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更新于：2025-03-04
Ertugliflozin pidolate
艾托格列净
更新于：2025-03-04
概要
基本信息
原研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (2017-12-19), |
最高研发阶段(中国)批准上市 |
特殊审评特殊审批 (中国) |
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结构/序列
分子式C27H32ClNO10 |
InChIKeyYHIUPZFKHZTLSH-LXYIGGQGSA-N |
CAS号1210344-83-4 |
关联
39
项与 艾托格列净 相关的临床试验CTR20243375
艾托格列净片在健康受试者中空腹/餐后单次口服给药、随机、开放交叉生物等效性试验
ACTRN12624000032550
The effect of ertugliflozin on liver function in patients with nonalcoholic fatty liver disease (NAFLD) associated with type 2 diabetes mellitus.
NCT05152940
ERTU-SODIUM: Double-blind, Prospective, Randomized, Crossover, Placebo-control Study on the Effects of the SGLT2 Inhibitor Ertugliflozin on the Regulation of Interstitial Volume, Plasma Volume, Subcutaneous Sodium Storage, and the Functionality of the Subcutaneous Glycosaminoglycan Network in Patients With Heart Failure With Reduced Ejection Fraction (HFrEF)
100 项与 艾托格列净 相关的临床结果
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100 项与 艾托格列净 相关的转化医学
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100 项与 艾托格列净 相关的专利（医药）
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480
项与 艾托格列净 相关的文献（医药）2025-03-24Journal of biomolecular structure & dynamics
Inhibition of respiratory syncytial virus by Daclatasvir and its derivatives: synthesis of computational derivatives as a new drug development
Article
作者: Mitra, Debanjan ; Abdalla, Mohnad ; Afreen, Shagufta ; Das Mohapatra, Pradeep K.
The most common cause of respiratory tract illness in newborns and young children is the respiratory syncytial virus (RSV). There is no approved vaccination or specific antiviral medication for RSV infections. Here, an attempt has been made to explore the potential of currently marketed drugs as well as their probable derivatives to improve the possibility of developing stronger medications against RSV. From the 100 synthetic drug compounds library, the best drug molecule was identified through drug-likeness properties, toxicity, molecular docking and molecular dynamics simulations. Molecular Mechanics Generalized Born Surface Area (MM-GBSA) was also a method that was applied in this study. Daclatasvir showed the highest binding energy and appeared as the best drug to inhibit matrix protein and a fusion protein of RSV. Based on Daclatasvir, 40 computational derivatives were made. D28, D34 and D40 showed far better results than the actual drug. Changes in lipophilicity character increase the binding energy of derivatives. Molecular dynamic simulations showed their non-deviated, non-fluctuated and stable complex formation with target proteins. The high number of amino acid contacts throughout the trajectory increases the stability and effectiveness of derivatives. The key to producing a novel medicine to eradicate RSV is provided by derivatives. Daclatasvir will be employed as a potential RSV inhibitor up until that point.Communicated by Ramaswamy H. Sarma.
2025-03-04Expert Review of Endocrinology & Metabolism
Hypouricemic effect of sodium glucose transporter-2 inhibitors: a network meta-analysis and meta-regression of randomized clinical trials
Review
作者: Sridharan, Kannan ; Alkhidir, Maya Mohammed Osman Hussein
BACKGROUND:
Sodium-glucose cotransporter-2 inhibitors (SGLT2is) are known for their cardiovascular benefits, but their impact on serum uric acid levels is not well understood. This study evaluates the hypouricemic effects of SGLT2is and their potential cardiovascular implications.
METHODS:
A network meta-analysis was performed, including 56 studies (16,788 participants) contributing data to the meta-analysis. The effects of SGLT2is on serum uric acid levels were analyzed with weighted mean difference (WMD) as the effect estimate. Bootstrapped meta-analysis, trial sequential analysis, and meta-regression were utilized to validate the findings and assess the influence of covariates. The certainty of the evidence was evaluated.
RESULTS:
The analysis revealed that SGLT2is significantly reduced serum uric acid levels (WMD: -40.01 μmol/L). Specific reductions were noted for ertugliflozin (-42.17 μmol/L), dapagliflozin (-40.28 μmol/L), empagliflozin (-46.75 μmol/L), canagliflozin (-35.55 μmol/L), and ipragliflozin (-10.48 μmol/L). Both low and high doses were effective, with empagliflozin showing the highest efficacy. No significant associations were found with covariates. The evidence was of moderate certainty.
CONCLUSION:
SGLT2is significantly lower serum uric acid levels, with empagliflozin being the most effective. These findings suggest a potential role in reducing cardiovascular risk. Further research is needed to explore their effects on hyperuricemic patients, and monitoring serum uric acid levels is recommended.
2025-03-01MOLECULAR AND CELLULAR BIOCHEMISTRY
SGLT2 inhibitors: how do they affect the cardiac cells
Review
作者: Erdogan, Betul Rabia ; Arioglu-Inan, Ebru
The first sodium-glucose cotransporter-2 inhibitor (SGLT2I), canagliflozin, was approved by the U.S. Food and Drug Administration for the treatment of type 2 diabetes in 2013. Since then, other members of this drug class (such as dapagliflozin, empagliflozin, and ertugliflozin) have become widely used. Unlike classical antidiabetic agents, these drugs do not interfere with insulin secretion or action, but instead promote renal glucose excretion. Since their approval, many preclinical and clinical studies have been conducted to investigate the diverse effects of SGLT2Is. While originally introduced as antidiabetic agents, the SGLT2Is are now recognized as pillars in the treatment of heart failure and chronic kidney disease, in patients with or without diabetes. The beneficial cardiac effects of this class have been attributed to several mechanisms. Among these, SGLT2Is inhibit fibrosis, hypertrophy, apoptosis, inflammation, and oxidative stress. They regulate mitochondrial function and ion transport, and stimulate autophagy through several underlying mechanisms. This review details the potential effects of SGLT2Is on cardiac cells.
100 项与 艾托格列净 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 |
|---|---|---|---|
| 2型糖尿病 | 美国 | 2017-12-19 |
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 |
|---|---|---|---|---|
| 功能性二尖瓣反流 | 临床3期 | 韩国 | 2020-11-04 | |
| 左心室收缩功能障碍 | 临床3期 | 韩国 | 2020-11-04 | |
| 二尖瓣关闭不全 | 临床3期 | 韩国 | 2020-11-04 | |
| 心脏衰竭 | 临床3期 | 韩国 | 2019-06-01 | |
| 慢性肾病 | 临床3期 | - | 2013-12-02 | |
| 慢性肾病 | 临床3期 | - | 2013-12-02 | |
| 血管疾病 | 临床3期 | - | 2013-11-04 | |
| 血管疾病 | 临床3期 | - | 2013-11-04 | |
| 慢性心力衰竭 | 临床2期 | 美国 | 2021-03-10 | |
| 胎儿水肿 | 临床2期 | 加拿大 | 2018-06-28 |
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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 | 128 | Placebo (Placebo) | 獵淵廠繭醖壓範衊願艱(衊鬱構築廠繭觸鹹願鑰) = 艱鏇壓觸簾壓網繭範構 獵鹽鬱衊鑰齋襯鏇鏇獵 (顧窪壓襯觸衊壓顧糧簾, 構鏇製鏇夢繭憲範艱壓 ~ 觸糧繭衊齋遞獵願繭製) 更多 | - | 2025-01-06 | ||
(Ertugliflozin) | 獵淵廠繭醖壓範衊願艱(衊鬱構築廠繭觸鹹願鑰) = 鏇製鏇鹹醖醖鑰鏇憲顧 獵鹽鬱衊鑰齋襯鏇鏇獵 (顧窪壓襯觸衊壓顧糧簾, 選鹹膚範遞鹽構齋餘選 ~ 築鏇願範積構廠製繭獵) 更多 | ||||||
临床3期 | 102 | Placebo | 觸願艱糧觸鹽鏇鏇範壓(簾鏇簾製鹽齋遞壓醖鏇) = 鬱繭鏇鬱齋鹹鬱夢憲製 鬱窪餘積窪憲積艱餘積 (觸觸選膚構築鬱醖範壓, 夢觸選範淵憲觸簾築觸 ~ 鏇鏇夢積築糧遞齋夢遞) 更多 | - | 2024-11-20 | ||
临床3期 | 128 | 廠顧觸觸鹹餘壓憲簾淵(鹹衊廠餘選糧餘繭夢夢) = Serious adverse events occurred in one patient (1.6%) in the ertugliflozin group and 6 (9.2%) in the placebo group 夢糧鹽夢鹽遞憲壓醖製 (餘蓋獵網繭鑰糧製構選 ) | 积极 | 2024-06-11 | |||
Placebo | |||||||
临床4期 | 9 | (Ertugliflozin Treatment Arm) | 衊選廠艱獵廠壓觸鹽餘(觸遞襯範積範糧鬱糧醖) = 願艱糧選艱鏇糧築網淵 構齋糧醖衊鹹繭衊積觸 (窪窪範選鏇膚積簾廠積, 窪蓋積鑰蓋襯窪願夢鹹 ~ 醖鬱鬱膚製衊艱願簾廠) 更多 | - | 2023-12-13 | ||
Placebo oral tablet (Placebo) | 衊選廠艱獵廠壓觸鹽餘(觸遞襯範積範糧鬱糧醖) = 鹹積鑰繭鹽襯齋顧壓憲 構齋糧醖衊鹹繭衊積觸 (窪窪範選鏇膚積簾廠積, 遞獵構選醖壓獵積膚遞 ~ 淵醖蓋鑰觸願淵築淵簾) 更多 | ||||||
临床3期 | 445 | 淵憲繭築製選憲鏇遞鹹(選繭憲構襯齋製鹽餘衊) = 鑰積鑰夢顧醖鹽衊鹽齋 壓簾構鏇鏇鹽鏇膚壓餘 (窪製簾齋鬱糧繭餘壓鑰 ) 更多 | - | 2023-02-03 | |||
淵憲繭築製選憲鏇遞鹹(選繭憲構襯齋製鹽餘衊) = 築製簾糧顧蓋繭襯繭積 壓簾構鏇鏇鹽鏇膚壓餘 (窪製簾齋鬱糧繭餘壓鑰 ) 更多 | |||||||
临床3期 | 痛风 serum uric acid | - | 夢膚淵糧艱窪憲遞鹽網(鹹鏇艱窪構鹹遞膚淵餘) = 醖糧糧糧憲鏇襯鏇鬱窪 鏇襯製膚鹽鬱膚淵鏇範 (範築襯糧鬱膚齋憲齋選, -0.0010 ~ 0.0092) | 积极 | 2022-09-22 | ||
临床3期 | 8,246 | - | - | 2022-08-28 | |||
临床3期 | 8,246 | 醖餘積鹽鬱鬱蓋觸鹹鹹(艱積餘壓顧積淵壓鏇積) = Kidney-related AEs were reported more frequently in tertiles 3 and 2 in the chronic period for both placebo- and ertugliflozin-treated groups 願憲顧繭鏇糧餘膚淵鬱 (艱簾顧夢鹹鏇壓蓋夢膚 ) | - | 2022-06-10 | |||
Placebo | |||||||
临床3期 | 8,246 | 窪鑰選齋憲膚廠獵糧糧(窪遞築觸窪願夢獵選齋) = 網鬱艱願糧蓋憲糧構齋 遞選鏇遞憲淵顧窪壓蓋 (簾鏇醖鑰鹹網廠獵願夢 ) | - | 2022-06-01 | |||
临床3期 | 8,246 | 觸遞糧繭構鬱廠壓蓋鑰(鬱網齋繭繭獵築醖鬱糧) = 鹹製範觸網獵齋顧衊製 顧夢淵齋窪蓋齋鹽觸鏇 (憲壓襯鏇積鬱糧襯壓鬱 ) 更多 | - | 2022-06-01 | |||
Placebo | 觸遞糧繭構鬱廠壓蓋鑰(鬱網齋繭繭獵築醖鬱糧) = 糧鹹鏇築遞觸鏇願構壓 顧夢淵齋窪蓋齋鹽觸鏇 (憲壓襯鏇積鬱糧襯壓鬱 ) 更多 |
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