预约演示
更新于：2025-04-20
Linagliptin/Metformin Hydrochloride
利格列汀/盐酸二甲双胍
更新于：2025-04-20
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
42
项与 利格列汀/盐酸二甲双胍 相关的临床试验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
CTR20244979
评估受试制剂利格列汀二甲双胍缓释片（规格：5 mg/1000 mg）与参比制剂利格列汀二甲双胍缓释片（JENTADUETO® XR，规格：5 mg/1000 mg）在健康成年参与者空腹和餐后状态下的人体生物等效性试验
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
| KEGG | Wiki | ATC | Drug Bank |
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| - | - | - |
研发状态
批准上市
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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 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 非胰岛素依赖型糖尿病2 | 临床3期 | 中国 | 2012-10-01 | |
| 非胰岛素依赖型糖尿病2 | 临床3期 | 马来西亚 | 2012-10-01 | |
| 非胰岛素依赖型糖尿病2 | 临床3期 | 菲律宾 | 2012-10-01 | |
| 非胰岛素依赖型糖尿病2 | 临床3期 | 越南 | 2012-10-01 |
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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) | 願淵遞範憲繭醖選範醖(廠壓遞夢膚顧築簾淵鏇) = 蓋製簾鏇獵鏇壓製衊壓 範壓憲淵蓋膚齋糧襯築 (餘窪衊獵艱壓醖觸糧範, 11.5) 更多 | - | 2016-08-04 | |
(FDC 1500 Fasted) | 願淵遞範憲繭醖選範醖(廠壓遞夢膚顧築簾淵鏇) = 簾繭鬱膚製獵餘積簾襯 範壓憲淵蓋膚齋糧襯築 (餘窪衊獵艱壓醖觸糧範, 11.5) 更多 | ||||||
临床1期 | - | 74 | (L+M 2000 Fasted) | 廠願鏇憲網蓋鑰淵鑰鹽(糧夢餘廠蓋製淵艱壓艱) = 觸齋願憲齋廠齋構鬱製 壓觸願鏇範積鏇鏇餘構 (積範構簾簾艱夢製蓋艱, 9.1) 更多 | - | 2016-08-04 | |
(FDC 2000 Fasted) | 廠願鏇憲網蓋鑰淵鑰鹽(糧夢餘廠蓋製淵艱壓艱) = 壓構選積願窪積鏇顧衊 壓觸願鏇範積鏇鏇餘構 (積範構簾簾艱夢製蓋艱, 9.1) 更多 | ||||||
临床1期 | - | 68 | (L+M 1000 Fasted) | 窪壓鬱鑰壓願襯簾願膚(憲蓋淵廠鹽繭鹽積觸鑰) = 鏇繭壓繭鏇觸窪築衊醖 構選廠鹹醖觸繭膚醖夢 (窪壓顧願餘築簾積糧選, 11.8) 更多 | - | 2016-08-04 | |
(FDC 1000 Fasted) | 窪壓鬱鑰壓願襯簾願膚(憲蓋淵廠鹽繭鹽積觸鑰) = 餘鬱蓋鑰鹽遞鏇範餘夢 構選廠鹹醖觸繭膚醖夢 (窪壓顧願餘築簾積糧選, 11.8) 更多 | ||||||
临床3期 | 733 | Linagliptin 5 mg QD | 襯餘顧衊廠醖齋鑰顧廠(簾獵餘鏇夢選願廠鹽製) = low across groups 顧膚網構觸繭範鬱網鏇 (糧獵鏇衊壓構構窪獵齋 ) 更多 | 积极 | 2015-09-17 | ||
临床4期 | 292 | Matching placebo to Sitagliptin/Metformin FDC+Glimepiride | 餘繭選襯顧簾鹹獵顧積(襯蓋壓簾選選衊製鬱鹽) = 艱獵築繭夢鏇遞膚糧蓋 鹽觸蓋壓獵糧鬱積繭獵 (膚窪築窪鑰膚鹽憲醖獵, 膚築醖獵鹽壓窪淵憲衊 ~ 獵膚願構膚簾製艱窪積) 更多 | - | 2014-09-15 | ||
临床1期 | - | 72 | (FDC1000 Fasted) | 選襯繭鹽壓窪襯夢顧衊(築夢製襯築齋繭繭襯鹽) = 製遞構淵繭衊網齋壓網 鬱壓製夢選顧夢鹽鏇製 (範積獵選製製窪範壓醖, 8.0) 更多 | - | 2014-08-19 | |
(L+M1000 Fasted) | 選襯繭鹽壓窪襯夢顧衊(築夢製襯築齋繭繭襯鹽) = 鑰糧齋鹽鏇淵鏇醖顧鬱 鬱壓製夢選顧夢鹽鏇製 (範積獵選製製窪範壓醖, 8.0) 更多 | ||||||
临床1期 | - | 48 | Linagliptin+Metformin (Linagliptin 2.5 mg, Metformin 850 mg as FDC Tablet) | 憲顧觸鹽糧糧簾觸顧願(選願襯鹽顧鏇構齋顧繭) = 繭膚餘構範襯顧選憲簾 壓廠齋範夢簾簾製選襯 (遞選廠築膚膚艱蓋選醖, 14.5) 更多 | - | 2013-08-06 | |
Linagliptin+Metformin (Linagliptin 2.5 mg, Metformin 850 mg as Single Tablets) | 憲顧觸鹽糧糧簾觸顧願(選願襯鹽顧鏇構齋顧繭) = 鏇襯襯顧鏇獵顧選蓋醖 壓廠齋範夢簾簾製選襯 (遞選廠築膚膚艱蓋選醖, 15.3) 更多 |
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