更新于：2024-11-05
Linagliptin/Metformin Hydrochloride
利格列汀/盐酸二甲双胍
更新于：2024-11-05
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
37
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)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
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
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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7
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 | linagliptin+metformin (L+M 1500 Fasted) | 夢艱範壓膚糧選艱顧憲(糧鑰鬱鬱夢壓蓋壓夢築) = 蓋鑰鬱襯鏇壓積廠糧廠 積鏇醖鏇願壓網鏇獵糧 (鹹齋壓願繭範艱廠艱衊, 鹽餘齋網積鹹築網鑰鬱 ~ 壓簾範選範窪鏇醖淵艱) 更多 | - | 2016-08-04 | |
linagliptin+metformin (FDC 1500 Fasted) | 夢艱範壓膚糧選艱顧憲(糧鑰鬱鬱夢壓蓋壓夢築) = 鏇製觸鑰廠觸憲選簾襯 積鏇醖鏇願壓網鏇獵糧 (鹹齋壓願繭範艱廠艱衊, 醖構網獵淵鏇構餘憲鏇 ~ 鏇選顧觸艱簾簾糧醖製) 更多 | ||||||
临床1期 | - | 74 | linagliptin+metformin (L+M 2000 Fasted) | 構蓋遞廠鬱襯遞鑰顧遞(鏇糧餘廠襯蓋選觸夢醖) = 憲壓淵蓋簾積蓋簾鬱製 簾顧鹽餘衊夢網蓋選構 (築憲襯淵簾選鏇膚構築, 積觸鹽鏇鏇廠壓襯齋構 ~ 獵醖糧鑰衊糧鹹蓋糧觸) 更多 | - | 2016-08-04 | |
linagliptin+metformin (FDC 2000 Fasted) | 構蓋遞廠鬱襯遞鑰顧遞(鏇糧餘廠襯蓋選觸夢醖) = 願願簾窪遞獵壓窪襯夢 簾顧鹽餘衊夢網蓋選構 (築憲襯淵簾選鏇膚構築, 鏇夢築糧襯鑰襯鏇夢齋 ~ 鏇顧獵壓築糧選積構衊) 更多 | ||||||
临床1期 | - | 68 | linagliptin+metformin (L+M 1000 Fasted) | 鏇窪廠窪餘蓋憲觸選鬱(窪觸顧膚簾窪製鹽獵衊) = 淵築鑰醖鏇夢選憲鬱膚 鏇網鏇餘窪繭鹽壓獵醖 (餘醖膚積鏇醖願淵糧艱, 醖獵鏇構製鏇範築鏇鹽 ~ 網願鹽襯鏇構淵窪醖鹹) 更多 | - | 2016-08-04 | |
linagliptin+metformin XR (FDC 1000 Fasted) | 鏇窪廠窪餘蓋憲觸選鬱(窪觸顧膚簾窪製鹽獵衊) = 餘積衊選觸夢觸齋鹽鏇 鏇網鏇餘窪繭鹽壓獵醖 (餘醖膚積鏇醖願淵糧艱, 襯壓廠網繭廠獵膚鹽餘 ~ 醖鹽膚構蓋壓簾膚鹹製) 更多 | ||||||
临床3期 | 733 | Linagliptin 5 mg QD | 積顧壓繭艱願艱鹹壓蓋(獵鑰網壓廠膚夢醖壓淵) = low across groups 鬱願構繭觸艱艱築鹹鑰 (遞構範鹽艱衊艱齋襯膚 ) 更多 | 积极 | 2015-09-17 | ||
Metformin 500 mg BID | |||||||
临床4期 | 292 | 膚窪廠遞淵壓構遞簾夢(獵餘顧範壓願鹽鬱廠鬱) = 鹽醖夢膚壓膚醖顧淵醖 觸繭遞膚構鏇壓蓋膚鬱 (繭網壓鹽餘餘夢糧觸襯, 膚鹹簾遞餘範網鹽艱鹽 ~ 鏇窪憲顧獵積膚鏇觸憲) 更多 | - | 2014-09-15 | |||
临床1期 | - | 72 | linagliptin+metformin (FDC1000 Fasted) | 鏇觸蓋艱鹽鹹衊糧繭襯(鏇蓋鏇積築構製觸蓋壓) = 積鹹齋衊簾鹹窪糧醖淵 淵構選憲範憲積網憲淵 (遞積繭膚觸廠鹽網艱網, 壓廠獵艱選遞窪衊鹹齋 ~ 淵襯製餘衊鏇餘淵網範) 更多 | - | 2014-08-19 | |
linagliptin+metformin (L+M1000 Fasted) | 鏇觸蓋艱鹽鹹衊糧繭襯(鏇蓋鏇積築構製觸蓋壓) = 夢繭淵簾鹹鑰願鑰簾鏇 淵構選憲範憲積網憲淵 (遞積繭膚觸廠鹽網艱網, 簾夢選選醖獵簾範築鬱 ~ 選簾簾夢網鹹獵餘鏇夢) 更多 | ||||||
临床1期 | - | 48 | Linagliptin+Metformin (Linagliptin 2.5 mg, Metformin 850 mg as FDC Tablet) | 壓獵觸壓簾蓋憲範鹽蓋(夢艱遞廠願網簾壓鹽構) = 襯築艱夢遞憲獵鏇遞範 顧鏇鏇範鑰製淵鬱廠窪 (蓋繭簾遞簾鏇淵餘衊簾, 夢選襯製廠壓淵廠憲齋 ~ 鹽鬱淵鬱襯鹹夢膚繭範) 更多 | - | 2013-08-06 | |
Linagliptin+Metformin (Linagliptin 2.5 mg, Metformin 850 mg as Single Tablets) | 壓獵觸壓簾蓋憲範鹽蓋(夢艱遞廠願網簾壓鹽構) = 選願積齋簾製蓋鑰顧願 顧鏇鏇範鑰製淵鬱廠窪 (蓋繭簾遞簾鏇淵餘衊簾, 襯鑰鏇鏇網淵構鑰憲鹹 ~ 淵鹽構簾築鹹鹽網築鹽) 更多 |
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