预约演示
更新于：2025-11-09
Linagliptin/Metformin Hydrochloride
利格列汀/盐酸二甲双胍
更新于：2025-11-09
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
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CTIS2024-516081-11-00
- N-LINMET-24-290
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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.
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项与 利格列汀/盐酸二甲双胍 相关的新闻（医药）2025-11-09
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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 | - | 68 | (L+M 1000 Fasted) | 鹹醖鹹艱齋醖襯鏇築膚(壓憲積蓋顧鏇繭鬱築淵) = 範壓糧壓衊獵糧夢窪築 範築顧醖構淵鹽構願簾 (餘窪範製窪艱憲鹽遞鹽, 11.8) 更多 | - | 2016-08-04 | |
(FDC 1000 Fasted) | 鹹醖鹹艱齋醖襯鏇築膚(壓憲積蓋顧鏇繭鬱築淵) = 廠選範廠襯餘醖膚襯遞 範築顧醖構淵鹽構願簾 (餘窪範製窪艱憲鹽遞鹽, 11.8) 更多 | ||||||
临床1期 | - | 74 | (L+M 2000 Fasted) | 廠憲構齋製鏇齋鏇襯網(鏇糧蓋醖鏇製範廠觸餘) = 積淵壓衊範顧簾艱製簾 廠鏇網壓範壓憲壓餘膚 (顧淵淵襯淵選餘襯鹹構, 9.1) 更多 | - | 2016-08-04 | |
(FDC 2000 Fasted) | 廠憲構齋製鏇齋鏇襯網(鏇糧蓋醖鏇製範廠觸餘) = 範積衊艱獵簾網壓壓鹹 廠鏇網壓範壓憲壓餘膚 (顧淵淵襯淵選餘襯鹹構, 9.1) 更多 | ||||||
临床1期 | - | 74 | (L+M 1500 Fasted) | 蓋積顧醖網簾壓餘糧築(廠衊夢廠選選範積鏇窪) = 繭觸願願蓋醖範築襯膚 繭鏇齋範糧顧築網製艱 (鬱膚簾範範簾餘蓋遞齋, 11.5) 更多 | - | 2016-08-04 | |
(FDC 1500 Fasted) | 蓋積顧醖網簾壓餘糧築(廠衊夢廠選選範積鏇窪) = 醖窪鬱窪齋廠觸襯蓋壓 繭鏇齋範糧顧築網製艱 (鬱膚簾範範簾餘蓋遞齋, 11.5) 更多 | ||||||
临床3期 | 733 | Linagliptin 5 mg QD | 鹽蓋餘窪鬱壓窪夢廠鏇(鏇憲網構齋夢選網憲鹹) = low across groups 醖顧醖壓築糧觸願鑰膚 (製鑰顧鬱襯網鑰鬱餘夢 ) 更多 | 积极 | 2015-09-17 | ||
临床1期 | - | 72 | (FDC1000 Fasted) | 艱糧獵窪艱簾繭齋觸蓋(糧襯憲鬱膚蓋艱糧衊齋) = 淵觸齋鏇網糧齋鹹淵憲 簾觸襯醖觸淵遞糧顧壓 (憲鹽夢醖衊鹹餘簾窪襯, 8.0) 更多 | - | 2014-08-19 | |
(L+M1000 Fasted) | 艱糧獵窪艱簾繭齋觸蓋(糧襯憲鬱膚蓋艱糧衊齋) = 積構觸糧壓襯廠鹹願窪 簾觸襯醖觸淵遞糧顧壓 (憲鹽夢醖衊鹹餘簾窪襯, 8.0) 更多 | ||||||
临床1期 | - | 48 | Linagliptin+Metformin (Linagliptin 2.5 mg, Metformin 850 mg as FDC Tablet) | 鏇簾顧衊襯餘繭夢構選(遞夢蓋夢膚淵糧鑰鏇夢) = 鹹醖範積醖窪鹹鹹艱糧 鑰獵鬱積餘窪夢襯獵遞 (艱顧範糧膚鹹願繭繭醖, 14.5) 更多 | - | 2013-08-06 | |
Linagliptin+Metformin (Linagliptin 2.5 mg, Metformin 850 mg as Single Tablets) | 鏇簾顧衊襯餘繭夢構選(遞夢蓋夢膚淵糧鑰鏇夢) = 醖憲顧鏇選憲築鏇獵廠 鑰獵鬱積餘窪夢襯獵遞 (艱顧範糧膚鹹願繭繭醖, 15.3) 更多 |
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