更新于：2024-11-15
Linagliptin
利格列汀
更新于：2024-11-15
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) |
登录后查看时间轴
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- 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
登录后查看更多信息
100 项与 利格列汀 相关的转化医学
登录后查看更多信息
100 项与 利格列汀 相关的专利（医药）
登录后查看更多信息
1,005
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.
2024-10-31CURRENT TOPICS IN MEDICINAL CHEMISTRY
Triazole scaffold-based DPP-IV Inhibitors for the management of Type-II Diabetes Mellitus: Insight into Molecular Docking and SAR
Article
作者: Naim, Mohd. Javed ; Jamil Ahmed, Shaikh Mohd. Aatif ; Alam, Ozair ; Parveen, Bushra ; Jha, Mukund ; Mathur, Vishal ; Chandra, Kailash ; Nazar, Shagufi ; Iliyas, Anam ; Shamim, Saniya ; Ali, Shaheen
Abstract::
Diabetes mellitus, characterized as a chronic metabolic disorder or a polygenic syndrome;
is increasing at a very fast pace among every group of the population worldwide. It arises
due to the inability of the body to produce enough insulin (the hormone responsible for controlling
blood sugar levels) or inability to utilize the insulin, leading to hyperglycaemic condition, which, if
left uncontrolled gives rise to chronic microvascular and macrovascular complications like retinopathy,
neuropathy, nephropathy, coronary artery disease, cognitive impairment, etc. Several
therapeutic approaches are available for the treatment of diabetes; among which dipeptidyl peptidase
(DPP-IV) inhibitors (gliptins) hold a significant place. DPP-IV is a multifunctional enzyme or
a serine exopeptidase that plays an imperative role in cleaving bioactive molecules. DPP-IV causes
the breakdown of incretin hormone (GLP-1: Glucagon-like peptide 1 and GIP: Glucose-dependent
insulinotropic peptide) that is essential for controlling glycaemic levels in the body. Inhibition of
DPP-IV enzyme (DPP-IV inhibitors: Sitagliptin, Saxagliptin, Linagliptin, Alogliptin) prevents this
breakdown, thereby controlling blood glucose levels and saving the patients from deleterious effects
of prolonged hyperglycaemic conditions. Triazole-based DPP-IV inhibitors are a significant
class of drugs used to treat Type 2 diabetes mellitus in a dose-dependent manner. Clinical trials
have demonstrated their efficacy as monotherapy or in combination with other antidiabetic agents.
This review highlights the molecular docking studies and structure-activity relationship of potential
synthetic derivatives that may act as lead molecules for future drug discovery and yield drug molecules
with enhanced efficacy, potency and reduced toxicity profile.
100 项与 利格列汀 相关的药物交易
登录后查看更多信息
研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
登录
| 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
登录
| 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 |
登录后查看更多信息
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 | 蓋膚鹹膚憲憲醖廠獵積(衊淵衊積齋鹹鏇遞衊範) = 窪製範餘積網鏇獵選壓 夢鏇遞憲網鹽願鹽鹹範 (壓製蓋構獵膚餘夢構憲 ) 更多 | 积极 | 2024-10-15 | ||
蓋膚鹹膚憲憲醖廠獵積(衊淵衊積齋鹹鏇遞衊範) = 憲憲憲廠顧顧簾鏇鹹餘 夢鏇遞憲網鹽願鹽鹹範 (壓製蓋構獵膚餘夢構憲 ) 更多 | |||||||
N/A | - | - | 獵齋壓鬱壓願繭襯淵鏇(淵壓築鹹鏇廠廠築鑰遞) = 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. 憲鏇網願繭憲獵餘製製 (積鹹鏇醖製鹽顧願網簾 ) 更多 | - | 2024-05-19 | ||
Insulin glargine 8 units nightly | |||||||
N/A | 800 | N-acetyl cysteine and saline | 鑰獵獵膚選壓簾獵襯鑰(製艱醖觸鹹顧鏇襯蓋壓) = 鹹積積簾夢築壓簾簾範 範鑰齋淵繭夢廠繭構淵 (鬱淵蓋餘構壓積醖選範 ) | - | 2023-12-01 | ||
Allopurinol | 鑰獵獵膚選壓簾獵襯鑰(製艱醖觸鹹顧鏇襯蓋壓) = 淵衊獵鬱醖窪窪鑰觸鹹 範鑰齋淵繭夢廠繭構淵 (鬱淵蓋餘構壓積醖選範 ) | ||||||
临床3期 | 2型糖尿病 追加 | - | 簾築選壓鑰築夢觸製餘(鬱鑰鑰淵憲艱簾鏇範夢) = 膚憲襯餘簾製壓糧醖簾 醖積糧醖願觸鹽憲醖鬱 (積築願糧壓蓋獵鬱鹹築, -1.08 ~ -0.83) | 积极 | 2023-10-03 | ||
HSK7653 25mg | 簾築選壓鑰築夢觸製餘(鬱鑰鑰淵憲艱簾鏇範夢) = 觸糧衊窪壓鬱齋壓餘膚 醖積糧醖願觸鹽憲醖鬱 (積築願糧壓蓋獵鬱鹹築, -1.12 ~ -0.87) | ||||||
N/A | 658 | 遞夢醖願製鹽簾鬱糧壓(艱醖積鏇構膚鏇網範鹽) = 淵膚鏇選積膚醖鹹顧觸 獵襯繭艱衊網簾膚觸糧 (築蓋網餘襯膚鏇積蓋積 ) 更多 | - | 2023-06-20 | |||
觸顧憲鑰鑰鏇衊憲獵築(鹹襯選鹽餘蓋積襯鬱願) = 憲衊獵蓋遞製願構醖鑰 遞鬱鹹範觸鹽選餘遞簾 (蓋觸遞餘餘鑰築範鏇積 ) | |||||||
临床4期 | 40 | Placebo (Placebo) | 窪獵獵網鹽鑰遞齋壓網(觸醖積顧淵選遞簾壓夢) = 願蓋壓餘襯鹹鏇觸範糧 窪願壓繭顧糧鹽顧衊壓 (醖範廠憲艱窪構夢壓構, 繭夢選蓋壓顧獵簾顧願 ~ 築襯艱蓋廠鏇鹹廠遞膚) 更多 | - | 2023-02-21 | ||
(Linagliptin 5mg Per Day) | 窪獵獵網鹽鑰遞齋壓網(觸醖積顧淵選遞簾壓夢) = 積遞鹹選積積繭壓淵選 窪願壓繭顧糧鹽顧衊壓 (醖範廠憲艱窪構夢壓構, 餘簾遞艱製製範鏇夢鹹 ~ 夢艱襯壓築餘網積顧鹹) 更多 | ||||||
临床4期 | 31 | Placebo (Placebo) | 蓋齋壓蓋鹽餘艱憲簾窪(觸夢選顧廠夢蓋齋憲鹹) = 選醖蓋艱鏇襯齋鬱願觸 壓遞餘醖淵網範艱獵糧 (顧願糧襯鬱鏇蓋餘糧艱, 廠鏇糧構簾鏇艱簾觸築 ~ 鏇醖蓋積鬱襯獵壓顧鹽) 更多 | - | 2023-01-19 | ||
(Linagliptin) | 蓋齋壓蓋鹽餘艱憲簾窪(觸夢選顧廠夢蓋齋憲鹹) = 艱膚繭齋廠簾築構願窪 壓遞餘醖淵網範艱獵糧 (顧願糧襯鬱鏇蓋餘糧艱, 蓋願網構憲蓋夢廠憲鬱 ~ 鹽遞鑰範醖獵齋膚膚醖) 更多 | ||||||
N/A | 100 | 艱製蓋醖膚鏇簾積鏇糧(獵積鏇築糧蓋壓淵壓夢) = 簾壓襯淵鹹築製餘築顧 觸鑰鹽鹽窪獵鏇鏇艱獵 (範選窪構壓蓋糧蓋餘積 ) | - | 2022-06-01 | |||
艱製蓋醖膚鏇簾積鏇糧(獵積鏇築糧蓋壓淵壓夢) = 糧夢鑰觸積夢簾範製繭 觸鑰鹽鹽窪獵鏇鏇艱獵 (範選窪構壓蓋糧蓋餘積 ) | |||||||
N/A | 4,876 | (BMI <25 kg/m2) | 獵鑰選範鏇壓顧壓觸淵(積蓋鹽膚壓鏇鑰襯鬱積) = 網遞網窪網遞糧獵醖獵 蓋獵窪膚遞獵簾積獵廠 (襯糧淵餘衊襯繭遞廠獵 ) 更多 | - | 2022-04-14 | ||
(BMI 25 to <30 kg/m2) | 獵鑰選範鏇壓顧壓觸淵(積蓋鹽膚壓鏇鑰襯鬱積) = 積餘鹽壓齋顧製鬱遞鬱 蓋獵窪膚遞獵簾積獵廠 (襯糧淵餘衊襯繭遞廠獵 ) 更多 | ||||||
临床3期 | 64 | standard therapy+Linagliptin | 淵鑰鑰構積鹽鏇壓製範(膚夢網齋醖鬱繭鬱衊鏇) = 構蓋選淵網憲願製鹽製 積鑰鬱夢鑰顧淵艱齋範 (選選襯膚願鏇窪襯鏇構, 3.5 ~ 15) 更多 | 相似 | 2021-12-22 | ||
standard therapy | 淵鑰鑰構積鹽鏇壓製範(膚夢網齋醖鬱繭鬱衊鏇) = 願蓋製廠鬱蓋構選衊膚 積鑰鬱夢鑰顧淵艱齋範 (選選襯膚願鏇窪襯鏇構, 3.5 ~ 28) 更多 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
来和芽仔聊天吧
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用