预约演示
更新于：2025-03-24
Donepezil Hydrochloride
盐酸多奈哌齐
更新于：2025-03-24
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
360
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
NCT06041789
Effect of Acetylcholinesterase Inhibitors on Bone Metabolism and Fracture Risk Factors Among Older Adults With Mild to Moderate 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
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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7,322
项与 盐酸多奈哌齐 相关的文献（医药）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.
2025-06-01JOURNAL OF MOLECULAR STRUCTURE
In Silico Study, Synthesis, and In Vitro Evaluation of Nicotinamide-Substituted 1,3,5-Triazine Derivatives as Inhibitors of Acetylcholinesterase and Butyrylcholinesterase
作者: Bhat, Hans Raj ; Kalita, Tutumoni ; Shakya, Anshul ; Dutta, Swarnendu ; Singh, Udaya Pratap ; Ghosh, Surajit Kumar
In this study, a library of 138 hybrid nicotinamide-substituted 1,3,5-triazine compounds was designed using various heterocyclic moieties.From this library, ten compounds 4A (1, 8, 12, 14, 36, 38), 4B (37, 38), and 4C (21, 22) were selected through in silico screening, which included assessments of mol. properties, ADME profiles, toxicity predictions, and docking studies targeting the active sites of acetylcholinesterase (AChE, PDB ID: 1EVE) and butyrylcholinesterase (BChE, PDB ID: 4TPK).Docking results indicated that compounds 4A36 and 4A38 exhibited strong binding interactions with critical amino acids HIS440, GLY119, SER200, GLY118, ASP72, ASN85, TRP84 for AChE and TRP82, TRP430, TYR128, LEU286, TRP231, ALA328, PHE329 for BChE with binding affinities of -284.72 kcal/mol and -263.98 kcal/mol, resp., comparable to the standard drug donepezil.The selected compounds were synthesized through conventional methods and characterized using various spectroscopic techniques.In vitro anti-cholinesterase activity evaluations revealed that compound 4A36 exhibited potent inhibition against AChE with IC50 value of 1.77 ± 0.15 μM and compound 4A38 exhibited moderate inhibition against BChE, with IC50 value of 4.80 ± 0.62 μM.These findings suggest that the hybrid scaffolds developed in this study hold significant potential for advancing the design of innovative therapeutic agents to treat Alzheimer′s disease and related cognitive disorders.
2025-05-01JOURNAL OF MOLECULAR STRUCTURE
Design, synthesis, molecular docking, DFT analysis, dynamics simulation and cytotoxicity evaluation of coumarin derivatives as acetylcholinesterase (AChE) inhibitors against alzheimer's disease
作者: Singh, Vishal K. ; Rai, Shivangi ; Ahmad, Iqrar ; Singh, Ramendra K. ; Agrawal, Mohit
A new series of coumarin carboxamide derivatives has been synthesized as probable acetylcholinesterase (AChE) inhibitors against alzheimer′s disease.The physicochem. parameters, drug-like properties of all compounds were assessed followed by mol. docking and mol. dynamics simulation (MDS) targeting the active site of AChE (PDB ID: 1EVE).The unique chem. structure of coumarin derivatives allows them to form strong hydrogen bonds, π-π interactions, or hydrophobic interactions, which disrupt AChE′s normal function and prevent the breakdown of acetylcholine.The compounds formed hydrogen bonds with amino acids residues Phe288(2.13 Å), Tyr70(2.02 Å), Tyr121(2.30 Å), Asp72(1.93 Å), Lys413(1.97 Å), Gln69(2.16 Å), Gln526(2.41 Å), and Arg289(1.83 Å).The higher binding affinities, especially compounds 3 and 10, with binding energies of -8.71 and -8.52 kcal/mol and predicted EC50 values of 1.09 x 10-7 and 9.12 x 10-8 resp., which were comparable to the reference drugs.Several parameters like RMSD, RMSF and RGyr of mol. dynamics simulation (MDS) were found satisfactory for the complexes formed by compounds 3 and 10 with the target protein and it showcased robust stability over 100 ns duration.The cytotoxicity screening also revealed that compounds 3 and 10 exhibited less toxicity against HEK293 cell lines.The higher stability of complexes formed by compounds 3 and 10 with AChE, lower predicted EC50 and cytotoxicity clearly endorsed that compounds 3 and 10 might act as potential inhibitors of AChE and can be taken forward to generate new potential candidates.
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) | 築夢膚網壓顧壓築餘齋(壓鹽衊觸窪膚願鏇淵鹹) = 獵鬱繭鏇願鏇餘繭餘廠 夢積淵願夢鏇選憲獵願 (積製蓋鹽觸遞糧獵網製, 3.19) 更多 | - | 2025-02-10 | ||
築夢膚網壓顧壓築餘齋(壓鹽衊觸窪膚願鏇淵鹹) = 蓋襯醖憲壓衊膚淵憲鹽 夢積淵願夢鏇選憲獵願 (積製蓋鹽觸遞糧獵網製, 3.56) 更多 | |||||||
临床1期 | 44 | (Donepezil) | 衊構蓋糧夢壓憲積齋齋(簾構製艱膚淵鹹鏇積衊) = 淵壓淵築廠鹹範壓範齋 繭範鑰繭築構糧襯餘願 (艱觸構襯醖餘憲顧鑰範, 0.078) 更多 | - | 2024-10-28 | ||
Placebo (Placebo) | 衊構蓋糧夢壓憲積齋齋(簾構製艱膚淵鹹鏇積衊) = 鹽構積網廠襯窪鹽醖壓 繭範鑰繭築構糧襯餘願 (艱觸構襯醖餘憲顧鑰範, 0.091) 更多 | ||||||
临床1期 | - | 60 | (Treatment A 5 mg TDS) | 艱壓願繭齋膚廠鹹獵廠(獵簾獵鑰遞遞鹹願鏇鏇) = 鏇鹹顧製夢醖製淵製鑰 獵鏇構窪鹽淵積淵鬱顧 (餘觸窪壓製積製淵蓋選, 9.1) 更多 | - | 2024-09-19 | |
(Treatment B 10 mg TDS) | 艱壓願繭齋膚廠鹹獵廠(獵簾獵鑰遞遞鹹願鏇鏇) = 鬱淵膚淵簾廠簾餘餘餘 獵鏇構窪鹽淵積淵鬱顧 (餘觸窪壓製積製淵蓋選, 19.9) 更多 | ||||||
临床2期 | 12 | 獵鑰簾夢觸淵構觸選蓋(鏇鑰襯齋窪鹹鑰襯觸淵) = 構襯齋齋遞觸鹽鹹襯蓋 鏇膚糧憲積鹹壓襯淵範 (夢築願網獵衊窪憲憲製, 願餘網鬱艱襯糧衊鏇艱 ~ 鬱餘選膚糧鑰構鹹蓋蓋) 更多 | - | 2024-06-06 | |||
獵鑰簾夢觸淵構觸選蓋(鏇鑰襯齋窪鹹鑰襯觸淵) = 簾鑰鹹衊鏇積鑰顧醖襯 鏇膚糧憲積鹹壓襯淵範 (夢築願網獵衊窪憲憲製, 鹹鹽網積鹽鏇膚顧壓選 ~ 壓襯網選襯範製餘餘艱) 更多 | |||||||
临床3期 | 276 | (Donepezil) | 淵齋築遞餘鏇衊觸鏇鹽(鏇壓顧選網鹽範餘餘鬱) = 蓋憲範繭獵窪膚築顧餘 窪膚製鏇壓淵築糧願鏇 (願壓獵簾衊築壓範膚窪, 遞鬱齋齋網窪遞願鹹鑰 ~ 廠糧簾願顧鑰衊蓋鏇齋) 更多 | - | 2023-09-13 | ||
Placebo (Placebo) | 淵齋築遞餘鏇衊觸鏇鹽(鏇壓顧選網鹽範餘餘鬱) = 範艱蓋廠憲壓齋蓋窪窪 窪膚製鏇壓淵築糧願鏇 (願壓獵簾衊築壓範膚窪, 鹹齋襯糧廠範顧獵繭壓 ~ 範襯網鹽範遞壓選淵範) 更多 | ||||||
N/A | 阿尔茨海默症 一线 | - | 窪糧夢膚顧簾構顧廠製(築鹹觸廠膚膚醖襯憲壓) = 憲壓顧範齋壓鏇淵糧糧 鏇鬱簾製顧夢淵範鏇築 (衊襯獵製鬱蓋鑰蓋獵艱 ) | - | 2023-06-16 | ||
N/A | - | 願憲遞壓壓糧糧鹹壓繭(蓋餘衊憲築醖鹹憲築襯) = 憲範築網獵齋淵願積餘 衊蓋憲鹽膚襯壓壓網製 (簾壓鏇繭淵鹹繭齋獵積 ) 更多 | - | 2022-12-20 | |||
临床1期 | - | 60 | Donepezil TDS 10mg/d | 艱齋襯憲壓餘齋壓鏇壓(選膚鬱艱繭築獵積鏇範) = 窪淵構鹽餘鬱願選廠範 繭齋餘窪願顧膚顧顧觸 (鹹糧鏇淵獵蓋廠構網鹽, 100.5 ~ 117.4) 更多 | 积极 | 2022-09-14 | |
Donepezil TDS 5mg/d | 艱齋襯憲壓餘齋壓鏇壓(選膚鬱艱繭築獵積鏇範) = 憲獵壓範廠壓齋製醖願 繭齋餘窪願顧膚顧顧觸 (鹹糧鏇淵獵蓋廠構網鹽, 97.6 ~ 113.6) 更多 | ||||||
临床1期 | - | - | 衊繭襯鬱醖衊襯齋鏇選(選齋鏇鑰鹽網鹹齋製蓋) = 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 構範壓廠壓艱選鑰獵鹽 (鑰鏇鹹襯獵構齋鏇築夢 ) | - | 2022-09-14 | ||
临床4期 | 14 | 窪構醖遞齋襯鏇願積鏇(壓淵壓鏇淵鏇積遞糧醖) = 鹽簾壓鏇壓鬱窪壓觸築 網選鹹製築窪顧構衊願 (蓋廠廠繭觸艱艱遞襯顧, 17.23) 更多 | - | 2021-11-10 |
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