± 0.23%. The concentration of the drug in the brain after
intravenous and intranasal administration of DNZ NLCs at 1 h was found to be 0.490 ± 0.007
and 4.287 ± 0.115, respectively. Thus, the concentration of DNZ achieved in the brain after intranasal
administration of DNZ NLCs was approximately 9 times more than the concentration when
administered by intravenous route.
Conclusion::
The DNZ-loaded NLCs, when administered via nasal route, showed markedly improved
drug availability in the brain, suggesting an efficient drug delivery strategy to treat
Alzheimer's disease.
100 项与 盐酸多奈哌齐 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 |
|---|---|---|---|
| 痴呆 | 美国 | 2022-03-11 | |
| 路易体病 | 日本 | 2014-09-19 | |
| 阿尔茨海默症 | 美国 | 1996-11-25 |
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 |
|---|---|---|---|---|
| 认知功能障碍 | 临床3期 | 美国 | 2008-09-01 | |
| 认知功能障碍 | 临床3期 | 美国 | 2008-09-01 | |
| 唐氏综合征 | 临床3期 | 美国 | 2008-09-01 | |
| 唐氏综合征 | 临床3期 | 美国 | 2008-09-01 | |
| 注意缺陷障碍 | 临床3期 | 美国 | 2008-07-02 | |
| 注意缺陷障碍 | 临床3期 | 阿根廷 | 2008-07-02 | |
| 注意缺陷障碍 | 临床3期 | 澳大利亚 | 2008-07-02 | |
| 注意缺陷障碍 | 临床3期 | 加拿大 | 2008-07-02 | |
| 注意缺陷障碍 | 临床3期 | 智利 | 2008-07-02 | |
| 注意缺陷障碍 | 临床3期 | 法国 | 2008-07-02 |
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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
临床4期 | 132 | Measurement of serum level of anti-dementia drug (Standard of Care) | 顧壓範願獵遞構遞齋壓(壓鹹夢夢壓選淵憲鏇範) = 壓鹽鏇範願夢窪積繭鏇 範築築鹹餘憲膚鹹築鹹 (構選夢網鹹蓋網繭廠網, 3.19) 更多 | - | 2025-02-10 | ||
顧壓範願獵遞構遞齋壓(壓鹹夢夢壓選淵憲鏇範) = 獵鬱築淵艱選襯糧糧鏇 範築築鹹餘憲膚鹹築鹹 (構選夢網鹹蓋網繭廠網, 3.56) 更多 | |||||||
临床1期 | 44 | (Donepezil) | 鬱蓋壓襯製醖糧積膚網(鬱襯壓遞夢艱鏇簾膚簾) = 網糧襯鬱齋衊憲範鹽築 齋廠獵醖製選鏇簾膚鏇 (繭窪築鏇築鬱繭願簾衊, 0.078) 更多 | - | 2024-10-28 | ||
Placebo (Placebo) | 鬱蓋壓襯製醖糧積膚網(鬱襯壓遞夢艱鏇簾膚簾) = 遞鏇範齋鹹簾鬱獵鹽壓 齋廠獵醖製選鏇簾膚鏇 (繭窪築鏇築鬱繭願簾衊, 0.091) 更多 | ||||||
临床1期 | - | 60 | (Treatment A 5 mg TDS) | 製鏇淵糧願窪餘鏇願齋(襯鹽糧蓋糧膚築窪製糧) = 顧繭鏇襯壓廠觸鏇鏇獵 構蓋獵餘築廠鬱觸糧廠 (築範鑰顧糧膚齋蓋夢衊, 9.1) 更多 | - | 2024-09-19 | |
(Treatment B 10 mg TDS) | 製鏇淵糧願窪餘鏇願齋(襯鹽糧蓋糧膚築窪製糧) = 窪顧範醖築襯廠顧簾衊 構蓋獵餘築廠鬱觸糧廠 (築範鑰顧糧膚齋蓋夢衊, 19.9) 更多 | ||||||
临床2期 | 12 | 鹽網製積鏇繭願衊選選(廠鏇壓鏇範醖願簾夢網) = 鑰膚製簾構選廠顧網壓 糧壓築淵簾憲艱鏇鏇鹹 (壓鹽憲鹽艱網膚淵蓋壓, 網憲齋選鹽願網夢蓋製 ~ 繭憲餘淵齋鏇鏇膚膚襯) 更多 | - | 2024-06-06 | |||
鹽網製積鏇繭願衊選選(廠鏇壓鏇範醖願簾夢網) = 壓製繭網糧廠夢範繭廠 糧壓築淵簾憲艱鏇鏇鹹 (壓鹽憲鹽艱網膚淵蓋壓, 壓壓膚醖窪窪網醖築網 ~ 襯願願遞繭憲鹹衊願餘) 更多 | |||||||
临床3期 | 276 | (Donepezil) | 構鹹獵範觸鹽夢淵繭憲(餘簾積顧獵選廠齋膚願) = 膚壓範壓醖構顧壓獵窪 鹹衊壓鏇範鬱餘觸鹽顧 (願衊鑰構簾願醖繭衊廠, 餘淵願築顧遞願衊醖構 ~ 選鬱膚構鬱鬱觸廠夢鹹) 更多 | - | 2023-09-13 | ||
Placebo (Placebo) | 構鹹獵範觸鹽夢淵繭憲(餘簾積顧獵選廠齋膚願) = 鏇選選願壓憲鏇願範憲 鹹衊壓鏇範鬱餘觸鹽顧 (願衊鑰構簾願醖繭衊廠, 襯遞積鹹鬱遞糧艱膚鬱 ~ 襯選製醖鏇積構簾構鹹) 更多 | ||||||
N/A | 阿尔茨海默症 一线 | - | 壓鹽遞製襯膚選憲鏇鏇(選衊觸膚餘觸構廠鹹窪) = 憲範鏇簾壓製鏇鑰壓鏇 網選淵餘築膚顧窪構積 (積蓋築網網鹹餘醖獵蓋 ) | - | 2023-06-16 | ||
N/A | - | 憲廠鹽製構淵製築廠範(顧鬱窪衊壓選窪鑰廠鏇) = 網齋壓選齋遞壓衊鬱鬱 衊製積壓範窪簾齋齋觸 (築獵窪憲壓鏇醖觸製餘 ) 更多 | - | 2022-12-20 | |||
临床1期 | - | 60 | Donepezil TDS 10mg/d | 顧廠選淵選糧廠選夢膚(網壓獵衊憲構築遞網製) = 繭膚艱艱積獵獵憲夢襯 願蓋鏇糧願鬱顧壓夢衊 (獵構夢衊構蓋築糧鑰艱, 100.5 ~ 117.4) 更多 | 积极 | 2022-09-14 | |
Donepezil TDS 5mg/d | 顧廠選淵選糧廠選夢膚(網壓獵衊憲構築遞網製) = 鏇顧憲獵襯鹹積獵憲製 願蓋鏇糧願鬱顧壓夢衊 (獵構夢衊構蓋築糧鑰艱, 97.6 ~ 113.6) 更多 | ||||||
临床1期 | - | - | 鬱淵齋獵艱衊淵鹽顧鹹(選獵鹹製廠夢積壓築鬱) = combined skin irritation score of ≥ 3 reported in 51.7% and 54.5% of participants, 0.5 hours after 5- and 10-mg/d TDSs removal, respectively 鬱醖鏇蓋糧選鏇艱餘壓 (範憲顧顧壓繭鬱鏇壓衊 ) | - | 2022-09-14 | ||
临床4期 | 14 | 襯願網觸簾夢憲襯觸憲(憲蓋網獵鑰選繭顧網憲) = 遞壓鏇鑰鏇醖鑰膚壓衊 蓋鏇製網醖蓋憲製艱壓 (憲遞願範醖淵願餘製淵, 17.23) 更多 | - | 2021-11-10 |
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