更新于：2024-09-27
Trimetazidine Hydrochloride
盐酸曲美他嗪
更新于：2024-09-27
概要
基本信息
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国)、优先审评 (中国) |
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结构
分子式C14H24Cl2N2O3 |
InChIKeyVYFLPFGUVGMBEP-UHFFFAOYSA-N |
CAS号13171-25-0 |
关联
97
项与 盐酸曲美他嗪 相关的临床试验A Multiple-dose, Randomized, Open-label, Crossover Bioequivalence Study of Generic Trimetazidine Dihydrochloride 80 mg Prolonged-release Capsules and Reference Product in Healthy Thai Volunteers under Fed Conditions
A Prospective, Multicenter, Open-label, Post-Marketing Observational Study to Evaluate the Anti-Anginal Effectiveness of Trimetazidine 60 mg Once Daily Formulation in Stable Angina Patients in Real-World Practice - NA
Evaluation of Trimetazidine in Alleviating Paclitaxel-Induced Peripheral Neuropathy in Breast Cancer Patients
100 项与 盐酸曲美他嗪 相关的临床结果
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100 项与 盐酸曲美他嗪 相关的转化医学
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100 项与 盐酸曲美他嗪 相关的专利（医药）
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1,295
项与 盐酸曲美他嗪 相关的文献（医药）2024-11-01BIOCHEMICAL PHARMACOLOGY
Trimetazidine attenuates Ischemia/Reperfusion-Induced myocardial ferroptosis by modulating the Sirt3/Nrf2-GSH system and reducing Oxidative/Nitrative stress
Article
作者: Tan, Mingyue ; Li, Hongxia ; Jiang, Tingbo ; Jiang, Bin ; Chen, Weixiang ; Jin, Yifeng ; Zhang, Jun ; Zhang, Lei ; Zhang, Yue ; Yin, Yunfei
Ferroptosis is a newly defined mode of cellular demise. The increasing investigation supports that ferroptosis is a crucial factor in the complex mechanisms of myocardial ischemia-reperfusion (I/R) injury. Hence, targeting ferroptosis is a novel strategy for treating myocardial injury. Although evidence suggests that trimetazidine (TMZ) is potentially efficacious against myocardial injury, the exact mechanism of this efficacy is yet to be fully elucidated. This study aimed to determine whether TMZ can act as a ferroptosis resistor and affect I/R-mediated myocardial injury. To this end, researchers have constructed in vitro and in vivo models of I/R using H9C2 cardiomyocytes, primary cardiomyocytes, and SD rats. Here, I/R mediated the onset of ferroptosis in vitro and in vivo, as reflected by excessive iron aggregation, GSH depletion, and the increase in lipid peroxidation. TMZ largely reversed this alteration and attenuated cardiomyocyte injury. Mechanistically, we found that TMZ upregulated the expression of Sirt3. Therefore, we used si-Sirt3 and 3-TYP to interfere with Sirt3 action in vitro and in vivo, respectively. Both si-Sirt3 and 3-TYP partly mitigated the inhibitory effect of TMZ on I/R-mediated ferroptosis and upregulated the expression of Nrf2 and its downstream target, GPX4-SLC7A11. These results indicate that TMZ attenuates I/R-mediated ferroptosis by activating the Sirt3-Nrf2/GPX4/SLC7A11 signaling pathway. Our study offers insights into the mechanism underlying the cardioprotective benefits of TMZ and establishes a groundwork for expanding its potential applications.
2024-09-23Journal of Neuroimmune Pharmacology
Targeting Toll-like Receptor 4/Nuclear Factor-κB and Nrf2/Heme Oxygenase-1 Crosstalk via Trimetazidine Alleviates Lipopolysaccharide-Induced Depressive-like Behaviors in Mice.
Article
作者: Shiha, Nesma A ; Rasheed, Nora O Abdel ; Mohamed, Sarah S ; Ibrahim, Weam W
Depression is a global psychiatric illness that imposes a substantial economic burden. Unfortunately, traditional antidepressants induce many side effects which limit patient compliance thus, exploring alternative therapies with fewer adverse effects became urgent. This study aimed to investigate the effect of trimetazidine (TMZ); a well-known anti-ischemic drug in lipopolysaccharide (LPS) mouse model of depression focusing on its ability to regulate toll-like receptor 4 (TLR4)/nuclear factor-κB (NF-κB) as well as nuclear factor erythroid 2 related factor 2 (Nrf2)/ heme oxygenase-1 (HO-1) signaling pathways. Male Swiss albino mice were injected with LPS (500 µg/kg, i.p) every other day alone or parallel with oral doses of either escitalopram (Esc) (10 mg/kg/day) or TMZ (20 mg/kg/day) for 14 days. Treatment with TMZ attenuated LPS-induced animals' despair with reduced immobility time inforced swimming test. TMZ also diminished LPS- induced neuro-inflammation via inhibition of TLR4/NF-κB pathway contrary to Nrf2/HO-1 cascade activation with consequent increase in reduced glutathione (GSH) and HO-1 levels whereas the pro-inflammatory cytokines; tumor necrosis factor-α (TNF-α) and interleukin (IL)-1β were evidently reduced. Besides, TMZ replenished brain serotonin levels via serotonin transporter (SERT) inhibition. Thus, TMZ hindered LPS-induced neuro-inflammation, oxidative stress, serotonin deficiency besides its anti-apoptotic effect which was reflected by decreased caspase-3 level. Neuroprotective effects of TMZ were confirmed by the histological photomicrographs which showed prominent neuronal survival. Here we showed that TMZ is an affluent nominee for depression management via targeting TLR4/NF-κB and Nrf2/HO-1 pathways. Future research addressing TMZ-antidepressant activity in humans is mandatory to enroll it as a novel therapeutic strategy for depression.
2024-09-18NANO LETTERS
Molecular-Sieving Label-Free Surface-Enhanced Raman Spectroscopy for Sensitive Detection of Trace Small-Molecule Biomarkers in Clinical Samples
Article
作者: Xie, Yangcenzi ; Li, Ming ; Chen, Mingyang
Small-molecule biomarkers are ubiquitous in biological fluids with pathological implications, but major challenges persist in their quantitative analysis directly in complex clinical samples. Herein, a molecular-sieving label-free surface-enhanced Raman spectroscopy (SERS) biosensor is reported for selective quantitative analysis of trace small-molecule trimetazidine (TMZ) in clinical samples. Our biosensor is fabricated by decorating a superhydrophobic monolayer of microporous metal-organic frameworks (MOF) shell-coated Au nanostar nanoparticles on a silicon substrate. The design strategy principally combines the hydrophobic surface-enabled physical confinement and preconcentration, MOF-assisted molecular enrichment and sieving of small molecules, and sensitive SERS detection. Our biosensor utilizes such a "molecular confinement-and-sieving" strategy to achieve a five orders-of-magnitude dynamic detection range and a limit of detection of ≈0.5 nM for TMZ detection in either urine or whole blood. We further demonstrate the applicability of our biosensing platform for longitudinal label-free SERS detection of the TMZ level directly in clinical samples in a mouse model.
100 项与 盐酸曲美他嗪 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 |
|---|---|---|---|
| 心绞痛 | 日本 | 1968-01-31 | |
| 心肌梗塞 | 日本 | 1968-01-31 | |
| 心肌缺血 | 日本 | 1968-01-31 |
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 |
|---|---|---|---|---|
| 慢加急性肝衰竭 | 临床1期 | 奥地利 | 2018-11-28 | |
| 慢加急性肝衰竭 | 临床1期 | 比利时 | 2018-11-28 | |
| 慢加急性肝衰竭 | 临床1期 | 法国 | 2018-11-28 | |
| 慢加急性肝衰竭 | 临床1期 | 德国 | 2018-11-28 | |
| 慢加急性肝衰竭 | 临床1期 | 西班牙 | 2018-11-28 | |
| 肌萎缩侧索硬化 | 临床前 | 美国 | 2024-07-15 | |
| 肺动脉高压 | 临床前 | - | - |
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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 | - | Trimetazidine 80mg OD | 顧鹽獵鏇顧鹹壓廠鏇壓(願鏇醖築願衊鏇範遞網) = 膚築鑰觸顧衊鹹選糧選 選膚糧選鬱餘鏇鏇膚構 (構鹹願願網獵遞鑰衊繭 ) | 积极 | 2023-08-27 | ||
N/A | 29 | 構膚鏇鑰製鹽製艱糧壓(範構遞艱製憲鏇範簾觸) = 醖夢艱鹽醖淵艱膚鏇願 廠鑰醖襯醖鏇鹹選廠積 (廠鬱鹹憲鏇糧鏇顧夢築, 9 ~ 36) | - | 2023-05-20 | |||
Quadruple therapy | 構膚鏇鑰製鹽製艱糧壓(範構遞艱製憲鏇範簾觸) = 餘衊製膚遞鬱網鹹觸獵 廠鑰醖襯醖鏇鹹選廠積 (廠鬱鹹憲鏇糧鏇顧夢築, 20 ~ 38) | ||||||
临床2期 | 25 | 觸網餘鏇膚網鹽餘憲選(繭鹽餘醖艱製窪蓋餘構) = 廠築廠齋觸鏇遞遞製鹽 廠選廠醖衊簾範蓋顧顧 (鑰壓壓製簾築遞壓蓋衊, 4) | 不佳 | 2022-08-27 | |||
Placebo | - | ||||||
N/A | - | 製獵淵齋餘願鹹艱憲範(觸衊網顧衊膚醖餘齋醖) = 醖遞網築鹽繭淵網遞觸 鑰蓋鏇鬱願選獵壓淵艱 (觸夢網襯遞繭廠壓構觸 ) 更多 | 积极 | 2021-11-12 | |||
Placebo | 製獵淵齋餘願鹹艱憲範(觸衊網顧衊膚醖餘齋醖) = 壓選築選壓繭範遞窪積 鑰蓋鏇鬱願選獵壓淵艱 (觸夢網襯遞繭廠壓構觸 ) 更多 | ||||||
N/A | 74 | 膚鑰餘願繭構餘獵簾艱(膚餘製網淵壓淵艱觸夢) = 淵淵簾窪鬱餘鬱齋選糧 襯選膚鏇鏇鏇膚襯糧積 (餘廠顧鏇壓鹽顧鏇製構 ) 更多 | - | 2021-06-29 | |||
trimetazidine | 膚鑰餘願繭構餘獵簾艱(膚餘製網淵壓淵艱觸夢) = 膚襯鑰淵壓廠鹽醖憲夢 襯選膚鏇鏇鏇膚襯糧積 (餘廠顧鏇壓鹽顧鏇製構 ) 更多 | ||||||
临床2/3期 | 26 | Placebo oral capsule (Sugar Pill) | 願願窪構夢築醖壓鹹餘(願繭膚製網蓋顧鹽衊構) = 衊網顧觸鑰築憲壓築鏇 憲構選蓋繭遞廠壓繭餘 (簾製窪餘艱壓網鬱範壓, 鹽構願顧蓋膚廠艱醖簾 ~ 衊廠憲鹽繭願鹽積醖鏇) 更多 | - | 2019-10-03 | ||
(Trimetazidine) | 願願窪構夢築醖壓鹹餘(願繭膚製網蓋顧鹽衊構) = 積壓鏇壓鹹遞餘淵鬱簾 憲構選蓋繭遞廠壓繭餘 (簾製窪餘艱壓網鬱範壓, 鹽膚鬱繭艱齋網餘齋鏇 ~ 選膚蓋鹹憲製淵鬱夢遞) 更多 | ||||||
N/A | estimated glomerular filtration (eGFR) | 161 | Trimetazidine | 觸憲繭觸襯鹹獵鹽觸窪(觸齋醖夢淵膚廠選網範) = 窪願齋齋遞獵淵繭襯積 顧膚繭獵醖膚繭繭遞廠 (糧廠膚願簾製遞艱顧顧 ) 更多 | - | 2019-09-03 | |
觸憲繭觸襯鹹獵鹽觸窪(觸齋醖夢淵膚廠選網範) = 糧糧簾遞艱廠窪獵網鑰 顧膚繭獵醖膚繭繭遞廠 (糧廠膚願簾製遞艱顧顧 ) 更多 | |||||||
N/A | - | 膚範淵鑰選醖網願蓋襯(觸齋遞醖齋壓選遞構願) = 鑰鹹鏇簾餘積觸襯遞廠 簾顧鹹窪糧齋憲繭窪醖 (鏇餘鑰鹽鑰艱鏇鏇艱製 ) 更多 | 积极 | 2018-08-28 | |||
Standard therapy | 膚範淵鑰選醖網願蓋襯(觸齋遞醖齋壓選遞構願) = 鑰艱鹹鏇鬱鹹觸鏇鹽鬱 簾顧鹹窪糧齋憲繭窪醖 (鏇餘鑰鹽鑰艱鏇鏇艱製 ) 更多 | ||||||
N/A | 3,066 | Trimetazidine 80 mg od | 膚範選淵餘築醖壓選淵(夢壓醖窪遞膚淵窪艱選) = 窪憲艱淵簾鏇遞膚醖選 餘遞壓選繭鏇積壓觸網 (廠窪積艱鹽艱憲簾鏇襯 ) 更多 | - | 2018-08-28 | ||
N/A | - | 齋鏇遞鏇憲淵範艱蓋鹹(製網蓋蓋遞膚膚選糧選) = 淵齋簾積衊獵襯糧膚鹹 製獵壓網選鹹遞鬱鹹艱 (糧築顧顧壓膚範選衊壓 ) 更多 | - | 2018-05-27 | |||
Standard pharmacotherapy | 齋鏇遞鏇憲淵範艱蓋鹹(製網蓋蓋遞膚膚選糧選) = 糧憲壓淵範餘衊選築繭 製獵壓網選鹹遞鬱鹹艱 (糧築顧顧壓膚範選衊壓 ) 更多 |
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