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

Start Date01 Oct 2020

Sponsor / Collaborator

LG Chem Ltd.

NCT04317703

/ CompletedPhase 1

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

Start Date19 Aug 2020

Sponsor / Collaborator

LG Chem Ltd.

NCT04255238

/ Unknown statusPhase 3

A Multicenter, Randomized, Double-blind, Double-dummy, Active-controlled, Parallel Group, Phase 3 Trial to Evaluate the Efficacy and Safety of Dual add-on Therapy With Gemigliptin 50 mg and Dapagliflozin 10 mg Added to Metformin Compared to add-on Therapy With Gemigliptin 50 mg in Combination With Metformin or Dapagliflozin 10 mg in Combination With Metformin in Patients With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control on Metformin Alone

The objective of this study is to evaluate the efficacy and safety of dual add-on therapy with Gemigliptin 50 mg and Dapagliflozin 10 mg added to Metformin compared to add-on therapy with Gemigliptin 50 mg in combination with Metformin or Dapagliflozin 10 mg in combination with Metformin in patients with type 2 diabetes mellitus who have inadequate glycemic control on metformin alone

Start Date30 Jun 2020

Sponsor / Collaborator

LG Chem Ltd.

100 Clinical Results associated with Gemigliptin L-tartrate Sesquihydrate

100 Translational Medicine associated with Gemigliptin L-tartrate Sesquihydrate

100 Patents (Medical) associated with Gemigliptin L-tartrate Sesquihydrate

154

Literatures (Medical) associated with Gemigliptin L-tartrate Sesquihydrate

01 Apr 2025·Diabetes, Obesity and Metabolism

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

Letter

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

01 Dec 2024·Sustainable Chemistry and Pharmacy

Efficient integration of analytical quality-by-design and tri-hued HPLC-DAD approach for synchronized assessment of gemigliptin and rosuvastatin in their fixed-dose pills: Application to stability study

Author: Kamal, Miranda F. ; Daabees, Hoda G. ; Talaat, Wael ; Mohyeldin, Sara M.

Life-threatening atherosclerotic cardiovascular disorder is a well-recognized risk among diabetics, which is clin. ascribed to their unbalanced plasma lipoproteins.Gemigliptin-Rosuvastatin is a recently introduced polytherapy prescribed for the management of diabetic dyslipidemia.Currently, the main focus of several analysts is to design more ecol. friendly sustainable approaches for pharmaceutical anal.In this context, an innovative tri-hued (green, blue, and white) stability-indicating HPLC-DAD approach was developed to concurrently quantify Gemigliptin and Rosuvastatin polypills.Consequently, a strategic integration between anal. quality-by-design and green/white anal. chem. principles was specifically designed to optimize efficiency and practicality while minimizing ecol. burden.Two exptl. designs, namely two-level fractional factorial and Box-Behnken designs, were employed for screening and optimization procedures, resp.Optimal separation was attained utilizing an Agilent HC-C18 column in conjunction with a mobile phase consisting of acetonitrile and 10 mM sodium dihydrogen phosphate buffer, pH 3 (60:40 volume/volume), eluted in an isocratic manner at a 1 mL/min flow rate.Both analytes exhibited good linearities within the concentration range of 0.5-100μg/mL.Furthermore, stability studies were conducted on both drugs in response to variable stress degradation scenarios.Fortunately, the adopted approach was well-suited to resolve the studied drugs from their resp. degradants, thereby verifying the method's stability-indicating power.Tri-hued evaluation for the implemented approach was performed via up-to-date metrics, specifically, the Anal. Eco-scale, AGREE, Blue Applicability Grade Index, and RGB 12.Ultimately, our adopted stability-indicating HPLC approach exhibited great sensitivity, specificity, applicability, and rapidity as well as being ecol. sound.It is worth noting that this is the first stability-indicating HPLC approach for simultaneous assessment of the studied drugs.

01 Nov 2024·Biochemical and Biophysical Research Communications

Gemigliptin mitigates TGF-β-induced renal fibrosis through FGF21-mediated inhibition of the TGF-β/Smad3 signaling pathway

Article

Author: Jung, Gwon-Soo ; Byun, Jun-Kyu

Fibroblast growth factor 21 (FGF21), a well-known regulator of metabolic disorders, exhibits the potential to prevent renal fibrosis by negatively regulating the transforming growth factor β (TGF-β)/Smad3 signaling pathway. Gemigliptin and other dipeptidyl peptidase-4 inhibitors are frequently used for the management of patients with type 2 diabetes. However, the protective effect of gemigliptin against renal fibrosis, particularly its potential to upregulate the expression of FGF21, remains incompletely understood. This study assessed the renoprotective effects of gemigliptin against TGF-β-induced renal fibrosis by enhancing the expression of FGF21 in the cultured human proximal tubular epithelial cell line HK-2. Treatment with FGF21 effectively prevented TGF-β-induced renal fibrosis by attenuating the TGF-β/Smad3 signaling pathway. Similarly, gemigliptin exhibited protective effects against TGF-β-induced renal fibrosis by mitigating TGF-β/Smad3 signaling through the upregulation of FGF21 expression. However, the protective effects of gemigliptin were blocked when FGF21 expression was knocked down in TGF-β-treated HK-2 cells. These results indicate that gemegliptin has the potential to exhibit protective effects against TGF-β-induced renal fibrosis by elevating FGF21 expression levels in cultured human proximal tubular epithelial cells.

News (Medical) associated with Gemigliptin L-tartrate Sesquihydrate

24 Nov 2023

·synapse.patsnap.com

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!

28 Feb 2023

·www.prnewswire.com

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

Phase 3License out/inClinical ResultFast Track

15 Dec 2022

·www.fiercebiotech.com

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.

Phase 3License out/inDrug ApprovalPhase 2Acquisition

100 Deals associated with Gemigliptin L-tartrate Sesquihydrate

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-	Gemigliptin L-tartrate Sesquihydrate	A10BH06	DB12412

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Diabetes Mellitus, Type 2	South Korea	LG Chem Ltd.	27 Jun 2012
Diabetes Mellitus, Type 2	South Korea	LG Life Sciences Ltd.	27 Jun 2012

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Diabetes Mellitus, Type 2	Discovery	United States	LG Chem Ltd.	05 Apr 2018
Diabetes Mellitus, Noninsulin-Dependent, 2	Discovery	-	LG Life Sciences Ltd.	17 Oct 2016
Diabetes Mellitus	Discovery	United States	LG Life Sciences Ltd.	01 Feb 2009

Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


SOLUTION 2 Study (ADA2023)	Not Applicable	Add-on	469	Gemigliptin and Dapagliflozin	(stqbddaqdx) = sabrqeayga okadkhwlws (gubbgydpgu )	Positive	20 Jun 2023
				Gemigliptin	(stqbddaqdx) = nkcjwyrpjt okadkhwlws (gubbgydpgu )
NCT05663736 (Pubmed)	Phase 4	Diabetes Mellitus, Type 2	-	Gemigliptin	(qnargnyeke) = Gemigliptin induced favorable changes in body composition vxgvuwyxnt (miehlqiuez )	-	12 Apr 2023
				Glimepiride
FC 092 (ERA2021)	Not Applicable	Diabetic Nephropathies hemoglobinA1C \| serum bone alkaline phosphatase \| urine neutrophil gelatinase-associated lipocalin (NGAL)/Cr ... View more	201	Gemigliptin 50 mg	uovhsrftme(fonvcgvucs) = qxduwnrilm axlmsaeady (chofxfaqtk )	Positive	29 May 2021
				Placebo	uovhsrftme(fonvcgvucs) = kykbuzvlky axlmsaeady (chofxfaqtk )
NCT02290301 (OPTIMUS, Pubmed \| Sci Rep)	Not Applicable	Diabetes Mellitus, Type 2	5,179	Gemigliptin	cxfexntujw(leqgiqwcrd) = qqzzswfspx dxorpxatmy (spaeiqekpp ) View more	-	04 Nov 2020
NCT02831361 (ZEUS II, Pubmed) Manual	Phase 3	Diabetes Mellitus, Type 2	283	gemigliptin	(snhyovjjyr): difference = -0.7 (95% CI, -0.9 to -0.4), P-Value = <0.0001 View more	Positive	01 Jan 2020
				Placebo
NCT01990469 (TROICA, Pubmed \| Diabetes Obes Metab) Manual	Phase 3	Diabetes Mellitus, Type 2	219	gemigliptin	(rmyulwxiwf) = xephafeghq ipevkkonau (wstbwouhmi ) View more	Positive	01 May 2017
				Placebo	(rmyulwxiwf) = ainrxvtaxj ipevkkonau (wstbwouhmi ) View more
ASN2016	Not Applicable	toxicity from adriamycin DPP-IV \| GLP-1 \| Bax/Bcl-2 ratio ... View more	-	Adriamycin	rzpaeouxoq(geapzahwkr) = ctlpjzdpuk htsraeewac (fbsfgouowo ) View more	Positive	15 Nov 2016
				Adriamycin+Gemigliptin	rzpaeouxoq(geapzahwkr) = dkednpwhrb htsraeewac (fbsfgouowo ) View more
NCT01968044 (GUARD study, EASD2016)	Phase 3	Diabetes Mellitus, Type 2 eGFR	-	Gemigliptin	(ryirdtafnx) = lwtyqirmck ikdgkszsaj (klzgqtlwuv, 0.14) View more	Positive	13 Sep 2016
				Placebo	(ryirdtafnx) = jivzthwinv ikdgkszsaj (klzgqtlwuv, 0.14)
NCT01787396 (EASD2015)	Phase 3	Diabetes Mellitus, Type 2	69	Gemigliptin 50 mg	gkytbgbszj(niabhdbisi) = reported more frequently in glimepiride group than in other groups lsuwwtfoni (patxrdqlgf )	Positive	17 Sep 2015
				Sitagliptin 100 mg
NCT01602003 (EASD2013)	Phase 3	Diabetes Mellitus, Type 2 Add-on	604	Gemigliptin 25 mg bid	orodnhrpyf(flehdymiwg) = an absence of body weight gain over 52 weeks gscikymwjh (hhxdyvsikk ) View more	Positive	25 Sep 2013

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