Food-effect Bioavailability of Gemigliptin and Dapagliflozin 50/10 mg Fixed Dose Combination Film-coated Tablet Under Fed and Fasting Conditions in Healthy Volunteers

A Randomized, Open-label, Single-dose, Two-way Crossover Study to Investigate Food-effect Bioavailability of Gemigliptin and Dapagliflozin 50/10 mg Fixed Dose Combination Film-coated Tablet under Fed and Fasting Conditions in Healthy Volunteers

开始日期2022-01-01

申办/合作机构

LG Chem Ltd.

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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项与吉格列汀酒石酸盐相关的文献（医药）

2024-07-01·Biochemistry and Biophysics Reports

Gemigliptin, a potent selective dipeptidyl peptidase 4 inhibitor, protects endothelial progenitor cells by oxidative stress via caspase-3 dependent pathway

Article

作者: Tariq, Amna Rashid ; Lee, Mijung ; Kim, Manho

Endothelial progenitor cells (EPCs) are exclusive players in vasculogenesis and endothelial regeneration. EPCs are of two types and their differentiation is mediated by different growth factors. A decrease in EPC number and function causes cardiovascular abnormalities and reduced angiogenesis. Various studies has documented a role of EPCs in diabetes. EPCs treatment with different drugs improve insulin secretion but causes other abnormalities. In vivo and in vitro studies have reported anti glycation effect of gemigliptin but no data is available on in vitro effect of gemigliptin on EPC number and functional credibility. The current study was aimed to find an in vitro effect of gemigliptin on EPC number and function along with an effective treatment dose of gemigliptin. EPCs were isolated, cultured and phenotypically characterized using Dil- AcLDL and ulex-lectin fluorescence staining. EPCs were then treated with different doses of Zemiglo and their viability analyzed with viability assay using water-soluble tetrazolium salt (WST-1), by Annexin V and Propidium Iodide (PI) staining, senescence-associated beta-galactosidase (SA-β-gal) staining, western blot and Flow cytometric analysis of apoptotic signals. The results demonstrated that the isolated EPCs has typical endothelial phenotypes. And these EPCs were of two types based on morphology i.e., early and late EPCs. Gemigliptin dose dependently improved the EPCs morphology and increased EPCs viability, the most effective dose being the 20 μM. Gemigliptin at 10 μM, 20 μM and 50 μM significantly increased the BCL-2 levels and at 20 μM significantly decreased the Caspase-3 levels in EPCs. In conclusion, gemigliptin dose dependently effects the EPCs viability and morphology through Caspase-3 signaling. Our results are the first report of gemigliptin effect on EPC viability and morphology.

2024-04-01·Heliyon

Improvement effect of gemigliptin on salivary gland dysfunction in exogenous methylglyoxal-injected rats

Article

作者: Kim, Junghyun ; Yu, Hwa Young ; Park, Su-Bin ; Jung, Woo Kwon

The symptom of hyposalivation associated with hypofunction of the salivary glands is a common feature of diabetes. Inadequate saliva production can cause tissue damage in the mouth, making it susceptible to infections and leading to oral health diseases. Previous studies have highlighted the harmful effects of methylglyoxal (MGO) and MGO-derived advanced glycation end products (AGEs) in diabetes. In this study, we investigated the protective effects of gemigliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor, against MGO-induced salivary gland dysfunction. MGO treatment of immortalized human salivary gland acinar cells induced apoptosis via reactive oxygen species (ROS)-mediated pathways, but this effect was mitigated by gemigliptin. In vivo experiments involved the simultaneous administration of MGO (17.25 mg/kg) with aminoguanidine (100 mg/kg) and gemigliptin (10 and 100 mg/kg) daily to rats for two weeks. Gemigliptin increased the saliva volume and amylase levels in MGO-injected rats. Gemigliptin reduced the DPP-4 activity in both the salivary glands and serum of MGO-injected rats. Furthermore, gemigliptin exerted anti-glycation effects by reducing the accumulation of AGEs in the saliva, salivary glands, and serum and suppressing the expression of the receptor for AGEs. These actions protected the salivary gland cells from ROS-mediated apoptosis. Overall, gemigliptin protected the salivary gland cells from ROS-mediated cell death, reduced the accumulation of amylase and mucins in the salivary glands, and enhanced the salivary function by upregulating aquaporin 5 expression, and it exerted protective effects against MGO-induced salivary gland dysfunction by enhancing the anti-glycation, antioxidant, and salivary secretion activities. Our findings suggest gemigliptin as a potential therapeutic for patients with salivary gland dysfunction caused by the complications of diabetes.

2024-01-05·Journal of Diabetes Research

A Multicenter, Randomized, Open-Label Study to Compare the Effects of Gemigliptin Add-on or Escalation of Metformin Dose on Glycemic Control and Safety in Patients with Inadequately Controlled Type 2 Diabetes Mellitus Treated with Metformin and SGLT-2 Inhibitors (SO GOOD Study)

Article

作者: Noh, Jung Hyun ; Ko, Seung-Hyun ; Choi, Sung Hee ; Moon, Min Kyong ; Rhee, Eun-Jung ; Kim, Hae Jin ; Hur, Kyu Yeon ; Jeong, In-Kyung

Background. We aimed to compare efficacy and safety between gemigliptin add-on and escalation of the metformin dose in patients with inadequately controlled type 2 diabetes mellitus (T2DM) despite treatment with metformin and SGLT2 inhibitors. Methods. This study was a multicenter, randomized, open-label, active-controlled, parallel-group comparative study. Patients with T2DM uncontrolled on metformin and SGLT2 inhibitors were randomized to receive gemigliptin 50 mg as an add-on (GEM group,

n = 37

) or escalation of the metformin dose (500 mg, MET group,

n = 38

) for 24 weeks. The primary endpoint was the change in glycosylated hemoglobin (HbA1c) from baseline to week 24. Results. At weeks 12 and 24, the reduction in HbA1c levels was significantly greater in the GEM group than in the MET group (GEM vs.

MET = - 0.64 % \pm 0.34 %

vs.

- 0.36 % \pm 0.50 %

p = 0.009

at week 12;

- 0.61 % \pm 0.35 %

vs.

- 0.33 % \pm 0.70 %

p = 0.045

at week 24). The proportions of patients who achieved target HbA1c levels of <7.0% at weeks 12 and 24 and <6.5% at week 12 were greater in the GEM group than in the MET group. An index of β-cell function was also significantly improved in the GEM group. The safety profiles were similar between the two groups. Conclusions. Gemigliptin add-on therapy may be more effective than metformin dose escalation in patients with T2DM insufficiently controlled using metformin and SGLT2 inhibitors, without safety concerns. This trial is registered with CRIS_number: KCT0003520.

项与吉格列汀酒石酸盐相关的新闻（医药）

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

2022-12-06

·BioSpace

Daewoong Pharmaceutical announces success in developing a new antidiabetic medication and its aims to enter the market in over 50 countries by 2030

Delivers new drug for two consecutive years by obtaining product license on "Envlo", Korea's 36th new drug from the Ministry of Food and Drug Safety Plans to enter the type 2 diabetes global market worth $71.4 billion Provides new and broad treatment options for patients with insufficient blood glucose control with three indications SEOUL, South Korea, Dec. 6, 2022 /PRNewswire/ -- Daewoong Pharmaceutical Co., Ltd. (CEO Jeon Sengho, Lee Changjae), a global healthcare company, announced on 5th that its "Envlo 0.3mg", a new sodium-glucose cotransporters 2 inhibitor (SGLT2) developed to treat type 2 diabetes mellitus obtained a product license from the Ministry of Food and Drug Safety on November 30. Envlo is indicated for monotherapy, combination therapy with Metformin and combination therapy with Metformin and Gemigliptin. SGLT2 inhibitors, which are rapidly replacing the global type 2 diabetes market worth $71.4 billion, are known to account for about $20.7 billion globally and $100 million in Korea as of 2021. Until now, the development and approval of SGLT2 inhibitors have been carried out mainly by multinational pharmaceutical companies. Daewoong Pharmaceutical, South Korea's leading healthcare company, became the first domestically to succeed in developing a new antidiabetic drug in this class by obtaining a product license. Daewoong Pharmaceutical plans to actively pursue the global market through this product. Daewoong Pharmaceutical plans to move quickly with the procedures concerning Envlo's insurance coverage and price in order to register the drug in National Health Insurance System with an indication of monotherapy, combination therapy with Metformin or Metformin & Gemigliptin in the first half of 2023. At the same time, the company has developed a roadmap to enter the global market over 10 countries including China, Brazil and Saudi Arabia by 2025 and 50 countries by 2030. The company is also running clinical trials for indication expansion while developing combination drugs. Daewoong Pharmaceutical aims to deliver the metformin combination drug in the second half of 2023, by accelerating the trial. The company estimates to achieve a cumulative three-year sale of 100 billion Korean Won. Earlier in October, Daewoong Pharmaceutical announced the Phase 3 study results of Envlo in patients with type 2 diabetes which have shown excellent hypoglycemic effect and the safety. In particular, Envlo has demonstrated its equivalent efficacy with 0.3 mg, which is less than one-thirtieth dosage of existing SGLT2 inhibitors. Its indication is also expected to provide a new treatment option for patients with insufficient blood sugar control. An official from Daewoong Pharmaceutical said, "While SGLT2 inhibitors are drawing the most attention in the global market, it is meaningful that we are the first company in Korea to develop the new diabetes medication in this class." The company official also added, "We will make our best effort to improve the quality of life of patients by providing the best-in-class antidiabetic drug. We will also contribute to the development of global pharmaceutical industry by continuously strengthening new drug development and global business through open collaboration with various partners." Meanwhile, Envlo, approved as the 36th new drug in Korea following the 34th new drug "Fexuclue" last year, listed its name as a first domestic drug to be designated for an accelerated approval by the Ministry of Food and Drug Safety in 2020. Company Codes: Korea:069620

临床3期上市批准临床结果

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

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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

未上市

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
2型糖尿病	药物发现	中国	华润双鹤药业股份有限公司	2019-06-23
非胰岛素依赖型糖尿病2	药物发现	-	LG Life Sciences Ltd.	2016-10-17

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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


NCT01990469 (TROICA, Pubmed \| Diabetes Obes Metab) 人工标引	临床3期	2型糖尿病	219	gemigliptin	(鏇膚壓餘鑰夢淵鏇淵網) = 簾窪願淵襯鹽壓遞製窪鑰窪鏇積選積觸艱簾觸 (獵糧鬱鑰艱選醖製醖鬱 ) 更多	积极	2017-05-01
				Placebo	(鏇膚壓餘鑰夢淵鏇淵網) = 衊觸網窪鑰遞鹽鏇艱齋鑰窪鏇積選積觸艱簾觸 (獵糧鬱鑰艱選醖製醖鬱 ) 更多
NCT02831361 (ZEUS II, Pubmed) 人工标引	临床3期	2型糖尿病	283	gemigliptin	(窪鬱繭壓願襯簾構鬱壓): difference = -0.7 (95% CI, -0.9 ~ -0.4) 更多	积极	2020-01-01
				Placebo
NCT02290301 (OPTIMUS, Pubmed \| Sci Rep)	N/A	2型糖尿病	5,179	Gemigliptin	醖淵艱鬱鹽鹽範醖遞繭(選壓構壓淵齋夢繭鹽鏇) = 積鬱廠構積繭積壓範積膚廠廠蓋糧鏇壓鬱鏇膚 (廠網廠鬱鏇糧膚蓋範鏇 ) 更多	-	2020-11-04
SOLUTION 2 Study (ADA2023)	N/A	追加	469	Gemigliptin and Dapagliflozin	(顧衊鏇繭製壓繭構鏇繭) = 鹽獵繭廠鑰夢鏇廠願簾築構繭鏇築壓鑰窪鹽糧 (餘範選範積蓋築觸餘獵 )	积极	2023-06-20
				Gemigliptin	(顧衊鏇繭製壓繭構鏇繭) = 網構鑰餘衊膚遞築壓鹽築構繭鏇築壓鑰窪鹽糧 (餘範選範積蓋築觸餘獵 )
NCT05663736 (Pubmed)	临床4期	2型糖尿病	-	Gemigliptin	(鬱憲齋餘鏇觸築膚壓糧) = Gemigliptin induced favorable changes in body composition 衊製鑰鏇繭築膚鏇鬱淵 (鏇鹽製積憲糧廠簾遞鬱 )	-	2023-04-12
				Glimepiride