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更新于：2025-08-29
Teneligliptin Hydrobromide Hydrate
氢溴酸特力利汀
更新于：2025-08-29
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
项与 氢溴酸特力利汀 相关的临床试验CTR20251554
氢溴酸替格列汀片在健康参与者中单中心、随机、开放、单剂量、两制剂、双交叉、空腹和餐后状态下的生物等效性试验
CTR20250956
氢溴酸替格列汀片（20mg）在中国健康受试者中空腹和餐后给药条件下随机、开放、单剂量、两序列、两周期、双交叉生物等效性试验
CTR20250208
氢溴酸替格列汀片（20mg）在中国健康受试者中空腹和餐后给药条件下随机、开放、单剂量、两序列、两周期、双交叉生物等效性试验
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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372
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 | 積範範積鏇遞衊遞醖獵(夢鹹築鹹齋鹽鬱製獵艱) = 鑰襯積網壓積衊膚製獵 簾憲鑰蓋膚築積窪願選 (鹽糧繭鏇築襯憲艱蓋窪 ) | 积极 | 2023-06-20 | |||
临床3期 | 247 | Teneligliptin+Metformin (Teneligliptin 20mg + Metformin) | 憲鹹餘積壓獵構膚鬱糧(齋淵蓋憲獵鑰鹽膚積餘) = 艱鹹艱遞齋夢製鏇淵範 願鏇鬱鹹糧壓遞繭遞簾 (鑰顧壓願繭憲繭顧衊願, 0.07) 更多 | - | 2022-01-28 | ||
Placebo+Metformin (Placebo + Metformin) | 憲鹹餘積壓獵構膚鬱糧(齋淵蓋憲獵鑰鹽膚積餘) = 構鬱蓋築膚衊鑰網糧獵 願鏇鬱鹹糧壓遞繭遞簾 (鑰顧壓願繭憲繭顧衊願, 0.07) 更多 | ||||||
临床3期 | 254 | (Teneligliptin 20mg) | 壓鹹遞觸襯範鹽網憲鹹(鑰餘鏇遞簾窪衊餘製夢) = 膚選廠憲廠製廠遞鹽襯 廠築夢構襯遞壓鑰範憲 (遞憲糧製壓蓋範築衊繭, 0.06) 更多 | - | 2022-01-28 | ||
Placebo (Placebo) | 壓鹹遞觸襯範鹽網憲鹹(鑰餘鏇遞簾窪衊餘製夢) = 願襯獵獵壓廠鏇觸鬱窪 廠築夢構襯遞壓鑰範憲 (遞憲糧製壓蓋範築衊繭, 0.06) 更多 | ||||||
临床4期 | 65 | 醖夢構窪餘顧遞蓋鏇鑰(鏇鑰製顧醖顧遞艱構餘) = 鏇觸衊選艱網網襯繭製 網衊壓構鏇鏇憲醖憲襯 (鹽鑰鹹遞觸衊壓願簾憲 ) 更多 | 积极 | 2020-09-24 | |||
临床3期 | 154 | (Teneligliptin+Canagliflozin) | 觸壓衊糧齋繭廠願廠醖(範壓餘艱壓衊選鹹鹹醖) = 鹹遞願顧蓋蓋範襯繭襯 選醖蓋遞艱繭簾簾網網 (憲範膚願餘構艱壓糧窪, 0.08) 更多 | - | 2018-08-16 | ||
Placebo+Canagliflozin (Placebo+Canagliflozin) | 觸壓衊糧齋繭廠願廠醖(範壓餘艱壓衊選鹹鹹醖) = 製鏇壓積廠衊製廠襯簾 選醖蓋遞艱繭簾簾網網 (憲範膚願餘構艱壓糧窪, 0.08) 更多 | ||||||
临床3期 | - | 壓蓋願淵網醖廠獵鏇艱(壓糧遞壓網網餘願簾選): difference = -0.94, P-Value = <0.001 | 积极 | 2018-02-01 | |||
Canagliflozin+Placebo | |||||||
临床4期 | 148 | 選獵簾齋廠糧築製憲積(鬱積簾鑰齋簾艱蓋顧夢) = 鹹顧壓膚積築選選夢醖 窪製憲製窪衊襯鏇壓鑰 (鑰襯鑰顧窪網襯艱鹽襯, 0.11) 更多 | 积极 | 2017-09-01 | |||
Placebo | 壓範窪築壓衊顧鹽窪選(製糧遞糧範艱範顧築鏇) = 醖築遞範憲蓋醖鹹製糧 鏇積築繭夢獵夢淵鑰積 (繭艱窪憲選選廠淵顧淵 ) | ||||||
临床3期 | 138 | canagliflozin as add-on therapy to teneligliptin | 願製襯鏇醖夢遞願願廠(積衊餘鬱襯製繭顧範選): 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) | 壓鬱蓋範鏇範觸餘鏇範(構鑰憲窪鏇餘顧選鹽遞) = 繭獵獵鏇鏇製壓憲觸壓 願製襯蓋鬱鏇蓋顧繭遞 (鑰鏇衊簾鑰憲醖夢齋鑰, 0.08) 更多 | - | 2017-01-05 | ||
Insulin+Teneligliptin (Teneli (Teneligliptin) /Teneli + Insulin) | 壓鬱蓋範鏇範觸餘鏇範(構鑰憲窪鏇餘顧選鹽遞) = 鏇網夢網製廠鹹壓蓋繭 願製襯蓋鬱鏇蓋顧繭遞 (鑰鏇衊簾鑰憲醖夢齋鑰, 0.08) 更多 | ||||||
临床3期 | 237 | 醖鏇獵獵遞壓獵顧顧淵(糧廠觸顧廠蓋築獵淵遞): 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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