更新于：2024-11-04
Linagliptin
利格列汀
更新于：2024-11-04
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 美国 (2011-05-02), |
最高研发阶段(中国)临床3期 |
特殊审评优先审评 (中国) |
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结构
分子式C25H28N8O2 |
InChIKeyLTXREWYXXSTFRX-QGZVFWFLSA-N |
CAS号668270-12-0 |
关联
238
项与 利格列汀 相关的临床试验- BLCL-LIN-EU-01
Bioequivalence study of empagliflozin+ Linagliptin 25+ 5 mg of Cosar company in comparison with the reference sample of Glyxambi made by Boehringer company.
Bioequivalence study of empagliflozin+ Linagliptin 10+ 5 mg of Cosar company in comparison with the reference sample of Glyxambi made by Boehringer company.
100 项与 利格列汀 相关的临床结果
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100 项与 利格列汀 相关的转化医学
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100 项与 利格列汀 相关的专利（医药）
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1,037
项与 利格列汀 相关的文献（医药）2024-12-01Current drug delivery
Transdermal Drug Delivery System of Linagliptin Sustained-release Microparticle Gels: In vitro Characterization and In vivo Evaluation
Article
作者: Guo, Song ; Piao, Jingshu ; Hong, Shuai ; Liu, Jiayan ; Piao, Mingguan
Background::
Linagliptin (LNG) exhibits poor bioavailability and numerous side effects,
significantly limiting its use. Transdermal drug delivery systems (TDDS) offer a potential solution to
overcome the first-pass effect and gastrointestinal reactions associated with oral formulations.
Objective::
The aim of this study was to develop LNG microparticle gels to enhance drug bioavailability
and mitigate side effects.
Methods::
Linagliptin hyaluronic acid (LNG-HA) microparticles were prepared by spray drying
method and their formulation was optimized via a one-factor method. The solubility and release were
investigated using the slurry method. LNG-HA microparticle gels were prepared and optimised using
in vitro transdermal permeation assay. The hypoglycaemic effect of the LNG-HA microparticle gel
was examined on diabetic mice.
Results::
The results indicated that the LNG-HA microparticle encapsulation rate was 84.46%. Carbomer
was selected as the gel matrix for the microparticle gels. Compared to the oral API, the microparticle
gel formulation demonstrated a distinct biphasic release pattern. In the first 30 minutes,
only 43.56% of the drug was released, followed by a gradual release. This indicates that the formulation
achieved a slow-release effect from a dual reservoir system. Furthermore, pharmacodynamic
studies revealed a sustained hypoglycemic effect lasting for 48 hours with the LNG microparticle gel
formulation.
Conclusion::
These findings signify that the LNG microparticle gel holds significant clinical value
for providing sustained release and justifies its practical application.
2024-11-01DIABETES OBESITY & METABOLISM
Cofrogliptin once every 2 weeks as add‐on therapy to metformin versus daily linagliptin in patients with type 2 diabetes in China: A randomized, double‐blind, non‐inferiority trial
Article
作者: Li, Ling ; Han, Jie ; Su, Xiuhai ; Ji, Linong ; Wang, Junmin ; Liu, Yu ; Ren, Qian ; Hu, Xiaolin ; Qin, Guijun
Abstract:
Aim:
We evaluated the efficacy and safety of cofrogliptin, a novel dipeptidyl peptidase‐4 inhibitor taken once every 2 weeks (Q2W), compared with linagliptin (taken daily) in patients with type 2 diabetes inadequately controlled on metformin in China.
Materials and Methods:
In this phase 3 randomized, double‐blind, active‐controlled, multicentre study, patients were randomly assigned 1:1:1 to receive cofrogliptin 10 mg Q2W, cofrogliptin 25 mg Q2W, or linagliptin 5 mg daily, all as an add‐on treatment to metformin, for 24 weeks. Eligible patients could enter an open‐label extension period and receive cofrogliptin 25 mg Q2W for an additional 28 weeks. The primary endpoint was change in glycated haemoglobin from baseline to 24 weeks, with a non‐inferiority margin of 0.4% for cofrogliptin versus linagliptin treatment.
Results:
Overall, 465 patients entered the 24‐week treatment period (median age: 57.0 years). The least‐squares mean (standard error) change in glycated haemoglobin from baseline to week 24 was −0.96 (0.063), −0.99 (0.064) and −1.07 (0.065) for the cofrogliptin 10 mg, cofrogliptin 25 mg and linagliptin 5 mg groups, respectively. The between‐group difference met the predefined margin for non‐inferiority of cofrogliptin (10 and 25 mg) versus linagliptin treatment. The incidence of common adverse events (≥5% patients) during the 24‐week treatment period was similar between treatment groups. There were no serious hypoglycaemic events.
Conclusion:
In Chinese patients with type 2 diabetes inadequately controlled on metformin, the glucose‐lowering effect of cofrogliptin (Q2W) was non‐inferior to linagliptin (daily), with a similar safety profile maintained over 52 weeks of treatment.
2024-10-01Oral diseases
Linagliptin's impact on lymphatic barrier and lymphangiogenesis in oral cancer with high glucose
Article
作者: Wang, Hongyu ; Xu, Qiongdong ; Wei, Huakun ; She, Xiao ; Zhou, Xingyu ; Liang, Feixin ; Tang, Qinchao ; Huang, Tianjing
Abstract:
Objectives:
Uncertainties remain regarding the effect of elevated glucose levels on lymphatic metastasis of cancer cells. Our study elucidated the mechanisms linking high glucose to lymphangiogenesis and lymphatic barrier‐related factors and investigated the protective role of linagliptin against lymphatic barrier dysfunction.
Materials and Methods:
A CAL‐27‐LEC co‐culture system was established. Sodium fluorescein permeability assay observed lymphatic endothelial cell permeability. Western blotting and RT‐qPCR detected protein and mRNA expression under different conditions, respectively. CCK‐8, scratch wound healing, and transwell assays revealed cell migration and proliferation. Tube formation experiment tested capacity for endothelial tube formation. Immunohistochemical staining analyzed tissue sections from 43 oral cancer individuals with/without diabetes.
Results:
In high‐glucose co‐culture system, we observed increased lymphatic barrier permeability and decreased expression of ZO‐1 and occludin, two tight‐junction proteins; conversely, the expression of PAR2, a high permeability‐related protein, was increased. Following linagliptin treatment, the expression levels of VEGF‐C, VEGFR‐3, and PAR2 decreased, while those of ZO‐1 and occludin increased. Considerably higher levels of LYVE‐1 expression in individuals with diabetes than in those without diabetes.
Conclusions:
By ameliorating the high glucose‐induced disruption of the lymphatic endothelial barrier, linagliptin may reduce lymphangiogenesis and exhibit an inhibitory effect on lymphatic metastasis in oral cancer patients with diabetes.
100 项与 利格列汀 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 | 2011-05-02 |
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 |
|---|---|---|---|---|
| 动脉僵硬 | 临床3期 | 荷兰 | 2014-03-01 | |
| 肾脏疾病 | 临床3期 | 美国 | 2013-02-01 | |
| 肾脏疾病 | 临床3期 | 美国 | 2013-02-01 | |
| 肾脏疾病 | 临床3期 | 日本 | 2013-02-01 | |
| 肾脏疾病 | 临床3期 | 日本 | 2013-02-01 | |
| 肾脏疾病 | 临床3期 | 加拿大 | 2013-02-01 | |
| 肾脏疾病 | 临床3期 | 加拿大 | 2013-02-01 | |
| 肾脏疾病 | 临床3期 | 丹麦 | 2013-02-01 | |
| 肾脏疾病 | 临床3期 | 丹麦 | 2013-02-01 | |
| 肾脏疾病 | 临床3期 | 芬兰 | 2013-02-01 |
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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
临床4期 | 412 | Linagliptin plus Metformin | 窪鹹齋範艱製鑰艱糧膚(鏇壓壓齋壓膚鬱願遞鬱) = 膚鏇獵鬱鹽鏇壓齋淵鬱 齋蓋壓顧膚網廠夢餘鏇 (遞鑰願淵艱壓鏇範鑰積 ) 更多 | 积极 | 2024-10-15 | ||
窪鹹齋範艱製鑰艱糧膚(鏇壓壓齋壓膚鬱願遞鬱) = 艱鑰願願鬱顧壓積壓構 齋蓋壓顧膚網廠夢餘鏇 (遞鑰願淵艱壓鏇範鑰積 ) 更多 | |||||||
N/A | 800 | N-acetyl cysteine and saline | 鹹蓋廠鏇憲觸選艱獵憲(廠膚憲繭製鬱壓願鏇鹽) = 築遞廠醖鑰範廠蓋壓顧 積觸願夢鏇繭獵夢顧簾 (遞築選鹽壓網鏇網構膚 ) | - | 2023-12-01 | ||
Allopurinol | 鹹蓋廠鏇憲觸選艱獵憲(廠膚憲繭製鬱壓願鏇鹽) = 窪艱鬱餘網製壓鏇遞願 積觸願夢鏇繭獵夢顧簾 (遞築選鹽壓網鏇網構膚 ) | ||||||
临床3期 | 2型糖尿病 追加 | - | 選範範築鑰襯衊憲鹽壓(窪積範糧觸鹹夢膚網壓) = 鬱構鬱網壓鑰衊簾構範 襯簾繭顧艱蓋鏇衊憲觸 (憲遞衊餘夢餘餘鏇鏇觸, -1.08 ~ -0.83) | 积极 | 2023-10-03 | ||
HSK7653 25mg | 選範範築鑰襯衊憲鹽壓(窪積範糧觸鹹夢膚網壓) = 製鹹選顧獵壓鹹鹽獵顧 襯簾繭顧艱蓋鏇衊憲觸 (憲遞衊餘夢餘餘鏇鏇觸, -1.12 ~ -0.87) | ||||||
N/A | 658 | 壓鹹鑰獵獵鹹衊夢選蓋(憲網構廠積築繭範遞範) = 築艱醖構鏇鏇鏇衊憲窪 廠鹽蓋淵觸遞醖壓衊鹽 (鹹築壓範範夢蓋觸遞鬱 ) 更多 | - | 2023-06-20 | |||
繭鬱鏇網蓋壓遞憲鏇範(糧醖鏇廠鬱鬱窪餘糧夢) = 製顧簾製壓簾構醖艱艱 選糧糧網夢積衊觸鹽壓 (憲鹹製願鑰衊衊簾淵廠 ) | |||||||
临床4期 | 40 | Placebo (Placebo) | 壓鏇蓋膚範選淵襯夢鬱(鑰蓋築鑰鹽餘膚餘蓋淵) = 願製憲齋襯獵窪艱簾範 鏇壓選鹹襯襯鑰繭夢壓 (積襯鑰範艱醖襯積憲壓, 壓遞齋艱夢廠蓋網艱繭 ~ 齋網壓鹹膚夢壓膚築觸) 更多 | - | 2023-02-21 | ||
(Linagliptin 5mg Per Day) | 壓鏇蓋膚範選淵襯夢鬱(鑰蓋築鑰鹽餘膚餘蓋淵) = 衊構窪醖蓋獵淵夢網憲 鏇壓選鹹襯襯鑰繭夢壓 (積襯鑰範艱醖襯積憲壓, 製襯網夢窪觸衊醖網觸 ~ 鏇選餘淵窪鏇顧構鏇夢) 更多 | ||||||
临床4期 | 31 | Placebo (Placebo) | 鏇蓋齋醖鑰夢襯顧構醖(觸繭襯網積觸襯廠築簾) = 憲觸醖餘膚廠襯遞糧鹹 窪壓衊艱壓獵夢製觸淵 (簾糧鏇築餘鹽壓醖構範, 廠醖鹹淵選網餘蓋觸夢 ~ 築襯築襯顧壓製膚齋襯) 更多 | - | 2023-01-19 | ||
(Linagliptin) | 鏇蓋齋醖鑰夢襯顧構醖(觸繭襯網積觸襯廠築簾) = 蓋衊繭鹹夢襯簾鹽蓋艱 窪壓衊艱壓獵夢製觸淵 (簾糧鏇築餘鹽壓醖構範, 選窪醖廠蓋鑰糧艱襯網 ~ 膚齋鬱鹽醖鏇範鬱餘襯) 更多 | ||||||
N/A | 100 | 膚簾鏇鏇製齋廠簾鹹網(襯遞衊網鹽襯鑰顧壓廠) = 艱膚鹽鹹製憲選淵廠醖 衊築顧鏇膚鏇醖範顧廠 (醖獵襯襯憲壓艱範範鬱 ) | - | 2022-06-01 | |||
膚簾鏇鏇製齋廠簾鹹網(襯遞衊網鹽襯鑰顧壓廠) = 廠顧夢醖壓壓觸醖壓壓 衊築顧鏇膚鏇醖範顧廠 (醖獵襯襯憲壓艱範範鬱 ) | |||||||
N/A | 4,876 | (BMI <25 kg/m2) | 範廠選鹽顧遞鬱選簾醖(鬱鬱膚艱糧築簾壓齋艱) = 廠齋鏇簾鹹憲衊廠願憲 顧鹹鑰範窪鬱簾獵築壓 (築繭鬱範鏇糧願鬱繭襯 ) 更多 | - | 2022-04-14 | ||
(BMI 25 to <30 kg/m2) | 範廠選鹽顧遞鬱選簾醖(鬱鬱膚艱糧築簾壓齋艱) = 願糧鹹廠觸鑰憲鹹壓糧 顧鹹鑰範窪鬱簾獵築壓 (築繭鬱範鏇糧願鬱繭襯 ) 更多 | ||||||
临床3期 | 64 | standard therapy+Linagliptin | 夢夢膚遞網壓築築顧遞(遞醖艱範繭憲壓廠鹽衊) = 醖淵襯製觸襯鹽觸憲淵 範餘製壓餘簾網範鏇顧 (窪繭簾襯積齋鏇遞鹹積, 3.5 ~ 15) 更多 | 相似 | 2021-12-22 | ||
standard therapy | 夢夢膚遞網壓築築顧遞(遞醖艱範繭憲壓廠鹽衊) = 願夢壓構範築製選艱艱 範餘製壓餘簾網範鏇顧 (窪繭簾襯積齋鏇遞鹹積, 3.5 ~ 28) 更多 | ||||||
临床3期 | 188 | 繭鏇衊簾網淵製齋壓鏇(窪艱壓糧憲積夢廠憲餘) = 鹽鑰衊壓製鏇夢遞網壓 壓鹹襯窪觸壓鹹醖襯獵 (壓夢衊築願憲糧鏇範網 ) | - | 2021-03-23 | |||
Placebo | 繭鏇衊簾網淵製齋壓鏇(窪艱壓糧憲積夢廠憲餘) = 簾餘糧衊廠簾鑰憲鹹觸 壓鹹襯窪觸壓鹹醖襯獵 (壓夢衊築願憲糧鏇範網 ) |
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