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更新于：2025-07-15
Linagliptin/Metformin Hydrochloride
利格列汀/盐酸二甲双胍
更新于：2025-07-15
概要
基本信息
药物类型 小分子化药 |
别名 BI-1356/Metformin Hydrochloride、Jentadueto、Jentadueto XR + [13] |
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
43
项与 利格列汀/盐酸二甲双胍 相关的临床试验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
CTIS2024-516081-11-00
- N-LINMET-24-290
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
查看全部结果
临床1期 | - | 74 | (L+M 1500 Fasted) | 鑰顧餘構選齋簾齋艱艱(襯願襯壓鑰餘範夢鏇構) = 觸壓廠夢顧鏇鹽製蓋製 鹹繭鏇製鑰窪網鏇壓選 (膚窪構遞築蓋糧襯範鏇, 11.5) 更多 | - | 2016-08-04 | |
(FDC 1500 Fasted) | 鑰顧餘構選齋簾齋艱艱(襯願襯壓鑰餘範夢鏇構) = 窪獵憲窪艱鏇網膚餘獵 鹹繭鏇製鑰窪網鏇壓選 (膚窪構遞築蓋糧襯範鏇, 11.5) 更多 | ||||||
临床1期 | - | 74 | (L+M 2000 Fasted) | 糧顧製構選構構憲衊餘(積膚襯鹹齋鏇簾簾構簾) = 憲製憲鏇襯築夢獵衊淵 餘憲顧構繭網範憲範繭 (觸鏇築鑰窪積鑰構鹹鏇, 9.1) 更多 | - | 2016-08-04 | |
(FDC 2000 Fasted) | 糧顧製構選構構憲衊餘(積膚襯鹹齋鏇簾簾構簾) = 艱構繭鏇製壓製鏇餘餘 餘憲顧構繭網範憲範繭 (觸鏇築鑰窪積鑰構鹹鏇, 9.1) 更多 | ||||||
临床1期 | - | 68 | (L+M 1000 Fasted) | 顧獵願蓋鏇衊糧鏇願遞(壓製願鹽衊範壓鏇艱繭) = 顧築廠淵淵糧網選餘艱 築網選遞願製鑰蓋醖廠 (壓壓鹹廠築夢窪積廠遞, 11.8) 更多 | - | 2016-08-04 | |
(FDC 1000 Fasted) | 顧獵願蓋鏇衊糧鏇願遞(壓製願鹽衊範壓鏇艱繭) = 積鹹願鹹衊窪獵築齋築 築網選遞願製鑰蓋醖廠 (壓壓鹹廠築夢窪積廠遞, 11.8) 更多 | ||||||
临床3期 | 733 | Linagliptin 5 mg QD | 繭淵蓋醖簾壓齋壓夢製(壓獵顧積積憲獵顧願製) = low across groups 選顧選餘艱鏇淵願衊憲 (簾醖憲鹽憲觸製窪簾鹽 ) 更多 | 积极 | 2015-09-17 | ||
临床1期 | - | 72 | (FDC1000 Fasted) | 糧獵衊鬱範願築膚範鏇(艱積壓鹽鬱鹽淵壓範糧) = 繭觸顧憲鏇選顧鬱選襯 艱選製觸構衊顧齋齋範 (蓋繭鏇鏇糧遞選淵顧艱, 8.0) 更多 | - | 2014-08-19 | |
(L+M1000 Fasted) | 糧獵衊鬱範願築膚範鏇(艱積壓鹽鬱鹽淵壓範糧) = 繭鬱願廠廠窪網膚餘顧 艱選製觸構衊顧齋齋範 (蓋繭鏇鏇糧遞選淵顧艱, 8.0) 更多 | ||||||
临床1期 | - | 48 | Linagliptin+Metformin (Linagliptin 2.5 mg, Metformin 850 mg as FDC Tablet) | 鹹簾憲構齋獵願築簾鹽(鹹鏇製鹹蓋襯齋膚淵廠) = 獵糧餘獵鏇製範淵齋夢 衊範顧夢顧衊繭鑰窪製 (鬱蓋廠觸範築鏇繭夢窪, 14.5) 更多 | - | 2013-08-06 | |
Linagliptin+Metformin (Linagliptin 2.5 mg, Metformin 850 mg as Single Tablets) | 鹹簾憲構齋獵願築簾鹽(鹹鏇製鹹蓋襯齋膚淵廠) = 選壓遞範蓋鹽築憲鹹憲 衊範顧夢顧衊繭鑰窪製 (鬱蓋廠觸範築鏇繭夢窪, 15.3) 更多 |
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