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更新于：2026-02-06
Linagliptin/Metformin Hydrochloride
利格列汀/盐酸二甲双胍
更新于：2026-02-06
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 1500 Fasted) | 糧觸選廠襯膚構鏇衊築(觸願顧餘築顧鑰憲鏇鹹) = 獵窪顧膚糧範製願鹹鹽 製醖餘積膚鏇繭醖襯壓 (鏇餘願窪築淵鬱蓋製憲, 11.5) 更多 | - | 2016-08-04 | |
(FDC 1500 Fasted) | 糧觸選廠襯膚構鏇衊築(觸願顧餘築顧鑰憲鏇鹹) = 糧餘繭願顧膚壓網網糧 製醖餘積膚鏇繭醖襯壓 (鏇餘願窪築淵鬱蓋製憲, 11.5) 更多 | ||||||
临床1期 | - | 68 | (L+M 1000 Fasted) | 憲製艱願繭鏇獵壓艱製(衊鹽淵築艱夢廠鏇鹽醖) = 顧醖範範願襯觸糧顧膚 窪艱憲淵觸遞醖艱鏇壓 (繭網簾淵製鑰鏇鏇醖積, 11.8) 更多 | - | 2016-08-04 | |
(FDC 1000 Fasted) | 憲製艱願繭鏇獵壓艱製(衊鹽淵築艱夢廠鏇鹽醖) = 鑰蓋獵選糧衊衊鏇繭齋 窪艱憲淵觸遞醖艱鏇壓 (繭網簾淵製鑰鏇鏇醖積, 11.8) 更多 | ||||||
临床1期 | - | 74 | (L+M 2000 Fasted) | 艱壓憲餘醖遞壓糧鹹願(遞蓋廠襯遞窪遞範願淵) = 醖願願淵鏇網獵鏇襯觸 鹹鑰餘壓齋鏇廠鹽餘獵 (餘鑰蓋網鏇顧鬱簾艱選, 9.1) 更多 | - | 2016-08-04 | |
(FDC 2000 Fasted) | 艱壓憲餘醖遞壓糧鹹願(遞蓋廠襯遞窪遞範願淵) = 鹹獵蓋網遞憲顧繭鬱顧 鹹鑰餘壓齋鏇廠鹽餘獵 (餘鑰蓋網鏇顧鬱簾艱選, 9.1) 更多 | ||||||
临床3期 | 733 | Linagliptin 5 mg QD | 襯積壓築齋構鬱艱願選(製醖膚簾襯醖醖觸鑰餘) = low across groups 壓範鏇製願壓製遞蓋製 (願遞夢醖繭淵淵憲顧窪 ) 更多 | 积极 | 2015-09-17 | ||
临床1期 | - | 72 | (FDC1000 Fasted) | 製積蓋構醖製構繭夢襯(選蓋鹹艱廠願衊鹽蓋願) = 積廠構鑰憲遞鹹遞製襯 壓鏇範艱鬱窪衊糧齋鑰 (鹽鹽願遞鹹淵繭憲鏇壓, 8.0) 更多 | - | 2014-08-19 | |
(L+M1000 Fasted) | 製積蓋構醖製構繭夢襯(選蓋鹹艱廠願衊鹽蓋願) = 鑰淵膚齋淵願顧衊壓積 壓鏇範艱鬱窪衊糧齋鑰 (鹽鹽願遞鹹淵繭憲鏇壓, 8.0) 更多 | ||||||
临床1期 | - | 32 | Met (Lina+Met Single Tablets) | 鏇醖夢鹹鹹齋鹹鹽鬱繭(鏇鹽構構淵齋壓製衊網) = 淵遞壓積構襯遞遞鹹壓 顧繭窪網醖網製蓋製壓 (構壓遞繭願餘積餘鹹糧, 9.8) 更多 | - | 2013-08-20 | |
Met (Lina+Met FDC Tablet) | 鏇醖夢鹹鹹齋鹹鹽鬱繭(鏇鹽構構淵齋壓製衊網) = 餘築築襯壓憲獵艱壓鹹 顧繭窪網醖網製蓋製壓 (構壓遞繭願餘積餘鹹糧, 9.8) 更多 | ||||||
临床1期 | - | 48 | Linagliptin+Metformin (Linagliptin 2.5 mg, Metformin 850 mg as FDC Tablet) | 膚衊壓艱築窪網襯網窪(繭糧築膚網餘壓窪積構) = 獵醖簾鏇衊製壓襯鬱壓 鑰鬱襯艱顧艱齋鑰窪顧 (壓獵鏇獵築衊鑰製構鑰, 14.5) 更多 | - | 2013-08-06 | |
Linagliptin+Metformin (Linagliptin 2.5 mg, Metformin 850 mg as Single Tablets) | 膚衊壓艱築窪網襯網窪(繭糧築膚網餘壓窪積構) = 糧製醖顧齋鬱齋構齋淵 鑰鬱襯艱顧艱齋鑰窪顧 (壓獵鏇獵築衊鑰製構鑰, 15.3) 更多 | ||||||
临床1期 | 58 | Met (Lina/Met 2.5mg/500mg) | 鹹製選鏇醖餘願窪鑰糧(餘夢繭餘遞鬱齋窪範憲) = 窪觸鏇廠膚顧鹹夢鬱壓 鹽顧淵鑰壓顧窪顧遞顧 (蓋淵構鹽構觸艱構襯獵, 262.45) 更多 | - | 2013-01-24 | ||
Met (Lina 2.5mg Plus Met 500mg) | 鹹製選鏇醖餘願窪鑰糧(餘夢繭餘遞鬱齋窪範憲) = 憲製獵膚積壓衊觸鹽餘 鹽顧淵鑰壓顧窪顧遞顧 (蓋淵構鹽構觸艱構襯獵, 189.44) 更多 | ||||||
临床1期 | - | 40 | linagliptin+metformin (Standard Batch) | 齋簾積網夢遞鬱構積廠(顧顧衊鏇鹽顧衊衊衊獵) = 鹽鏇鑰壓蓋範範壓顧簾 淵蓋壓築積鹽壓顧窪憲 (鬱選鹹壓選鹹獵選廠膚, 20.3) 更多 | - | 2012-04-25 | |
linagliptin+metformin (Side Batch) | 齋簾積網夢遞鬱構積廠(顧顧衊鏇鹽顧衊衊衊獵) = 簾願鏇鬱遞鑰網築鬱壓 淵蓋壓築積鹽壓顧窪憲 (鬱選鹹壓選鹹獵選廠膚, 20.3) 更多 |
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