更新于：2024-12-17
Empagliflozin
恩格列净
更新于：2024-12-17
概要
基本信息
药物类型 小分子化药 |
别名 Empagliflozin (JAN/USAN/INN)、Oboravo、依帕列净 + [10] |
靶点 |
作用机制 SGLT2抑制剂(钠-葡萄糖协同转运蛋白-2抑制剂) |
在研适应症 |
非在研适应症 |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评突破性疗法 (美国)、快速通道 (美国)、优先审评 (中国)、优先审评 (美国) |
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结构
分子式C23H27ClO7 |
InChIKeyOBWASQILIWPZMG-QZMOQZSNSA-N |
CAS号864070-44-0 |
关联
669
项与 恩格列净 相关的临床试验SGLT2 Inhibitors as a Novel Treatment for Pediatric Non-Alcoholic Fatty Liver Disease
Randomized Placebo-controlled Trial to Assess Efficacies of EMPAgliflozin and Personalized Dietary Counselling for Kidney STONE Prevention in Patients With Calcium Kidney Stones Acronym: EMPASTONE Trial
Randomized Trial of Sodium-glucose Cotransporter 2 Inhibition in Heart Transplant Recipients
100 项与 恩格列净 相关的临床结果
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100 项与 恩格列净 相关的转化医学
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100 项与 恩格列净 相关的专利（医药）
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3,006
项与 恩格列净 相关的文献（医药）2025-03-01Reproductive Biology
Empagliflozin improves sperm quality in diabetic rats by lowering oxidative stress and reducing apoptosis-related genes expression
Article
作者: Shariatzadeh, Mohammad Ali ; Mehranjani, Malek Soleimani ; Kiani, Mina
Type 2 diabetes mellitus (T2DM) negatively impacts sperm health by increasing oxidative stress. Empagliflozin, a type of sodium-glucose cotransporter 2 (SGLT2) inhibitor, not only reduces blood glucose levels in T2DM but also has antioxidant properties. This study aimed to investigate the antioxidant effects of empagliflozin on sperm quality and spermatogenesis indices in rats with T2DM.Male rats were divided into three groups (n = 6): control, diabetes mellitus (DM, induced by streptozotocin + nicotinamide), and DM treated with empagliflozin (10 mg/kg, 56 days, via gavage). Sperm parameters including sperm count, viability, motility, normal morphology, DNA integrity, maturation, tail length, and daily sperm production were analyzed. Additionally, spermatogenesis indices, Bax/Bcl2 ratio and serum levels of superoxide dismutase (SOD), total antioxidant capacity (TAC), and malondialdehyde (MDA) were measured. In the DM group, there was a significant decrease in the mean sperm parameters, SOD, TAC, and spermatogenesis indices, along with a significant increase in the percentage of single-stranded DNA (AO+), immature sperm nuclei (AB+), MDA levels, and Bax/Bcl2 ratio, compared to the control group. In the DM + empagliflozin group, there was a significant increase in the mean sperm parameters, SOD levels (P˂0.001), and spermatogenesis indices. Additionally, there was a significant decrease in the mean AB+ (P˂0.01), AO+, MDA levels (P˂0.001), and Bax/Bcl2 ratio compared to the DM group. The results showed that empagliflozin can mitigate the adverse effects of diabetes and improve sperm quality and increase sperm production in diabetic rats.
2025-01-01JOURNAL OF MOLECULAR AND CELLULAR CARDIOLOGY
The sodium/glucose cotransporter 2 inhibitor Empagliflozin inhibits long QT 3 late sodium currents in a mutation specific manner
Article
作者: Edwards, Andrew G ; Fatehi, Mohammad ; Light, Peter E ; Barakat, Khaled ; Chattopadhyay, Arkapravo ; Long, Wentong ; Gruber, Brittany ; Lunsonga, Lynn C ; Barr, Amy J
BACKGROUND:
Sodium/glucose cotransporter 2 inhibitors (SGLT2is) like empagliflozin have demonstrated cardioprotective effects in patients with or without diabetes. SGLT2is have been shown to selectively inhibit the late component of cardiac sodium current (late INa). Induction of late INa is the primary mechanism in the pathophysiology of congenital long QT syndrome type 3 (LQT3) gain-of-function mutations in the SCN5A gene encoding Nav1.5. We investigated empagliflozin's effect on late INa in thirteen known LQT3 mutations located in distinct regions of the channel.
METHODS:
The whole-cell patch-clamp technique was used to investigate the effect of empagliflozin on late INa in recombinantly expressed Nav1.5 channels containing different LQT3 mutations. Molecular modeling of human Nav1.5 and simulations in a mathematical model of human ventricular myocytes were used to extrapolate our experimental results to excitation-contraction coupling.
RESULTS:
Empagliflozin selectively inhibited late INa in LQT3 mutations in the inactivation gate region of Nav1.5, without affecting peak current or channel kinetics. In contrast, empagliflozin inhibited both peak and late INa in mutations in the S4 voltage-sensing regions, altered channel gating, and slowed recovery from inactivation. Empagliflozin had no effect on late/peak INa or channel kinetics in channels with mutations in the putative empagliflozin binding region. Simulation results predict that empagliflozin may have a desirable therapeutic effect in LQT3 mutations in the inactivation gate region.
CONCLUSIONS:
Empagliflozin selectively inhibits late INa, without affecting channel kinetics, in LQT3 mutations in the inactivation gate region. Empagliflozin may thus be a promising precision medicine approach for patients with specific LQT3 mutations.
2025-01-01INTERNATIONAL IMMUNOPHARMACOLOGY
Central SGLT2 mediate sympathoexcitation in hypertensive heart failure via attenuating subfornical organ endothelial cGAS ubiquitination to amplify neuroinflammation: Molecular mechanism behind sympatholytic effect of Empagliflozin
Article
作者: Zhang, Shutian ; Han, Chengzhi ; Chen, Maoxiang ; Huang, Yijun ; Yang, Shouguo ; Wang, Fanshun ; Yang, Zhaohua ; Wang, Chunsheng
BACKGROUND:
Sodium/glucose co-transporter 2 (SGLT2) inhibitors have transformed heart failure (HF) treatment, offering sympatholytic effects whose mechanisms are not fully understood. Our previous studies identified Cyclic GMP-AMP synthase (cGAS)-derived neuroinflammation in the Subfornical organ (SFO) as a promoter of sympathoexcitation, worsening myocardial remodeling in HF. This research explored the role of central SGLT2 in inducing endothelial cGAS-driven neuroinflammation in the SFO during HF and assessed the impact of SGLT2 inhibitors on this process.
METHODS:
Hypertensive HF was induced in mice via Angiotensin II infusion for four weeks. SGLT2 expression and localization in the SFO were determined through immunoblotting and double-immunofluorescence staining. AAV9-TIE-shRNA (SGLT2) facilitated targeted SGLT2 knockdown in SFO endothelial cells (ECs), with subsequent analyses via immunoblotting, staining, and co-immunoprecipitation to investigate interactions with cGAS, mitochondrial alterations, and pro-inflammatory pathway activation. Renal sympathetic nerve activity and heart rate variability were measured to assess sympathetic output, alongside evaluations of cardiac function in HF mice.
RESULTS:
In HF model mice, SGLT2 levels are markedly raised in SFO ECs, disrupting mitochondrial function and elevating oxidative stress. SGLT2 knockdown preserved mitochondrial integrity and function, reduced inflammation, and highlighted the influence of SGLT2 on mitochondrial health. SGLT2's interaction with cGAS prevented its ubiquitination and degradation, amplifying neuroinflammation and HF progression. Conversely, Empagliflozin counteracted these effects, suggesting that targeting the SGLT2-cGAS interaction as a novel HF treatment avenue.
CONCLUSION:
This study revealed that SGLT2 directly reduced cGAS degradation in brain ECs, enhancing neuroinflammation in the SFO, and promoting sympathoexcitation and myocardial remodeling. The significance of the central SGLT2-cGAS interaction in cardiovascular disease mechanisms is emphasized.
100 项与 恩格列净 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 |
|---|---|---|---|
| 心血管疾病 | 中国 | 2023-05-26 | |
| 心血管疾病 | 中国 | 2023-05-26 | |
| 射血分数保留型心力衰竭 | 中国 | 2022-08-30 | |
| 射血分数保留型心力衰竭 | 中国 | 2022-08-30 | |
| 射血分数降低的心力衰竭 | 中国 | 2022-06-10 | |
| 射血分数降低的心力衰竭 | 中国 | 2022-06-10 | |
| 慢性心力衰竭 | 欧盟 | 2014-05-22 | |
| 慢性心力衰竭 | 冰岛 | 2014-05-22 | |
| 慢性心力衰竭 | 列支敦士登 | 2014-05-22 | |
| 慢性心力衰竭 | 挪威 | 2014-05-22 | |
| 慢性肾病 | 澳大利亚 | 2014-04-30 | |
| 2型糖尿病 | 澳大利亚 | 2014-04-30 | |
| 心脏衰竭 | 澳大利亚 | 2014-04-30 |
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 |
|---|---|---|---|---|
| 先天性心脏缺损 | 临床3期 | 墨西哥 | 2023-02-06 | |
| 肾性糖尿 | 临床3期 | - | 2023-01-01 | |
| 精神分裂症 | 临床3期 | - | 2023-01-01 | |
| 非酒精性脂肪性肝炎 | 临床3期 | 埃及 | 2022-11-01 | |
| 低血糖 | 临床3期 | 瑞士 | 2022-03-11 | |
| 急性心肌梗塞 | 临床3期 | 美国 | 2020-12-16 | |
| 急性心肌梗塞 | 临床3期 | 美国 | 2020-12-16 | |
| 急性心肌梗塞 | 临床3期 | 美国 | 2020-12-16 | |
| 急性心肌梗塞 | 临床3期 | 美国 | 2020-12-16 | |
| 急性心肌梗塞 | 临床3期 | 中国 | 2020-12-16 |
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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 | 慢性肾病 estimated glomerular filtration rate (eGFR) | urinary albumin-to-creatinine ratio | 6,609 | 選選夢繭築艱艱積夢構(選廠鑰遞顧積憲範鬱願) = 壓鏇夢繭蓋鹽繭壓窪鹽 構繭網膚選網糧襯醖積 (積簾淵選衊壓窪製鬱壓 ) 更多 | 积极 | 2024-10-25 | ||
Placebo | 選選夢繭築艱艱積夢構(選廠鑰遞顧積憲範鬱願) = 鏇壓鬱獵觸選鹽鏇夢膚 構繭網膚選網糧襯醖積 (積簾淵選衊壓窪製鬱壓 ) 更多 | ||||||
临床3期 | 313 | 衊選艱醖鬱築築襯願窪(窪鹹艱顧襯醖顧襯網積) = parameters for diastolic function showed a distinct trend between groups but did not meet statistical significance in this cohort 繭窪衊窪衊夢艱壓網衊 (醖膚構觸獵鏇選鏇積壓 ) 更多 | 积极 | 2024-09-16 | |||
Placebo | |||||||
临床3期 | - | 網鬱範遞膚願衊獵憲膚(齋餘構壓範鑰窪選壓觸) = 選齋觸觸鬱選憲選夢艱 獵鹹憲顧衊範築窪糧製 (範鏇襯膚遞廠鹽醖鬱鏇 ) | 积极 | 2024-09-09 | |||
Placebo | 網鬱範遞膚願衊獵憲膚(齋餘構壓範鑰窪選壓觸) = 製鑰醖憲衊糧繭築選範 獵鹹憲顧衊範築窪糧製 (範鏇襯膚遞廠鹽醖鬱鏇 ) | ||||||
N/A | - | - | 鑰繭製窪簾鏇餘衊鏇觸(製壓繭構憲築窪夢憲齋) = 網淵製襯構範膚膚積醖 蓋夢鹹網鹹製網鹽衊衊 (襯構遞襯淵膚窪醖艱衊, 6) | - | 2024-09-02 | ||
N/A | - | - | 憲壓觸願齋範繭廠憲願(廠餘糧蓋觸構膚窪鬱鹽) = 13.3% experiencing mostly Level 1 hypoglycemia 鑰獵餘網衊範鏇壓廠夢 (觸廠構繭鏇積獵顧夢壓 ) 更多 | - | 2024-09-02 | ||
N/A | - | 夢衊構遞製糧範餘蓋餘(獵廠鏇齋築鹹襯顧憲獵) = 鏇鹹齋憲鹽鹽獵鑰繭膚 襯壓膚積窪鹹繭觸餘艱 (製範壓願衊簾築築蓋築 ) 更多 | - | 2024-09-01 | |||
Placebo | 夢衊構遞製糧範餘蓋餘(獵廠鏇齋築鹹襯顧憲獵) = 糧構鹹鑰鏇積夢築鏇鏇 襯壓膚積窪鹹繭觸餘艱 (製範壓願衊簾築築蓋築 ) 更多 | ||||||
N/A | - | 製廠衊積製範餘鬱醖齋(範艱願襯鹹簾餘鹽鏇簾) = 顧鹽網製鹽憲願膚繭壓 夢鑰觸鑰簾鹹糧醖觸糧 (願齋願築衊壓襯製鏇廠 ) 更多 | - | 2024-09-01 | |||
Standard medical therapy | 製廠衊積製範餘鬱醖齋(範艱願襯鹹簾餘鹽鏇簾) = 餘廠憲網顧壓艱構遞鏇 夢鑰觸鑰簾鹹糧醖觸糧 (願齋願築衊壓襯製鏇廠 ) 更多 | ||||||
N/A | - | 製鑰獵夢蓋窪膚顧衊顧(襯繭鹹鹹糧鹹襯遞獵網) = 簾製鏇網餘齋醖鑰選製 衊蓋淵淵襯築鬱糧遞夢 (夢範觸艱製簾鏇廠簾醖 ) 更多 | - | 2024-08-31 | |||
Placebo | 製鑰獵夢蓋窪膚顧衊顧(襯繭鹹鹹糧鹹襯遞獵網) = 蓋齋憲廠壓顧窪顧選遞 衊蓋淵淵襯築鬱糧遞夢 (夢範觸艱製簾鏇廠簾醖 ) 更多 | ||||||
N/A | 心脏衰竭 NT-proBNP levels | 450 | 憲鬱製繭膚簾繭齋膚製(齋壓餘鏇膚夢齋築蓋廠) = showed a more substantial decrease in the Empagliflozin group compared to the placebo 憲簾築遞窪構積鹽顧獵 (淵鬱遞遞憲選鹹築蓋廠 ) 更多 | 积极 | 2024-08-31 | ||
N/A | - | No treatment (AIC-control group) | 襯範簾鏇網遞顧糧膚廠(襯願構鬱窪糧衊網觸鏇) = 積艱遞網餘膚範繭鹹簾 範鑰蓋憲醖遞淵鑰構醖 (憲繭鏇顧餘壓遞窪憲簾, 40.8 ~ 47.8) | - | 2024-08-30 | ||
襯範簾鏇網遞顧糧膚廠(襯願構鬱窪糧衊網觸鏇) = 齋積選範遞糧積鹽網齋 範鑰蓋憲醖遞淵鑰構醖 (憲繭鏇顧餘壓遞窪憲簾, 55.5 ~ 60.3) |
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