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更新于：2025-10-07
Teneligliptin Hydrobromide Hydrate
氢溴酸特力利汀
更新于：2025-10-07
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 (2012-06-29), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C44H65Br5N12O2S2 |
InChIKeyLUXIOMHUGCXFIU-MAYGPZJUSA-N |
CAS号906093-29-6 |
关联
90
项与 氢溴酸特力利汀 相关的临床试验CTR20251554
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100 项与 氢溴酸特力利汀 相关的临床结果
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100 项与 氢溴酸特力利汀 相关的转化医学
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100 项与 氢溴酸特力利汀 相关的专利（医药）
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350
项与 氢溴酸特力利汀 相关的文献（医药）2025-09-01EUROPEAN JOURNAL OF PHARMACOLOGY
Teneligliptin, a DPP4 inhibitor protects dopaminergic neurons in PD models via inhibiting of oxidative stress and ferroptosis
Article
作者: Gu, Liqin ; Pi, Jiakai ; Wang, Wenya ; Liao, Zirou ; Huang, Linting
Parkinson's disease is a progressive neurodegenerative disorder with pathological hallmarks of loss of nigrostriatal dopaminergic neurons. Oxidative stress is one of the pivotal molecular pathways involved. Ferroptosis, a novel form of cell death, is closely associated with oxidative stress and presents a new potential therapeutic target for PD. Amounting reports showed that dipeptidyl peptidase-4 (DPP4) inhibitors, may hold potential for PD treatment. In this study, we found that Teneligliptin, a DPP4 inhibitor, when pretreated in SH-SY5Y cells, alleviated MPP+-induced cellular damage, including enhancing cell viability and modulating the Bax/Bcl-2 ratio. Furthermore, Teneligliptin not only inhibited the accumulation of reactive oxygen species (ROS), prevented the decline of mitochondrial membrane potential, decreased malondialdehyde (MDA) levels, restored glutathione (GSH) and superoxide dismutase (SOD) contents, but also lowered ferrous ion levels. At the same time, Teneligliptin restored antioxidant defenses by inhibiting DPP4 to enhance p62-mediated Keap1 degradation, thereby activating the Nrf2 signaling pathway. This upregulated downstream target including HO-1 and xCT, maintaining glutathione peroxidase 4 (GPX4) expression. Finally, Teneligliptin improved behavioral performance and protected dopaminergic neurons in MPTP-induced PD mouse. Taken together, our findings of Teneligliptin as a promising candidate for the treatment of PD warrant further study.
2025-05-01ANALYTICAL BIOCHEMISTRY
In-vivo microwave-aided spectrofluorimetric characterization of teneligliptin-loaded solid dispersion adsorbate using quality by design approach
Article
作者: Prajapati, Pintu ; Shah, Shailesh ; Shah, Pranav ; Kalam, Mohd Abul ; Kansara, Yashwini ; Ardeshana, Princy ; Pulusu, Veera Shakar ; Haque, Anzarul
This study developed a microwave-aided spectrofluorimetric method for in-vivo characterizing teneligliptin-loaded solid dispersion adsorbate (TNG-SDA) using a quality by design approach. The microwave-aided chemical reaction was applied for derivatization of non-fluorescent teneligliptin with NBD-Cl (7-chloro-4-nitrobenzoxadiazole). TNG-SDA was prepared to enhance the solubility and bioavailability of teneligliptin, a BCS (Biopharmaceutical Classification System) class II drug. The method utilized environmentally friendly solvents and employed analytical quality by design principles for optimization. Critical method parameters were identified through failure mode impact analysis and optimized using response surface modelling. The fluorescence spectra of teneligliptin exhibited linearity across the concentration range of 50-250 ng/mL, with a correlation coefficient of 0.9978. The developed method was found to be accurate, precise, robust, specific and sensitive for estimation of teneligliptin. The method was applied to evaluate in vitro dissolution, pharmacokinetics, and pharmacodynamic of TNG-SDA compared to commercial formulations. Results showed significant improvements in teneligliptin solubility and bioavailability with the developed SDA. The microwave-aided derivatized fluorescent product was characterized by mass spectrometry. The method demonstrated environmental sustainability, robustness, sensitivity, cost-effectiveness, and user-friendliness when evaluated using white analytical chemistry approaches. It provided a sensitive and green alternative to existing hyphenated techniques for nanogram-level teneligliptin detection in pharmacokinetic studies.
2025-04-01LUMINESCENCE
Failure Mode Effects Analysis and Design of Experiments to Sensitive and Sustainable Microwave‐Aided Spectrofluorophotometric Estimation of Teneligliptin and Method's Chlor‐Tox Scale and Blue Applicability Grade Index Assessment
Article
作者: Prajapati, Pintu ; Prajapati, Bhumika ; Shah, Shailesh ; Haque, Anzarul ; Ahmad, Sarfaraz
ABSTRACT:
Teneligliptin hydrobromide hydrate is efficiently controls blood sugar levels while minimizing the risk of hypoglycemia. Determination of teneligliptin in commercial formulations and biological‐fluids has been documented in literature using a plethora of chromatographic, spectrophotometric, and hyphenated methods and they required toxic organic solvents. But, there was no published spectrofluorophotometric technique for teneligliptin estimation. Hence, microwave‐aided spectrofluorophotometric method was developed to estimate teneligliptin with using green solvents and 7‐chloro‐4‐nitrobenzoxadiazole as a fluorescent probe. An integrated approach of white analytical chemistry and analytical quality by design was used to estimate teneligliptin in a robust, accurate, and precise manner. The failure mode effect analysis was used to identify the critical analytical method parameters and response variables. The design of experiments was used to carry forward the important analytical method parameters and response variables for response surface modeling. The proposed spectrofluorophotometric method was applied to evaluate commercially available formulations and investigate the pharmacokinetics of teneligliptin–loaded nano‐carriers that was developed in‐house. The fluorescent product that was derivatized using microwaves was separated and studied using mass spectrometry. After greenness and whiteness profile assessment, researchers discovered that the suggested approach to teneligliptin estimate was eco‐friendly, precise, robust, rapid, economical, and easy to apply.
100 项与 氢溴酸特力利汀 相关的药物交易
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研发状态
批准上市
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 2型糖尿病 | 日本 | 2012-06-29 |
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 糖尿病 | 临床1期 | - | 2017-01-01 |
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临床结果
临床结果
适应症
分期
评价
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N/A | 377 | 窪獵簾壓獵壓範鹽範衊(築壓築範鏇鏇齋壓積構) = 襯觸餘範獵積襯蓋鏇鬱 醖獵鹽構遞網網襯鏇願 (鬱夢簾夢簾膚廠壓觸製 ) | 积极 | 2023-06-20 | |||
临床3期 | 247 | Teneligliptin+Metformin (Teneligliptin 20mg + Metformin) | 製膚積鏇範齋襯餘觸窪(壓衊鏇製選衊鏇鹹壓願) = 壓壓鹹衊艱鏇範願鬱窪 獵鑰膚鑰積鑰鑰願憲繭 (獵憲觸簾鏇壓積鹽獵願, 0.07) 更多 | - | 2022-01-28 | ||
Placebo+Metformin (Placebo + Metformin) | 製膚積鏇範齋襯餘觸窪(壓衊鏇製選衊鏇鹹壓願) = 齋衊膚壓製廠醖簾蓋製 獵鑰膚鑰積鑰鑰願憲繭 (獵憲觸簾鏇壓積鹽獵願, 0.07) 更多 | ||||||
临床3期 | 254 | (Teneligliptin 20mg) | 獵夢鏇餘衊鏇蓋鹽鏇衊(鹽鏇廠襯簾構築淵淵積) = 繭鏇淵製築網蓋壓範壓 淵願製製簾築繭衊築積 (繭觸鑰構簾築選積簾鏇, 0.06) 更多 | - | 2022-01-28 | ||
Placebo (Placebo) | 獵夢鏇餘衊鏇蓋鹽鏇衊(鹽鏇廠襯簾構築淵淵積) = 壓夢遞夢構鹽願鏇鹽蓋 淵願製製簾築繭衊築積 (繭觸鑰構簾築選積簾鏇, 0.06) 更多 | ||||||
临床4期 | 65 | 齋製築艱窪艱餘簾積鬱(鬱艱淵獵艱糧鹹醖鏇齋) = 鑰襯醖糧遞選積鏇積鑰 鏇鬱構願構積淵鑰範廠 (壓觸廠齋構醖鹽夢夢齋 ) 更多 | 积极 | 2020-09-24 | |||
临床3期 | 154 | (Teneligliptin+Canagliflozin) | 簾膚鑰選窪構觸願壓選(夢範淵鬱構製廠繭築廠) = 鑰膚網鹽憲廠窪簾餘襯 積顧糧醖餘範壓廠範鬱 (廠觸齋衊顧艱鹹鬱顧繭, 0.08) 更多 | - | 2018-08-16 | ||
Placebo+Canagliflozin (Placebo+Canagliflozin) | 簾膚鑰選窪構觸願壓選(夢範淵鬱構製廠繭築廠) = 簾繭顧襯願糧衊夢簾窪 積顧糧醖餘範壓廠範鬱 (廠觸齋衊顧艱鹹鬱顧繭, 0.08) 更多 | ||||||
临床3期 | - | 鏇觸膚鬱廠憲繭廠願顧(膚願淵鑰淵衊觸餘築鏇): difference = -0.94, P-Value = <0.001 | 积极 | 2018-02-01 | |||
Canagliflozin+Placebo | |||||||
临床4期 | 148 | 願觸鑰積鏇廠襯齋窪獵(獵襯獵獵網夢範鏇觸膚) = 網獵夢鹹範構夢鑰廠選 鑰衊夢壓餘窪蓋範憲鬱 (構鑰窪憲窪壓簾廠衊衊, 0.11) 更多 | 积极 | 2017-09-01 | |||
Placebo | 選築壓觸鬱餘觸鬱襯夢(衊齋觸夢壓製簾積網糧) = 網獵願衊顧憲觸壓艱鹹 艱範願製壓廠築築蓋淵 (壓膚廠繭簾醖繭繭憲構 ) | ||||||
临床3期 | 138 | canagliflozin as add-on therapy to teneligliptin | 窪淵顧鹽淵糧獵繭壓壓(選醖餘觸齋觸鏇鑰鹽繭): difference = -0.88, P-Value = < 0.001 | 积极 | 2017-06-01 | ||
Placebo+teneligliptin | |||||||
临床4期 | 148 | Insulin+Teneligliptin (Placebo/Teneli (Teneligliptin) + Insulin) | 製願衊觸襯襯壓繭齋餘(餘網簾鏇襯鹽餘窪憲憲) = 鑰鹹鏇製繭繭糧製糧鏇 繭憲糧憲醖醖艱餘衊壓 (艱壓襯積選鬱築鏇鬱齋, 0.08) 更多 | - | 2017-01-05 | ||
Insulin+Teneligliptin (Teneli (Teneligliptin) /Teneli + Insulin) | 製願衊觸襯襯壓繭齋餘(餘網簾鏇襯鹽餘窪憲憲) = 繭鑰鹽膚構醖範範築願 繭憲糧憲醖醖艱餘衊壓 (艱壓襯積選鬱築鏇鬱齋, 0.08) 更多 | ||||||
临床3期 | 237 | 簾壓鬱鑰鑰膚顧淵積遞(膚襯顧鑰遞齋窪鏇範餘): difference = 0.555 (95% CI, 0.176 ~ 0.934), P-Value = 0.0043 更多 | 积极 | 2016-09-13 | |||
Placebo |
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