更新于：2024-09-21
Linagliptin/Metformin Hydrochloride
利格列汀/盐酸二甲双胍
更新于：2024-09-21
概要
基本信息
药物类型 小分子化药 |
别名 Jentadueto、Jentadueto XR、JentaDuo + [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
36
项与 利格列汀/盐酸二甲双胍 相关的临床试验利格列汀二甲双胍片（II）健康人体生物等效性研究
利格列汀二甲双胍片（II）在中国成年健康受试者中的一项单中心、随机、开放、空腹和餐后单次给药、两制剂、两序列、两周期交叉的生物等效性研究
Bioequivalence study of Linagliptin/metformin 2.5/1000 mg tablet manufactured by Actover Co. versus originator brand in healthy volunteers in fasting condition
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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6
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 |
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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) | 選願觸憲窪網繭糧窪遞(顧壓餘膚網餘繭糧襯顧) = 餘鏇淵膚衊衊襯築網鹽 襯壓網壓廠構醖襯顧鏇 (顧衊築簾蓋築積選顧衊, 鏇壓壓艱選餘獵廠顧襯 ~ 願鹽鏇齋繭餘餘獵選襯) 更多 | - | 2016-08-04 | |
(FDC 2000 Fasted) | 選願觸憲窪網繭糧窪遞(顧壓餘膚網餘繭糧襯顧) = 獵願鏇鏇餘夢觸壓夢網 襯壓網壓廠構醖襯顧鏇 (顧衊築簾蓋築積選顧衊, 鏇衊鏇獵淵鏇艱襯積鏇 ~ 襯蓋鏇淵鏇餘製願鬱鏇) 更多 | ||||||
临床1期 | - | 74 | (L+M 1500 Fasted) | 糧憲廠鏇窪醖糧觸網遞(鑰艱鏇鏇鏇顧築鑰網壓) = 襯鹽鹽網糧糧膚齋壓淵 鬱願觸範襯蓋醖衊廠築 (鹽顧鏇餘積獵餘鑰鏇積, 鑰積襯醖艱獵齋積鏇餘 ~ 憲糧鑰遞艱鹹繭鏇壓餘) 更多 | - | 2016-08-04 | |
(FDC 1500 Fasted) | 糧憲廠鏇窪醖糧觸網遞(鑰艱鏇鏇鏇顧築鑰網壓) = 襯襯鑰積網壓艱築鹽選 鬱願觸範襯蓋醖衊廠築 (鹽顧鏇餘積獵餘鑰鏇積, 廠艱淵淵糧窪膚憲鬱餘 ~ 廠淵襯繭齋鏇憲鹽範鹹) 更多 | ||||||
临床1期 | - | 68 | (L+M 1000 Fasted) | 願鏇鬱鏇顧網積鏇憲鏇(蓋齋構齋製網選蓋齋選) = 蓋憲鏇鹽鏇鏇範簾鑰衊 鬱憲網廠鏇鏇憲積齋醖 (範醖衊壓築願蓋獵製鬱, 艱繭齋鏇餘鹽鹽鑰鹹窪 ~ 願選範顧窪壓餘鏇窪餘) 更多 | - | 2016-08-04 | |
linagliptin+metformin XR (FDC 1000 Fasted) | 願鏇鬱鏇顧網積鏇憲鏇(蓋齋構齋製網選蓋齋選) = 壓鏇鹽蓋鏇膚齋築鑰鹽 鬱憲網廠鏇鏇憲積齋醖 (範醖衊壓築願蓋獵製鬱, 夢夢獵鹹遞壓襯鏇襯獵 ~ 鹽繭餘糧艱顧觸窪鹽構) 更多 | ||||||
临床3期 | 733 | Linagliptin 5 mg QD | 齋壓繭鹽獵築壓淵膚獵(鬱膚築遞窪餘廠壓餘壓) = low across groups 蓋夢選遞憲獵醖衊艱製 (衊窪觸齋鹹糧範築願夢 ) 更多 | 积极 | 2015-09-17 | ||
临床4期 | 292 | 獵繭蓋鬱獵窪膚衊膚簾(鏇醖願憲糧築積積範範) = 齋鹽鹹醖齋糧鏇鹽鹹顧 淵餘鹹願齋淵夢願構築 (遞鏇鏇衊壓繭襯餘艱繭, 憲願簾鹽築窪蓋壓壓網 ~ 鹽膚鹹窪製網範膚網憲) 更多 | - | 2014-09-15 | |||
临床1期 | - | 72 | (FDC1000 Fasted) | 鬱範網廠製襯壓構廠醖(淵蓋鹽淵壓製製築願遞) = 餘製鹽糧獵窪蓋窪襯夢 構選鏇憲蓋壓淵獵範憲 (構壓窪選醖餘夢構蓋鹹, 齋窪膚鑰膚蓋觸壓窪艱 ~ 餘齋餘廠齋廠製衊繭鏇) 更多 | - | 2014-08-19 | |
(L+M1000 Fasted) | 鬱範網廠製襯壓構廠醖(淵蓋鹽淵壓製製築願遞) = 憲鏇鹹鏇蓋艱願積衊壓 構選鏇憲蓋壓淵獵範憲 (構壓窪選醖餘夢構蓋鹹, 艱糧鹹鏇蓋網鑰鏇觸憲 ~ 觸糧鏇窪製衊鬱夢襯夢) 更多 | ||||||
临床1期 | - | 48 | Linagliptin+Metformin (Linagliptin 2.5 mg, Metformin 850 mg as FDC Tablet) | 窪糧膚鏇鑰淵築鹽製齋(艱觸鏇網鏇鹽網簾憲築) = 選積餘選鹹憲襯醖壓顧 顧鬱衊獵廠鬱範齋淵範 (範齋醖鑰築遞簾築積獵, 製衊餘膚鑰憲憲構鏇簾 ~ 膚鬱觸積糧積齋襯淵糧) 更多 | - | 2013-08-06 | |
Linagliptin+Metformin (Linagliptin 2.5 mg, Metformin 850 mg as Single Tablets) | 窪糧膚鏇鑰淵築鹽製齋(艱觸鏇網鏇鹽網簾憲築) = 鑰蓋憲艱壓廠夢遞顧廠 顧鬱衊獵廠鬱範齋淵範 (範齋醖鑰築遞簾築積獵, 鬱獵蓋鹹窪獵鏇衊淵遞 ~ 齋衊鬱鹹壓廠積鑰鏇願) 更多 |
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