恩格列净/利格列汀/二甲双胍(Empagliflozin/Linagliptin/Metformin Hydrochloride) - 药物靶点：DPP-4 x PRKAB1 x SGLT2_在研适应症：2型糖尿病_专利_临床

概要

基本信息

药物类型

小分子化药

别名

EmpaLinaMet XR、Empagliflozin/Linagliptin/Metformin、Empagliflozin/metformin/linagliptin

+ [5]

靶点

DPP-4 x PRKAB1 x SGLT2

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)、SGLT2抑制剂(钠-葡萄糖协同转运蛋白-2抑制剂)

治疗领域

内分泌与代谢疾病

在研适应症

2型糖尿病

非在研适应症-

原研机构

Boehringer Ingelheim GmbH

在研机构

Boehringer Ingelheim Pharmaceuticals, Inc.

非在研机构

Boehringer Ingelheim GmbH

最高研发阶段批准上市

首次获批日期

美国 (2020-01-27),

2型糖尿病

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C23H27ClO7

InChIKeyOBWASQILIWPZMG-QZMOQZSNSA-N

CAS号864070-44-0

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关联

3

项与恩格列净/利格列汀/二甲双胍相关的临床试验

NCT03629054

/ Completed临床1期

Bioequivalence of a Low Strength Fixed Dose Combination Tablet of Empagliflozin/Linagliptin/Metformin Extended Release Compared to the Free Combination of Empagliflozin, Linagliptin, and Metformin Extended Release Tablets Following Oral Administration in Healthy Male and Female Subjects (an Open-label, Randomised, Single-dose, Two-period, Two-sequence Crossover Study)

The primary objective of this trial is to establish the bioequivalence of two empagliflozin/linagliptin/metformin extended release (XR) fixed dose combination (FDC) tablets (Test, T) compared with the same doses of the individual components given in separate tablets (Reference, R) when administered together after a high-fat, high-calorie meal.
The assessment of safety and tolerability will be the secondary objective of this trial.

开始日期2018-08-27

申办/合作机构

Boehringer Ingelheim GmbH

[+1]

NCT03259490

/ Completed临床1期

Bioequivalence of a Fixed Dose Combination Tablet of Empagliflozin/Linagliptin/Metformin Extended Release Compared to the Free Combination of Empagliflozin, Linagliptin, and Metformin Extended Release Tablets Following Oral Administration in Healthy Male and Female Subjects (an Open-label, Randomised, Single-dose, Two-period, Two-sequence Crossover Study)

To establish the bioequivalence of one fixed dose combination (FDC) tablet of empagliflozin/linagliptin/metformin extended release (XR) versus the free combination of empagliflozin tablet, linagliptin tablet, and metformin XR tablets administered as a single dose under fed conditions

开始日期2017-08-31

申办/合作机构

Boehringer Ingelheim GmbH

[+1]

NCT02821910

/ Completed临床1期

Relative Bioavailability of Two FDC Tablet Strengths of Empagliflozin/Linagliptin/Metformin Extended Release Compared to the Free Combination of Empagliflozin, Linagliptin and Metformin Extended Release Following Oral Administration in Healthy Male and Female Subjects (an Open-label, Randomised, Single-dose, Two-period, Two-sequence Crossover Study)

The purpose of this trial is to demonstrate the relative bioavailability of 2 newly developed fixed dose combinations (FDC) tablets containing empagliflozin, linagliptin & metformin extended release (XR) and the single tablets of empagliflozin, linagliptin and metformin XR administered simultaneously.

开始日期2016-07-20

申办/合作机构

Boehringer Ingelheim GmbH

[+1]

100 项与恩格列净/利格列汀/二甲双胍相关的临床结果

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100 项与恩格列净/利格列汀/二甲双胍相关的转化医学

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100 项与恩格列净/利格列汀/二甲双胍相关的专利（医药）

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2

项与恩格列净/利格列汀/二甲双胍相关的文献（医药）

2023-03-15·BMC chemistry

HPLC-DAD technique for the quantification of a recently approved anti-diabetic triple combination along with two toxic official impurities: Toxicity confirmation aided by molecular docking application.

Article

作者: Eissa, Maya S. ; Bahgat, Eman A. ; Hashem, Hisham ; Kamel, Ebraam B. ; Saleh, Hanaa

BACKGROUNDGliflozins and gliptins are two distinct groups of pharmacological drugs that reduce blood glucose levels in individuals with type II diabetes in various ways that may perform their functions harmoniously. Trijardy^® tablet, which contains empagliflozin, linagliptin, and metformin, was recently approved. The scientific database does not yet have a method that is sensitive enough to quantify the aforementioned medications in the presence of metformin official toxic impurities melamine and cyanoguanidine. Molecular docking modeling was utilized in this work to further prove the toxicity of melamine.METHODSThe five analytes listed before were quantified using RP-HPLC-diode array detector and a Zorbax^® C8 column (4.6 × 250 mm, 5 μm) with isocratic mobile phase composed of acetonitrile and 0.05 M potassium dihydrogen phosphate buffer, which had been treated by ?-phosphoric acid to restore a pH of 4.0 (90:10, v/v) at a flow rate of 1.2 mL/min and the eluted peaks were scanned at 250 nm.CONCLUSIONThe utilization of the simplest isocratic elution mode give the current technique a significant time-and cost-saving benefit. The current method can quantify the triple therapy agents in the presence of each other as well as with two official toxic impurities of metformin in one short analytical run.

2020-06-01·The Medical letter on drugs and therapeutics4区 · 医学

In brief: Trijardy XR - a new 3-drug combination for Type 2 diabetes.

4区 · 医学

Article

1

项与恩格列净/利格列汀/二甲双胍相关的新闻（医药）

2022-08-30

·药时代

最强DPP-4、SGLT-2和二甲双胍将联合组成复方制剂

DPP-4和SGLT-2作为糖尿病口服药最热门的两个靶点，分别由默沙东的西格列汀(商品名为：Januvia/捷诺维)和勃林格殷格翰的恩格列净(商品名为：Jardiance/欧唐静)独占鳌头，两款产品在2021年分别为两家公司带来了33.24亿美元和61.4亿美元收入，远超同类竞争者。最强DPP-4抑制剂和SGLT-2抑制剂和经典糖尿病药物二甲双胍有望组成新的复方制剂。当然，实现该组合的并非两家竞争者，毕竟默沙东（西格列汀和艾托格列净）和勃林格殷格翰（利格列汀和恩格列净）都具有自己独立开发的DPP-4抑制剂和SGLT-2抑制剂，不会轻易和对方联合。近日，国家药品监督管理局颁发《药物临床试验批准通知书》，同意越洋医药开展临床试验，研究证明恩格列净西格列汀二甲双胍缓释片的临床优势，三个活性成分具有各自的降糖作用、机制互补。根据越洋医药发布的公告显示：恩格列净西格列汀二甲双胍缓释片是越洋医药研发的改良型新药，拟用于2型糖尿病的治疗。越洋医药已对活性成分的释放行为进行调控，以利更好地控制患者血糖水平。此外，每日服用一次，减少患者服药次数，从而提高患者服药的依从性。越洋医药拥有此产品的自主知识产权。此改良型新药的研发始于2020年，其临床试验申请于2022年6月15日被国家药监局正式受理。由于化药复方制剂的特殊性，相关的新药临床试验技术指导原则尚未颁发。越洋医药于8月19日获得临床批件一事显示：在获得批准进行三方缓控释改良型新药临床试验方面，越洋医药为国内首家，也属于国际首创新药。在含有DPP-4抑制剂和SGLT-2抑制剂复方糖尿病开发方面，默沙东的西格列汀/艾托格列净片（商品名为：Steglujan），勃林格殷格翰的恩格列净/利格列汀/盐酸二甲双胍缓释片（商品名为：Trijardy XR）、恩格列净利格列汀片（商品名为：Glyxambi），另一家竞争者阿斯利康的达格列净/沙格列汀片（商品名为：Qtern），已在美国或/和欧盟等地区获批上市。值得一提的是，阿斯利康的达格列净/盐酸二甲双胍/盐酸沙格列汀缓释片（商品名为：Qternmet XR）在美国获批上市后现已撤市。我国糖尿病患者人数已超过1.4亿，复方降糖药正在成为重要治疗手段。越洋医药开发的恩格列净西格列汀二甲双胍缓释片理论上是最强DPP-4、SGLT-2和二甲双胍的组合，将会给临床提供一种“更为理想”的选择。封面图来源：123rf版权声明/免责声明本文为授权转载文章，版权归拥有者。仅供感兴趣的个人谨慎参考，非商用，非医用、非投资用。欢迎朋友们批评指正！衷心感谢！文中图片、视频为授权正版作品，或来自微信公共图片库，或取自公司官网/网络根据CC0协议使用，版权归拥有者。任何问题，请与我们联系（电话：13651980212。微信：27674131。邮箱：contact@drugtimes.cn）。衷心感谢！推荐阅读新一代全球「最畅销」小分子药之争，暂时没结果，因为两个药的试验全失败了...从任正非的“寒气论”和《华为的冬天》想到中国药企出海。晶泰、药明生物、恒瑞、信达荣登福布斯榜单！。。。| 药时代出海系列庄辉院士 | 新疾病谱召唤新药共赴临床“肝”需「孤注一掷」的头对头试验，国产新药拿什么赌明天？研究了半个世纪，终于成功了！辉瑞又抢先一步，即将登陆「百亿美元」大市场优时比就左乙拉西坦注射用浓溶液暂停进口进行回应眼内给药迎来新格局｜脉络膜上腔微注射开启糖尿病性黄斑水肿治疗新时代谢雨礼博士 | 药物创新：more is different罗氏旗下基因泰克首次从中国创新药企获得潜在药物全球开发及商业化权益海阔凭药去，大道创新行! 2022第三届中国新药CMC高峰论坛与您再约上海！（第一轮通知）半年营收超10亿，复宏汉霖半年报业绩亮眼，彰显Biopharma实力点击这里，报名参加第三届中国新药CMC高峰论坛！

小分子药物

100 项与恩格列净/利格列汀/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

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
2型糖尿病	美国	Boehringer Ingelheim Pharmaceuticals, Inc.	2020-01-27

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT03629054 (CTgov)	临床1期	-	30	Empagliflozin, Metformin HCl, Linagliptin (fixed dose combination) (Test Treatment (T))	鹹壓淵鹽淵鬱鑰簾觸繭(構壓艱窪選獵構憲築衊) = 積夢襯簾遞鬱夢構範遞鹹廠淵蓋築衊糧壓艱獵 (範憲願壓窪齋獵顧鬱簾, 鑰簾積簾艱醖顧積鬱夢 ~ 艱壓鬱獵觸鹹淵遞遞衊) 更多	-	2020-02-21
				Linagliptin+Metformin HCl+Empagliflozin (Reference Treatment (R))	鹹壓淵鹽淵鬱鑰簾觸繭(構壓艱窪選獵構憲築衊) = 顧餘衊廠蓋壓構鬱繭餘鹹廠淵蓋築衊糧壓艱獵 (範憲願壓窪齋獵顧鬱簾, 艱鹽簾膚鬱積製觸艱壓 ~ 餘積製淵築鬱鏇齋廠繭) 更多