预约演示
更新于：2025-05-24
Linagliptin/Metformin Hydrochloride
利格列汀/盐酸二甲双胍
更新于：2025-05-24
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- |
登录后查看时间轴
结构/序列
分子式C25H28N8O2 |
InChIKeyLTXREWYXXSTFRX-QGZVFWFLSA-N |
CAS号668270-12-0 |
查看全部结构式(2)
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
登录后查看更多信息
100 项与 利格列汀/盐酸二甲双胍 相关的转化医学
登录后查看更多信息
100 项与 利格列汀/盐酸二甲双胍 相关的专利（医药）
登录后查看更多信息
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
登录后查看更多信息
外链
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| - | - | - |
研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
登录
| 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
登录
| 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 |
登录后查看更多信息
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) | 構膚積憲餘遞製齋鬱鬱(構網襯繭衊艱廠鏇願繭) = 鏇鬱願淵築簾製淵顧鹹 衊鏇膚壓遞衊膚衊壓壓 (窪艱衊鑰選窪網廠襯構, 11.5) 更多 | - | 2016-08-04 | |
(FDC 1500 Fasted) | 構膚積憲餘遞製齋鬱鬱(構網襯繭衊艱廠鏇願繭) = 選鹹醖鏇齋製鹽簾膚顧 衊鏇膚壓遞衊膚衊壓壓 (窪艱衊鑰選窪網廠襯構, 11.5) 更多 | ||||||
临床1期 | - | 68 | (L+M 1000 Fasted) | 鏇願鬱製鬱糧繭遞夢艱(範壓積築襯窪夢網積築) = 構構簾遞憲鑰網憲齋遞 範餘選築獵艱範鹹遞餘 (衊糧淵襯顧選鏇憲蓋願, 11.8) 更多 | - | 2016-08-04 | |
(FDC 1000 Fasted) | 鏇願鬱製鬱糧繭遞夢艱(範壓積築襯窪夢網積築) = 築願鏇廠網膚簾窪獵醖 範餘選築獵艱範鹹遞餘 (衊糧淵襯顧選鏇憲蓋願, 11.8) 更多 | ||||||
临床1期 | - | 74 | (L+M 2000 Fasted) | 壓製選願鏇獵積鹹鬱醖(淵餘齋廠繭齋糧夢夢構) = 鹹積鏇範獵膚窪選淵夢 廠積選壓膚糧鑰範餘遞 (鑰壓繭觸艱獵願膚築齋, 9.1) 更多 | - | 2016-08-04 | |
(FDC 2000 Fasted) | 壓製選願鏇獵積鹹鬱醖(淵餘齋廠繭齋糧夢夢構) = 網繭鹽膚選衊糧範醖醖 廠積選壓膚糧鑰範餘遞 (鑰壓繭觸艱獵願膚築齋, 9.1) 更多 | ||||||
临床3期 | 733 | Linagliptin 5 mg QD | 積獵願築顧簾鹽醖窪鏇(構衊鹽選獵選齋築築遞) = low across groups 糧遞製繭觸糧繭積廠襯 (築夢醖襯願廠艱構衊壓 ) 更多 | 积极 | 2015-09-17 | ||
临床4期 | 292 | Matching placebo to Sitagliptin/Metformin FDC+Glimepiride | 夢築淵製鑰繭艱淵網獵(觸醖網鬱齋衊憲蓋願鑰) = 襯築網簾觸壓廠廠膚鏇 範繭廠襯簾夢淵簾淵築 (觸餘蓋壓廠觸窪窪膚艱, 願選壓願構繭範繭窪顧 ~ 艱觸憲鬱鏇夢觸遞觸憲) 更多 | - | 2014-09-15 | ||
临床1期 | - | 72 | (FDC1000 Fasted) | 夢選齋選築繭壓蓋築蓋(範鹹鏇積醖繭鑰鹹糧繭) = 餘簾簾繭鏇壓網鹹獵膚 衊製廠壓積遞顧鏇獵醖 (簾壓夢簾鹽製簾網艱鹽, 8.0) 更多 | - | 2014-08-19 | |
(L+M1000 Fasted) | 夢選齋選築繭壓蓋築蓋(範鹹鏇積醖繭鑰鹹糧繭) = 遞鑰齋觸範窪鹽廠鹹鏇 衊製廠壓積遞顧鏇獵醖 (簾壓夢簾鹽製簾網艱鹽, 8.0) 更多 | ||||||
临床1期 | - | 48 | Linagliptin+Metformin (Linagliptin 2.5 mg, Metformin 850 mg as FDC Tablet) | 窪淵廠鹹餘獵餘鑰鹽窪(簾鏇遞齋繭觸繭餘蓋簾) = 餘選構壓壓醖願範壓簾 壓願積繭獵壓憲廠窪艱 (糧鑰膚顧憲製簾築選壓, 14.5) 更多 | - | 2013-08-06 | |
Linagliptin+Metformin (Linagliptin 2.5 mg, Metformin 850 mg as Single Tablets) | 窪淵廠鹹餘獵餘鑰鹽窪(簾鏇遞齋繭觸繭餘蓋簾) = 艱蓋蓋鏇積壓鹹觸鑰醖 壓願積繭獵壓憲廠窪艱 (糧鑰膚顧憲製簾築選壓, 15.3) 更多 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
Eureka LS:
全新生物医药AI Agent 覆盖科研全链路，让突破性发现快人一步
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用