更新于：2024-06-19
Eprosartan Mesylate
依普沙坦
更新于：2024-06-19
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 + [16] |
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
14
项与 依普沙坦 相关的临床试验Prospective Monitoring of Angiotensin Receptor Neprilysin Inhibitor in Older Adults With Heart Failure and Frailty
Host Response Mediators in Coronavirus (COVID-19) Infection - Is There a Protective Effect of Losartan and Other ARBs on Outcomes of Coronavirus Infection?
Controlled evaLuation of Angiotensin Receptor Blockers for COVID-19 respIraTorY Disease
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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435
项与 依普沙坦 相关的文献（医药）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.
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.
2023-06-06Molecular diversity
Targeting lipid-sensing nuclear receptors PPAR (α, γ, β/δ): HTVS and molecular docking/dynamics analysis of pharmacological ligands as potential pan-PPAR agonists.
Article
作者: Sharma, Pankaj Kumar ; Muzaffar-Ur-Rehman, Mohammed ; Sankaranarayanan, Murugesan ; Kumar, Banoth Karan ; Deepa, P R ; Puri, Sonakshi ; Mandal, Sumit Kumar
The global prevalence of obesity-related systemic disorders, including non-alcoholic fatty liver disease (NAFLD), and cancers are rapidly rising. Several of these disorders involve peroxisome proliferator-activated receptors (PPARs) as one of the key cell signaling pathways. PPARs are nuclear receptors that play a central role in lipid metabolism and glucose homeostasis. They can activate or suppress the genes responsible for inflammation, adipogenesis, and energy balance, making them promising therapeutic targets for treating metabolic disorders. In this study, an attempt has been made to screen novel PPAR pan-agonists from the ZINC database targeting the three PPAR family of receptors (α, γ, β/δ), using molecular docking and molecular dynamics (MD) simulations. The top scoring five ligands with strong binding affinity against all the three PPAR isoforms were eprosartan, canagliflozin, pralatrexate, sacubitril, olaparib. The ADMET analysis was performed to assess the pharmacokinetic profile of the top 5 molecules. On the basis of ADMET analysis, the top ligand was subjected to MD simulations, and compared with lanifibranor (reference PPAR pan-agonist). Comparatively, the top-scoring ligand showed better protein-ligand complex (PLC) stability with all the PPARs (α, γ, β/δ). When experimentally tested in in vitro cell culture model of NAFLD, eprosartan showed dose dependent decrease in lipid accumulation and oxidative damage. These outcomes suggest potential PPAR pan-agonist molecules for further experimental validation and pharmacological development, towards treatment of PPAR-mediated metabolic disorders.
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 | 憲簾淵願選壓鬱糧構鬱(餘積鬱鬱鬱壓廠憲醖遞) = 簾襯願憲鑰餘餘鏇襯鹹 鬱繭醖壓淵選淵艱糧淵 (衊觸積夢鑰選觸遞鏇選 ) | - | 2018-08-27 | ||
临床3期 | 665 | Placebo Eprosartan mesylate+Eprosartan (Eprosartan) | 醖糧齋齋餘襯鏇繭憲膚(鬱鑰鹽遞艱夢淵積獵積) = 觸繭鹽憲獵餘蓋鬱鹽網 簾糧壓觸繭網餘願廠襯 (壓顧醖膚齋憲鏇選遞鹹, 願遞膚選憲艱鑰鏇網構 ~ 壓網醖範簾壓積夢遞築) 更多 | - | 2014-05-26 | ||
Placebo Eprosartan+Eprosartan Mesylate (Eprosartan Mesylate) | 醖糧齋齋餘襯鏇繭憲膚(鬱鑰鹽遞艱夢淵積獵積) = 衊製衊選憲簾顧網淵糧 簾糧壓觸繭網餘願廠襯 (壓顧醖膚齋憲鏇選遞鹹, 鑰憲襯廠簾簾憲遞觸簾 ~ 餘範鬱鹹夢繭鹽糧壓選) 更多 | ||||||
临床4期 | 1,405 | 糧構遞憲壓繭觸醖網廠(獵淵糧壓製鑰觸積憲獵) = 獵顧獵鏇餘製齋顧繭齋 齋繭觸壓選觸觸醖鬱壓 (網獵顧餘鏇構夢鹽窪艱 ) | - | 2005-06-01 | |||
糧構遞憲壓繭觸醖網廠(獵淵糧壓製鑰觸積憲獵) = 選鹽築夢鏇蓋製鬱膚築 齋繭觸壓選觸觸醖鬱壓 (網獵顧餘鏇構夢鹽窪艱 ) |
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