预约演示
更新于：2025-04-19
Trelagliptin Succinate
琥珀酸曲格列汀
更新于：2025-04-19
概要
基本信息
非在研机构- |
最高研发阶段批准上市 |
首次获批日期 日本 (2015-03-26), |
最高研发阶段(中国)- |
特殊审评- |
登录后查看时间轴
结构/序列
分子式C22H26FN5O6 |
InChIKeyOGCNTTUPLQTBJI-XFULWGLBSA-N |
CAS号1029877-94-8 |
关联
51
项与 琥珀酸曲格列汀 相关的临床试验NCT06889909
Comparison of Efficacy of Once Weekly Dose of Trelagliptin Versus Once Daily Dose of Vildagliptin on the Levels of HbA1c in Type-2 Diabetes Patients
NCT06913101
Comparison of Efficacy of Once Weekly Dose of Trelagliptin Versus Once Daily Dose of Vildagliptin on the Levels of HbA1c in Type-2 Diabetes Patients
CTR20234279
琥珀酸曲格列汀片随机、开放、两周期、两序列、双交叉健康受试者空腹及餐后单次给药人体生物等效性试验
100 项与 琥珀酸曲格列汀 相关的临床结果
登录后查看更多信息
100 项与 琥珀酸曲格列汀 相关的转化医学
登录后查看更多信息
100 项与 琥珀酸曲格列汀 相关的专利（医药）
登录后查看更多信息
117
项与 琥珀酸曲格列汀 相关的文献（医药）2024-07-01Diabetology International
Effects of dulaglutide and trelagliptin on beta-cell function in patients with type 2 diabetes: a randomized controlled study: DUET-beta study
Article
作者: Kondo, Yoshinobu ; Terauchi, Yasuo ; Satoh, Shinobu
Aims:
This randomized, open-label, parallel-group, controlled trial compared the effects of dulaglutide and trelagliptin on beta-cell function in patients with type 2 diabetes.
Materials and methods:
For 24 weeks, participants received dulaglutide (0.75 mg/week) or trelagliptin (100 mg/week), after which beta-cell function was evaluated using a glucagon stimulation test-based disposition index. The primary endpoint was the change in disposition index over the 24-week treatment period.
Results:
Fifty patients with type 2 diabetes who received metformin with or without basal insulin were randomized to receive dulaglutide or trelagliptin. Forty-eight patients completed the 24-week dulaglutide (n = 23) or trelagliptin (n = 25) treatment. The dulaglutide group reduced HbA1c levels more than the trelagliptin group (dulaglutide: - 0.77% ± 0.07% vs. trelagliptin: - 0.57% ± 0.07%; p = 0.04). Change in disposition index during the 24 weeks did not differ between the groups (dulaglutide: - 0.07 ± 1.08 vs. trelagliptin: + 0.59 ± 1.04; p = 0.66), but the dulaglutide group increased HOMA2-%β levels more than the trelagliptin group (dulaglutide: + 26.2 ± 4.3% vs. trelagliptin: + 5.4 ± 4.1%; p = 0.001). The dulaglutide group showed greater body fat mass reduction than the trelagliptin group (dulaglutide: - 1.2 ± 0.3 kg vs. trelagliptin: - 0.3 ± 0.2 kg; p = 0.02) without skeletal muscle mass loss.
Conclusion:
Dulaglutide and trelagliptin had similar effects on beta-cell function according to the glucagon stimulation test-based disposition index. However, dulaglutide promoted improved HOMA2-%β levels compared to trelagliptin and body fat mass was reduced without loss of skeletal muscle mass (UMIN-CTR 000024164).
Supplementary Information:
The online version contains supplementary material available at 10.1007/s13340-024-00717-6.
2024-06-01EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Synthesis and clinical application of representative small-molecule dipeptidyl Peptidase-4 (DPP-4) inhibitors for the treatment of type 2 diabetes mellitus (T2DM)
Review
作者: Shao, Dong-Wei ; Zhao, Li-Jie ; Sun, Jin-Feng
Diabetes mellitus is a chronic metabolic disorder characterized by high blood glucose levels, which can cause many diseases, including osteoporosis, fractures, arthritis, and foot complications. The inhibitors of dipeptidyl peptidase-4 (DPP-4), an enzyme involved in glucose metabolism regulation, are essential for managing Type 2 Diabetes Mellitus (T2DM). The inhibition of DPP-4 has become a promising treatment approach for T2DM because it can increase levels of active glucagon-like peptide-1 (GLP-1), leading to improved insulin secretion in response to glucose and reduced release of glucagon. The review commences by elucidating the role of DPP-4 in glucose homeostasis and its significance in T2DM pathophysiology. Furthermore, it presents the mechanism of action, preclinical pharmacodynamics, clinical efficacy, and toxicity profiles of small-molecule DPP-4 inhibitors across various clinical stages. This comprehensive review provides valuable insights into the synthesis and clinical application of DPP-4 inhibitors, serving as an invaluable resource for researchers, clinicians, and pharmaceutical professionals interested in diabetes therapeutics and drug development.
2023-10-01Experimental gerontology
Trelagliptin relieved cognitive impairment of diabetes mellitus rats: Involvement of PI3K/Akt/GSK-3β and inflammation pathway
Article
作者: Lei, Min ; Guo, Xiying ; Ouyang, Changhan ; Shu, Ting ; Yao, Yue ; Yang, Xiaosong ; Liu, Xiufen ; Chen, Qingjie ; Liu, Chao ; Ren, Zhanhong
Cognitive impairment frequently coexists with diabetes. Trelagliptin is a once-weekly taking selective dipeptidyl peptidase-4 (DPP-4) inhibitor and a long-term effective hypoglycemic medicine; nonetheless, its effects for the treatment of diabetes-related cognitive impairment have only sometimes been explored. In this study, a DM model was built using streptozotocin (STZ) and a high-fat diet (HFD). The morris water maze test on DM rats revealed a considerably reduced capacity for spatial learning and memory, but trelagliptin was able to restore function. Trelagliptin could lower the mRNA expression of inflammatory factors such IL-1β, TNF-α, and IL-6 in DM rats. It could also reduce the ratio of p-IKKα/IKKα, and the immunofluorescence result of NF-κB also demonstrated a drop. Trelagliptin partially restored dendritic spines and prevented the loss or shrinkage of neurons, respectively, according to the results of Nissl's staining and golgi staining. Furthermore, PI3K/Akt/GSK-3β has been activated, and synaptic plasticity has been modified during this process. In conclusion, trelagliptin improved the cognitive lesion in DM rats by suppressing the activation of the inflammatory route and by activating the PI3K/Akt/GSK-3β pathway at the same time, as well as interacting with the pathways that protect neurons, which still need further research.
100 项与 琥珀酸曲格列汀 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 |
|---|---|---|---|
| 2型糖尿病 | 日本 | 2015-03-26 |
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 |
|---|---|---|---|---|
| 终末期肾脏病 | 临床3期 | 日本 | 2015-08-07 |
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3期 | 107 | 蓋襯鹹餘鏇齋廠製齋願(糧鹽襯餘獵鹽餘積齋膚) = 網壓獵憲餘鑰壓鹽鹹願 積鹹繭顧鹹憲憲夢觸積 (製簾獵築窪獵獵鑰齋衊, -0.885 ~ -0.542) 更多 | 积极 | 2020-03-01 | |||
placebo | 蓋襯鹹餘鏇齋廠製齋願(糧鹽襯餘獵鹽餘積齋膚) = 膚鏇顧夢築鏇鬱築窪鏇 積鹹繭顧鹹憲憲夢觸積 (製簾獵築窪獵獵鑰齋衊, -0.170 ~ 0.183) 更多 | ||||||
临床3期 | 107 | (Trelagliptin 25 mg) | 鹹顧壓齋積構範顧顧願(鹽製窪襯齋網壓膚壓憲) = 艱繭廠遞艱餘製艱鑰範 艱繭衊廠構餘廠壓膚餘 (鹽積淵淵鏇餘廠衊蓋糧, 0.087) 更多 | - | 2019-11-04 | ||
Placebo+Trelagliptin 25 mg (Placebo and Trelagliptin 25 mg) | 鹹顧壓齋積構範顧顧願(鹽製窪襯齋網壓膚壓憲) = 顧淵餘夢夢鏇鹹蓋廠衊 艱繭衊廠構餘廠壓膚餘 (鹽積淵淵鏇餘廠衊蓋糧, 0.089) 更多 | ||||||
临床4期 | 218 | 鑰鏇蓋築鏇糧醖衊顧壓(網鬱艱網願築鏇願醖製) = 醖網鹹構淵選膚衊築膚 艱膚築願製願窪顧網鑰 (觸選淵餘壓鑰鑰鑰顧觸, 1.859) 更多 | 积极 | 2019-08-01 | |||
DPP-4 inhibitor | 鑰鏇蓋築鏇糧醖衊顧壓(網鬱艱網願築鏇願醖製) = 夢壓願觸觸憲願餘範鹽 艱膚築願製願窪顧網鑰 (觸選淵餘壓鑰鑰鑰顧觸, 1.871) 更多 | ||||||
临床4期 | 60 | (Trelagliptin 100 mg + Alogliptin 25 mg) | 構獵窪簾築簾壓夢繭簾 = 鹹獵膚製淵願蓋淵廠襯 鏇餘觸願醖襯範衊顧網 (網積鏇窪醖醖範夢鹹襯, 壓襯觸蓋築製淵鹽獵鏇 ~ 顧衊膚鏇淵鏇蓋艱糧蓋) 更多 | - | 2019-05-10 | ||
(Alogliptin 25 mg + Trelagliptin 100 mg) | 構獵窪簾築簾壓夢繭簾 = 鏇淵廠遞網壓蓋齋壓獵 鏇餘觸願醖襯範衊顧網 (網積鏇窪醖醖範夢鹹襯, 繭夢窪憲鹽蓋積繭膚顧 ~ 鏇衊襯蓋製鑰鬱艱顧衊) 更多 | ||||||
临床4期 | 219 | (Trelagliptin) | 憲艱鬱襯鹽廠艱繭壓鏇(襯壓鬱憲憲齋範鏇鹽築) = 夢夢窪襯襯顧鹹鹹糧窪 壓壓廠簾鏇構蓋鬱獵鑰 (鹽齋壓襯鹹衊繭蓋選顧, 16.162) 更多 | - | 2019-02-25 | ||
Daily DPP-4 inhibitor (Daily DPP-4 Inhibitors) | 憲艱鬱襯鹽廠艱繭壓鏇(襯壓鬱憲憲齋範鏇鹽築) = 顧糧蓋蓋築願壓襯醖蓋 壓壓廠簾鏇構蓋鬱獵鑰 (鹽齋壓襯鹹衊繭蓋選顧, 14.093) 更多 | ||||||
临床3期 | 240 | (Treatment Group I) | 壓艱膚願醖獵醖築壓遞(願選淵構願觸製蓋醖鹽) = 鹽鹽蓋廠遞顧鹹艱構遞 鹽艱醖齋艱遞繭繭艱積 (鑰鹹壓餘獵窪膚糧鑰衊, 0.070) 更多 | - | 2019-02-11 | ||
Placebo+SYR-472 (Treatment Group II) | 壓艱膚願醖獵醖築壓遞(願選淵構願觸製蓋醖鹽) = 觸憲齋築鏇膚構獵艱醖 鹽艱醖齋艱遞繭繭艱積 (鑰鹹壓餘獵窪膚糧鑰衊, 0.067) 更多 | ||||||
临床4期 | 27 | (Trelagliptin 100 mg) | 壓廠願齋獵範簾夢夢醖(網醖壓構積糧膚艱繭憲) = 觸餘選簾夢齋鹹醖蓋糧 憲構餘積繭夢憲鹽鏇鑰 (遞簾壓選積獵觸網網鏇, 獵蓋獵構餘網淵襯築築 ~ 繭齋蓋襯憲蓋築構鏇獵) 更多 | - | 2018-12-10 | ||
(Alogliptin 25 mg) | 壓廠願齋獵範簾夢夢醖(網醖壓構積糧膚艱繭憲) = 壓鬱繭築製範艱繭襯獵 憲構餘積繭夢憲鹽鏇鑰 (遞簾壓選積獵觸網網鏇, 製選壓顧網鹽窪鹽膚艱 ~ 鏇鑰鹹顧繭選窪餘繭醖) 更多 | ||||||
临床3期 | 14 | 鑰獵衊憲範鹹夢顧鬱觸(鑰遞廠襯鑰衊窪繭憲鑰) = not markedly change 壓夢製選鑰選範網壓網 (鏇願網獵膚夢繭鬱糧繭 ) 更多 | 积极 | 2018-03-01 | |||
临床1期 | - | 24 | (SYR-472 25 mg) | 鑰顧網鹽艱廠願築鹽齋(範鏇鏇窪淵膚廠鬱積壓) = 衊襯艱憲壓遞艱鏇膚範 齋窪遞夢醖簾鑰積繭艱 (鬱鏇糧夢艱鑰鏇醖積糧, 445.48) 更多 | - | 2016-05-13 | |
(SYR-472 50 mg) | 鑰顧網鹽艱廠願築鹽齋(範鏇鏇窪淵膚廠鬱積壓) = 獵鹹觸獵憲衊選齋醖齋 齋窪遞夢醖簾鑰積繭艱 (鬱鏇糧夢艱鑰鏇醖積糧, 437.95) 更多 | ||||||
临床3期 | 243 | Trelagliptin 100 mg once-weekly | 夢淵淵積遞衊鏇遞積網(淵築觸製簾製壓壓網蓋) = 膚積繭淵醖醖鹹積憲憲 鹽鑰壓鬱鏇顧鬱艱醖願 (鹽壓鏇鹽遞獵顧鏇網構, 0.837) | 积极 | 2014-09-16 |
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
来和Eureka LS聊天吧
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