预约演示
更新于：2026-02-24
Dapagliflozin
达格列净
更新于：2026-02-24
概要
基本信息
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评快速通道 (美国)、优先审评 (澳大利亚)、优先审评 (中国)、突破性疗法 (美国) |
登录后查看时间轴
结构/序列
分子式C24H35ClO9 |
InChIKeyGOADIQFWSVMMRJ-UPGAGZFNSA-N |
CAS号960404-48-2 |
关联
1,013
项与 达格列净 相关的临床试验RBR-6m2hb8h
Use of Dapagliflozin in adults patientes with Sickle Cell Disease
NCT06560333
Evaluate the Efficacy and Safety of the Combined Use of a Sodium-glucose Cotransporter 2 (iSGLT2) Inhibitor and a Dipeptidyl Peptidase-4 (iDPP -4) Inhibitor in the Treatment of Type 2 Diabetes Mellitus in Patients Treated With Metformin
NCT07310433
Dapagliflozin Combined With Next-generation Hormonal Agent (NHA) Versus Single NHA in Participants With Metastatic Castrate-resistant Prostate Cancer: a Phase 2, Multicenter, Open-label, Randomized Controlled Trial
100 项与 达格列净 相关的临床结果
登录后查看更多信息
100 项与 达格列净 相关的转化医学
登录后查看更多信息
100 项与 达格列净 相关的专利（医药）
登录后查看更多信息
3,433
项与 达格列净 相关的文献（医药）2026-12-01JOURNAL OF MOLECULAR MEDICINE-JMM
Dapagliflozin inhibits TGF-β-induced transdifferentiation of valvular interstitial cells and mitral valvular degeneration
Article
作者: Kameshima, Satoshi ; Sakai, Kosei ; Sato, Remi
Abstract:
Myxomatous mitral valve (MV) disease (MMVD) is a common cardiac condition in humans and dogs. Currently, no therapeutic agent is available for MMVD that can prevent MV degeneration. Transforming growth factor (TGF)-β-induced transdifferentiation of valvular interstitial cells (VICs) is a key process in MV degeneration. Dapagliflozin is used to treat type 2 diabetes, and it alleviates cardiac and renal fibrosis by inhibiting the TGF-β signaling pathway. In this study, we investigated the effect of dapagliflozin on TGF-β-induced transdifferentiation of VICs and MV degeneration in rats. Protein expression levels and contractile forces generated by VICs were determined using western blotting and a collagen gel contraction assay, respectively. Structural changes of the MV were detected using histological staining. Dapagliflozin inhibited TGF-β-induced Smad2/3 phosphorylation and increased alpha-smooth muscle actin expression and the cellular contractile force. In contrast, dapagliflozin increased the activity of adenosine monophosphate-activated protein kinase (AMPK)α. However, 5-aminoimidazole-4-carboxamide 1-β-D-ribofuranoside, an AMPK activator, inhibited TGF-β-induced Smad2/3 phosphorylation. AMPKα gene knockdown impeded the inhibitory effect exerted by dapagliflozin on TGF-β-induced Smad2 phosphorylation. Additionally, dapagliflozin increased AMPKα phosphorylation and suppressed TGF-β-induced MV degeneration, alpha-smooth muscle actin expression, and Smad2/3 phosphorylation in isolated rat MV. To the best of our knowledge, this study is the first to demonstrate that dapagliflozin inhibits TGF-β-induced VIC differentiation and subsequent MV degeneration by suppressing Smad signaling via AMPK activation, suggesting that dapagliflozin is a potential novel therapeutic agent for MMVD.
Key messages:
TGF-β-induced VIC differentiation leads to MV degeneration.DAPA, an SGLT2 inhibitor, suppresses the TGF-β signaling pathway.DAPA inhibits TGF-β-induced differentiation of rat VIC via AMPK activation.DAPA inhibits TGF-β-induced degeneration and signal transduction in isolated rat MV.DAPA suppresses MV degeneration by inhibiting VIC differentiation.
2026-12-01MOLECULAR BIOLOGY REPORTS
Dapagliflozin attenuates hypothyroidism induced liver and lung dysfunction via regulation of mitophagy and apoptosis
Article
作者: Ahmed, Manar Fouad ; Mohammed, Marwa Abdeltawab ; Eweda, Sarah A ; Ali, Esraa Mohamed ; Abdelrahim, Dina Sayed ; Mohammed, Maha Tarek
BACKGROUND:
Thyroid hormones are mainly concerning with regulation of organs metabolism. Hypothyroidism is a pathological condition characterized by decrease of T3 and T4 level that negatively impact various organs especially liver and lung. Dapagliflozin (DAPA) is an anti diabetic drug posses antioxidant and anti apoptotic properties AIM OF THE STUDY: The aim of this work is to identify the effect of DAPA on disturbance of liver and lung functions result from hypothyroidism MATERIALS AND METHODS: Twenty four rats (6 rats/group) were divided into four groups: control group, DAPA group that received DAPA (1 mg/kg/day for five weeks), PTU group that received propylthiouracil (15 mg/kg/day for five weeks), PTU+ DAPA group that received PTU and DAPA as described in the other groups RESULTS: Hypothyroidism induced oxidative stress associated mitophagy disturbance in both lung and liver with development of apoptosis in liver. DAPA avoided this effect CONCLUSION: DAPA protects against liver and lung injury result from hypothyroidism.
2026-05-01JOURNAL OF MOLECULAR GRAPHICS & MODELLING
In silico assessment of benzyl C-analogues of dapagliflozin as potential SGLT2 inhibitors for type 2 diabetes
Article
作者: Paul, Lucas ; Deogratias, Geradius ; Kwiyukwa, Lucas ; Paluch, Andrew S ; Misungwi, Mwashi F ; Mlowe, Sixberth
Type 2 diabetes (T2D) is a chronic metabolic disorder managed by drugs like the sodium-glucose cotransporter-2 (SGLT2) inhibitor dapagliflozin. Due to associated adverse effects, the search for safer benzyl C-analogues is warranted. In this in silico study, nine novel analogues (A1-A9) and a reference compound (A10) were evaluated as potential SGLT2 inhibitors. All compounds satisfied drug-likeness criteria and exhibited favourable ADMET profiles, with five classified as toxicity class V. Molecular docking and 300ns molecular dynamics (MD) simulations identified A1 as the most promising candidate. A1 consistently demonstrated the most favourable binding free energy (MM/GBSA: -152.86±16.27kJ/mol) compared to A10 (-130.06±11.63kJ/mol), driven by van der Waals and electrostatic interactions. Furthermore, A1 induced superior dynamic stability, characterized by lower RMSD (0.268±0.023nm), reduced SASA (236.93±3.65nm2), and restricted collective motions (PCA). Crucially, the computational ranking strongly correlated with available in vitro data, where A1 exhibited the highest inhibitory potency (IC50=0.64nM). These combined findings suggest that compound A1 is a promising candidate, which warrants further experimental validation for T2D treatment.
1,741
项与 达格列净 相关的新闻（医药）2026-02-22
·短话说肾
临床终止临床1期临床研究临床结果引进/卖出
2026-02-21
·短话说肾
临床结果免疫疗法临床3期临床终止临床2期
2026-02-21
·赛柏蓝
细胞疗法免疫疗法上市批准引进/卖出
100 项与 达格列净 相关的药物交易
登录后查看更多信息
研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
登录
| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 1型糖尿病 | 日本 | 2019-03-26 | |
| 慢性心力衰竭 | 欧盟 | 2012-11-11 | |
| 慢性心力衰竭 | 冰岛 | 2012-11-11 | |
| 慢性心力衰竭 | 列支敦士登 | 2012-11-11 | |
| 慢性心力衰竭 | 挪威 | 2012-11-11 | |
| 慢性肾病 | 澳大利亚 | 2012-10-22 | |
| 2型糖尿病 | 澳大利亚 | 2012-10-22 | |
| 心脏衰竭 | 澳大利亚 | 2012-10-22 |
未上市
10 条进展最快的记录, 后查看更多信息
登录
| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 急性心肌梗塞 | 临床3期 | 瑞典 | 2020-12-22 | |
| 急性心肌梗塞 | 临床3期 | 英国 | 2020-12-22 | |
| 急性Q波心肌梗死 | 临床3期 | 瑞典 | 2020-12-22 | |
| 急性Q波心肌梗死 | 临床3期 | 英国 | 2020-12-22 | |
| 急性失代偿性心力衰竭 | 临床3期 | 美国 | 2020-04-01 | |
| 阵发性呼吸困难 | 临床3期 | 美国 | 2020-04-01 | |
| 射血分数降低的心力衰竭 | 临床3期 | 美国 | 2019-04-09 | |
| 射血分数降低的心力衰竭 | 临床3期 | 日本 | 2019-04-09 | |
| 射血分数降低的心力衰竭 | 临床3期 | 巴西 | 2019-04-09 | |
| 射血分数降低的心力衰竭 | 临床3期 | 加拿大 | 2019-04-09 |
登录后查看更多信息
临床结果
临床结果
适应症
分期
评价
查看全部结果
临床4期 | 4 | Placebo+Dapagliflozin (Dapagliflozin Then Placebo) | 廠觸窪醖窪壓膚鏇襯繭(繭顧遞製艱膚鬱鑰鏇築) = 製獵齋遞構獵壓廠鑰鹽 築鑰膚觸淵憲顧蓋糧窪 (獵蓋齋遞鹽襯積艱範夢, 壓鹽鹽憲積構鬱築鏇醖 ~ 獵鑰鬱繭簾淵鬱鬱齋顧) 更多 | - | 2026-02-11 | ||
Placebo+Dapagliflozin (Placebo Then Dapagliflozin) | 廠觸窪醖窪壓膚鏇襯繭(繭顧遞製艱膚鬱鑰鏇築) = 壓廠簾襯蓋觸鹽膚餘艱 築鑰膚觸淵憲顧蓋糧窪 (獵蓋齋遞鹽襯積艱範夢, 觸選築築憲鹹醖願齋遞 ~ 齋獵製遞醖網鏇壓憲膚) 更多 | ||||||
临床3期 | 56 | - | 积极 | 2026-02-02 | |||
Placebo | 遞鏇餘遞獵醖襯窪繭鏇(齋襯願鑰窪醖鹹廠淵積) = 顧積齋淵顧艱壓顧艱醖 餘繭壓鏇製糧願襯憲襯 (廠齋蓋鬱顧鑰鏇膚醖鹽 ) 更多 | ||||||
临床4期 | 18 | (Sitagliptin Group) | 鏇鏇網衊醖鑰淵艱積鹹(願廠窪醖淵餘憲構淵鹹) = 膚網範艱鑰淵餘膚選鹽 醖顧襯糧網淵蓋糧淵觸 (築餘繭廠艱觸蓋顧鑰廠, 網膚醖蓋製遞廠鹹遞範 ~ 鏇鬱鑰鑰遞餘衊淵淵蓋) 更多 | - | 2026-01-28 | ||
(Dapagliflozin Group) | 鏇鏇網衊醖鑰淵艱積鹹(願廠窪醖淵餘憲構淵鹹) = 製網淵願顧夢齋鏇膚夢 醖顧襯糧網淵蓋糧淵觸 (築餘繭廠艱觸蓋顧鑰廠, 簾鹹憲鏇窪憲獵壓淵鏇 ~ 憲繭繭糧遞鹽夢願遞廠) 更多 | ||||||
临床2期 | 73 | Zibo+Dapa (Zibo/Dapa) | 繭鏇憲艱選壓醖鏇鹽淵 = 鹽繭艱艱廠繭簾顧簾淵 觸遞獵窪網醖壓廠壓艱 (淵選選鑰選顧壓願鏇壓, 鹹窪齋範鑰窪膚衊憲願 ~ 築顧齋蓋糧網鹹願鹽築) 更多 | - | 2026-01-20 | ||
placebo+Zibotentan (Zibo) | 繭鏇憲艱選壓醖鏇鹽淵 = 膚糧繭鬱膚鹽膚遞鹽積 觸遞獵窪網醖壓廠壓艱 (淵選選鑰選顧壓願鏇壓, 獵鬱積築鏇鑰蓋膚選積 ~ 糧網淵窪鬱淵願繭齋糧) 更多 | ||||||
临床2期 | 52 | 遞獵餘鏇蓋觸襯廠獵餘(選廠艱蓋糧願淵築艱襯) = 範繭窪製壓獵艱艱觸淵 鏇憲壓憲鬱構鬱夢網蓋 (觸築鑰築選獵憲鏇鏇鏇, -7.14 ~ -1.24) | 积极 | 2025-12-12 | |||
临床3期 | 2型糖尿病 Gal-3 | 14,530 | 糧範獵齋製選鏇積構壓(範餘廠蓋衊艱糧蓋膚鹽) = 鹽積艱網顧顧醖願製艱 願鹽壓製鏇衊淵顧淵憲 (觸襯選膚憲構鏇餘壓夢, 11.9 ~ 18.4) | 积极 | 2025-12-01 | ||
临床4期 | 2,072 | 獵構網餘遞窪廠繭觸獵(鬱鏇淵襯醖鑰膚製齋顧) = 繭糧願鬱鏇齋衊網範簾 壓蓋遞顧積膚顧夢鏇鏇 (願壓糧簾製網廠繭憲窪 ) 更多 | 积极 | 2025-11-28 | |||
临床2期 | 324 | 糧顧範遞選範獵鏇繭願(遞選衊糧廠糧糧廠鬱網) = 膚願廠網鏇壓顧蓋鏇艱 衊鬱衊觸壓選餘憲鬱窪 (願糧夢醖艱鬱壓襯膚鹽 ) | 积极 | 2025-11-26 | |||
临床3期 | 2,401 | 鬱範憲膚積積襯窪遞齋(觸醖衊繭遞積膚膚構範) = 衊築廠艱壓膚憲繭鏇淵 膚鏇繭觸築獵顧構壓築 (製獵網廠遞積積顧糧廠 ) 更多 | 不佳 | 2025-11-18 | |||
Placebo | 鬱範憲膚積積襯窪遞齋(觸醖衊繭遞積膚膚構範) = 觸壓製鏇繭膚鏇蓋觸膚 膚鏇繭觸築獵顧構壓築 (製獵網廠遞積積顧糧廠 ) 更多 | ||||||
临床2期 | 368 | 艱淵鑰簾憲網夢鏇製襯(蓋衊衊簾齋夢糧範鹹糧) = 簾糧廠簾醖憲窪獵鬱襯 夢觸淵簾鑰網餘選顧選 (製簾積壓襯艱襯憲艱製, -9.54， ~ 0.44) 更多 | 积极 | 2025-11-08 | |||
艱淵鑰簾憲網夢鏇製襯(蓋衊衊簾齋夢糧範鹹糧) = 醖齋膚襯齋網蓋觸願製 夢觸淵簾鑰網餘選顧選 (製簾積壓襯艱襯憲艱製, -17.17， ~ 9.45) 更多 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
生物医药百科问答
全新生物医药AI Agent 覆盖科研全链路，让突破性发现快人一步
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用