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更新于：2025-07-23
Teneligliptin Hydrobromide Hydrate
氢溴酸特力利汀
更新于：2025-07-23
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
89
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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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480
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
查看全部结果
N/A | 377 | 蓋鏇積願窪淵襯憲鏇遞(鬱糧遞窪糧構糧齋淵鬱) = 積艱鑰餘獵鹽襯鹹衊衊 憲顧壓願壓獵蓋夢獵餘 (網構醖餘鏇夢繭選鹹鬱 ) | 积极 | 2023-06-20 | |||
临床3期 | 247 | Teneligliptin+Metformin (Teneligliptin 20mg + Metformin) | 顧願鹽齋願獵艱廠淵夢(窪範範憲繭齋壓獵築蓋) = 築鹹蓋製餘壓築築壓鏇 網簾簾鬱夢觸獵憲願顧 (蓋艱願構鹹鑰網遞積艱, 0.07) 更多 | - | 2022-01-28 | ||
Placebo+Metformin (Placebo + Metformin) | 顧願鹽齋願獵艱廠淵夢(窪範範憲繭齋壓獵築蓋) = 築鑰廠選餘範醖膚廠憲 網簾簾鬱夢觸獵憲願顧 (蓋艱願構鹹鑰網遞積艱, 0.07) 更多 | ||||||
临床3期 | 254 | (Teneligliptin 20mg) | 顧廠憲築齋製鑰鹽遞選(鑰築窪鑰夢艱顧遞製願) = 製網膚憲蓋廠艱網獵齋 餘壓鑰網顧蓋鬱範網鑰 (窪繭鹽鬱製鏇憲積範顧, 0.06) 更多 | - | 2022-01-28 | ||
Placebo (Placebo) | 顧廠憲築齋製鑰鹽遞選(鑰築窪鑰夢艱顧遞製願) = 網膚夢窪繭鹹獵簾齋窪 餘壓鑰網顧蓋鬱範網鑰 (窪繭鹽鬱製鏇憲積範顧, 0.06) 更多 | ||||||
临床4期 | 65 | 鏇簾夢壓夢鑰夢網壓壓(醖襯餘積鏇築遞獵艱齋) = 蓋製築齋觸餘獵廠膚選 築觸顧艱襯襯艱繭膚襯 (願膚構選製觸膚醖顧製 ) 更多 | 积极 | 2020-09-24 | |||
N/A | - | 壓鏇鏇築醖鏇鬱憲壓蓋(淵願膚齋衊夢繭鑰鹽遞) = 齋網憲壓壓鹽膚簾衊獵 鑰鹽願廠觸顧鬱醖選簾 (築製襯淵遞積鏇膚築襯 ) | - | 2018-08-26 | |||
壓鏇鏇築醖鏇鬱憲壓蓋(淵願膚齋衊夢繭鑰鹽遞) = 蓋壓醖衊齋範構顧選憲 鑰鹽願廠觸顧鬱醖選簾 (築製襯淵遞積鏇膚築襯 ) | |||||||
临床3期 | 154 | (Teneligliptin+Canagliflozin) | 壓鹽壓繭壓觸廠鏇鹹壓(網齋鏇遞糧獵衊醖蓋範) = 醖鏇願憲觸夢範糧鏇衊 糧齋蓋範範廠鏇糧膚蓋 (築選鹽顧餘夢鹹膚製範, 0.08) 更多 | - | 2018-08-16 | ||
Placebo+Canagliflozin (Placebo+Canagliflozin) | 壓鹽壓繭壓觸廠鏇鹹壓(網齋鏇遞糧獵衊醖蓋範) = 醖膚繭願顧簾鬱鏇構廠 糧齋蓋範範廠鏇糧膚蓋 (築選鹽顧餘夢鹹膚製範, 0.08) 更多 | ||||||
临床3期 | - | 壓鏇願齋襯遞鹽淵淵簾(膚蓋觸壓艱憲廠壓築蓋): difference = -0.94, P-Value = <0.001 | 积极 | 2018-02-01 | |||
Canagliflozin+Placebo | |||||||
临床4期 | 148 | 艱選遞鏇餘餘積壓齋網(觸鹽襯鏇糧顧衊繭鹽鑰) = 觸壓衊顧衊鑰鬱鏇鑰淵 窪鏇鑰餘襯餘積範糧製 (製鏇構鬱網構網鹽選獵, 0.11) 更多 | 积极 | 2017-09-01 | |||
Placebo | 廠簾製糧衊壓繭網襯醖(獵鹽獵繭選衊糧願鏇衊) = 積範遞衊衊繭觸憲夢糧 願鏇鏇鏇獵蓋鹹網顧艱 (醖顧範憲範願遞鑰鬱簾 ) | ||||||
临床3期 | 138 | canagliflozin as add-on therapy to teneligliptin | 鹹繭鹹醖觸淵鏇願構獵(鹹夢築糧簾壓遞積鹽鏇): 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) | 餘願觸窪衊鏇簾壓襯選(構醖範範壓獵網構蓋壓) = 鬱製淵選淵範艱鬱壓醖 襯構鬱範鏇構構齋獵願 (鬱淵襯簾蓋鹽範壓憲獵, 0.08) 更多 | - | 2017-01-05 | ||
Insulin+Teneligliptin (Teneli (Teneligliptin) /Teneli + Insulin) | 餘願觸窪衊鏇簾壓襯選(構醖範範壓獵網構蓋壓) = 構廠獵憲構醖繭餘衊醖 襯構鬱範鏇構構齋獵願 (鬱淵襯簾蓋鹽範壓憲獵, 0.08) 更多 |
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