更新于：2024-12-06
Eprosartan Mesylate
依普沙坦
更新于：2024-12-06
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 |
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
分子式C24H28N2O7S2 |
InChIKeyDJSLTDBPKHORNY-XMMWENQYSA-N |
CAS号144143-96-4 |
关联
9
项与 依普沙坦 相关的临床试验Host Response Mediators in Coronavirus (COVID-19) Infection - Is There a Protective Effect of Losartan and Other ARBs on Outcomes of Coronavirus Infection?
A Prospective, Randomized, Double-Blind, Parallel-Group Study to Compare the Effect of Eprosartan and Eprosartan Mesylate on Blood Pressure in Subjects with Essential Hypertension
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
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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440
项与 依普沙坦 相关的文献（医药）2024-10-02Expert Review of Cardiovascular Therapy
The role of eprosartan in the management of essential hypertension: literature review and expert opinion
Review
作者: Escobar, Carlos ; Rivadulla, Claudio ; Chandrappa, Shukrath ; Mazón, Pilar
INTRODUCTION:
Eprosartan is an angiotensin receptor blocker (ARB) used for management of essential hypertension. With unique pharmacological characteristics, dual action mechanism, and clinical effectiveness, eprosartan offers additional advantages over other ARBs in specific patient populations.
AREAS COVERED:
A comprehensive review of the literature was performed across publicly available databases, with no time limitations, to ensure the inclusion of all relevant studies. The review focuses on presenting the efficacy and safety profile of eprosartan, alone or in combination with other agents. Additionally, it explores the etiology of hypertension concerning the structure and function of angiotensin II type 1 receptors. Further, the efficacy of eprosartan in special populations and its additional benefits are also discussed.
EXPERT OPINION:
Eprosartan effectively reduces blood pressure (BP), with a 24-hour BP-lowering effect at 600 mg/day. Eprosartan demonstrates similar or better efficacy than other ARBs, such as telmisartan and losartan, particularly in managing coagulation-related abnormalities and peripheral resistance. In combination therapy, eprosartan with hydrochlorothiazide significantly enhances BP reduction. Eprosartan is well-tolerated, with a low incidence of adverse events, making it a reliable choice for long-term hypertension management across various patient populations, such as those with comorbid diabetes and renal disease and older adults.
2024-05-01The Annals of pharmacotherapy
Angiotensin Receptor Blocker–Related Sprue-like Enteropathy: Review of Food and Drug Administration Adverse Event Reporting System
Article
作者: Ehrenpreis, Eli D ; Papasotiriou, Sam ; Meader, Ryan ; Ahdi, Hardeep ; Dang, Hoang
Background::
Sprue-like enteropathy (SE) related to olmesartan use was first reported in 2012. In 2017, the manufacturer of Benicar paid $300 million for 2300 claims for olmesartan-related SE.
Objective::
A study in 2019 suggested that SE was related to olmesartan and with the possibility of angiotensin receptor blocker (ARB) class effect. To further characterize this condition, our group examined reports of ARB-related SE to Food and Drug Administration Adverse Event Reporting System (FAERS).
Methods::
All reports of ARB-related SE from January 2017 to December 2021 were downloaded from the FAERS database. Gastrointestinal adverse events including SE were reviewed. Reporter categories included physicians, pharmacists, other health care professionals, consumers, and attorneys.
Results::
A total of 106 590 reports of ARB-related adverse effects were analyzed. Sprue-like enteropathy was identified in 4337 cases (4.1% of total reports). Of these, 4240 cases (98.0%) of ARB-related SE were reported in patients using products with olmesartan, and 97 cases of SE were reported for all other ARBs (eprosartan, losartan, telmisartan, irbesartan, valsartan, and candesartan). Reports of olmesartan-related SE increased rapidly in 2017, continued at a high rate in 2018 and 2019, and essentially stopped in 2020 and 2021.
Conclusions and Relevance::
Reports to FAERS for ARB-related SE are mostly related to olmesartan. There was a steep decline in reports of olmesartan-related SE following the lawsuit with potential of lawyer interference. There are reports of SE related to ARBs other than olmesartan, with increased physician awareness and the potential to discover a class effect with future studies.
2023-11-24Journal of biomolecular structure & dynamics
Exploring the possibility of drug repurposing for cancer therapy targeting human lactate dehydrogenase A: a computational approach
Article
作者: Paul, Sanjay Kumar ; Paul, Ayantika ; Dutta Chowdhury, Kaustav ; Haldar, Rajen ; Dey, Santi Ranjan
Human lactate dehydrogenase A (LDHA) is an anaerobic glycolytic enzyme involved in the inter-conversion of pyruvate to lactate. The level of LDHA in various types of cancer cells is found to be elevated and the dependence of cancer cells on anaerobic glycolysis is viewed as the reason for this elevation. Moreover, inhibition of LDHA activity has been shown to be effective in impairing the growth of tumors, making the LDHA as a potential target for cancer therapy. In this computational study, we have performed a pharmacophore based screening of approved drugs followed by a molecular docking based screening to find a few potential LDHA inhibitors. Molecular dynamics simulations have also been performed to examine the stability of the LDHA-drug complexes as obtained from the docking study. The result of the study showed that darunavir, moxalactam and eprosartan can bind to the active site of LDHA with high affinity in comparison to two known synthetic inhibitors of LDHA. The results of the molecular dynamics simulation showed that these drugs can bind stably with the enzyme through hydrogen bond and hydrophobic interactions. Hence, it is concluded that darunavir, moxalactam and eprosartan may be considered as potential inhibitors of LDHA and can be used for cancer therapy after proper validation of their effectiveness through in vitro, in vivo and clinical trials.Communicated by Ramaswamy H. Sarma.
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
N/A | 原发性高血压 N-terminal pro-brain natriuretic peptide (NT-proBNP) | 165 | 簾鑰窪範築廠簾網網簾(襯鏇築壓醖繭網遞蓋糧) = 夢鬱醖網衊鹽鏇鏇鬱壓 襯網衊鑰鹽構鬱襯鹽蓋 (簾鏇遞蓋窪遞觸衊簾鬱 ) | - | 2018-08-27 | ||
临床3期 | 665 | Placebo Eprosartan mesylate+Eprosartan (Eprosartan) | 衊膚築繭衊繭鹽遞夢窪(壓淵選襯窪構簾襯淵糧) = 鬱獵願繭積廠繭選蓋獵 遞齋蓋膚觸鏇壓醖齋鏇 (鹹構夢醖鬱範夢憲壓糧, 願鬱壓糧餘選顧壓糧願 ~ 願範餘積窪夢壓構製壓) 更多 | - | 2014-05-26 | ||
Placebo Eprosartan+Eprosartan Mesylate (Eprosartan Mesylate) | 衊膚築繭衊繭鹽遞夢窪(壓淵選襯窪構簾襯淵糧) = 範衊繭觸構繭窪醖鏇齋 遞齋蓋膚觸鏇壓醖齋鏇 (鹹構夢醖鬱範夢憲壓糧, 襯蓋選積窪餘鬱觸壓製 ~ 壓鑰築築觸遞鑰獵構鏇) 更多 | ||||||
临床4期 | 1,405 | 遞鏇積鏇遞範淵窪齋觸(艱選夢積鹽顧鏇獵襯艱) = 窪鏇觸廠網夢鑰選鏇網 願窪顧膚廠鹽餘製簾製 (窪糧顧衊廠鏇顧積範鬱 ) | - | 2005-06-01 | |||
遞鏇積鏇遞範淵窪齋觸(艱選夢積鹽顧鏇獵襯艱) = 鹹觸築鏇積繭簾鑰齋衊 願窪顧膚廠鹽餘製簾製 (窪糧顧衊廠鏇顧積範鬱 ) |
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