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https://www.readbyqxmd.com/read/29147952/gemigliptin-a-novel-dipeptidyl-peptidase-iv-inhibitor-exerts-a-synergistic-cytotoxicity-with-the-histone-deacetylase-inhibitor-pxd101-in-thyroid-carcinoma-cells
#1
S H Kim, J G Kang, C S Kim, S-H Ihm, M G Choi, H J Yoo, S J Lee
PURPOSE: The influence of the dipeptidyl peptidase-IV inhibitor gemigliptin alone or in combination with the histone deacetylase inhibitor PXD101 on survival of thyroid carcinoma cells was investigated. METHODS: SW1736, TPC-1, 8505C and BCPAP human thyroid carcinoma cells were used. To assess cell survival, cell viability, the percentage of viable cells and dead cells, cytotoxic activity, ATP levels and FACS analysis were measured. To validate the impact of gemigliptin combined with PXD101, the interactions were estimated by obtaining combination index in cells treated with two agents...
November 16, 2017: Journal of Endocrinological Investigation
https://www.readbyqxmd.com/read/28982310/the-dipeptidyl-peptidase-iv-inhibitor-gemigliptin-alone-or-in-combination-with-nvp-auy922-has-a-cytotoxic-activity-in-thyroid-carcinoma-cells
#2
Si Hyoung Kim, Jun Goo Kang, Chul Sik Kim, Sung-Hee Ihm, Moon Gi Choi, Hyung Joon Yoo, Seong Jin Lee
The effect of the dipeptidyl peptidase-IV inhibitor gemigliptin alone or in combination with the heat shock protein 90 inhibitor NVP-AUY922 (AUY922) on survival of thyroid carcinoma cells was elucidated. The SW1736 and TPC-1 human thyroid carcinoma cells were used. Cell viability, the percentage of viable cells, cytotoxic activity, the percentage of apoptotic cells, and mitochondrial membrane potential were measured. To evaluate the combined effect of gemigliptin with AUY922, the interactions were estimated by calculating combination index...
October 2017: Tumour Biology: the Journal of the International Society for Oncodevelopmental Biology and Medicine
https://www.readbyqxmd.com/read/28719008/comparative-efficacy-and-safety-of-gemigliptin-versus-linagliptin-in-type-2-diabetes-patients-with-renal-impairment-a-40-week-extension-of-the-guard-randomized-study
#3
Sang Youb Han, Sun Ae Yoon, Byoung Geun Han, Sung Gyun Kim, Young-Il Jo, Kyung Hwan Jeong, Kook-Hwan Oh, Hyeong Cheon Park, Sun-Hee Park, Shin-Wook Kang, Ki-Ryang Na, Sun Woo Kang, Nam-Ho Kim, Younghwan Jang, Bogyeong Kim, Seonghye Shin, Dae Ryong Cha
AIMS: The long-term safety and efficacy of gemigliptin was evaluated in the present extension study after a 12-week study during a 40-week follow-up period. METHODS: The main study was a randomized, placebo-controlled, double-blinded, phase IIIb study in which 50 mg of gemigliptin (N = 66) or placebo (N = 66) was administered to patients with type 2 diabetes mellitus (T2DM) and moderate or severe renal impairment over a 12-week period. Patients with a glycated haemoglobin (HbA1c) level of 7% to 11% and an estimated glomerular filtration rate (eGFR) of 15 to 59 mL/min/1...
July 18, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28686724/dipeptidyl-peptidase-4-inhibitor-gemigliptin-protects-against-vascular-calcification-in-an-experimental-chronic-kidney-disease-and-vascular-smooth-muscle-cells
#4
Soon-Youn Choi, Hye-Myung Ryu, Eun-Joo Oh, Ji-Young Choi, Jang-Hee Cho, Chan-Duck Kim, Yong-Lim Kim, Sun-Hee Park
Although dipeptidyl peptidase-4 inhibitors, a class of antidiabetic drugs, have various pleiotropic effects, it remains undetermined whether gemigliptin has a beneficial effect on vascular calcification. Therefore, this study was performed to evaluate the effect of gemigliptin on vascular calcification in a rat model of adenine-induced chronic kidney disease and in cultured vascular smooth muscle cells. Gemigliptin attenuated calcification of abdominal aorta and expression of RUNX2 in adenine-induced chronic kidney disease rats...
2017: PloS One
https://www.readbyqxmd.com/read/28326327/ameliorating-effect-of-gemigliptin-on-renal-injury-in-murine-adriamycin-induced-nephropathy
#5
Da Rae Kim, Shin Yeong Lee, Jin Sug Kim, Yang Gyun Kim, Ju-Young Moon, Sang Ho Lee, Tae Won Lee, Chun Gyoo Ihm, Kyung Hwan Jeong
Background. Previous studies have shown the antiapoptotic and anti-inflammatory potential of DPP-IV inhibitor in experimental models of renal injury. We tested whether DPP-IV inhibitor (gemigliptin) ameliorates renal injury by suppressing apoptosis, inflammation, and oxidative stress in mice with adriamycin nephropathy. Methods. Mice were treated with normal saline (control), gemigliptin (GM), adriamycin (ADR), or adriamycin combined with gemigliptin (ADR+GM). Apoptosis, inflammation, and oxidative stress were analyzed via western blotting, real-time PCR, light microscopy, and immunofluorescence...
2017: BioMed Research International
https://www.readbyqxmd.com/read/28058753/effect-of-gemigliptin-on-glycaemic-variability-in-patients-with-type-2-diabetes-stable-study
#6
Se E Park, Byung W Lee, Jae H Kim, Woo J Lee, Jae H Cho, Chang H Jung, Seung H Lee, Sunghwan Suh, Gwong C Hur, Sung H Kim, Young H Jang, Cheol Y Park
The aim of this study was to evaluate the effect of gemigliptin vs sitagliptin or glimepiride as initial combination therapy with metformin on glycaemic variability and to assess the correlation between glycaemic variability reduction and the dipeptidyl peptidase-4 (DPP-4) inhibition in patients with type 2 diabetes. This multicentre, randomized, active-controlled, open-label exploratory study included 69 patients with HbA1c > 7.5%. Subjects were randomized to receive gemigliptin 50 mg (n = 24), sitagliptin 100 mg (n = 23) or glimepiride 2 mg (n = 22) for 12 weeks...
June 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28026912/efficacy-and-safety-of-gemigliptin-a-dipeptidyl-peptidase-4-inhibitor-in-patients-with-type-2-diabetes-mellitus-inadequately-controlled-with-combination-treatment-of-metformin-and-sulphonylurea-a-24-week-multicentre-randomized-double-blind-placebo-controlled
#7
RANDOMIZED CONTROLLED TRIAL
Chang Ho Ahn, Kyung Ah Han, Jae Myung Yu, Joo Young Nam, Kyu Jeung Ahn, Tae Keun Oh, Hyoung Woo Lee, Dae Ho Lee, Jaetaek Kim, Choon Hee Chung, Tae Sun Park, Byung Joon Kim, Seok Won Park, Hyeong Kyu Park, Kwang Jae Lee, Sang-Wook Kim, Jeong Hyun Park, Kwan Pyo Ko, Chong Hwa Kim, Hyunjin Lee, Hak Chul Jang, Kyong Soo Park
AIMS: To assess the efficacy and safety of gemigliptin, a dipeptidyl peptidase-4 inhibitor, added to metformin and sulphonylurea in patients with type 2 diabetes (T2DM). MATERIALS AND METHODS: We conducted a randomized, double-blind, placebo-controlled trial in 219 Korean patients inadequately controlled with metformin and glimepiride. Participants were randomized to gemigliptin 50 mg once daily or placebo added to metformin and glimepiride. The primary endpoint was change in glycated haemoglobin (HbA1c) level from baseline to week 24...
May 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28019072/efficacy-safety-and-albuminuria-reducing-effect-of-gemigliptin-in-korean-type-2-diabetes-patients-with-moderate-to-severe-renal-impairment-a-12-week-double-blind-randomized-study-the-guard-study
#8
RANDOMIZED CONTROLLED TRIAL
Sun A Yoon, Byoung G Han, Sung G Kim, Sang Y Han, Young I Jo, Kyung H Jeong, Kook H Oh, Hyeong C Park, Sun H Park, Shin W Kang, Ki R Na, Sun W Kang, Nam H Kim, Young H Jang, Seong H Shin, Dae R Cha
AIMS: This multicentre, randomized, double-blind study investigated the efficacy and safety of gemigliptin in Korean type 2 diabetes mellitus (T2DM) patients with moderate to severe renal impairment (RI). METHODS: The study comprised a 12-week main part and a 40-week extension. We report here the results from the main part. In total, 132 patients were randomized to receive gemigliptin (n = 66) or placebo (n = 66). Changes in glycated haemoglobin (HbA1c; primary endpoint), other glycaemic control parameters (fasting plasma glucose, glycated albumin and fructosamine), lipid profiles, renal function parameters and safety profiles were evaluated...
April 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/27918207/gemigliptin-ameliorates-western-diet-induced-metabolic-syndrome-in-mice
#9
Seung Hee Choi, Jaechan Leem, Sungmi Park, Chong-Kee Lee, Keun-Gyu Park, In-Kyu Lee
Dipeptidyl peptidase 4 (DPP-4) inhibitors are widely used antihyperglycemic agents for type 2 diabetes mellitus. Recently, increasing attention has been focused on the pleiotropic actions of DPP-4 inhibitors. The aim of the present study was to examine whether gemigliptin, a recently developed DPP-4 inhibitor, could ameliorate features of metabolic syndrome. Mice were fed a Western diet (WD) for 12 weeks and were subsequently divided into 2 groups: mice fed a WD diet alone or mice fed a WD diet supplemented with gemigliptin for an additional 4 weeks...
February 2017: Canadian Journal of Physiology and Pharmacology
https://www.readbyqxmd.com/read/27868366/effects-of-gemigliptin-a-dipeptidyl-peptidase-4-inhibitor-on-lipid-metabolism-and-endotoxemia-after-a-high-fat-meal-in-patients-with-type-2-diabetes
#10
RANDOMIZED CONTROLLED TRIAL
Chang Ho Ahn, Eun Ky Kim, Se Hee Min, Tae Jung Oh, Young Min Cho
We aimed to investigate the effects of gemigliptin, a dipeptidyl peptidase-4 inhibitor, on postprandial lipoprotein levels and endotoxemia in a randomized, double-blind, placebo-controlled, crossover study. Ten people with type 2 diabetes mellitus (T2DM), inadequately controlled with oral antidiabetic medications and/or lifestyle modification, were randomized to gemigliptin or placebo for 4 weeks. At the end of each treatment phase, the study participants underwent a high-fat meal tolerance test and needle aspiration of abdominal subcutaneous adipose tissue...
March 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/27766241/gemigliptin-an-update-of-its-clinical-use-in-the-management-of-type-2-diabetes-mellitus
#11
REVIEW
Sung-Ho Kim, Jung-Hwa Yoo, Woo Je Lee, Cheol-Young Park
Dipeptidyl peptidase-4 (DPP-4) inhibitors are a new class of oral antidiabetic agent for the treatment of type 2 diabetes mellitus. They increase endogenous levels of incretin hormones, which stimulate glucose-dependent insulin secretion, decrease glucagon secretion, and contribute to reducing postprandial hyperglycemia. Although DPP-4 inhibitors have similar benefits, they can be differentiated in terms of their chemical structure, pharmacology, efficacy and safety profiles, and clinical considerations. Gemigliptin (brand name: Zemiglo), developed by LG Life Sciences, is a potent, selective, competitive, and long acting DPP-4 inhibitor...
October 2016: Diabetes & Metabolism Journal
https://www.readbyqxmd.com/read/27619558/efficacy-and-safety-of-initial-combination-therapy-with-gemigliptin-and-metformin-compared-with-monotherapy-with-either-drug-in-patients-with-type-2-diabetes-a-double-blind-randomized-controlled-trial-inicom-study
#12
RANDOMIZED CONTROLLED TRIAL
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...
January 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/27298192/pharmacological-profiles-of-gemigliptin-lc15-0444-a-novel-dipeptidyl-peptidase-4-inhibitor-in-vitro-and-in-vivo
#13
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
https://www.readbyqxmd.com/read/27098503/renoprotective-effect-of-gemigliptin-a-dipeptidyl-peptidase-4-inhibitor-in-streptozotocin-induced-type-1-diabetic-mice
#14
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
https://www.readbyqxmd.com/read/26959365/the-dose-dependent-organ-specific-effects-of-a-dipeptidyl-peptidase-4-inhibitor-on-cardiovascular-complications-in-a-model-of-type-2-diabetes
#15
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
https://www.readbyqxmd.com/read/26391252/gemigliptin-a-dipeptidyl-peptidase-4-inhibitor-inhibits-retinal-pericyte-injury-in-db-db-mice-and-retinal-neovascularization-in-mice-with-ischemic-retinopathy
#16
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
https://www.readbyqxmd.com/read/26297911/a-dipeptidyl-peptidase-iv-inhibitor-improves-hepatic-steatosis-and-insulin-resistance-by-ampk-dependent-and-jnk-dependent-inhibition-of-lect2-expression
#17
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
https://www.readbyqxmd.com/read/26187356/dipeptidyl-peptidase-4-inhibition-by-gemigliptin-prevents-abnormal-vascular-remodeling-via-nf-e2-related-factor-2-activation
#18
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
https://www.readbyqxmd.com/read/26173919/clinical-pharmacology-of-dipeptidyl-peptidase-4-inhibitors-indicated-for-the-treatment-of-type-2-diabetes-mellitus
#19
REVIEW
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
https://www.readbyqxmd.com/read/26021829/effects-of-a-dpp4-inhibitor-on-cisplatin-induced-acute-kidney-injury-study-protocol-for-a-randomized-controlled-trial
#20
RANDOMIZED CONTROLLED TRIAL
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...
May 29, 2015: Trials
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