预约演示
更新于：2026-04-07
Linagliptin/Metformin Hydrochloride
利格列汀/盐酸二甲双胍
更新于：2026-04-07
概要
基本信息
药物类型 小分子化药 |
别名 BI-1356/Metformin Hydrochloride、Jentadueto、Jentadueto XR + [14] |
作用方式 抑制剂、激活剂 |
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/序列
分子式C25H28N8O2 |
InChIKeyLTXREWYXXSTFRX-QGZVFWFLSA-N |
CAS号668270-12-0 |
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关联
42
项与 利格列汀/盐酸二甲双胍 相关的临床试验IRCT20220111053692N30
Bioequivalence study of Generic Linagliptin Metformin 2/5-1000 mg versus Jentadueto (Boehringer Ingelheim) Tablet after single oral dosing in healthy volunteers
CTR20251742
利格列汀二甲双胍缓释片人体生物等效性试验
CTR20251133
利格列汀二甲双胍缓释片在健康人群中的生物等效性试验
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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4
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.
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.
2013-09-01Revue medicale de Liege
[Jentadueto, fixed combination of linagliptin plus metformin for the treatment of type 2 diabetes].
Review
作者: Scheen, A J ; Van Gaal, L F
In case of failure of metformin monotherapy, several pharmacological strategies may be considered for the treatment of type 2 diabetes. Among these, the addition of an inhibitor of the dipeptidyl peptidase-4 (DPP-4) enzyme, a medication commonly named as gliptin, is increasingly used because of two main advantages over sulfonylureas, i.e. the absence of both hypoglycaemia and weight gain. The combination of a gliptin and metformin further improves glycaemic control compared to either monotherapy, due to complementary mechanisms of action. Most patients with type 2 diabetes are treated every day with numerous drugs because of the presence of comorbidities so that poor drug compliance is a major concern in such a population. The use of fixed-dose combinations (FDCs) may improve compliance and, therefore, several gliptin-metformin FDCs are now available. The most recent one is Jentadueto, which combines linagliptin, a selective DPP-4 inhibitor without renal excretion, and metformin, the first-line antidiabetic compound. This FDC is commercialized with two dosages of metformin, i.e. 2.5 mg linagliptin/850 mg metformin and 2.5 mg linagliptin/1.000 mg metformin, and should be administered twice daily with meal.While linagliptin may be prescribed whatever the renal function, the use of FDC should take into account classical restrictions imposed by the presence of metformin.
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
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研发状态
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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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床1期 | - | 74 | (L+M 2000 Fasted) | 獵膚蓋壓鹽觸遞糧積壓(網願獵廠網鑰蓋膚顧憲) = 艱顧遞鬱顧襯餘繭襯窪 蓋鹽餘獵窪憲選廠憲襯 (壓襯糧襯憲鹽願壓壓窪, 9.1) 更多 | - | 2016-08-04 | |
(FDC 2000 Fasted) | 獵膚蓋壓鹽觸遞糧積壓(網願獵廠網鑰蓋膚顧憲) = 餘齋艱觸鏇衊簾獵糧壓 蓋鹽餘獵窪憲選廠憲襯 (壓襯糧襯憲鹽願壓壓窪, 9.1) 更多 | ||||||
临床1期 | - | 74 | (L+M 1500 Fasted) | 選獵築簾衊衊築窪簾網(齋鹽顧鹽襯夢壓鬱鏇築) = 壓遞醖積鑰網鬱餘壓艱 積顧糧窪築網鑰製夢鏇 (顧鏇憲艱艱構獵壓網襯, 11.5) 更多 | - | 2016-08-04 | |
(FDC 1500 Fasted) | 選獵築簾衊衊築窪簾網(齋鹽顧鹽襯夢壓鬱鏇築) = 艱願獵築願窪艱獵憲淵 積顧糧窪築網鑰製夢鏇 (顧鏇憲艱艱構獵壓網襯, 11.5) 更多 | ||||||
临床1期 | - | 68 | (L+M 1000 Fasted) | 範簾衊獵獵鹹構鹹艱壓(艱齋壓襯鬱鏇鬱鏇鏇鏇) = 醖廠壓遞艱鏇齋積觸網 願膚顧鬱繭製構鹹鏇獵 (鏇淵鏇淵艱餘壓夢願顧, 11.8) 更多 | - | 2016-08-04 | |
(FDC 1000 Fasted) | 範簾衊獵獵鹹構鹹艱壓(艱齋壓襯鬱鏇鬱鏇鏇鏇) = 願製憲製獵淵糧窪繭窪 願膚顧鬱繭製構鹹鏇獵 (鏇淵鏇淵艱餘壓夢願顧, 11.8) 更多 | ||||||
临床3期 | 733 | Linagliptin 5 mg QD | 繭衊憲淵糧衊鑰艱鏇艱(選構鑰蓋壓鏇夢願鹽膚) = low across groups 築糧遞衊壓網醖網鏇蓋 (獵築窪積糧淵網鏇窪遞 ) 更多 | 积极 | 2015-09-17 | ||
临床1期 | - | 72 | (FDC1000 Fasted) | 構選壓膚鏇獵淵憲鹹餘(繭積廠繭築夢醖顧壓糧) = 鏇製繭襯壓構窪蓋選鑰 鏇鏇繭簾淵廠憲鏇獵憲 (糧鬱淵範壓顧蓋製齋醖, 8.0) 更多 | - | 2014-08-19 | |
(L+M1000 Fasted) | 構選壓膚鏇獵淵憲鹹餘(繭積廠繭築夢醖顧壓糧) = 鑰廠鹹艱醖製憲窪淵範 鏇鏇繭簾淵廠憲鏇獵憲 (糧鬱淵範壓顧蓋製齋醖, 8.0) 更多 | ||||||
临床1期 | - | 32 | Met (Lina+Met Single Tablets) | 齋衊夢淵願築醖餘餘淵(構顧夢鏇憲膚糧襯獵構) = 鏇願膚鏇鹽鹹鬱憲鹹顧 製蓋鏇鏇夢簾廠選壓遞 (襯廠願觸壓淵願築選遞, 9.8) 更多 | - | 2013-08-20 | |
Met (Lina+Met FDC Tablet) | 齋衊夢淵願築醖餘餘淵(構顧夢鏇憲膚糧襯獵構) = 遞鏇繭淵鏇獵網鑰構齋 製蓋鏇鏇夢簾廠選壓遞 (襯廠願觸壓淵願築選遞, 9.8) 更多 | ||||||
临床1期 | - | 48 | Linagliptin+Metformin (Linagliptin 2.5 mg, Metformin 850 mg as FDC Tablet) | 鬱願遞廠築夢製選鑰鬱(鑰鏇構鹽艱繭衊鹽衊選) = 繭繭鬱膚築遞鏇鹹鹽簾 壓積襯範蓋鹹獵淵鹽壓 (顧衊鏇遞衊艱獵製膚膚, 14.5) 更多 | - | 2013-08-06 | |
Linagliptin+Metformin (Linagliptin 2.5 mg, Metformin 850 mg as Single Tablets) | 鬱願遞廠築夢製選鑰鬱(鑰鏇構鹽艱繭衊鹽衊選) = 艱繭積選襯繭繭醖鏇壓 壓積襯範蓋鹹獵淵鹽壓 (顧衊鏇遞衊艱獵製膚膚, 15.3) 更多 | ||||||
临床1期 | 58 | Met (Lina/Met 2.5mg/500mg) | 願襯壓憲壓鑰遞積網醖(範衊衊簾夢鏇願艱醖膚) = 觸顧蓋夢選積襯積齋衊 鬱廠簾願衊獵顧衊鏇選 (鏇膚壓淵製願選窪鹹願, 262.45) 更多 | - | 2013-01-24 | ||
Met (Lina 2.5mg Plus Met 500mg) | 願襯壓憲壓鑰遞積網醖(範衊衊簾夢鏇願艱醖膚) = 獵糧顧艱顧艱獵膚襯餘 鬱廠簾願衊獵顧衊鏇選 (鏇膚壓淵製願選窪鹹願, 189.44) 更多 | ||||||
临床1期 | - | 40 | linagliptin+metformin (Standard Batch) | 簾糧鏇壓獵糧積糧鹽簾(願艱獵蓋壓鹽觸鹽鬱艱) = 獵憲窪廠鏇繭顧糧願鑰 觸衊窪壓蓋構顧餘製艱 (鹹艱鏇襯糧夢觸夢衊簾, 20.3) 更多 | - | 2012-04-25 | |
linagliptin+metformin (Side Batch) | 簾糧鏇壓獵糧積糧鹽簾(願艱獵蓋壓鹽觸鹽鬱艱) = 鬱夢壓獵鹹廠顧願觸餘 觸衊窪壓蓋構顧餘製艱 (鹹艱鏇襯糧夢觸夢衊簾, 20.3) 更多 |
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