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Soo Lim, Kyung Ah Han, JaeMyung Yu, Parinya Chamnan, Eun Sook Kim, Kun-Ho Yoon, Sam Kwon, Min Kyong Moon, Kwan Woo Lee, Dong-Jun Kim, Mikyung Kim, Manaj Wongtanate, Eun Young Kim, Sung-Ho Kim, Moon-Kyu Lee
BACKGROUND: Gemigliptin is a new dipeptidyl peptidase-IV inhibitor. We investigated the efficacy and safety of initial combination therapy with gemigliptin and metformin compared with monotherapy with either drug in patients with type 2 diabetes (T2D). METHODS: A total of 433 T2D patients with a glycosylated haemoglobin (HbA1c) level of 7.5% to 11.0% and a fasting plasma glucose (FPG) concentration <270 mg/dL were randomly assigned to 3 groups: (1) gemigliptin 50 mg qd + metformin 1000 to 2000 mg qd (titrated individually), (2) gemigliptin 50 mg qd, or (3) metformin 1000 to 2000 mg qd...
September 13, 2016: Diabetes, Obesity & Metabolism
Sung-Ho Kim, Eunsoo Jung, Min Kyung Yoon, O Hwan Kwon, Dal-Mi Hwang, Dong-Wook Kim, Junghyun Kim, Sun-Mee Lee, Hyeon Joo Yim
Gemigliptin, a novel dipeptidyl peptidase (DPP)-4 inhibitor, is approved for use as a monotherapy or in combination therapy to treat hyperglycemia in patients with type 2 diabetes mellitus. In this study, we investigated the pharmacological profiles of gemigliptin in vitro and in vivo and compared them to those of the other DPP-4 inhibitors. Gemigliptin was a reversible and competitive inhibitor with a Ki value of 7.25±0.67nM. Similar potency was shown in plasma from humans, rats, dogs, and monkeys. The kinetics of DPP-4 inhibition by gemigliptin was characterized by a fast association and a slow dissociation rate compared to sitagliptin (fast on and fast off rate) or vildagliptin (slow on and slow off rate)...
October 5, 2016: European Journal of Pharmacology
Gwon Soo Jung, Jae Han Jeon, Mi Sun Choe, Sung Woo Kim, In Kyu Lee, Mi Kyung Kim, Keun Gyu Park
BACKGROUND: Dipeptidyl peptidase-4 (DPP-4) inhibitors are widely used in the treatment of patients with type 2 diabetes and have proven protective effects on diabetic kidney disease (DKD). Whether DPP-4 inhibitors have renoprotective effects on insulin-deficient type 1 diabetes has not been comprehensively examined. The aim of this study was to determine whether gemigliptin, a new DPP-4 inhibitor, has renoprotective effects in streptozotocin (STZ)-induced type 1 diabetic mice. METHODS: Diabetes was induced by intraperitoneal administration of a single dose of STZ...
June 2016: Diabetes & Metabolism Journal
Ju-Young Moon, Jong Shin Woo, Jung-Woo Seo, Arah Lee, Dong Jin Kim, Yang-Gyun Kim, Se-Yeun Kim, Kyung Hye Lee, Sung-Jig Lim, Xian Wu Cheng, Sang-Ho Lee, Weon Kim
OBJECTIVE: Although dipeptidyl peptidase-4 (DPP-4) inhibitors have been suggested to have a non-glucoregulatory protective effect in various tissues, the effects of long-term inhibition of DPP-4 on the micro- and macro-vascular complications of type 2 diabetes remain uncertain. The aim of the present study was to investigate the organ-specific protective effects of DPP-4 inhibitor in rodent model of type 2 diabetes. METHODS: Eight-week-old diabetic and obese db/db mice and controls (db/m mice) received vehicle or one of two doses of gemigliptin (0...
2016: PloS One
Eunsoo Jung, Junghyun Kim, Chan-Sik Kim, Sung-Ho Kim, Myung-Haing Cho
Retinal pericyte loss and neovascularization are characteristic features of diabetic retinopathy. Gemigliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor, has shown robust blood-glucose lowering effects in type 2 diabetic patients, but its effects on diabetic retinopathy have not yet been reported. We evaluated the efficacy of gemigliptin on retinal vascular leakage in db/db mice, which is an animal model for type 2 diabetes, and neovascularization in oxygen-induced retinopathy (OIR) mice, which is an animal model for ischemic proliferative retinopathy...
December 2015: Biochimica et Biophysica Acta
Hwan-Jin Hwang, Tae Woo Jung, Baek-Hui Kim, Ho Cheol Hong, Ji A Seo, Sin Gon Kim, Nan Hee Kim, Kyung Mook Choi, Dong Seop Choi, Sei Hyun Baik, Hye Jin Yoo
Leukocyte cell-derived chemotaxin 2 (LECT2) is a recently discovered hepatokine that mediates obesity-related metabolic disturbances. Dipeptidyl peptidase-4 (DPP-4) inhibitors are novel therapeutic agents for inflammatory disorders including nonalcoholic fatty liver disease (NAFLD). However, no research has examined the connections or functions of LECT2 and the novel DPP-4 inhibitor, gemigliptin, in NAFLD pathogenesis. High-fat diet (HFD)-fed C57BL/6 mice were used to investigate the effect of gemigliptin on hepatic steatosis and LECT2 expression...
November 1, 2015: Biochemical Pharmacology
Seung Hee Choi, Sungmi Park, Chang Joo Oh, Jaechan Leem, Keun-Gyu Park, In-Kyu Lee
Dipeptidyl peptidase-4 (DPP-4) inhibitors exert a potent anti-hyperglycemic effect and reduce cardiovascular risk in type 2 diabetic patients. Several studies have shown that DPP-4 inhibitors including sitagliptin have beneficial effects in atherosclerosis and cardiac infarction involving reactive oxygen species. Here, we show that gemigliptin can directly attenuate the abnormal proliferation and migration of vascular smooth muscle cells (VSMCs) via enhanced NF-E2-related factor 2 (Nrf2) activity. Gemigliptin dramatically prevented ligation injury-induced neointimal hyperplasia in mouse carotid arteries...
October 2015: Vascular Pharmacology
Xiao-Wu Chen, Zhi-Xu He, Zhi-Wei Zhou, Tianxin Yang, Xueji Zhang, Yin-Xue Yang, Wei Duan, Shu-Feng Zhou
Dipeptidyl peptidase-4 (DPP-4) inhibitors are a class of oral antidiabetic drugs that improve glycaemic control without causing weight gain or increasing hypoglycaemic risk in patients with type 2 diabetes mellitus (T2DM). The eight available DPP-4 inhibitors, including alogliptin, anagliptin, gemigliptin, linagliptin, saxagliptin, sitagliptin, teneligliptin, and vildagliptin, are small molecules used orally with identical mechanism of action and similar safety profiles in patients with T2DM. DPP-4 inhibitors may be used as monotherapy or in double or triple combination with other oral glucose-lowering agents such as metformin, thiazolidinediones, or sulfonylureas...
October 2015: Clinical and Experimental Pharmacology & Physiology
Seon Ha Baek, Se Hyun Kim, Jin Won Kim, Yu Jung Kim, Keun-Wook Lee, Ki Young Na
BACKGROUND: Cisplatin is a potent chemotherapeutic agent, but its nephrotoxicity, which results in acute kidney injury (AKI), often limits its clinical application. Although many studies have attempted to target the mechanism responsible for its nephrotoxicity, no such method has been demonstrated to be effective in clinical trials. Recently, a dipeptidyl peptidase-4 (DPP4) inhibitor has been reported to have a renoprotective effect in a mouse model of cisplatin-induced AKI. Therefore, we will evaluate whether a DPP4 inhibitor protects the kidney from cisplatin-induced injury in humans...
2015: Trials
Eunsoo Jung, Junghyun Kim, Sung Ho Kim, Sanghwa Kim, Myung-Haing Cho
Podocytes participate in the formation and regulation of the glomerular filtration barrier. Loss of podocytes occurs during the early stages of diabetic nephropathy and impairs glomerular filtration. Dipeptidyl peptidase-4 (DPP-4) inhibitors are widely used as anti-diabetic agents in clinical practice. In this study, we showed that gemigliptin, a novel DPP-4 inhibitor, reduced podocyte apoptosis in type 2 diabetic db/db mice without reducing hyperglycemia. Gemigliptin (100mg/kg/day) was administered orally for 12 weeks in db/db mice...
August 15, 2015: European Journal of Pharmacology
Sang-In Park, Howard Lee, Jaeseong Oh, Kyoung Soo Lim, In-Jin Jang, Jeong-Ae Kim, Jong Hyuk Jung, Kyung-Sang Yu
BACKGROUND: In type 2 diabetes mellitus, fixed-dose combination (FDC) can provide the complementary benefits of correction of multiple pathophysiologic defects such as dysfunctions in glycemic or metabolic control while improving compliance compared with separate tablets taken together. The objective of the study reported here was to compare the pharmacodynamic (PD), pharmacokinetic (PK), and tolerability profiles of gemigliptin and extended-release metformin (metformin XR) between FDC and separate tablets...
2015: Drug Design, Development and Therapy
Hwan-Jin Hwang, Hye Soo Chung, Tae Woo Jung, Ja Young Ryu, Ho Cheol Hong, Ji A Seo, Sin Gon Kim, Nan Hee Kim, Kyung Mook Choi, Dong Seop Choi, Sei Hyun Baik, Hye Jin Yoo
Recently, dipeptidyl peptidase-IV (DPP-IV) inhibitor, a major anti-hyperglycemic agent, has received substantial attention as a possible therapeutic target for inflammatory diseases such as atherosclerosis. However, the direct molecular mechanisms through which DPP-IV inhibitor mediates anti-inflammatory effects in vascular endothelial cells have not been clarified. The effects of the DPP-IV inhibitor, gemigliptin, were analyzed in human umbilical vein endothelial cells (HUVECs) and THP-1 cells. Using Western blotting, we demonstrated that gemigliptin efficiently increased the level of AMP-activated protein kinase (AMPK) and Akt phosphorylation in a dose-dependent manner...
April 15, 2015: Molecular and Cellular Endocrinology
Eunsoo Jung, Junghyun Kim, Sung Ho Kim, Sanghwa Kim, Myung-Haing Cho
This study evaluated the inhibitory effects of gemigliptin, a highly selective dipeptidyl peptidase-4 inhibitor, on the formation of advanced glycation end products (AGEs) and AGE cross-links with proteins in in vitro as well as in type 2 diabetic db/db mice. In in vitro assay, gemigliptin dose-dependently inhibited methylglyoxal-modified AGE-bovine serum albumin (BSA) formation (IC50=11.69 mM). AGE-collagen cross-linking assays showed that gemigliptin had a potent inhibitory effect (IC50=1.39 mM) on AGE-BSA cross-links to rat tail tendon collagen, and its activity was stronger than aminoguanidine (IC50=26...
December 5, 2014: European Journal of Pharmacology
Hee Youn Choi, Hyeong-Seok Lim, Yo Han Kim, Hae Sun Jeon, Mi Jo Kim, Shi Hyang Lee, Jong Hyuk Jung, Young Kyoung Lee, Hyun Jeong Kim, Kyun-Seop Bae
OBJECTIVE: Gemigliptin is a selective DPP4 inhibitor used to treat type 2 diabetes. The objective of this study was to evaluate the pharmacokinetics (PKs) of gemigliptin, rosuvastatin, and irbesartan monotherapies and combination therapies. RESEARCH DESIGN AND METHODS: Randomized, open-label, three-treatment, six-sequence, three-period, crossover studies were performed on healthy male volunteers. The three treatments were: 50 mg gemigliptin alone; 20 mg rosuvastatin (part A) or 300 mg irbesartan alone (part B); and rosuvastatin or irbesartan with concomitant gemigliptin...
February 2015: Current Medical Research and Opinion
Hee Youn Choi, Yo Han Kim, Mi Jo Kim, Shi Hyang Lee, Keunsu Bang, Song Han, Hyeong-Seok Lim, Kyun-Seop Bae
PURPOSE: Gemigliptin is approved for the treatment of type II diabetes mellitus. Sulfonylureas are commonly used in combination with other antidiabetic drugs to improve glycemic control. The objective of this study was to evaluate the pharmacokinetics, safety, and tolerability of gemigliptin and glimepiride combination therapy compared with those of monotherapies. METHODS: A randomized, open-label, crossover study was performed on healthy Korean male volunteers...
September 2014: Drugs in R&D
Hwan-Jin Hwang, Tae Woo Jung, Ja Young Ryu, Ho Cheol Hong, Hae Yoon Choi, Ji A Seo, Sin Gon Kim, Nan Hee Kim, Kyung Mook Choi, Dong Seop Choi, Sei Hyun Baik, Hye Jin Yoo
The direct effects of dipeptidyl peptidase-IV (DPP-IV) inhibitors on endoplasmic reticulum (ER) stress-induced apoptosis and inflammation in cardiomyocytes have not been elucidated. H9c2 cell viability, which was reduced by tunicamycin, was increased after DPP-IV inhibitor gemigliptin treatment. Gemigliptin significantly decreased the tunicamycin-mediated increase in glucose regulated protein 78 (GRP78) expression and ER stress-mediated signaling molecules such as protein kinase RNA-like endoplasmic reticulum kinase (PERK)/C-EBP homologous protein (CHOP) and inositol-requiring enzyme 1α (IRE1α)/c-Jun N-terminal kinase (JNK)-p38...
July 5, 2014: Molecular and Cellular Endocrinology
Yoon Kim, Unyong Kim, In Sook Kim, Sung-Hack Lee, Jaeick Lee, Dong-Hyun Kim, Hye Hyun Yoo
1. The absorption, distribution, metabolism and excretion of a novel dipeptidyl peptidase IV inhibitor, gemigliptin, were examined following single oral administration of (14)C-labeled gemigliptin to rats. 2. The (14)C-labeled gemigliptin was rapidly absorbed after oral administration, and its bioavailability was 95.2% (by total radioactivity). Distribution to specific tissues other than the digestive organs was not observed. Within 7 days after oral administration, 43.6% of the administered dose was excreted via urine and 41...
July 2014: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
J H Shon, N Kim, S J Park, M K Oh, E Y Kim, S H Lee, Y H Kim, J G Shin
This study evaluated the effects of renal impairment (RI) and haemodialysis (HD) on the pharmacokinetics of gemigliptin, a novel dipeptidyl peptidase-4 (DPP-4) inhibitor. After a 100 mg administration to subjects with normal renal function (n = 23) or RI (n = 24), plasma, urine or dialysate samples were analysed. Control subjects were matched to patients based on age, gender and body mass index. Patients with mild, moderate, severe RI and end-stage renal disease (ESRD) showed 1.20, 2.04, 1.50 and 1.66-fold (1...
October 2014: Diabetes, Obesity & Metabolism
Dongseong Shin, Young Min Cho, SeungHwan Lee, Kyoung Soo Lim, Jeong-Ae Kim, Ji-Yung Ahn, Joo-Youn Cho, Howard Lee, In-Jin Jang, Kyung-Sang Yu
BACKGROUND AND OBJECTIVE: Gemigliptin is a novel dipeptidyl peptidase-4 (DPP-4) inhibitor used in the treatment of type 2 diabetes mellitus. This study evaluated possible pharmacodynamic and pharmacokinetic interactions between gemigliptin and metformin and investigated their tolerability. METHODS: A randomized, open-label, multiple-dose, three-treatment, three-period, three-sequence crossover study was conducted in healthy male subjects. Twenty-seven subjects received gemigliptin (50 mg once daily), metformin (1,000 mg twice a day), or both drugs for 7 days per dosing period...
June 2014: Clinical Drug Investigation
Hee Youn Choi, Yook-Hwan Noh, Yo Han Kim, Mi Jo Kim, Shi Hyang Lee, Jeong-Ae Kim, Bogyeong Kim, Hyeong-Seok Lim, Kyun-Seop Bae
OBJECTIVES: For patient convenience, a gemigliptin/metformin sustainedrelease fixed-dose combination (FDC) tablet was developed. This study was conducted to investigate the effects of food on the pharmacokinetic (PK) profile of the FDC tablets. MATERIALS AND METHODS: This was an open-label, randomized, single dose, 2-period, 2-sequence crossover study in 24 healthy male volunteers. The FDC tablets (25/500 mg × 2 tablets) were administered in high-fat fed and fasted states on separate occasions, and each subject was randomly allocated to each sequence with a 7-day washout period...
May 2014: International Journal of Clinical Pharmacology and Therapeutics
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