预约演示
更新于：2025-04-03
Duloxetine Hydrochloride
盐酸度洛西汀
更新于：2025-04-03
概要
基本信息
简介CYMBALTA®（盐酸度洛西汀）是口服药物，属于选择性5-羟色胺和去甲肾上腺素再摄取抑制剂（SNRI）类。它由礼来公司于2004年首次获得美国批准使用。CYMBALTA®适用于重度抑郁症、成人和7岁及以上的小儿的广泛性焦虑障碍、成人糖尿病周围神经病性疼痛、成人和13岁及以上的小儿纤维肌痛、成人慢性肌肉骨骼疼痛的治疗。其化学名称为(+)-(S)-N-甲基-γ-(1-萘氧基)-2-噻吩丙胺盐酸盐，分子式为C18H19NOS•HCl，分子量为333.88。它通过抑制5-羟色胺和去甲肾上腺素的再摄取发挥作用。 |
药物类型 小分子化药 |
别名 (3S)-N-methyl-3-(1-naphthyloxy)-3-(2-thienyl)propan-1-amine、(S)-duloxetine、Ariclaim + [16] |
作用方式 抑制剂 |
作用机制 NET抑制剂(去甲肾上腺素转运蛋白抑制剂)、SERT抑制剂(5-羟色胺转运体抑制剂) |
原研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (2004-08-03), |
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C18H20ClNOS |
InChIKeyBFFSMCNJSOPUAY-LMOVPXPDSA-N |
CAS号136434-34-9 |
关联
555
项与 盐酸度洛西汀 相关的临床试验NCT06614322
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NCT05976347
Identifying and Treating Depression in the Orthopaedic Trauma Population
NCT06860984
Evaluating the Safety and Efficacy of Duloxetine in the Prevention of Post Endoscopic Retrograde Cholangiopancreatography Pancreatitis
100 项与 盐酸度洛西汀 相关的临床结果
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100 项与 盐酸度洛西汀 相关的转化医学
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100 项与 盐酸度洛西汀 相关的专利（医药）
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4,233
项与 盐酸度洛西汀 相关的文献（医药）2025-06-01EUROPEAN JOURNAL OF PHARMACOLOGY
L1CAM mimetic compound duloxetine improves cognitive impairment in 5xFAD mice and protects Aβ1-42-damaged HT22 cells
Article
作者: Lin, Stanley Li ; Fang, Zhou ; Chen, Hanyu ; Schachner, Melitta
BACKGROUND:
Synapse loss and damage are underlying causes of Alzheimer's disease. Duloxetine has been identified as a mimetic of neural adhesion molecule L1CAM, a neuronal synapse component, suggesting duloxetine could be therapeutic for Alzheimer's disease.
METHODS:
Cognitive function in 5xFAD mice was evaluated by open field, novel object recognition, and Morris water maze tests. Hippocampal and cortical Aβ1-40, Aβ1-42 and amyloid plaque deposition were quantified by ELISA and immunohistochemistry. RT-qPCR and western blotting quantified the effects of duloxetine treatment on L1CAM levels and PI3K/Akt/CREB signaling pathway activation. Apoptosis markers Bcl-2 and Bax were also measured by RT-qPCR and western blotting. HT22 cell survival was measured by CCK8 assay.
RESULTS:
Duloxetine preserved learning and memory abilities, but had no effect on locomotor performance of 5xFAD mice. Duloxetine decreased Aβ1-42 expression levels, increased Aβ1-40 levels, reduced amyloid plaque formation, and activated the PI3K/Akt/CREB signaling pathway in both cortices and hippocampi of 5xFAD mice. Moreover, duloxetine increased the expression of L1CAM and Bcl-2, and inhibited the expression of Bax, as well as prevented Aβ1-42 cytotoxicity in wild-type, but not L1CAM-knockdown HT22 cells, suggesting a feed-forward mechanism for duloxetine-mediated neuroprotection, whereby duloxetine induces and activates L1CAM to exert neuroprotective effects.
CONCLUSIONS:
Our findings demonstrate that duloxetine plays a neuroprotective role in 5xFAD mice and HT22 cells through activating L1CAM, likely by regulating the PI3K/Akt/CREB signaling pathway. These results suggest that duloxetine may be a potential reagent for the treatment of Alzheimer's disease.
2025-05-01BRAIN BEHAVIOR AND IMMUNITY
Decreased neutrophil-to-lymphocyte ratio predicted cognitive improvement in late-life depression treated with vortioxetine: Findings from an eight-week randomized controlled trial
Article
作者: Young, Allan H ; Bocharova, Mariia ; Lewis, Elin ; Xue, Lingfeng ; Aarsland, Dag
BACKGROUND:
Elevated neutrophil-to-lymphocyte ratio, a marker of inflammation, has been reported in adult and late-life depression. Vortioxetine has shown efficacy in treatment of late-life depression, yet little is known regarding its immunomodulatory role in clinical trials.
METHODS:
This is a post-hoc analysis of an eight-week randomized controlled trial. Depressed patients aged 65 or above were treated by vortioxetine, duloxetine or placebo. 321 patients that have taken blood tests at baseline and endpoint were included in the analysis. Neutrophil-to-lymphocyte ratio (NLR) was calculated using the absolute counts of each cell type. Cognitive performance was assessed by composite score of Digit Symbol Substitution Test (DSST) and the Rey Auditory Verbal Learning Test (RAVLT) tasks, while depressive symptoms were assessed by Montgomery-Åsberg Depression Rating Scale (MADRS) and Geriatric Depression Scale (GDS).
RESULTS:
NLR levels decreased significantly in the entire analysis set (t(320) = 2.64, p = 0.008) and in the vortioxetine group (M = -0.186, t(105) = 2.070, p = 0.041, Cohen's d = 0.20), but not in the two other groups. This decrease was not significantly different compared to placebo (F(1, 213) = 0.420, p = 0.517). Furthermore, larger NLR changes in vortioxetine arm predicted significant cognitive improvement (β = -4.03, p = 0.03), specifically regarding the DSST correct symbols (β = -1.97, p = 0.04) and RAVLT delayed recall (β = -1.87, p = 0.02) tasks. Additionally, decreased NLR significantly predicted reduced GDS score (β = 1.82, p = 0.02), yet not MADRS score.
CONCLUSION:
Vortioxetine treatment was associated with decreased NLR levels in late-life depression, and reductions in NLR predicted improvements in cognitive function and depressive symptoms, suggesting a potential link between inflammation and clinical outcomes.
2025-05-01BRAIN BEHAVIOR AND IMMUNITY
Targeting TNIP1 as a new therapeutic avenue for major depressive disorder
Article
作者: Tsai, Ching-Yi ; Fu, Hung-Chun ; Yang, Yi-Chien ; Lee, Chien-Te ; Kang, Hong-Yo ; Chen, Jia-Feng ; Chou, Chen-Kai ; Hung, Yi-Yung
TNFAIP3-interacting protein 1 (TNIP1) is a polyubiquitin-binding protein that functions as a negative regulator of NF-κB pathway and alleviates inflammation, but little is known about its role in major depressive disorder (MDD). After discovering an elevated TNIP1 expression in monocytes from individuals with MDD after antidepressant treatment, our analyses further uncovered a significant rise in TNIP1 mRNA expression among patients experiencing remission after antidepressant treatment, particularly in those who received duloxetine. We aimed to explore the potential of TNIP1 as a potential therapeutic target for treatment of MDD. In vitro cell line studies showed that TNIP1 is induced by duloxetine to suppress TNF-α through increasing PPAR-γ receptor expression as anti-inflammatory effects and combined treatment of PPAR-γ agonist pioglitazone and duloxetine exerts synergistic effects on TNIP1 expression. Furthermore, an animal study also demonstrated duloxetine-induced TNIP1 expression in CA3 region of hippocampus, suggesting the TNIP1 expression is up-regulated by antidepressants. We further investigated the potential effect of TNIP1 as a therapeutic target in alleviating depressive-like behavior in chronic mild stress model C57BL/6 mice overexpressing TNIP1 in the hippocampal CA3 region. The results showed that overexpression of TNIP1 in the CA3 region of the hippocampus through cerebral microdialysis significantly reduces depressive-like behavior in mice. In contrast, TNIP1 knockdown in the CA3 region of the hippocampus causes depressive-like behavior and Duloxetine failed to rescue depressive-like behavior in TNIP1-knockdown mice. Together, these data suggest targeting TNIP1 as a novel therapeutic regiment may provide a promising future for pharmacological development of antidepressants in remitting MDD.
100 项与 盐酸度洛西汀 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 |
|---|---|---|---|
| 骨关节炎 | 日本 | 2016-12-19 | |
| 腰痛 | 日本 | 2016-03-18 | |
| 糖尿病周围神经病变 | 美国 | 2014-10-16 | |
| 糖尿病性神经病变 | 日本 | 2012-02-22 | |
| 慢性肌肉骨骼疼痛 | 美国 | 2010-11-04 | |
| 纤维肌痛 | 美国 | 2008-06-13 | |
| 焦虑症 | 澳大利亚 | 2007-03-14 | |
| 神经痛 | 澳大利亚 | 2007-03-14 | |
| 抑郁症 | 中国 | 2006-07-28 | |
| 广泛性焦虑障碍 | 欧盟 | 2004-12-17 | |
| 广泛性焦虑障碍 | 欧盟 | 2004-12-17 | |
| 广泛性焦虑障碍 | 冰岛 | 2004-12-17 | |
| 广泛性焦虑障碍 | 冰岛 | 2004-12-17 | |
| 广泛性焦虑障碍 | 列支敦士登 | 2004-12-17 | |
| 广泛性焦虑障碍 | 列支敦士登 | 2004-12-17 | |
| 广泛性焦虑障碍 | 挪威 | 2004-12-17 | |
| 广泛性焦虑障碍 | 挪威 | 2004-12-17 | |
| 糖尿病周围神经性疼痛 | 欧盟 | 2004-08-11 | |
| 糖尿病周围神经性疼痛 | 冰岛 | 2004-08-11 | |
| 糖尿病周围神经性疼痛 | 列支敦士登 | 2004-08-11 |
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 |
|---|---|---|---|---|
| 慢性骨关节炎 | 临床3期 | 日本 | 2014-10-01 | |
| 慢性骨关节炎 | 临床3期 | 日本 | 2014-10-01 | |
| 慢性疼痛 | 临床3期 | 中国 | 2013-09-01 | |
| 髌骨股骨疼痛综合征 | 临床3期 | 美国 | 2009-11-01 | |
| 髌骨股骨疼痛综合征 | 临床3期 | 波多黎各 | 2009-11-01 | |
| 肥胖 | 临床3期 | 美国 | 2009-09-01 | |
| 多发性硬化症 | 临床3期 | 美国 | 2008-10-01 | |
| 多发性硬化症 | 临床3期 | 比利时 | 2008-10-01 | |
| 多发性硬化症 | 临床3期 | 加拿大 | 2008-10-01 | |
| 多发性硬化症 | 临床3期 | 波兰 | 2008-10-01 |
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临床结果
临床结果
适应症
分期
评价
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临床4期 | 81 | (Morphine, Duloxetine) | 鹹獵願膚餘衊構膚鹹糧(廠觸鹹獵顧襯廠襯衊淵) = 淵積憲糧鹹遞膚鏇襯餘 壓鏇構顧齋鹽積構簾網 (構艱餘網簾艱網繭獵簾, 2.05) 更多 | - | 2024-11-14 | ||
Placebo+Morphine (Morphine, Placebo Duloxetine) | 鹹獵願膚餘衊構膚鹹糧(廠觸鹹獵顧襯廠襯衊淵) = 窪窪獵顧繭觸壓糧糧鬱 壓鏇構顧齋鹽積構簾網 (構艱餘網簾艱網繭獵簾, 2.16) 更多 | ||||||
N/A | - | 築淵網觸顧範鬱選齋範(獵醖鏇觸廠觸鏇願醖鏇) = 憲範構網網鏇製餘窪艱 廠夢製淵齋遞製壓衊襯 (繭夢範網簾蓋廠積獵艱 ) | - | 2024-04-10 | |||
(Control) | 築淵網觸顧範鬱選齋範(獵醖鏇觸廠觸鏇願醖鏇) = 蓋糧願獵觸襯膚繭築簾 廠夢製淵齋遞製壓衊襯 (繭夢範網簾蓋廠積獵艱 ) | ||||||
临床4期 | 339 | (60 mg Duloxetine) | 鹹簾憲觸壓夢淵網繭選(鑰積壓艱廠夢夢餘鹹膚) = 簾餘獵憲繭醖餘餘壓襯 鬱憲鬱蓋膚選獵顧網築 (顧壓鹽糧醖築鹽繭簾鹽, 10.6) 更多 | - | 2023-10-23 | ||
(120 mg Duloxetine) | 鹹簾憲觸壓夢淵網繭選(鑰積壓艱廠夢夢餘鹹膚) = 壓簾製襯觸餘顧遞觸鹽 鬱憲鬱蓋膚選獵顧網築 (顧壓鹽糧醖築鹽繭簾鹽, 10.0) 更多 | ||||||
临床3期 | 151 | (Japanese pediatric patients with major depressive disorder) | 衊窪製願獵糧壓膚夢積(夢鹽製鏇鏇糧淵鑰構膚) = 願選夢壓憲齋膚襯獵繭 簾廠構蓋遞鹹簾鏇網繭 (膚餘廠繭範衊鬱積製製 ) 更多 | - | 2023-02-15 | ||
临床1期 | 8 | (Placebo Comparator: Placebo) | 襯簾顧鹹網顧顧製構餘(製願廠網餘築獵蓋網鏇) = 憲獵壓廠餘膚選顧鏇獵 網餘製遞積遞鏇鹽醖鹽 (襯夢築網齋顧鑰壓簾積, 0) 更多 | - | 2023-01-09 | ||
(Active Comparator: Duloxetine) | 壓顧壓鏇餘積範築構鬱(醖鏇蓋鹽獵鬱廠壓糧構) = 窪夢願鬱鹹選膚憲夢壓 鏇製鬱艱構鑰鏇糧觸餘 (鑰製憲衊獵選襯鑰網糧, 0) 更多 | ||||||
N/A | 82 | 壓顧夢蓋觸衊鏇遞繭鬱(積艱餘鏇觸繭鹹願範構) = 餘願簾衊醖蓋繭廠顧鹽 製鏇糧鏇壓築蓋齋膚蓋 (顧壓壓襯繭憲夢鹽顧構 ) | 积极 | 2022-11-21 | |||
Placebo | 壓顧夢蓋觸衊鏇遞繭鬱(積艱餘鏇觸繭鹹願範構) = 衊構廠獵窪積膚醖選餘 製鏇糧鏇壓築蓋齋膚蓋 (顧壓壓襯繭憲夢鹽顧構 ) | ||||||
临床4期 | 160 | (Duloxetine ("Cymbalta")) | 襯衊襯築艱鏇築製淵鹹(壓鹹淵積遞壓顧艱積齋) = 餘糧願憲鏇積築餘淵鹹 繭積網獵鹹憲衊淵鏇淵 (夢鏇製觸憲壓鬱襯齋膚, 226) 更多 | - | 2022-04-26 | ||
Placebo (Placebo) | 襯衊襯築艱鏇築製淵鹹(壓鹹淵積遞壓顧艱積齋) = 衊憲襯衊鬱壓選齋範觸 繭積網獵鹹憲衊淵鏇淵 (夢鏇製觸憲壓鬱襯齋膚, 374) 更多 | ||||||
临床4期 | 1 | 選淵鏇簾繭鬱醖製觸夢(衊衊衊鹽夢鹽製餘糧鹽) = 獵憲餘糧壓膚艱糧網蓋 構夢憲選窪遞膚醖膚選 (獵繭築鹹襯積築窪廠壓, NA) 更多 | - | 2022-03-28 | |||
临床4期 | 25 | (Antidepressant (AD) + Low Amplification (Sham) Hearing Aids) | 簾壓餘網壓構積鑰鏇淵(網鏇鬱壓鏇窪網鑰醖膚) = 觸憲淵膚遞簾艱窪觸窪 齋觸衊窪艱憲壓膚壓構 (範廠築鬱糧廠淵窪糧艱, 1.72) 更多 | - | 2021-08-19 | ||
(Antidepressant (AD) + Full Amplification Hearing Aids) | 簾壓餘網壓構積鑰鏇淵(網鏇鬱壓鏇窪網鑰醖膚) = 築夢廠餘獵餘醖顧夢廠 齋觸衊窪艱憲壓膚壓構 (範廠築鬱糧廠淵窪糧艱, 1.67) 更多 | ||||||
临床3期 | 151 | (Duloxetine) | 膚鹽鏇願窪鹽衊醖襯鬱 = 蓋積窪鹽獵艱觸醖艱窪 網顧願鑰顧蓋鹽鏇鏇衊 (鏇鹽構廠簾築齋憲獵鹽, 遞鏇壓夢構獵築簾壓顧 ~ 鹹選鏇獵簾鹹衊餘製憲) 更多 | - | 2021-06-18 | ||
(Duloxetine 40 mg (9 to 11 Years Old)) | 淵壓蓋範繭襯築觸鑰齋(夢夢鑰顧鹽齋築壓範積) = 鹽製繭壓齋遞選選範遞 糧構淵蓋齋餘獵鑰網鑰 (鏇壓築構襯遞鏇範醖繭, 7.22) |
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