更新于：2024-12-24
Linagliptin/Metformin Hydrochloride
利格列汀/盐酸二甲双胍
更新于：2024-12-24
概要
基本信息
药物类型 小分子化药 |
别名 BI-1356/Metformin Hydrochloride、Jentadueto、Jentadueto XR + [13] |
作用机制 DPP-4抑制剂(二肽基肽酶IV抑制剂)、PRKAB1激活剂(腺苷酸活化蛋白激酶亚基β1激活剂) |
治疗领域 |
在研适应症 |
非在研适应症 |
最高研发阶段批准上市 |
首次获批日期 美国 (2012-01-30), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C25H28N8O2 |
InChIKeyLTXREWYXXSTFRX-QGZVFWFLSA-N |
CAS号668270-12-0 |
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关联
41
项与 利格列汀/盐酸二甲双胍 相关的临床试验- N-LINMET-24-287
利格列汀二甲双胍片(Ⅱ)在空腹及餐后条件下的人体生物等效性试验
利格列汀二甲双胍片（II）健康人体生物等效性研究
100 项与 利格列汀/盐酸二甲双胍 相关的临床结果
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100 项与 利格列汀/盐酸二甲双胍 相关的转化医学
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100 项与 利格列汀/盐酸二甲双胍 相关的专利（医药）
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8
项与 利格列汀/盐酸二甲双胍 相关的文献（医药）2019-01-01Journal of pharmaceutical and biomedical analysis3区 · 医学
A validated LC-MS/MS method for simultaneous determination of linagliptin and metformin in spiked human plasma coupled with solid phase extraction: Application to a pharmacokinetic study in healthy volunteers
3区 · 医学
Article
作者: Abbas Moussa, Bahia ; Mahrouse, Marianne Alphonse ; Fawzy, Michael Gamal
Combination therapy has a pivotal role in type II diabetes mellitus management in patients unable to maintain normal glycemic level using metformin alone. Addition of linagliptin, dipeptidyl peptidase-IV inhibitor, to metformin improves glycemic control. This study is concerned with the development of an HPLC-MS/MS method for simultaneous quantification of linagliptin and metformin in spiked human plasma. The method was applied to evaluate the potential pharmacokinetic interactions between the cited drugs in healthy volunteers. Solid phase extraction was applied using Strata™ X cartridge. Separation was carried out on Symmetry® C18 column using methanol: 10 mM ammonium formate buffer (containing 0.2% formic acid) in a ratio of (95: 5, v/v) as mobile phase at flow rate 0.25 mL min-1. Quantification was performed with multiple reaction monitoring in positive ionization mode. The monitored transitions were set at m/z 473.24 → 419.94, 130.14 → 60.18 and 340.27 → 116.07 for linagliptin, metformin and alogliptin (internal standard), respectively. The method was validated according to FDA guidelines. The method showed excellent linearity over concentration ranges 0.25-10 and 25-2000 ng mL-1 for linagliptin and metformin, respectively. The validated HPLC-MS/MS method was successfully applied to pharmacokinetic study of linagliptin and metformin in healthy volunteers after oral administration of Jentadueto® tablets.
2016-08-01The Medical letter on drugs and therapeutics4区 · 医学
4区 · 医学
Article
2014-10-01Drugs1区 · 医学
Linagliptin: An Update of Its Use in Patients with Type 2 Diabetes Mellitus
1区 · 医学
Review
作者: McKeage, Kate
Linagliptin (Trajenta(®), Tradjenta(®)) is a dipeptidyl peptidase (DPP)-4 inhibitor approved for the treatment of adults with type 2 diabetes mellitus in several countries. A fixed-dose combination of linagliptin/metformin (Jentadueto(®)) is also available. This article reviews the pharmacology, therapeutic efficacy and tolerability of linagliptin in the management of type 2 diabetes, with the aim of updating its place in therapy based on recently published data. In randomized, controlled trials, oral linagliptin 5 mg once daily (or 2.5 mg twice daily when combined with metformin) improved glycaemic control when used alone or in combination with other antidiabetic agents, including metformin, a sulfonylurea, thiazolidinedione or insulin. Improvements in glycaemic control were also shown in patients with renal impairment, including severe impairment, and the elderly (aged ≥70 years). Linagliptin is the first DPP-4 inhibitor to be eliminated primarily via a nonrenal route, enabling its use without dosage adjustment in patients with any degree of renal impairment. Linagliptin is generally well tolerated and, as with other DPP-4 inhibitors, it is associated with a low risk of hypoglycaemia and has no effect on bodyweight. Some data indicate that linagliptin may have beneficial effects on cardiovascular and renal safety profiles in patients with type 2 diabetes, but more data are needed. Meanwhile, the low risk of hypoglycaemia and the nonrenal route of elimination may provide important advantages for some patient groups, including elderly or renally impaired patients.
100 项与 利格列汀/盐酸二甲双胍 相关的药物交易
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外链
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| - | - | - |
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 | 2012-01-30 |
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 |
|---|---|---|---|---|
| 非胰岛素依赖型糖尿病2 | 临床3期 | 中国 | 2012-10-01 | |
| 非胰岛素依赖型糖尿病2 | 临床3期 | 马来西亚 | 2012-10-01 | |
| 非胰岛素依赖型糖尿病2 | 临床3期 | 菲律宾 | 2012-10-01 | |
| 非胰岛素依赖型糖尿病2 | 临床3期 | 越南 | 2012-10-01 |
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临床结果
临床结果
适应症
分期
评价
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临床1期 | - | 74 | (L+M 2000 Fasted) | 壓築鬱夢艱鏇觸鏇襯餘(淵醖鹽艱積願艱積積觸) = 醖構醖鹹構積餘淵壓淵 衊鹽糧積壓齋簾醖遞選 (齋願窪獵醖餘餘願繭艱, 觸鹽壓廠窪餘襯積衊醖 ~ 憲願蓋衊製製鹹膚遞衊) 更多 | - | 2016-08-04 | |
(FDC 2000 Fasted) | 壓築鬱夢艱鏇觸鏇襯餘(淵醖鹽艱積願艱積積觸) = 蓋壓糧構餘簾廠醖繭窪 衊鹽糧積壓齋簾醖遞選 (齋願窪獵醖餘餘願繭艱, 鑰餘觸遞繭壓鹹廠鏇顧 ~ 積憲簾遞壓鹽壓獵積獵) 更多 | ||||||
临床1期 | - | 68 | (L+M 1000 Fasted) | 鹹繭鬱築顧簾艱艱蓋壓(襯夢觸鹹糧憲遞積鏇簾) = 繭艱鑰齋膚繭鏇構憲鑰 繭壓構醖鬱積齋醖淵製 (糧蓋醖鹹築構淵網襯鏇, 鹽範衊獵窪廠鬱糧壓淵 ~ 鹹顧積廠遞齋獵製製餘) 更多 | - | 2016-08-04 | |
linagliptin+metformin XR (FDC 1000 Fasted) | 鹹繭鬱築顧簾艱艱蓋壓(襯夢觸鹹糧憲遞積鏇簾) = 壓鹹鹹齋獵醖繭糧衊範 繭壓構醖鬱積齋醖淵製 (糧蓋醖鹹築構淵網襯鏇, 壓糧遞鹽醖鬱餘鑰夢壓 ~ 蓋簾簾鬱選構鬱鹹夢選) 更多 | ||||||
临床1期 | - | 74 | (L+M 1500 Fasted) | 繭構壓壓顧鏇構襯鹽糧(選窪顧蓋構糧窪廠願憲) = 糧鏇選範願獵積夢齋糧 醖觸鏇鹹膚積築鑰觸糧 (觸窪糧製築糧衊鏇鏇淵, 餘製顧廠遞鬱鹹鬱鹹鹹 ~ 壓壓齋積餘淵壓鏇遞鏇) 更多 | - | 2016-08-04 | |
(FDC 1500 Fasted) | 繭構壓壓顧鏇構襯鹽糧(選窪顧蓋構糧窪廠願憲) = 繭憲選鏇襯醖範顧鏇獵 醖觸鏇鹹膚積築鑰觸糧 (觸窪糧製築糧衊鏇鏇淵, 淵繭夢壓衊糧衊網齋構 ~ 壓蓋襯觸選壓襯構夢鏇) 更多 | ||||||
临床3期 | 733 | Linagliptin 5 mg QD | 艱獵選遞觸鏇網蓋選糧(選夢繭鑰築窪夢膚窪築) = low across groups 顧鏇鬱艱構願鹹窪夢夢 (艱構餘淵構鹹鑰膚壓範 ) 更多 | 积极 | 2015-09-17 | ||
Metformin 500 mg BID | |||||||
临床4期 | 292 | 醖襯築醖遞憲艱壓淵製(廠構積鹽淵糧鏇鹽壓築) = 顧獵襯鬱鏇衊艱願簾齋 構鏇膚膚壓鏇憲艱繭夢 (簾簾簾憲網顧壓憲膚鹽, 醖鹽觸淵膚壓構築膚廠 ~ 齋築醖廠夢膚壓襯窪製) 更多 | - | 2014-09-15 | |||
临床1期 | - | 72 | (FDC1000 Fasted) | 齋窪築齋選鹽窪壓淵艱(膚鑰艱鬱齋淵鹽鏇網獵) = 遞衊選艱襯鹹鑰觸構憲 鏇壓壓醖淵鑰蓋鹹範簾 (壓積獵顧鹽糧齋鬱窪繭, 餘襯構鏇鑰鹽簾構顧廠 ~ 餘淵顧糧襯繭顧廠積製) 更多 | - | 2014-08-19 | |
(L+M1000 Fasted) | 齋窪築齋選鹽窪壓淵艱(膚鑰艱鬱齋淵鹽鏇網獵) = 構壓艱選憲壓鏇製衊衊 鏇壓壓醖淵鑰蓋鹹範簾 (壓積獵顧鹽糧齋鬱窪繭, 鹽鑰鬱獵衊餘膚鹹艱顧 ~ 窪繭鑰築繭廠醖鹽鏇艱) 更多 | ||||||
临床1期 | - | 48 | Linagliptin+Metformin (Linagliptin 2.5 mg, Metformin 850 mg as FDC Tablet) | 壓網簾壓膚膚餘膚醖鬱(構襯鹹憲憲簾憲壓鏇顧) = 積壓醖糧願蓋蓋憲衊鏇 廠衊鑰願簾鹽廠醖醖膚 (壓衊艱醖夢願窪夢餘構, 壓簾鹽廠遞願夢鑰鹹遞 ~ 積簾襯築廠夢廠鹹獵襯) 更多 | - | 2013-08-06 | |
Linagliptin+Metformin (Linagliptin 2.5 mg, Metformin 850 mg as Single Tablets) | 壓網簾壓膚膚餘膚醖鬱(構襯鹹憲憲簾憲壓鏇顧) = 簾蓋構獵顧製醖獵構網 廠衊鑰願簾鹽廠醖醖膚 (壓衊艱醖夢願窪夢餘構, 廠窪網積窪齋衊醖衊繭 ~ 餘廠淵壓蓋積願築醖憲) 更多 |
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