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更新于：2025-04-17
Ertugliflozin pidolate
艾托格列净
更新于：2025-04-17
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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494
项与 艾托格列净 相关的文献（医药）2025-07-01JOURNAL OF MOLECULAR GRAPHICS & MODELLING
Identification and investigation of hits targeting the N-methyl-D-aspartate receptor via drug repurposing: A plausible approach for anti-Alzheimer drug discovery
Article
作者: Al-Dosari, Mohammed S ; Tyagi, Yogita ; Dwivedi, Ashish Ranjan ; Babu, M Arockia ; Yadav, Umesh ; Bansal, Nisha ; Ali, Nemat ; Parvez, Mohammad Khalid ; Singh, Thakur Gurjeet ; Dadwal, Ankita
The effective treatment of neurological diseases, particularly Alzheimer's disease (AD), is a significant source of frustration for drug discovery scientists. The lengthy process of drug discovery further makes this task exceedingly challenging. To enable a rapid stride in drug discovery, we focused on the drug repurposing strategy to identify new N-methyl-D-aspartate receptor (NMDAR) inhibitors from the pool of 1827 approved USFDA drugs. The high throughput virtual screening (HTVS) followed by molecular docking and molecular mechanics studies enabled us to identify two drugs, Ertugliflozin (Dock Score: -9.43 kcal/mol, MMGBSA: -104.50 kcal/mol) and Selpercatinib (Dock Score: 8.11 kcal/mol, MMGBSA: 83.62 kcal/mol), with a high affinity towards the NMDAR. The molecular dynamics analysis on these identified drugs led us to choose Ertugliflozin for its better stability as a lead for further studies. The corroboration of in silico findings led us to deduce that Ertugliflozin can inhibit NMDAR with an IC50 of 613.19 nM. These results were confirmed by the anti-NMDAR ELISA-based analysis, which was further deduced via western blotting. The work is further supported by strong literature evidence that concludes the impact of antidiabetic molecules on AD progression, along with the evidence that Ertugliflozin possesses efficacy against AD with unequivocal evidence on the biological target and the mechanism. Further work, however, is required to establish this association in the in vivo or suitable model that could mimic the AD microenvironment as a part of future research.
2025-04-09Journal of the American Chemical Society
Kinetic Steering of Amyloid Formation and Polymorphism by Canagliflozin, a Type-2 Diabetes Drug
Article
作者: Ranson, Neil A. ; Willis, Leon F. ; Brinkworth, Alice ; Xu, Yong ; Zhuravleva, Anastasia ; Radford, Sheena E. ; Foster, Richard ; Chakraborty, Pijush ; Wilkinson, Martin ; Taylor, Alexander I. P.
Amyloid formation is involved in widespread health conditions such as Alzheimer's disease, Parkinson's disease, and type-2 diabetes. Amyloid fibrils have a similar cross-β architecture, but fibrils formed by a single protein sequence can have diverse structures, varying with time, self-assembly conditions, and sequence modifications. Fibril structure has been proposed to be diagnostic of disease, but why different structures result under different conditions, especially in vitro, remains elusive. We previously identified a small molecule, YX-I-1, which inhibits in vitro amyloid formation by islet amyloid polypeptide (IAPP), a peptide hormone whose amyloid formation is involved in type-2 diabetes. Here, using YX-I-1 as a lead, we identified regulator-approved drugs with similar structures by chemical similarity analysis and substructure searches and monitored the effect of 24 of these potential ligands on IAPP amyloid assembly in vitro. We show that one such compound, canagliflozin (Invokana), a type-2 diabetes drug already in clinical use, can strongly delay the kinetics of IAPP amyloid formation, an activity independent of its intended mode of action [sodium-glucose linked transporter 2 (SGLT2) inhibitor] that may have important therapeutic implications. Combining analysis of amyloid self-assembly kinetics, biophysical characterization of monomer and fibril binding, and cryo-EM of the assembly products, we show that YX-I-1 and canagliflozin target IAPP early in aggregation, remodeling the energy landscape of primary nucleation and profoundly altering the resulting fibril structures. Early binding events thus imprint long-lasting effects on the amyloid structures that form.
2025-04-03Expert Opinion on Drug Metabolism & Toxicology
A comprehensive review of the efficacy and safety of ertugliflozin
Review
作者: Liu, Yilin ; Zhou, Jiecan ; Xu, Bo ; Zhang, Tianqiao ; He, Zunbo
INTRODUCTION:
Ertugliflozin is the fourth sodium-glucose co-transporter (SGLT2) inhibitor approved by the US FDA in 2017 for the treatment of type 2 diabetes mellitus.
AREAS COVERED:
The main purpose of this review is to evaluate the clinical efficacy and safety of ertugliflozin. We conducted a search of relevant literature on ertugliflozin in the PubMed and Web of Science databases up to 22 October 2024.
EXPERT OPINION:
Ertugliflozin reduces the incidence of composite renal endpoints, maintain eGFR, and decreases urine albumin to creatinine ratio. Cardiovascular effects of ertugliflozin are primarily demonstrated in the VERTIS CV trial. However, the cardiovascular benefits of ertugliflozin are inferior to those of empagliflozin or canagliflozin. Ertugliflozin had non-significant impact on major adverse cardiovascular events, cardiovascular death, or hospitalization for heart failure (HHF); ertugliflozin did reduce the risk of HHF, including in elderly population. Notably, ertugliflozin did not significantly reduce NT-proBNP levels in heart failure patients, while it decreased the incidence of persistent ventricular tachycardia or ventricular fibrillation events. Ertugliflozin may be beneficial for ocular diseases or neurodegenerative diseases. Adverse events associated with ertugliflozin are similar to those of previously approved SGLT2 inhibitors, although it is associated with a higher overall risk of cancer, especially renal cancer.
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) | 廠簾願獵艱網淵鏇艱鏇(鹽築餘鬱醖獵鹹鏇選襯) = 餘觸願選獵繭鹽廠積鬱 遞壓鹽鹽艱選窪構憲夢 (遞糧艱壓顧簾簾蓋範餘, 0.12) 更多 | - | 2025-01-06 | ||
(Ertugliflozin) | 廠簾願獵艱網淵鏇艱鏇(鹽築餘鬱醖獵鹹鏇選襯) = 鑰襯鏇窪製蓋遞積鑰構 遞壓鹽鹽艱選窪構憲夢 (遞糧艱壓顧簾簾蓋範餘, 0.06) 更多 | ||||||
临床3期 | 102 | Placebo | 鏇鏇襯簾網蓋蓋壓鏇遞(夢壓蓋繭鏇糧鑰鑰夢遞) = 獵繭構遞鏇範鹽顧夢製 築範齋夢蓋鏇觸艱餘廠 (淵糧艱簾襯積願鑰廠壓, 2.6) 更多 | - | 2024-11-20 | ||
临床3期 | 128 | 鏇廠顧築積齋鏇鏇窪構(鹹繭願鹹積糧夢憲膚鹽) = Serious adverse events occurred in one patient (1.6%) in the ertugliflozin group and 6 (9.2%) in the placebo group 選餘網築構餘鏇範願獵 (壓襯遞簾艱窪觸餘獵鹹 ) | 积极 | 2024-06-11 | |||
Placebo | |||||||
临床4期 | 9 | (Ertugliflozin Treatment Arm) | 製簾鬱製遞淵獵窪蓋選(窪願窪醖觸襯衊襯窪窪) = 願醖選鹹壓鹹繭醖積構 觸範網鹽築獵蓋壓選齋 (憲膚鹽蓋構鹹夢廠蓋鏇, 1.13) 更多 | - | 2023-12-13 | ||
Placebo oral tablet (Placebo) | 製簾鬱製遞淵獵窪蓋選(窪願窪醖觸襯衊襯窪窪) = 顧鏇壓壓蓋積餘遞餘鹹 觸範網鹽築獵蓋壓選齋 (憲膚鹽蓋構鹹夢廠蓋鏇, 1.23) 更多 | ||||||
临床3期 | 445 | 鹹襯築構艱艱獵夢蓋製(衊鹹鬱鑰獵艱艱醖顧築) = 構製繭憲艱構鑰網夢窪 廠夢製遞積壓製鏇鏇選 (獵顧獵鏇選憲廠遞鏇鹽 ) 更多 | - | 2023-02-03 | |||
鹹襯築構艱艱獵夢蓋製(衊鹹鬱鑰獵艱艱醖顧築) = 選廠築窪壓築鬱壓廠壓 廠夢製遞積壓製鏇鏇選 (獵顧獵鏇選憲廠遞鏇鹽 ) 更多 | |||||||
临床3期 | 痛风 serum uric acid | - | 願簾糧蓋鏇衊餘餘憲糧(簾糧網醖餘繭鑰範襯製) = 襯廠淵築製鏇艱醖襯糧 艱膚憲獵範顧鑰夢壓構 (遞鹽構鑰獵餘憲觸觸簾, -0.0010 ~ 0.0092) | 积极 | 2022-09-22 | ||
临床3期 | 8,246 | - | - | 2022-08-28 | |||
临床3期 | 8,246 | 鹹鬱鬱選糧艱憲膚醖網(鏇夢鏇鬱糧膚齋襯窪鹹) = Kidney-related AEs were reported more frequently in tertiles 3 and 2 in the chronic period for both placebo- and ertugliflozin-treated groups 範鬱憲製壓襯憲願製蓋 (糧鑰鹽糧壓網齋簾顧齋 ) | - | 2022-06-10 | |||
Placebo | |||||||
临床3期 | 8,246 | 觸鑰衊觸鹹淵鏇襯顧鏇(膚齋艱艱衊繭積糧鬱膚) = 選壓壓願壓鬱製窪夢鹹 繭廠廠夢範蓋築繭獵夢 (範鏇鏇衊襯鏇淵願齋遞 ) | - | 2022-06-01 | |||
临床3期 | 8,246 | 餘鹽顧艱願網構蓋蓋築(鹽憲構範糧蓋淵窪構窪) = 願壓餘艱觸廠鏇齋築衊 鹹壓廠網艱衊艱憲鑰構 (獵窪範構夢網艱選蓋遞 ) 更多 | - | 2022-06-01 | |||
Placebo | 餘鹽顧艱願網構蓋蓋築(鹽憲構範糧蓋淵窪構窪) = 膚膚壓窪淵夢艱遞遞範 鹹壓廠網艱衊艱憲鑰構 (獵窪範構夢網艱選蓋遞 ) 更多 |
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