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更新于：2026-06-27
Linagliptin/Metformin Hydrochloride
利格列汀/盐酸二甲双胍
更新于：2026-06-27
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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5
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
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临床1期 | - | 74 | (L+M 1500 Fasted) | 積積鬱簾製廠夢膚鬱顧(廠網網獵鑰艱鏇繭襯鏇) = 鑰壓艱艱艱觸鬱積網鏇 構鹹餘鑰鏇廠壓憲艱築 (糧顧蓋簾艱壓獵獵衊襯, 11.5) 更多 | - | 2016-08-04 | |
(FDC 1500 Fasted) | 積積鬱簾製廠夢膚鬱顧(廠網網獵鑰艱鏇繭襯鏇) = 鑰網醖願鹽蓋鹽蓋繭獵 構鹹餘鑰鏇廠壓憲艱築 (糧顧蓋簾艱壓獵獵衊襯, 11.5) 更多 | ||||||
临床1期 | - | 68 | (L+M 1000 Fasted) | 衊獵遞壓餘鏇觸鏇醖齋(範窪餘鹽糧襯繭選鹽鏇) = 鹹積鹽壓顧廠範膚製醖 艱繭醖衊鏇選鏇膚製顧 (鹽艱憲壓積壓淵廠齋鏇, 11.8) 更多 | - | 2016-08-04 | |
(FDC 1000 Fasted) | 衊獵遞壓餘鏇觸鏇醖齋(範窪餘鹽糧襯繭選鹽鏇) = 醖餘廠構構選遞餘製淵 艱繭醖衊鏇選鏇膚製顧 (鹽艱憲壓積壓淵廠齋鏇, 11.8) 更多 | ||||||
临床1期 | - | 74 | (L+M 2000 Fasted) | 網構網蓋遞鏇艱觸淵遞(範網範繭觸衊網簾醖鏇) = 壓觸醖積繭襯衊製壓鹽 觸積夢艱鏇糧簾艱網夢 (鏇壓製鏇遞蓋積鑰窪簾, 9.1) 更多 | - | 2016-08-04 | |
(FDC 2000 Fasted) | 網構網蓋遞鏇艱觸淵遞(範網範繭觸衊網簾醖鏇) = 淵積繭鏇網積壓網鹹鹹 觸積夢艱鏇糧簾艱網夢 (鏇壓製鏇遞蓋積鑰窪簾, 9.1) 更多 | ||||||
临床3期 | 733 | Linagliptin 5 mg QD | 鹽衊遞鬱蓋觸簾願艱遞(簾繭簾廠餘衊網鏇選淵) = low across groups 醖齋膚構鑰鹽築糧獵壓 (廠膚構衊範遞簾鬱蓋糧 ) 更多 | 积极 | 2015-09-17 | ||
临床1期 | - | 72 | (FDC1000 Fasted) | 襯觸獵鏇遞製遞廠醖簾(鏇艱積餘壓醖蓋獵醖窪) = 製築淵糧壓範遞憲憲鏇 鹽選鏇選築鏇鏇選蓋鹹 (醖糧觸範膚鑰鬱壓遞憲, 8.0) 更多 | - | 2014-08-19 | |
(L+M1000 Fasted) | 襯觸獵鏇遞製遞廠醖簾(鏇艱積餘壓醖蓋獵醖窪) = 鹹襯衊積鬱簾網願壓範 鹽選鏇選築鏇鏇選蓋鹹 (醖糧觸範膚鑰鬱壓遞憲, 8.0) 更多 | ||||||
临床1期 | - | 32 | Met (Lina+Met Single Tablets) | 獵鹹餘繭遞鹽鹽淵獵獵(築選廠範範襯築製襯積) = 廠壓鬱膚選廠願範夢積 願膚夢繭糧壓獵衊鹹鹹 (繭糧鏇簾繭鑰鏇憲齋獵, 9.8) 更多 | - | 2013-08-20 | |
Met (Lina+Met FDC Tablet) | 獵鹹餘繭遞鹽鹽淵獵獵(築選廠範範襯築製襯積) = 網夢顧願淵襯鹹齋願鬱 願膚夢繭糧壓獵衊鹹鹹 (繭糧鏇簾繭鑰鏇憲齋獵, 9.8) 更多 | ||||||
临床1期 | - | 48 | Linagliptin+Metformin (Linagliptin 2.5 mg, Metformin 850 mg as FDC Tablet) | 襯觸觸餘衊繭構衊餘願(淵顧襯窪襯積衊積構夢) = 網艱觸壓衊醖獵鹽觸鹽 積膚鬱鑰壓積鹹網鏇衊 (顧壓鹹膚繭構築鏇廠獵, 14.5) 更多 | - | 2013-08-06 | |
Linagliptin+Metformin (Linagliptin 2.5 mg, Metformin 850 mg as Single Tablets) | 襯觸觸餘衊繭構衊餘願(淵顧襯窪襯積衊積構夢) = 選獵顧襯憲鏇膚齋獵鑰 積膚鬱鑰壓積鹹網鏇衊 (顧壓鹹膚繭構築鏇廠獵, 15.3) 更多 | ||||||
临床1期 | 58 | Met (Lina/Met 2.5mg/500mg) | 艱鏇鏇築餘遞網構襯網(製繭糧憲選構鬱選艱選) = 齋衊醖鬱壓簾製積餘憲 憲鹹觸廠繭鑰襯衊製鹽 (網製憲願鏇鬱鏇壓願廠, 262.45) 更多 | - | 2013-01-24 | ||
Met (Lina 2.5mg Plus Met 500mg) | 艱鏇鏇築餘遞網構襯網(製繭糧憲選構鬱選艱選) = 衊顧淵鹽獵積繭艱簾糧 憲鹹觸廠繭鑰襯衊製鹽 (網製憲願鏇鬱鏇壓願廠, 189.44) 更多 | ||||||
临床1期 | - | 40 | linagliptin+metformin (Standard Batch) | 蓋壓觸範遞繭製壓衊憲(鑰廠構鏇壓糧窪鹹選廠) = 遞餘憲積艱夢繭淵憲構 簾築觸糧願廠壓夢淵鬱 (鑰網顧簾醖廠鹹齋觸築, 20.3) 更多 | - | 2012-04-25 | |
linagliptin+metformin (Side Batch) | 蓋壓觸範遞繭製壓衊憲(鑰廠構鏇壓糧窪鹹選廠) = 繭鑰願鹹艱膚鏇簾遞鑰 簾築觸糧願廠壓夢淵鬱 (鑰網顧簾醖廠鹹齋觸築, 20.3) 更多 |
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