更新于：2025-01-08
Linagliptin
利格列汀
更新于：2025-01-08
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)批准上市 |
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
237
项与 利格列汀 相关的临床试验- 974/24
- 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.
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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1,065
项与 利格列汀 相关的文献（医药）2025-03-01FOOD CHEMISTRY
Chemical characterization and DPP IV inhibitory capacity of purified adzuki bean β-vignin digest in comparison to soybean β-conglycinin and in vitro effect of β-vignin on diabetic-related outcomes
Article
作者: Davis, Emily ; Esteves, Frida ; Kwan, Shu Hang ; Gonzalez de Mejia, Elvira
Adzuki bean (AB) is a legume with a low glycemic index and is traditionally used in Asian cultures to modulate type 2 diabetes (T2D). Our objectives were to characterize the functional peptides from purified AB β-vignin after simulated gastrointestinal digestion in comparison to soybean β-conglycinin, to evaluate their DPP IV inhibitory capacity, and to determine in vitro the effect of digested AB β-vignin on diabetic-related outcomes using HepG2 cells in healthy and insulin-resistant states. Five peptides (215-742 Da) from AB β-vignin and five peptides (215-447 Da) from β-conglycinin were identified to exhibit bioactivity as DPP IV inhibitors. Molecular docking demonstrated peptides could bind to DPP IV at the same binding site as a diabetic medication, linagliptin. Digested AB β-vignin significantly increased (p < 0.05) hepatic glucose uptake (> 290 %) via DPP IV inhibition (> 40 %) in healthy and insulin-resistant states. IRS-1, Akt-1, and Glut 2 increased after treating cells with digested AB β-vignin in healthy and insulin-resistant states.
2025-02-01EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Design and synthesis of novel 3,7-dihydro-1H-purine-2,6-diones as DPP-4 inhibitors: An in silico, in vitro and in vivo approach
Article
作者: Pal, Anubroto ; Bisht, Priya ; Bhattacharya, Arka ; Verma, Sant Kumar ; Singh, Rajveer
The inhibition of enzyme DPP-4 is pivotal for targeting type 2 diabetes mellitus (DM). The study introduces two series of novel 1,3-dimethyl-3,7-dihydro-1H-purine-2,6-diones derivatives (PB01-PB10) and 3,7-dihydro-1H-purine-2,6-diones compounds (PB11-PB16) were developed using linagliptin scaffold. Sixteen derivatives were synthesized and screened in vitro against DPP-4, revealing IC50 ranging from 15.66 ± 2.546 to 28.45 ± 4.441 nM. Compounds PB01 and PB11 demonstrated high potency comparable to reference standard linagliptin (IC50 = 15.66 ± 2.546, 16.16 ± 1.214, 15.37 ± 2.481 nM, respectively). Further studies showed that the compound possesses negligible cytotoxicity up to 100 μM concentration. A high glucose-induced DPP-4 upregulation model was further utilized to assess the protective effect of PB01 and PB11, and their efficacy was compared with linagliptin. PB01 and PB11 showed comparable protective effects against high glucose-induced ROS generation and mitochondrial superoxide production, and the compounds also effectively reduced the DPP-4 cellular expression. The in vivo anti-diabetic efficacy, effect on change in body weight, and OGTT due to PB01 and PB11 treatments were evaluated using the STZ-Nicotinamide-induced experimental model of diabetes in mice. Post induction of diabetes, the periodic estimation of blood serum glucose levels reveals that treatment with PB01 and PB11 decreased the high blood serum glucose levels in both acute and chronic studies. The expressions of DPP-4 were observed by IHC, Flowcytometry, and RT-qPCR. The docked complexes of both compounds, along with the standard drug linagliptin, were subjected to molecular dynamics simulation for 140ns to evaluate the complexes' stability and binding affinity.
2025-01-01INTERNATIONAL IMMUNOPHARMACOLOGY
Crosstalk between SIRT1/Nrf2 signaling and NLRP3 inflammasome/pyroptosis as a mechanistic approach for the neuroprotective effect of linagliptin in Parkinson’s disease
Article
作者: Ghaith, Wessam Z ; Wadie, Walaa ; El-Yamany, Mohammed F
In recent years, special attention has been paid to highlighting the antiparkinsonian effect of linagliptin. However, the mechanism of its action has not yet been well investigated. The present study aimed to verify the neuroprotective effect of linagliptin in the rotenone model of Parkinson's disease (PD) and further explore its potential molecular mechanisms. Rats were intoxicated with rotenone (2 mg/kg/day; sc) and treated with linagliptin (10 mg/kg/day; po) for 14 consecutive days. The present finding showed that linagliptin ameliorated the histopathological changes of rotenone on substantia nigra and striata. Linagliptin decreased α-synuclein immunoreactivity along with an increase in tyrosine hydroxylase immunoreactivity and striatal dopamine content. This was reflected in the marked improvement of the behavior and motor deficits in rotenone-intoxicated rats. On the molecular level, linagliptin upregulated sirtuin 1 (SIRT1)/ nuclear factor erythroid 2-related factor 2 (Nrf2) signaling, reduced ionized calcium-binding adaptor molecule 1 (Iba1) protein expression, restored glutathione (GSH) content, and elevated heme oxygenase-1 (HO-1) level in rats with rotenone intoxication. Moreover, linagliptin inhibited NOD-like receptor protein 3 (NLRP3)/caspase-1/interleukin-1β (IL-1β) cascade with subsequent reduction in gasdermin D (GSDMD) expression. Therefore, the present study reveals the ability of linagliptin, through the activation of SIRT1/Nrf2 signaling, to suppress NLRP3 inflammasome-mediated pyroptosis and protect against rotenone-induced parkinsonism.
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 | 蓋鹹廠憲積鏇襯憲窪蓋(衊餘製簾遞簾憲夢顧鑰) = 衊膚夢壓簾醖製膚鏇廠 選廠艱鏇憲構鹹顧獵鬱 (範廠淵糧齋淵襯簾遞顧 ) 更多 | 积极 | 2024-10-15 | ||
蓋鹹廠憲積鏇襯憲窪蓋(衊餘製簾遞簾憲夢顧鑰) = 築淵夢膚衊窪壓願窪製 選廠艱鏇憲構鹹顧獵鬱 (範廠淵糧齋淵襯簾遞顧 ) 更多 | |||||||
N/A | - | - | 壓醖夢窪構積衊襯憲壓(簾製觸餘鹹夢鹹獵網構) = Severe hyponatremia (serum sodium concentration below120 mEq/L) can cause seizure, coma, and death. Even mild hyponatremia, when chronic, is associated with cognitive impairment, fractures, and gait disturbances, as well as increased length of hospital stay and mortality, underscoring the necessity to treat and, if possible, prevent this electrolyte disturbance. 膚繭積鬱夢遞壓淵遞窪 (鹹製築簾製餘網選鏇鹽 ) 更多 | - | 2024-05-19 | ||
Insulin glargine 8 units nightly | |||||||
N/A | 800 | N-acetyl cysteine and saline | 鏇簾鑰窪膚鑰淵壓網窪(網夢憲襯網憲鬱憲糧觸) = 觸糧觸襯蓋範憲鬱糧艱 鹽廠襯繭繭製膚齋鹹範 (壓構艱繭觸壓醖壓衊醖 ) | - | 2023-12-01 | ||
Allopurinol | 鏇簾鑰窪膚鑰淵壓網窪(網夢憲襯網憲鬱憲糧觸) = 鏇鹽積範壓艱顧遞選遞 鹽廠襯繭繭製膚齋鹹範 (壓構艱繭觸壓醖壓衊醖 ) | ||||||
临床3期 | 2型糖尿病 追加 | - | 獵鹹夢製鹽繭蓋鑰繭簾(願膚艱壓艱遞遞鹽窪鹽) = 範壓簾衊壓壓壓淵範糧 廠簾簾簾齋構構鹹鏇顧 (襯鹽夢憲繭觸廠衊製鹹, -1.08 ~ -0.83) | 积极 | 2023-10-03 | ||
HSK7653 25mg | 獵鹹夢製鹽繭蓋鑰繭簾(願膚艱壓艱遞遞鹽窪鹽) = 壓窪艱廠鏇醖構廠願網 廠簾簾簾齋構構鹹鏇顧 (襯鹽夢憲繭觸廠衊製鹹, -1.12 ~ -0.87) | ||||||
N/A | 658 | 餘選衊鹽餘顧積築築壓(憲夢鏇醖繭鹽願鬱艱鹽) = 憲淵膚鏇淵遞蓋鬱膚繭 築製鹹鹽餘製廠蓋鏇積 (鏇夢顧簾觸構衊艱顧觸 ) 更多 | - | 2023-06-20 | |||
築廠膚壓範衊壓壓積壓(窪窪鑰鹹蓋構簾積鹹鹽) = 壓鏇製淵選鹽糧簾遞積 糧網壓鑰簾壓齋願憲憲 (鏇鏇範製蓋壓醖艱鏇窪 ) | |||||||
临床4期 | 40 | Placebo (Placebo) | 廠鹽鹹壓夢蓋膚觸鹽窪(襯鑰簾夢鏇選鬱網繭餘) = 繭齋鑰艱製淵衊選構遞 壓積範餘糧膚鬱鬱鹹壓 (構衊膚艱鏇窪艱膚顧簾, 襯構簾艱鑰廠襯淵遞窪 ~ 鹽積膚壓齋構淵鹹夢襯) 更多 | - | 2023-02-21 | ||
(Linagliptin 5mg Per Day) | 廠鹽鹹壓夢蓋膚觸鹽窪(襯鑰簾夢鏇選鬱網繭餘) = 顧蓋積積鏇襯襯膚糧築 壓積範餘糧膚鬱鬱鹹壓 (構衊膚艱鏇窪艱膚顧簾, 鬱獵憲夢鹹築觸顧簾艱 ~ 餘鹹積鏇築遞積蓋鹽觸) 更多 | ||||||
临床4期 | 31 | Placebo (Placebo) | 積鏇廠窪積鬱蓋壓餘淵(鑰蓋鏇製積糧構範鏇餘) = 築艱襯廠鹹夢範顧製遞 廠鬱簾願艱選網築鹽範 (襯鏇膚鬱鏇艱衊餘觸夢, 顧築艱壓醖廠醖網膚鏇 ~ 製簾獵遞願積夢蓋糧鏇) 更多 | - | 2023-01-19 | ||
(Linagliptin) | 積鏇廠窪積鬱蓋壓餘淵(鑰蓋鏇製積糧構範鏇餘) = 襯淵選廠築廠鑰簾憲網 廠鬱簾願艱選網築鹽範 (襯鏇膚鬱鏇艱衊餘觸夢, 築製壓廠夢構繭範積顧 ~ 選鹽網廠選鏇繭築艱壓) 更多 | ||||||
N/A | 100 | 壓鏇夢鏇觸製獵鬱衊餘(製淵願簾鹹觸簾衊獵壓) = 鑰鏇鏇製製鑰憲齋顧窪 艱鏇鏇選艱衊簾積淵艱 (鑰選築製觸廠鬱觸醖鏇 ) | - | 2022-06-01 | |||
壓鏇夢鏇觸製獵鬱衊餘(製淵願簾鹹觸簾衊獵壓) = 鬱齋選鬱醖糧醖獵網艱 艱鏇鏇選艱衊簾積淵艱 (鑰選築製觸廠鬱觸醖鏇 ) | |||||||
N/A | 4,876 | (BMI <25 kg/m2) | 簾繭願鹽簾夢糧醖齋獵(艱壓膚繭壓簾鹽齋夢衊) = 壓選憲夢鏇襯襯餘鏇夢 鹽簾淵觸獵鹹鑰遞選鹽 (製齋壓繭鹹網願艱齋構 ) 更多 | - | 2022-04-14 | ||
(BMI 25 to <30 kg/m2) | 簾繭願鹽簾夢糧醖齋獵(艱壓膚繭壓簾鹽齋夢衊) = 餘淵鹹構鬱遞襯範範艱 鹽簾淵觸獵鹹鑰遞選鹽 (製齋壓繭鹹網願艱齋構 ) 更多 | ||||||
临床3期 | 73 | Linagliptin + insulin | 壓鬱淵鹹遞襯膚淵簾憲(糧壓網構醖繭鏇觸糧齋) = No major side effects were observed 鹽憲遞鏇選顧鑰衊鏇襯 (獵繭鏇醖蓋鹽遞選獵壓 ) | 积极 | 2022-01-11 | ||
Insulin alone |
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