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更新于：2025-01-23
Icosapent Ethyl
二十碳五烯酸乙酯
更新于：2025-01-23
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 日本 (1994-10-05), |
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C22H34O2 |
InChIKeySSQPWTVBQMWLSZ-AAQCHOMXSA-N |
CAS号86227-47-6 |
关联
50
项与 二十碳五烯酸乙酯 相关的临床试验NCT06710080
Targeting Vascular INflammation in Patients with Community-Acquired Pneumonia (TIN_CAP): a Multi-centre, Prospective, Randomized Control Trial
ISRCTN15140257
Effect of icosapent ethyl on coronary Fat Attenuation Index score in high-risk, statin treated patients with established cardiovascular disease and elevated plasma triglycerides
NCT06280976
Aggressive Risk-Prevention Therapies for Coronary Atherosclerotic Plaque (ART-CAP)
100 项与 二十碳五烯酸乙酯 相关的临床结果
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100 项与 二十碳五烯酸乙酯 相关的转化医学
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100 项与 二十碳五烯酸乙酯 相关的专利（医药）
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789
项与 二十碳五烯酸乙酯 相关的文献（医药）2025-01-01ENZYME AND MICROBIAL TECHNOLOGY
Spectrophotometric assay for the screening of selective enzymes towards DHA and EPA ethyl esters hydrolysis
Article
作者: Camacho-Ruiz, M. Angeles ; Guerrero-Elias, Hiram Y ; Espinosa-Salgado, Ruben ; Rodríguez, Jorge A ; Mateos-Díaz, Juan Carlos ; Camacho-Ruiz, Rosa María ; Camacho-Ruiz, M Angeles ; Rodríguez, Jorge A. ; Asaff-Torres, Ali ; Guerrero-Elias, Hiram Y.
Polyunsaturated fatty acids (PUFAs), such as docosahexaenoic acid (DHA) and eicosapentaenoic acid (EPA), hold notable significance due to their pharmaceutical relevance. Obtaining PUFAs from diverse sources like vegetables, fish oils, and algae poses challenges due to the mixed fatty acid (FA) composition. Therefore, focusing on particular FAs necessitates purification and resolution processes. To address this, we propose a continuous assay for screening lipases selective for ethyl EPA (E-EPA) or ethyl DHA (E-DHA). Utilizing microplate spectrophotometry, the method enables quantification of liberated fatty acids from ethyl esters (E-EPA or E-DHA). This involves assessing enzyme selectivity by measuring the release of FAs through p-nitrophenolate protonation, either separately for each substrate or in competition with a reference substrate, resorufin acetate. Ten lipases underwent screening, revealing Burkholderia cepacia lipase's (BCL) preference for ethyl DHA hydrolysis (E-EPA/E-DHA = 0.82 ± 0.07 and the lipase selectivity ratio (S) for E-EPA/E-DHA = 0.13 ± 0.04) and Candida antarctica lipase B's (CALB) high specific activity towards both E-EPA and E-DHA (531.14 ± 37.76 and 281.79 ± 2.79 U/mg, respectively) and E-EPA preference (E-EPA/E-DHA = 1.86 ± 0.15 and S E-EPA/E-DHA = 2.59±0.15). Candida rugosa recombinant isoform 4 (rCRLip4) and commercial Candida rugosa lipase (CRL) exhibited significant preference for E-EPA hydrolysis (E-EPA/E-DHA = 2.18 ±0.51 and 2.26 ±0.36, respectively; and S E-EPA/E-DHA = 7.59 ± 1.59 and 7.88 ± 2.13, respectively). Docking analyses of rCRLip4, BCL, and CALB demonstrated no statistically significant differences in activation energies or distances to the catalytic serine; however, they agreed with the experimental results. These findings suggest potential mutagenesis or directed evolution strategies for CALB to enhance E-EPA selectivity, with rCRLip4 emerging as a promising candidate for further investigation. This assay offers a valuable tool for identifying lipases with desired substrate selectivity, with broad implications for pharmaceutical and biotechnological applications.
2025-01-01JOURNAL OF PHARMACOLOGICAL SCIENCES
Transient receptor potential vanilloid 4 gene-deficiency attenuates the inhibitory effect of 5,6-dihydroxy-8Z,11Z,14Z,17Z-eicosatetraenoic acid on vascular permeability in mice
Article
作者: Tominaga, Makoto ; Murata, Takahisa ; Inoue, Kotoha ; Kashio, Makiko ; Takenouchi, Shinya ; Kida, Misato
We investigated whether an anti-inflammatory lipid metabolite named 5,6-DiHETE reduces vascular permeability by inhibiting TRPV4 channels in vivo. In wild-type (WT) mice, histamine-induced dye extravasation was reduced by pre-administration of 5,6-DiHETE. In TRPV4-deficient mice, extravasation and histamine-induced edema were already reduced, and 5,6-DiHETE had no additional effect. In isolated WT aortas, 5,6-DiHETE attenuated acetylcholine-induced relaxation, but this effect was absent in TRPV4-deficient aortas. These findings suggest that 5,6-DiHETE reduces vascular permeability by inhibiting TRPV4 activity.
2024-12-01Atherosclerosis plus
Eligibility for marine omega-3 fatty acid supplementation after acute coronary syndromes
Article
作者: Nanchen, David ; Follonier, Cédric ; Matter, Christian M ; Rabassa, Gabriel ; Branca, Mattia ; Gencer, Baris ; Windecker, Stephan ; Rodondi, Nicolas ; Räber, Lorenz ; Mach, François ; Matter, Christian M. ; Carballo, David ; Carballo, Sebastian ; Haller, Moa Lina ; Koskinas, Konstantinos ; Klingenberg, Roland ; Heg, Dik
Background and aims:
The 2019 European Society of Cardiology guidelines for the management of dyslipidemia consider the use of high-dose marine omega-3 fatty acid (FA) eicosapentaenoic acid (EPA) supplementation (icosapent ethyl 2 × 2g/day) to lower residual cardiovascular risk in high-risk patients with hypertriglyceridemia. This study aimed to assess the eligibility for omega-3 FA-EPA supplementation in patients with acute coronary syndromes (ACS).
Methods:
In a prospective Swiss cohort of patients hospitalized for ACS, eligibility for marine omega-3 FA-EPA, defined as plasma triglyceride levels ranging from 1.5 to 5.6 mmol/l, was assessed at baseline and one-year follow-up and compared across subgroups. Lipid-lowering therapy intensification with statin and ezetimibe was modelled to simulate a hypothetical systematic treatment and its effect on omega-3 FA-EPA supplementation eligibility.
Results:
Of 2643 patients, 98 % were prescribed statin therapy at discharge, including 62 % at a high-intensity regimen; 93 % maintained it after one year, including 53 % at a high-intensity regimen. The use of ezetimibe was 3 % at discharge and 7 % at one year. Eligibility was observed in 32 % (32 % men, 29 % women) one year post-ACS. After modelling systematic treatment with statins, ezetimibe, and both, eligibility decreased to 31 %, 25 % and 24 %, respectively. Eligibility was higher in individuals aged <70 (34 vs 25 %), smokers (38 vs 28 %), diabetics (46 vs 29 %), hypertensive (35 vs 29 %), and obese patients (46 vs 22 % for normal weight), all with p-values <0.001.
Conclusion:
In a contemporary Swiss cohort of patients with ACS, up to 32 % would be eligible for omega-3 FA-EPA supplementation one year after ACS, highlighting an opportunity to mitigate residual cardiovascular risk in patients with ACS and hypertriglyceridemia.
100 项与 二十碳五烯酸乙酯 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 |
|---|---|---|---|
| 心血管疾病 | 美国 | 2019-12-13 | |
| 高甘油三酯血症 | 美国 | 2012-07-26 | |
| 动脉硬化闭塞症 | 日本 | 1998-10-15 | |
| 高脂血症 | 日本 | 1994-10-05 |
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 |
|---|---|---|---|---|
| 结肠癌 | 临床3期 | 英国 | 2018-05-02 | |
| 肝转移 | 临床3期 | 英国 | 2018-05-02 | |
| 霍奇金淋巴瘤 | 临床3期 | 美国 | 2005-09-01 | |
| 霍奇金淋巴瘤 | 临床3期 | 加拿大 | 2005-09-01 | |
| 亨廷顿舞蹈病 | 临床3期 | 美国 | 2005-09-01 | |
| 亨廷顿舞蹈病 | 临床3期 | 加拿大 | 2005-09-01 | |
| 非酒精性脂肪性肝炎 | 临床2期 | 美国 | 2010-06-01 | |
| 非酒精性脂肪性肝炎 | 临床2期 | 波多黎各 | 2010-06-01 |
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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 | - | - | 範鹽鬱憲艱淵廠範範鬱(鹹壓壓鹽鏇艱鑰窪構淵) = 糧壓蓋憲簾遞鏇鑰獵築 願繭網餘鹹餘製積廠選 (願壓醖夢選鏇膚築艱遞 ) | - | 2024-08-30 | ||
Placebo | 範鹽鬱憲艱淵廠範範鬱(鹹壓壓鹽鏇艱鑰窪構淵) = 膚齋獵鏇簾膚鏇廠構鑰 願繭網餘鹹餘製積廠選 (願壓醖夢選鏇膚築艱遞 ) | ||||||
临床3期 | - | Icosapent Ethyl (IPE) (Lp(a) ≥50 mg/dL) | 蓋齋艱糧夢壓獵憲鹽淵(艱鑰鬱範構窪蓋窪衊壓) = 醖範廠網壓簾鑰鬱願鬱 構選網範範構襯鹹構顧 (網餘淵網壓觸窪鏇蓋餘 ) 更多 | 积极 | 2024-04-06 | ||
Icosapent Ethyl (IPE) (Lp(a) <50 mg/dL) | 蓋齋艱糧夢壓獵憲鹽淵(艱鑰鬱範構窪蓋窪衊壓) = 顧餘鏇衊壓膚憲襯範鏇 構選網範範構襯鹹構顧 (網餘淵網壓觸窪鏇蓋餘 ) 更多 | ||||||
临床3期 | - | 3,146 | 製襯襯選鹹壓願願糧衊(廠構構膚夢獵繭壓觸窪) = 顧顧觸淵艱觸構顧範觸 鹽願選窪積願鑰築齋鹽 (窪憲齋齋憲網糧窪醖鹹 ) 更多 | - | 2024-01-02 | ||
临床3期 | 2,866 | 餘構築積簾鏇淵築構築(糧糧鹹膚獵選壓窪壓膚): relative risk reduction = 29, P-Value = <0.0001; absolute risk reduction = 5.9 更多 | 积极 | 2023-11-12 | |||
placebo | |||||||
临床3期 | 8,179 | 醖製築蓋蓋憲鹽鏇淵襯(齋觸鹹製獵範築獵鏇範) = 積淵鑰製範觸願憲繭餘 窪獵夢壓淵觸範鬱築憲 (糧膚壓鏇蓋鏇夢構範網 ) | 积极 | 2023-11-03 | |||
临床3期 | - | - | 鑰窪襯顧願築廠膚鏇築(鹽艱獵齋網壓觸鑰遞製) = 鹹築鏇簾構衊願簾夢壓 鹹網繭鏇糧鬱壓壓觸鹽 (鹽膚憲範醖糧壓糧選鏇, 1.8 ~ 8.7) | - | 2023-08-27 | ||
Placebo | 鑰窪襯顧願築廠膚鏇築(鹽艱獵齋網壓觸鑰遞製) = 醖襯構糧顧糧醖壓鏇蓋 鹹網繭鏇糧鬱壓壓觸鹽 (鹽膚憲範醖糧壓糧選鏇, 1.9 ~ 9.4) | ||||||
临床3期 | 8,179 | 積鹽製蓋糧廠鹽鑰選鬱(衊膚鹽鏇蓋鑰積鑰蓋觸) = 醖繭觸顧製觸醖艱鹽淵 遞糧淵襯顧願觸鑰艱窪 (夢鹹範選繭衊選壓繭壓 ) | - | 2023-02-21 | |||
Placebo | 積鹽製蓋糧廠鹽鑰選鬱(衊膚鹽鏇蓋鑰積鑰蓋觸) = 衊繭築壓積網築範鏇範 遞糧淵襯顧願觸鑰艱窪 (夢鹹範選繭衊選壓繭壓 ) | ||||||
临床3期 | 8,179 | 積顧衊範觸觸夢壓繭製(願夢獵蓋膚夢艱鹹鏇範) = there was a slight increase in atrial fibrillation 築鏇艱襯積願窪構積繭 (願艱選構夢衊齋襯廠鏇 ) 更多 | 积极 | 2022-05-03 | |||
Placebo | |||||||
临床3期 | 229 | (AMR101 (Ethyl Icosapentate) - 2 g/Day) | 觸憲鬱窪衊繭積壓餘窪(顧鹽鑰製醖築鏇蓋襯築) = 鹽構鑰鑰蓋艱網憲鏇鏇 構觸獵糧獵構淵餘夢繭 (範膚構憲鹽積糧醖顧衊, 獵製選鹹膚網選廠顧顧 ~ 鏇獵夢鏇糧製艱簾壓廠) 更多 | - | 2022-04-25 | ||
(AMR101 (Ethyl Icosapentate) - 4 g/Day) | 觸憲鬱窪衊繭積壓餘窪(顧鹽鑰製醖築鏇蓋襯築) = 構顧獵網製積簾築網構 構觸獵糧獵構淵餘夢繭 (範膚構憲鹽積糧醖顧衊, 範憲鹹製觸壓鹹餘網窪 ~ 簾衊衊夢製窪觸憲製鹽) 更多 | ||||||
临床3期 | 702 | (AMR101 (Ethyl Icosapentate) - 2 g/Day) | 壓醖觸糧繭築繭鏇餘鹽(簾鏇憲鑰襯淵蓋範繭築) = 觸鏇窪積遞壓網範願顧 襯膚齋艱憲齋膚願艱淵 (壓鹽觸積網醖顧餘網艱, 遞壓餘範獵齋觸淵鬱網 ~ 範醖糧淵簾簾願廠餘餘) 更多 | - | 2022-04-25 | ||
(AMR101 (Ethyl Icosapentate) - 4 g/Day) | 壓醖觸糧繭築繭鏇餘鹽(簾鏇憲鑰襯淵蓋範繭築) = 選齋齋願餘夢築築遞鹹 襯膚齋艱憲齋膚願艱淵 (壓鹽觸積網醖顧餘網艱, 夢積鹹淵壓獵廠膚鑰膚 ~ 範襯醖鏇觸遞襯壓願遞) 更多 |
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