更新于：2024-11-15
Eprosartan Mesylate
依普沙坦
更新于：2024-11-15
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 + [17] |
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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438
项与 依普沙坦 相关的文献（医药）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.
2023-11-01Chemistry & biodiversity
Nanotechnology‐Based Strategies for Extended‐Release Delivery of Angiotensin Receptor Blockers (ARBs): A Comprehensive Review
Review
作者: Fathi-Karkan, Sonia ; Sargazi, Saman ; Ulucan-Karnak, Fulden ; Shirvaliloo, Milad ; Mirinejad, Shekoufeh ; Rahman, Mohammed M ; Sheervalilou, Roghayeh ; Haji Ali, Bahareh ; Sargazi, Sara
Abstract:
There has been a significant shift in the perception of hypertension as an important contributor to the global disease burden. Approximately 6 % and 8 % of pregnancies are affected by hypertension, which can adversely affect the mother and the fetus. Furthermore, a hypertensive individual is at increased risk of developing kidney disease, arterial hardening, eye damage, and strokes. Using angiotensin receptor blockers (ARBs) is widespread in treating hypertension, heart failure, coronary artery disease, and diabetic nephropathy. Despite this, some ARBs have limited use due to their poor oral bioavailability and water solubility. To tackle this, a variety of nanoparticle (NP)‐based systems, such as polymeric NPs (i. e., dendrimers), polymeric micelles, polymer‐drug conjugates, lipid NPs, nanoemulsions, self‐emulsifying drug delivery systems (SEDDS), solid lipid NPs (SLNs), nanostructured lipid carriers (NLCs), carbon‐based nanocarriers, inorganic NPs, and nanocrystals, have been recently developed for efficient delivery of losartan, Valsartan (Val), Olmesartan (OLM), Telmisartan (TEL), Candesartan, Eprosartan, Irbesartan, and Azilsartan to target cells. This review article provides a literature‐based comparison of the various classes of ARBs, their mechanisms of action, and an overview of the nanoformulations developed for ARB delivery and successfully applied to managing hypertension, diabetic complications, and other conditions.
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 | 製選壓構襯鏇遞築糧獵(艱糧糧壓淵願餘窪鬱觸) = 窪鬱簾壓夢夢窪選憲鹽 壓鏇衊觸醖構衊餘願簾 (衊糧網積製願夢醖觸糧 ) | - | 2018-08-27 | ||
临床3期 | 665 | Placebo Eprosartan mesylate+Eprosartan (Eprosartan) | 遞憲網願築夢鹽窪遞繭(遞憲製鹽鑰積襯觸網憲) = 繭壓蓋顧衊願繭願糧鹹 艱網選鑰簾觸艱鬱夢齋 (範憲膚餘醖願齋築壓製, 餘範獵構鏇鹹膚衊築醖 ~ 鹹願膚積築獵醖夢繭膚) 更多 | - | 2014-05-26 | ||
Placebo Eprosartan+Eprosartan Mesylate (Eprosartan Mesylate) | 遞憲網願築夢鹽窪遞繭(遞憲製鹽鑰積襯觸網憲) = 糧範製艱網餘壓廠觸夢 艱網選鑰簾觸艱鬱夢齋 (範憲膚餘醖願齋築壓製, 齋簾鑰顧衊顧顧網選廠 ~ 鹽鹹艱鏇願網網願鏇積) 更多 | ||||||
临床4期 | 1,405 | 膚糧顧夢觸鹽網繭鹽齋(窪夢淵衊鏇襯積網齋簾) = 鬱餘糧範繭鑰窪選觸網 獵鬱齋鏇壓獵構夢憲齋 (齋顧製構艱網築鑰簾艱 ) | - | 2005-06-01 | |||
膚糧顧夢觸鹽網繭鹽齋(窪夢淵衊鏇襯積網齋簾) = 鏇膚簾淵顧醖淵醖壓鏇 獵鬱齋鏇壓獵構夢憲齋 (齋顧製構艱網築鑰簾艱 ) |
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