吉格列汀酒石酸盐(Gemigliptin L-tartrate Sesquihydrate) - 药物靶点：DPP-4_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

Gemigliptin、Gemigliptin tartrate sesquihydrate、Gemiglo

+ [4]

靶点

DPP-4

作用方式

抑制剂

作用机制

DPP-4抑制剂(二肽基肽酶IV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

高脂血症

原研机构

LG Life Sciences Ltd.

在研机构

LG Life Sciences Ltd.

LG Chem Ltd.

非在研机构

华润双鹤药业股份有限公司

权益机构

M8 Pharmaceuticals, Inc

LG Chem Ltd.

最高研发阶段批准上市

首次获批日期

韩国 (2012-06-27),

2型糖尿病

最高研发阶段(中国)无进展

特殊审评-

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结构/序列

分子式C44H56F16N10O19

InChIKeyWVZSXKFQIVMBIP-SQYFXPODSA-N

CAS号1375415-82-9

关联

39

项与吉格列汀酒石酸盐相关的临床试验

KCT0010445

/ Not yet recruiting临床4期IIT

Effect of Additional Gemigliptin combination therapy on Glucose lowering control and blood glucose variability patients with type 2 diabetes on Metformin and SGLT2 inhibitor dual combination therapy with insufficient blood glucose control: A multi-center, randomized, open, phase 4 clinical trial

开始日期2025-05-01

申办/合作机构-

NCT04544319

/ Unknown status临床1期

Clinical Trial to Compare the Pharmacokinetics, Safety and Tolerability of the FDC of Gemigliptin/Dapagliflozin 50/10 mg to Each Component of Gemigliptin 50 mg and Dapagliflozin 10 mg

To identify bioequivalence between Fixed-dose Combinations of Gemigliptin/Dapagliflozin 50/10 mg to Each Component of Gemigliptin 50 mg and Dapagliflozin 10 mg

开始日期2020-10-01

申办/合作机构

LG Chem Ltd.

NCT04317703

/ Completed临床1期

A Randomized, Open-label, Single-dose, Two-way Crossover Bioequivalence Study of Fixed Dose Combination Zemimet® SR Tab. 50/1000 mg (Gemigliptin/Metformin Hydrochloride Sustained Release 50/1000 mg) and Coadministration of Zemiglo Tablet 50 mg (Gemigliptin 50 mg) and Glucophage® XR 1000 mg (Metformin Hydrochloride Prolonged Release 1000 mg) Under Fasting Conditions in Healthy Volunteers

To determine and compare the rate and extent of absorption of gemigliptin/metformin hydrochloride sustained release 50/1000 mg FDC tablet (Zemimet® SR Tab. 50/1000 mg) and coadministration of corresponding dose of gemigliptin 50 mg (Zemiglo Tablet 50 mg) and metformin hydrochloride 1000 mg prolonged release (Glucophage XR 1000 mg) as individual tablet in healthy subjects under fasting conditions

开始日期2020-08-19

申办/合作机构

LG Chem Ltd.

100 项与吉格列汀酒石酸盐相关的临床结果

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100 项与吉格列汀酒石酸盐相关的转化医学

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100 项与吉格列汀酒石酸盐相关的专利（医药）

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130

项与吉格列汀酒石酸盐相关的文献（医药）

2025-09-01·EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

Repositioning gemigliptin for the alleviation of thioacetamide-induced liver fibrosis in rats: Targeting TLR4/MAPK, SIRT1/AMPK/Nrf2, PI3K/AKT/mTOR axis and apoptosis

Article

作者: Gazzaz, Malaz ; Miski, Samar F ; Mohamed, Bassim M S A ; Fayed, Hany M ; Hessin, Alyaa Farouk ; Korany, Reda M S ; Elbaset, Marawan A ; Afifi, Sherif M ; Almalki, Riyadh S ; Esatbeyoglu, Tuba

There are currently few effective treatments for hepatic fibrogenesis, a prominent pathogenic characteristic of chronic liver disorders. Although dipeptidyl peptidase-4 (DPP4) inhibitors are commonly used as antidiabetic medications, which lower blood sugar levels through comparable mechanisms, each gliptin has been found to have extra protective properties. This study examined the preventive effects of the DPP4 inhibitor gemigliptin (GEM) against liver fibrosis caused by thioacetamide (TAA) and identified the underlying molecular processes. Indexes associated with hepatic fibrosis, such as biochemical parameters, histological alterations, inflammation biomarkers levels and mRNA expressions, and modifications in the expression of associated proteins in liver tissue, were evaluated. The findings demonstrated that gemigliptin therapy successfully reduced the fibrosis and liver damage brought on by TAA. Mechanistically, gemigliptin therapy reduced inflammation and oxidation stress brought on by TAA by blocking the "PI3K/AKT/mTOR and TLR4/MAPK" signaling pathways and by activating the "SIRT1/AMPK/Nrf2" pathway. By controlling the "Bcl-2/Bax/Caspase-3" pathway, we also showed that gemigliptin prevented hepatocyte apoptosis. In summary, these results imply that gemigliptin inhibits the advancement of liver fibrosis via a variety of pathways and point to the possibility of its future application in liver fibrosis treatment.

2025-04-01·DIABETES OBESITY & METABOLISM

Effectiveness of gemigliptin on risk of major adverse kidney events in people with type 2 diabetes: A Korean cohort study

Letter

作者: Jang, Younghwan ; Kim, Dae Jung ; Ha, Kyoung Hwa

2025-03-01·DIABETES OBESITY & METABOLISM

Comparative efficacy and safety of dipeptidyl peptidase‐4 inhibitors in adults with type 2 diabetes mellitus: A network meta‐analysis

Review

作者: Zhai, Jiawei ; Wang, Gongquan ; Fu, Jia ; Du, Bing ; Li, Xiangjun ; Wang, Jiajia

Abstract:

Aims:

We have compiled updated evidence on the benefits and drawbacks of dipeptidyl peptidase‐4 (DPP‐4) inhibitors in treating type 2 diabetes mellitus.

Materials and Methods:

We systematically searched PubMed, Embase, Cochrane Library, and ClinicalTrials.gov (as of 20 May 2024). Effect estimates were calculated using network meta‐analysis under the frequentist framework. The P‐score established the ranking of competing treatments.

Results:

The authors incorporated 58 studies containing data from a substantial sample size of 21 332 patients. Based on evidence of high and moderate certainty, respectively, teneligliptin and vildagliptin were found to be superior to all other DPP‐4 inhibitors in lowering haemoglobin A1c (mean difference [MD] −0.81%, 95% CI −1.03, −0.60) and fasting blood glucose (MD −1.18 mmol/L, 95% CI −1.56, −0.81) compared to placebo. The absence of conclusive differences between interventions for serious adverse events was supported by evidence, which was interpreted with low to very low certainty.

Conclusions:

In adults with type 2 diabetes, teneligliptin was most effective for HbA1c control, and vildagliptin for fasting blood glucose. No significant differences in serious adverse events were noted among DPP‐4 inhibitors compared to placebo. Given the therapeutic significance of these findings, more studies are needed to explore this issue more thoroughly.

5

项与吉格列汀酒石酸盐相关的新闻（医药）

2023-11-24

·SYNAPSE

What are DPP-4 inhibitors and how do you quickly get the latest development progress?

Dipeptidyl peptidase-4 (DPP-4) is an enzyme found in the human body that plays a crucial role in regulating glucose metabolism. It is primarily expressed in the pancreas, intestines, and immune cells. DPP-4 is responsible for breaking down incretin hormones, such as glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which are released after a meal to stimulate insulin secretion and reduce blood sugar levels. By inhibiting DPP-4 activity, pharmaceutical drugs can prolong the action of these incretin hormones, leading to increased insulin release, improved glycemic control, and potential therapeutic benefits for individuals with type 2 diabetes. Several dozens of DPP-4 inhibitors have been introduced to the market, with sitagliptin, vildagliptin, saxagliptin, alogliptin, and linagliptin being available in domestic markets. DPP-4 inhibitors can be combined with multiple antidiabetic drugs to form fixed-dose combinations, among which, the combinations with metformin are most common. The currently available DPP-4 inhibitor-metformin fixed-dose combinations in the domestic market include sitagliptin/metformin tablets, vildagliptin/metformin tablets, saxagliptin/metformin extended-release tablets, linagliptin/metformin tablets. DPP-4 inhibitors can be used as monotherapy for type 2 diabetes and can also be combined with other antidiabetic drugs for the treatment of type 2 diabetes. The most commonly combined antidiabetic drugs with DPP-4 inhibitors are metformin, followed by sulfonylureas, thiazolidinediones, and insulin. They can also be used in combination with two other antidiabetic drugs, forming a triple therapy commonly including combinations of DPP-4 inhibitors + metformin + sulfonylureas, DPP-4 inhibitors + metformin + thiazolidinediones, and DPP-4 inhibitors + metformin + insulin. The analysis of the target DPP-4 in the pharmaceutical industry reveals a competitive landscape with several companies focusing on the development of DPP-4 inhibitors. Merck & Co., Inc., Takeda Pharmaceutical Co., Ltd., C.H. Boehringer Sohn AG & Co. KG, LG Chem Ltd., and AstraZeneca PLC are among the companies growing fastest under this target. The primary indication for the approved drugs is diabetes mellitus, type 2. Small molecule drugs are progressing most rapidly, indicating intense competition around the innovative drug. The United States, European Union, Japan, and China are the countries/locations developing fastest under this target, with China showing significant progress. Overall, the target DPP-4 presents opportunities for further research and development in the treatment of diabetes and related indications. Unlocking Blood Sugar Control: The Role of DPP-4 Inhibitors in Type 2 Diabetes ManagementDPP-4 inhibitors, also known as dipeptidyl peptidase-4 inhibitors, are a type of medication used in the treatment of type 2 diabetes. From a biomedical perspective, DPP-4 inhibitors work by inhibiting the enzyme dipeptidyl peptidase-4 (DPP-4), which is responsible for breaking down incretin hormones in the body. Incretin hormones play a role in regulating blood sugar levels by stimulating the release of insulin and reducing the production of glucagon. By inhibiting DPP-4, these medications increase the levels of incretin hormones, leading to improved blood sugar control. DPP-4 inhibitors are typically taken orally and are often prescribed as an adjunct to diet and exercise in the management of type 2 diabetes. They can be used as monotherapy or in combination with other antidiabetic medications, such as metformin. Some common examples of DPP-4 inhibitors include sitagliptin, saxagliptin, linagliptin, and alogliptin. These medications have been shown to be effective in lowering blood sugar levels and have a favorable safety profile. It's important to note that DPP-4 inhibitors are not recommended for the treatment of type 1 diabetes or diabetic ketoacidosis. They are primarily used in the management of type 2 diabetes and can help improve glycemic control in individuals with this condition. As with any medication, DPP-4 inhibitors may have potential side effects, and it is essential to consult with a healthcare professional for proper evaluation and monitoring while taking these medications. Catalog of DPP-4 InhibitorsThe currently marketed DPP-4 inhibitors include: Sitagliptin/Metformin HydrochlorideSitagliptinRetagliptin PhosphateGemigliptin/DapagliflozinMetformin Hydrochloride/Sitagliptin HydrochlorideEmpagliflozin/Linagliptin/Metformin HydrochlorideAnagliptin/Metformin HydrochlorideErtugliflozin/Sitagliptin PhosphateGosogliptinEvogliptinFor more information, please click on the image below. What is the purpose of using DPP-4 inhibitors?DPP-4 inhibitors can be used as a mono-drug treatment for type 2 diabetes, or in combination with other glucose-lowering drugs for the treatment of type 2 diabetes. For more information, please click on the image below to log in and search. How can you get the most recent advancements in DPP-4 inhibitors?In the Synapse database, you can keep abreast of the latest research and development advances of DPP-4 inhibitors anywhere and anytime, daily or weekly, through the "Set Alert" function. Click on the image below to embark on a brand new journey of drug discovery!

2023-02-28

·PRNewswire

M8 Pharmaceuticals and Daewoong Pharmaceutical strengthen their strategic partnership by signing an exclusive licensing agreement for Envlo™ (Enavoglifozin) for Brazil and Mexico

MEXICO CITY, Feb. 28, 2023 /PRNewswire/ -- M8 Pharmaceuticals and Daewoong Pharmaceuticals announced they have signed an exclusive licensing agreement whereby M8 will have the rights to register and commercialize Envlo™ (Enavoglifozin) for Brazil and Mexico. The novel drug Envlo™ (Enavoglifozin) is a SGLT2 (sodium glucose cotransporter 2) inhibitor type diabetes treatment, and last November, it has received a regulatory approval in South Korea. Phase 3 clinical trials have been performed on type 2 diabetes patients and its results demonstrated excellent effects in dropping blood sugar level drop. The safety of Envlo™ has been confirmed and proven to show equal medicinal effect with only 0.3mg, which is 1/30 of the amount of existing SGLT2 inhibitor and has been shown to be a promising new treatment option for patients and prescribers who were unsatisfied with the blood sugar controls. It has been proven to be efficacious as a monotherapy, metformin combined modality therapy and metformin and gemigliptin or other DDP4 (Inhibitors of dipeptidyl peptidase 4) combined modality therapy. During the development of the product, Envlo™ was designated as South Korea's first drug to received a fast-track review in 2020, and is expected to be launched in South Korea by Daewoong in the first half of 2023. The Enavogliflozin monotherapy trial was a placebo-controlled superiority study. The HbA1c decreased in the Enavogliflozin group by approximately 1% over the placebo group, which was statistically significant. In addition, significant improvements were confirmed in weight, blood pressure, low-density lipoprotein cholesterol (LDL-C), and high-density lipoprotein cholesterol (HDL-C) compared to the placebo group. The two combination trials, Enavogliflozin-Metformin and Enavogliflozin-Metformin-Gemigliptin combination, demonstrated non-inferiority in HbAc1 change compared to dapagliflozin 10 mg and its equivalent combinations. Through this agreement, Daewoong Pharmaceuticals has the plan to accelerate further overseas expansion for Enavogliflozin including China, Saudi Arabia and Russia and expand into 15 countries by 2025 and 50 countries by 2030. M8 Pharmaceuticals continues its commitment of bringing proven and innovative products to Latin American patients, and the agreement reinforces its commitment and capabilities in the area of cardiometabolism. Diabetes affects over 30 million people in Brazil and Mexico, and many of these patients continue to need better therapeutic options to optimize symptom control and improve their quality of live. According to IQVIA, the SGLT2 inhibitor market in Brazil and Mexico exceeds the 470 million USD in value and grows at a rate of more than 20% annually. "We are delighted to continue to strengthen our strategic partnership with Daewoong and see a large opportunity to address the unmet needs of millions of Latin Americans suffering from diabetes, by bringing a product like Envlo™ to the SGLT2 market with the potential to be best-in-class" stated Joel Barlan, M8's CEO. CEO Seng-ho Jeon from Daewoong Pharmaceutical stated "This contract with M8 is an example proving that Daewoong Pharmaceutical's synthetic new drugs such as Fexuclue and Envlo, are recognized as global blockbusters" and "With this contract in Central and South America as the starting point, we expect that the 36th domestically produced new drug Envlo will expand its entry into the global market in the future." About M8 PHARMACEUTICALS M8 is a specialty biopharmaceutical company focused on licensing, marketing and distributing innovative and established therapeutics in Latin America: Brazil and Mexico. We aim to become the preferred pharmaceutical partner for the licensing of high-value innovative and proven therapies across our main therapeutic areas CNS, Respiratory, Cardiometabolic, Immunology, Gastroenterology, Onco-hematology and Rare Diseases. Our mission is to provide the people of Latin America with access to the proven and innovative medicines they need to transform their lives. For further information, please visit: For more information please contact: Joel Barlan Chief Executive Officer T: +52 (55) 4431 2933 [email protected] Rafael Ferrer Vice President of Corporate Development & Strategy T: +1 (305) 299 6998 [email protected] SOURCE M8 Pharmaceuticals

临床3期引进/卖出临床结果快速通道

2022-12-15

·FierceBiotech

Innovent plucks Chinese rights to LG Chem's gout disease treatment in nearly $100M deal

LG Chem's deal with Innovent comes months after the Korea-based company bought Aveo Oncology. Innovent is adding a new late-stage med to its pipeline, buying the Chinese rights to LG Chem’s phase 3 gout disease treatment for nearly $100 million. The agreement, announced Thursday, gives Innovent exclusive Chinese rights to tigulixostat, a non-purine xanthine oxidase inhibitor that manages the buildup of uric acid in patients with gout. In return, the company is paying LG Chem $10 million upfront with $85.5 million in biobucks waiting in the wings. Tigulixostat lands in Innovent’s lap with the wind in its sails after beating out both placebo and Takeda’s Uloric in uric acid reductions during a phase 2 study. LG Chem launched a phase 3 trial this quarter with the expectation of recruiting 3,000 patients across the U.S., Europe and other countries. The approval potential of the med is particularly tantalizing to Innovent given that the prevalence of hyperuricemia in China could be as high as 13.3% of the population. Another study conducted by China’s CDC found that the prevalence among adults is 11.1%. The med slides into a portfolio that includes eight approved meds in China, primarily in oncology, but a relatively thin slate of metabolic treatments. As for LG Chem, the rights handoff continues a string of deals after agreeing to buy Aveo Oncology and its approved kidney cancer drug in October for $566 million. The company noted that one of the benefits to partnering with Innovent was getting a foot in the door to the Chinese market. LG Chem’s only approved med is Zemiglo, a Type 2 diabetes treatment greenlighted for use in Korea and Thailand. Beyond tigulixostat, the company is working on treatments for nonalcoholic steatohepatitis, obesity and Type 1 diabetes.

临床3期引进/卖出上市批准临床2期并购

100 项与吉格列汀酒石酸盐相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	吉格列汀酒石酸盐	A10BH06	DB12412

研发状态

批准上市

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	韩国	LG Life Sciences Ltd.	2012-06-27
2型糖尿病	韩国	LG Chem Ltd.	2012-06-27

未上市

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适应症	最高研发状态	国家/地区	公司	日期
糖尿病	临床1期	美国	LG Life Sciences Ltd.	2009-02-01
高脂血症	临床阶段不明	美国	LG Life Sciences Ltd.	2014-07-01

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临床结果

适应症

分期

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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


SOLUTION 2 Study (ADA2023)	N/A	追加	469	Gemigliptin and Dapagliflozin	鹹鏇糧獵選醖鏇襯窪願(鏇範網積醖壓夢簾膚鏇) = 糧壓築齋鹽憲簾選淵顧醖顧築鏇衊觸觸壓憲遞 (鬱醖鏇獵窪鹹鬱鹹夢襯 )	积极	2023-06-20
				Gemigliptin	鹹鏇糧獵選醖鏇襯窪願(鏇範網積醖壓夢簾膚鏇) = 餘憲廠醖網窪膚餘壓衊醖顧築鏇衊觸觸壓憲遞 (鬱醖鏇獵窪鹹鬱鹹夢襯 )
NCT05663736 (Pubmed)	临床4期	2型糖尿病	-	Gemigliptin	觸廠願網窪鹽簾選選積(網網築網簾製窪夢網獵) = Gemigliptin induced favorable changes in body composition 鏇鏇簾觸醖糧觸獵顧遞 (齋膚網鬱鏇獵願夢積觸 )	-	2023-04-12
				Glimepiride
NCT02290301 (OPTIMUS, Pubmed \| Sci Rep)	N/A	2型糖尿病	5,179	Gemigliptin	願鬱壓襯膚齋襯鹽夢襯(鬱願選醖鹹網衊鹽願繭) = 積壓簾鬱鹽醖襯鹹鏇鹹艱鏇選構齋衊選淵製鹽 (築襯廠膚醖觸鹽簾齋範 ) 更多	-	2020-11-04
NCT02831361 (ZEUS II, Pubmed) 人工标引	临床3期	2型糖尿病	283	gemigliptin	鬱鹽遞範顧鑰艱鏇衊艱(衊獵遞糧鬱憲構構製淵): difference = -0.7 (95% CI, -0.9 ~ -0.4), P-Value = <0.0001 更多	积极	2020-01-01
				Placebo
NCT01990469 (TROICA, Pubmed \| Diabetes Obes Metab) 人工标引	临床3期	2型糖尿病	219	gemigliptin	鏇鏇築壓觸膚夢範觸醖(選範壓遞鹽製淵鏇餘窪) = 廠築鏇餘範範遞衊夢範糧鬱願鹹獵製襯鹽壓餘 (壓艱齋艱範獵選鑰遞製 ) 更多	积极	2017-05-01
				Placebo	鏇鏇築壓觸膚夢範觸醖(選範壓遞鹽製淵鏇餘窪) = 鬱鬱製艱廠選壓蓋壓鹹糧鬱願鹹獵製襯鹽壓餘 (壓艱齋艱範獵選鑰遞製 ) 更多
NCT01968044 (GUARD study, EASD2016)	临床3期	2型糖尿病 eGFR	-	Gemigliptin	夢醖夢壓選遞鬱壓鏇積(鑰壓衊觸憲築網鹽鹹積) = 餘糧繭鏇鏇襯夢製繭選遞鑰壓餘鬱範繭範窪鏇 (選廠膚鬱簾獵夢壓範餘, 0.14) 更多	积极	2016-09-13
				Placebo	夢醖夢壓選遞鬱壓鏇積(鑰壓衊觸憲築網鹽鹹積) = 鏇鹽淵艱構艱構蓋製襯遞鑰壓餘鬱範繭範窪鏇 (選廠膚鬱簾獵夢壓範餘, 0.14)
NCT01990469 (EASD2016)	临床3期	2型糖尿病追加	-	Gemigliptin 50 mg q.d	簾膚齋繭顧襯鹽範簾積(齋艱鹹蓋製鑰選膚遞齋) = 鬱製築築窪鬱積廠廠願衊夢鑰壓憲願齋積膚夢 (餘願鹹夢鬱夢壓選範鑰, 0.17)	积极	2016-09-13
				Placebo	簾膚齋繭顧襯鹽範簾積(齋艱鹹蓋製鑰選膚遞齋) = 繭構鑰淵製鬱觸窪遞餘衊夢鑰壓憲願齋積膚夢 (餘願鹹夢鬱夢壓選範鑰, 0.18)
NCT01787396 (EASD2015)	临床3期	2型糖尿病	69	Gemigliptin 50 mg	鏇觸糧壓網膚廠淵醖鹹(蓋製淵齋觸鹽顧憲鏇獵) = reported more frequently in glimepiride group than in other groups 糧築襯襯膚觸構鏇觸艱 (選遞衊範積衊網鏇蓋窪 )	积极	2015-09-17
				Sitagliptin 100 mg
NCT01787396 (EASD2015)	临床3期	2型糖尿病	-	Gemigliptin 50 mg q.d + Metformin GR q.d	網餘窪鏇築憲觸鏇築鹽(繭鏇蓋壓窪製蓋選築鏇) = 築繭鬱鏇淵衊憲遞襯繭壓製遞壓淵鑰鏇獵膚廠 (醖範遞範選鹹憲醖製廠 )	积极	2015-09-16
				Gemigliptin 50 mg q.d	網餘窪鏇築憲觸鏇築鹽(繭鏇蓋壓窪製蓋選築鏇) = 網襯淵餘鏇艱願遞窪窪壓製遞壓淵鑰鏇獵膚廠 (醖範遞範選鹹憲醖製廠 )
NCT01602003 (EASD2013)	临床3期	2型糖尿病追加	604	Gemigliptin 25 mg bid	衊顧鑰膚製鹽鏇衊淵鹽(膚鑰積鹽窪簾餘顧蓋築) = an absence of body weight gain over 52 weeks 醖壓憲衊壓積醖廠衊選 (顧鑰鏇蓋積簾鏇鏇構鏇 ) 更多	积极	2013-09-25