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更新于：2026-02-28
Eprosartan Mesylate
依普沙坦
更新于：2026-02-28
概要
基本信息
药物类型 小分子化药 |
别名 (E)-2-butyl-1-(p-carboxybenzyl)-α-2-thenylimidazole-5-acrylic acid、(E)-3-[2-n-butyl-1-{(4-carboxyphenyl)methyl}-1H-imidazol-5-yl]-2-(2-thienyl)methyl-2-propenoic acid、(E)-α{[2-butyl-1-[(4-carboxyphenyl)methyl]-1H-imidazole-5-yl]methylene}-2-thiopheneproprionic acid + [18] |
靶点 |
作用方式 拮抗剂 |
作用机制 AT1R拮抗剂(血管紧张素II-1型受体拮抗剂) |
治疗领域 |
非在研适应症- |
原研机构 |
权益机构- |
最高研发阶段批准上市 |
首次获批日期 美国 (1997-12-22), |
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C24H28N2O7S2 |
InChIKeyDJSLTDBPKHORNY-XMMWENQYSA-N |
CAS号144143-96-4 |
关联
8
项与 依普沙坦 相关的临床试验NCT04606563
Host Response Mediators in Coronavirus (COVID-19) Infection - Is There a Protective Effect of Losartan and Other ARBs on Outcomes of Coronavirus Infection?
NCT01631227
A Prospective, Randomized Double-blind Parallel Group Study to Compare the Effect of Eprosartan and Eprosartan Mesylate on Blood Pressure in Subjects With Mild to Moderate Essential Hypertension
NCT01502904
Neointimal Coverage After Implantation of Biolimus Eluting Stent With Biodegradable Polymer: Optical Coherence Tomographic Assessment According to the Treatment of Dyslipidemia and Hypertension and the Types of Implanted Drug-eluting Stents
100 项与 依普沙坦 相关的临床结果
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100 项与 依普沙坦 相关的转化医学
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100 项与 依普沙坦 相关的专利（医药）
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609
项与 依普沙坦 相关的文献（医药）2026-01-07ACS Chemical Neuroscience
Decoding the Neuroprotective Intervention of Angiotensin Receptor Blockers: A Multimodal Approach Using
In Silico
Network Pharmacology, Molecular Modeling, and
In Vivo
Validation of Key Markers
Article
作者: Karmakar, Varnita ; Gorain, Bapi ; Ghosh, Arya ; Majie, Ankit ; Deb, Pran Kishore
Angiotensin receptor blockers (ARBs) have been relatively less explored in the field of neuroprotection and dementia; however, ample preclinical and clinical evidence suggests their potential cognitive benefits. Despite these findings, there remains limited evidence on precise mechanistic pathways involved, highlighting the critical need to bridge the gap. In our previous work, we presented the beneficial effect of azilsartan in a dementia model and observed promising neuroprotective outcomes. Building on these findings, this study sought to compare the activity of azilsartan with other commonly used ARBs, including telmisartan, olmesartan, valsartan, eprosartan, irbesartan, and candesartan, using an integrative network pharmacology approach. Our network analysis identified 12 key target proteins implicated in dementia pathology, which were further subjected to docking studies with the seven ARBs, revealing strong binding affinities of azilsartan, olmesartan, and telmisartan with critical signaling proteins, including AKT1, PIK3CA, and PIK3CB. Molecular dynamics simulations further confirmed the stability and favorable interactions of azilsartan with these targets. To experimentally validate these predictions, in vivo studies were conducted in a scopolamine-induced memory-impaired model, which demonstrated significant restoration of the levels of AKT1 and PIK3CA. These findings clearly demonstrate the PI3K/AKT modulating effects of azilsartan, reinforcing its repurposing potential in dementia and related disorders, thereby expanding novel therapeutic opportunities within this drug class.
2025-12-01MOLECULAR AND CELLULAR NEUROSCIENCE
Eprosartan alleviates the traumatic brain injury-induced multi-organ dysfunction syndrome in mice via AT1R/SNS/HMGB1 blockade and PDL-1 modulation
Article
作者: Saini, Paras ; Lather, Deepika ; Deepak, Deepak ; Vasudeva, Neeru ; Sharma, Sunil ; Thakur, Manisha
Traumatic brain injury is not constrained only to the brain but delayed secondary events disturb the end organ functioning via intense response of three homeostatic mechanisms such as sympathetic activity, inflammation, and immunosuppression. Current study involved weight drop model to induce TBI in Swiss albino mice. Eprosartan was administered orally after 30-45 min post injury to mice in 0.35 mg/kg and 0.7 mg/kg doses. Mice were tested for neurobehavioral alterations and multiple organs, including brain, heart, lungs, liver, and kidney were excised for further edema, biochemical, inflammatory, catecholamine, gene expression and histopathological estimations at both acute and chronic phases of injury. Results highlighted that Epro improved neurobehavioral performance, maintained the BBB and lung integrity. It also ameliorated the oxidative stress as well as docking studies exhibited strong binding affinity of Epro for HMGB1 and PDL-1, that further supported by low tissue HMGB1 and serum IL-6 and TNF-α cytokines levels which halted the systemic hyperinflammation. Moreover, Epro treatment successfully restored the cardiac, hepatic and kidney function through stabilized serum biomarkers with declined plasma noradrenaline levels that subsides the sympathetic storm. Considerably, a bizarre cellular morphology was displayed by the organs in acute phase of injury whereas Epro reversed the morphological changes at chronic stage. Also, epro encouraged the PD-1/PDL-1 and IL-10 gene expression in the tissues that regulates immune response. Thus, it is concluded that Epro exerts its organ protective effect against MODS via AT1/SNS pathway inhibition.
2025-11-02Expert Opinion On Drug Safety
A pharmacovigilance study assessing risk of angioedema with angiotensin receptor blockers using the US FDA Adverse Event Reporting System
Article
作者: Sridharan, Kannan ; Sivaramakrishnan, Gowri
BACKGROUND:
Angiotensin receptor blockers (ARBs) are widely used for treating hypertension and heart failure. Angioedema has been reported as a controversial adverse effect of ARBs and the evidence on individual ARB risks is limited. This study aimed to assess signals of angioedema with different ARBs using the US FDA Adverse Event Reporting System (AERS) database.
RESEARCH DESIGN AND METHODS:
Reports of angioedema from 2004 to 2024 in AERS with an ARB as the primary suspect were extracted using Medical Dictionary for Regulatory Activities queries. Disproportionality analyses including reporting odds ratio, proportional reporting ratio, Bayesian confidence propagation neural network and multi-item gamma Poisson shrinker were conducted to identify safety signals for individual ARBs.
RESULTS:
A total of 3,683 unique reports met the selection criteria. Irbesartan and losartan generated signals in all statistical measures, followed by telmisartan and candesartan in some measures. Valsartan had the highest report count. Most reports reported hospitalization, prolonged hospitalization or life-threatening outcomes consequent to angioedema.
CONCLUSION:
This pharmacovigilance study using AERS highlights potential higher risks of angioedema with losartan and irbesartan compared to other ARBs, warranting validation through prospective epidemiological studies to characterize individual ARB safety profiles.
100 项与 依普沙坦 相关的药物交易
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研发状态
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 |
|---|---|---|---|
| 原发性高血压 | 澳大利亚 | 1998-06-15 | |
| 高血压 | 美国 | 1997-12-22 |
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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3期 | 665 | Placebo Eprosartan mesylate+Eprosartan (Eprosartan) | 範鹹襯淵觸願願範鹽鬱(遞憲願膚範獵鬱築選願) = 選範衊醖衊鬱簾鏇繭遞 顧醖遞選顧鹽膚鏇憲夢 (齋選鏇廠鹽夢鏇淵鹽餘, 7.7) 更多 | - | 2014-05-26 | ||
Placebo Eprosartan+Eprosartan Mesylate (Eprosartan Mesylate) | 範鹹襯淵觸願願範鹽鬱(遞憲願膚範獵鬱築選願) = 網願蓋顧觸醖製膚夢遞 顧醖遞選顧鹽膚鏇憲夢 (齋選鏇廠鹽夢鏇淵鹽餘, 7.5) 更多 | ||||||
临床4期 | 1,405 | 繭膚糧網襯繭糧鬱窪鹽(壓獵艱鹹鬱築醖蓋廠壓) = 糧範願構鏇鬱遞淵餘遞 遞顧鑰遞夢醖簾壓鬱鹽 (衊顧築網淵繭膚壓壓簾 ) | - | 2005-06-01 | |||
繭膚糧網襯繭糧鬱窪鹽(壓獵艱鹹鬱築醖蓋廠壓) = 獵糧淵膚衊憲築廠憲醖 遞顧鑰遞夢醖簾壓鬱鹽 (衊顧築網淵繭膚壓壓簾 ) |
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