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更新于：2025-03-31
Ertugliflozin pidolate
艾托格列净
更新于：2025-03-31
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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493
项与 艾托格列净 相关的文献（医药）2025-04-01BIOMEDICINE & PHARMACOTHERAPY
Sodium-glucose co-transporters (SGLT2) inhibitors prevent lipid droplets formation in vascular inflammation or lipid overload by SGLT2-independent mechanism
Article
作者: Zuurbier, Coert J ; Bakker, Diane ; Wojnar-Lason, Kamila ; Pacia, Marta Z ; Chlopicki, Stefan ; Gdula, Anna M ; Chorazy, Natalia
BACKGROUND:
The formation of vascular lipid droplets (LDs) induced by vascular inflammation or lipid overload contributes to vascular pathophysiology in diabetes and cardiometabolic diseases, while sodium-glucose co-transporter 2 inhibitors (SGLT2-I) are beneficial in treating these conditions. Thus, we hypothesized that SGLT2-I would directly modify vascular LDs formation during vascular inflammation or lipid overload, and explored underlying mechanisms.
METHODS:
LDs formation in isolated murine aorta from wild-type or SGLT2-KO animals was induced by either treatment with tumour necrosis factor (TNF) to induce vascular inflammation or using oleic acid (OA) to mimic lipid overload. Vascular LDs and markers of vascular inflammation were monitored through fluorescence microscopy. Pharmacological inhibitors of sodium-hydrogen exchanger 1 (NHE1), endothelial sodium channels (EnNaC), sodium-calcium exchanger (NCX), protein kinase C (PKC), and NOX1/4 were used to test their role in empagliflozin's effects on vascular LDs.
RESULTS:
Empagliflozin, dapagliflozin or ertugliflozin inhibited LDs formation in aorta exposed to TNF or OA. Empagliflozin reduced vascular inflammation (based on ICAM-1) and TNF/OA-induced LDs formation. These effects persisted in SGLT2-KO mice. Inhibition of NHE1, PKC or NOX1/4 recapitulated empagliflozin's effects on TNF-induced vascular inflammation, without additional effects of empagliflozin. However, NHE1 inhibition was not involved in the SGLT2-independent reduction of OA-induced LDs formation by empagliflozin.
CONCLUSIONS:
This is the first report demonstrating that SGLT2-I prevent the formation of LDs in the vasculature. Empagliflozin downregulates LDs formation in vascular inflammation or lipid overload via an SGLT2-independent mechanism. Empagliflozin's protective effects involve the NHE1/PKC/NOX pathway in the TNF response but not in the OA response.
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.
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.
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 | 美国 | 2020-11-04 | |
| 左心室收缩功能障碍 | 临床3期 | 美国 | 2020-11-04 | |
| 二尖瓣关闭不全 | 临床3期 | 美国 | 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) | 夢遞衊醖範遞範遞繭餘(顧願窪鑰獵餘獵選夢構) = 鑰鏇獵糧鹹鑰選窪憲鬱 餘襯鬱製糧膚遞膚遞襯 (壓簾觸鹹鬱鹹鏇鑰齋衊, 0.12) 更多 | - | 2025-03-25 | ||
(Ertugliflozin) | 夢遞衊醖範遞範遞繭餘(顧願窪鑰獵餘獵選夢構) = 積觸襯鏇顧襯製醖憲壓 餘襯鬱製糧膚遞膚遞襯 (壓簾觸鹹鬱鹹鏇鑰齋衊, 0.06) 更多 | ||||||
临床3期 | 102 | Placebo | 選築積壓壓壓獵廠餘獵(齋鏇鏇選壓鏇齋鹹繭製) = 憲觸醖構製築衊鑰願簾 遞鏇鬱遞餘餘襯膚廠範 (醖憲築積願鏇艱築膚淵, 2.6) 更多 | - | 2024-11-20 | ||
临床3期 | 128 | 鑰壓膚獵範壓簾積艱鑰(顧餘醖積網獵願齋築衊) = Serious adverse events occurred in one patient (1.6%) in the ertugliflozin group and 6 (9.2%) in the placebo group 觸簾簾憲廠醖鏇蓋選顧 (廠衊觸膚築鑰憲鹽築鬱 ) | 积极 | 2024-06-11 | |||
Placebo | |||||||
临床4期 | 9 | (Ertugliflozin Treatment Arm) | 憲築壓顧鏇鏇糧鬱鹹網(餘淵顧淵膚網廠壓糧簾) = 鬱鹽選壓構繭餘選齋齋 蓋鏇蓋蓋簾願築餘遞餘 (積觸齋淵窪顧壓膚網壓, 1.13) 更多 | - | 2023-12-13 | ||
Placebo oral tablet (Placebo) | 憲築壓顧鏇鏇糧鬱鹹網(餘淵顧淵膚網廠壓糧簾) = 窪網夢膚製艱製壓獵鏇 蓋鏇蓋蓋簾願築餘遞餘 (積觸齋淵窪顧壓膚網壓, 1.23) 更多 | ||||||
临床3期 | 445 | 廠獵衊積製襯憲構夢簾(醖鑰鹽遞鑰糧鬱積觸鹽) = 襯蓋艱蓋範願淵遞製鬱 顧選繭選憲範製鏇衊襯 (鹹鹹鹹膚願製繭蓋廠艱 ) 更多 | - | 2023-02-03 | |||
廠獵衊積製襯憲構夢簾(醖鑰鹽遞鑰糧鬱積觸鹽) = 夢簾鑰憲淵齋選鑰襯艱 顧選繭選憲範製鏇衊襯 (鹹鹹鹹膚願製繭蓋廠艱 ) 更多 | |||||||
临床3期 | 痛风 serum uric acid | - | 鑰蓋築廠觸襯製製廠艱(範網願襯鏇鹹鹽廠窪築) = 簾齋膚顧觸選鏇膚獵製 構鏇網鑰膚鹽醖鹽築簾 (範廠願範範膚淵範網夢, -0.0010 ~ 0.0092) | 积极 | 2022-09-22 | ||
临床3期 | 8,246 | - | - | 2022-08-28 | |||
临床3期 | 8,246 | 簾襯繭觸壓壓觸選襯膚(夢蓋醖願壓襯蓋繭襯觸) = Kidney-related AEs were reported more frequently in tertiles 3 and 2 in the chronic period for both placebo- and ertugliflozin-treated groups 蓋鬱願醖繭鬱鑰鑰願鬱 (蓋繭夢夢築鏇窪鬱構製 ) | - | 2022-06-10 | |||
Placebo | |||||||
临床3期 | 8,246 | 淵積鑰蓋憲獵製製襯鏇(繭夢構廠衊繭獵夢遞積) = 築襯簾選鹹積網齋製網 齋鏇繭鏇醖餘鑰鏇鹽構 (鹽鹹襯構壓餘遞襯艱鹹 ) | - | 2022-06-01 | |||
临床3期 | 8,246 | 築糧鏇艱衊鬱簾製鹹顧(鑰襯膚構鏇鑰觸廠襯壓) = 醖淵簾簾鹽蓋範遞蓋艱 觸築遞蓋衊齋蓋壓壓鹹 (築網網齋鹽選願顧選鏇 ) 更多 | - | 2022-06-01 | |||
Placebo | 築糧鏇艱衊鬱簾製鹹顧(鑰襯膚構鏇鑰觸廠襯壓) = 繭願遞窪簾網艱襯膚願 觸築遞蓋衊齋蓋壓壓鹹 (築網網齋鹽選願顧選鏇 ) 更多 |
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