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      KCI등재 SCOPUS SCIE

      Lobeglitazone: A Novel Thiazolidinedione for the Management of Type 2 Diabetes Mellitus

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      https://www.riss.kr/link?id=A107493829

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      다국어 초록 (Multilingual Abstract)

      Type 2 diabetes mellitus (T2DM) is characterized by insulin resistance and β-cell dysfunction. Among available oral antidiabetic agents, only the thiazolidinediones (TZDs) primarily target insulin resistance. TZDs improve insulin sensitivity by activating peroxisome proliferator-activated receptor γ. Rosiglitazone and pioglitazone have been used widely for T2DM treatment due to their potent glycemic efficacy and low risk of hypoglycemia. However, their use has decreased because of side effects and safety issues, such as cardiovascular concerns and bladder cancer. Lobeglitazone (Chong Kun Dang Pharmaceutical Corporation), a novel TZD, was developed to meet the demands for an effective and safe TZD. Lobeglitazone shows similar glycemic efficacy to pioglitazone, with a lower effective dose, and favorable safety results. It also showed pleiotropic effects in preclinical and clinical studies.
      In this article, we summarize the pharmacologic, pharmacokinetic, and clinical characteristics of lobeglitazone.
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      Type 2 diabetes mellitus (T2DM) is characterized by insulin resistance and β-cell dysfunction. Among available oral antidiabetic agents, only the thiazolidinediones (TZDs) primarily target insulin resistance. TZDs improve insulin sensitivity by activ...

      Type 2 diabetes mellitus (T2DM) is characterized by insulin resistance and β-cell dysfunction. Among available oral antidiabetic agents, only the thiazolidinediones (TZDs) primarily target insulin resistance. TZDs improve insulin sensitivity by activating peroxisome proliferator-activated receptor γ. Rosiglitazone and pioglitazone have been used widely for T2DM treatment due to their potent glycemic efficacy and low risk of hypoglycemia. However, their use has decreased because of side effects and safety issues, such as cardiovascular concerns and bladder cancer. Lobeglitazone (Chong Kun Dang Pharmaceutical Corporation), a novel TZD, was developed to meet the demands for an effective and safe TZD. Lobeglitazone shows similar glycemic efficacy to pioglitazone, with a lower effective dose, and favorable safety results. It also showed pleiotropic effects in preclinical and clinical studies.
      In this article, we summarize the pharmacologic, pharmacokinetic, and clinical characteristics of lobeglitazone.

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      참고문헌 (Reference)

      1 Choung S, "Treat-ment with lobeglitazone attenuates hepatic steatosis in diet-induced obese mice" 2018 : 4292509-, 2018

      2 Park MK, "Tolerability and pharmacokinetics of lobeglitazone, a novel peroxisome proliferator-activated receptor-γ agonist, after a single oral administration in healthy female subjects" 34 : 467-474, 2014

      3 Kim JW, "Tolerability and pharmacokinetics of lobeglitazone(CKD-501), a peroxisome proliferator-activated receptor-γ agonist : a singleand multiple-dose, double-blind, randomized control study in healthy male Korean subjects" 33 : 1819-1830, 2011

      4 Soccio RE, "Thiazolidinediones and the promise of insulin sensitization in type 2 diabetes" 20 : 573-591, 2014

      5 Lebovitz HE, "Thiazolidinediones : the forgotten diabetes medications" 19 : 151-, 2019

      6 Lim S, "Therapeutic efficacy and safety of initial triple combination of metformin, sitagliptin, and lobeglitazone in drug-naïve patients with type 2 diabetes : initial triple study" 8 : e000807-, 2020

      7 Choi JY, "Therapeutic effects of targeted PPARγ activation on inflamed highrisk plaques assessed by serial optical imaging in vivo" 8 : 45-60, 2018

      8 Kahn SE, "The relative contributions of insulin resistance and beta-cell dysfunction to the pathophysiology of type 2 diabetes" 46 : 3-19, 2003

      9 Rosenblatt S, "The impact of pioglitazone on glycemic control and atherogenic dyslipidemia in patients with type 2 diabetes mellitus" 12 : 413-423, 2001

      10 Kwon MJ, "The direct effect of lobeglitazone, a new thiazolidinedione, on pancreatic beta cells : a comparison with other thiazolidinediones" 151 : 209-223, 2019

      1 Choung S, "Treat-ment with lobeglitazone attenuates hepatic steatosis in diet-induced obese mice" 2018 : 4292509-, 2018

      2 Park MK, "Tolerability and pharmacokinetics of lobeglitazone, a novel peroxisome proliferator-activated receptor-γ agonist, after a single oral administration in healthy female subjects" 34 : 467-474, 2014

      3 Kim JW, "Tolerability and pharmacokinetics of lobeglitazone(CKD-501), a peroxisome proliferator-activated receptor-γ agonist : a singleand multiple-dose, double-blind, randomized control study in healthy male Korean subjects" 33 : 1819-1830, 2011

      4 Soccio RE, "Thiazolidinediones and the promise of insulin sensitization in type 2 diabetes" 20 : 573-591, 2014

      5 Lebovitz HE, "Thiazolidinediones : the forgotten diabetes medications" 19 : 151-, 2019

      6 Lim S, "Therapeutic efficacy and safety of initial triple combination of metformin, sitagliptin, and lobeglitazone in drug-naïve patients with type 2 diabetes : initial triple study" 8 : e000807-, 2020

      7 Choi JY, "Therapeutic effects of targeted PPARγ activation on inflamed highrisk plaques assessed by serial optical imaging in vivo" 8 : 45-60, 2018

      8 Kahn SE, "The relative contributions of insulin resistance and beta-cell dysfunction to the pathophysiology of type 2 diabetes" 46 : 3-19, 2003

      9 Rosenblatt S, "The impact of pioglitazone on glycemic control and atherogenic dyslipidemia in patients with type 2 diabetes mellitus" 12 : 413-423, 2001

      10 Kwon MJ, "The direct effect of lobeglitazone, a new thiazolidinedione, on pancreatic beta cells : a comparison with other thiazolidinediones" 151 : 209-223, 2019

      11 Chalasani N, "The diagnosis and management of non-alcoholic fatty liver disease : practice guideline by the American Gastroenterological Association, American Association for the Study of Liver Diseases, and American College of Gastroenterology" 142 : 1592-1609, 2012

      12 Lee YS, "The antidiabetic drug lobeglitazone protects mice from lipogenesisinduced liver injury via mechanistic target of rapamycin complex 1 inhibition" 9 : 539-, 2018

      13 Rocha RF, "The antidiabetic drug lobeglitazone has the potential to inhibit PTP1B activity" 100 : 103927-, 2020

      14 Lee MA, "Structures of PPARγcomplexed with lobeglitazone and pioglitazone reveal key determinants for the recognition of antidiabetic drugs" 7 : 16837-, 2017

      15 Jang JY, "Structural basis for the enhanced anti-diabetic efficacy of lobeglitazone on PPARγ" 8 : 31-, 2018

      16 Kim SH, "Safety and efficacy of lobeglitazone monotherapy in patients with type 2 diabetes mellitus over 52 weeks : an open-label extension study" 110 : e27-30, 2015

      17 Bilezikian JP, "Rosiglitazone decreases bone mineral density and increases bone turnover in postmenopausal women with type 2 diabetes mellitus" 98 : 1519-1528, 2013

      18 Ali AA, "Rosiglitazone causes bone loss in mice by suppressing osteoblast differentiation and bone formation" 146 : 1226-1235, 2005

      19 Yan H, "Pioglitazone use in patients with diabetes and risk of bladder cancer : a systematic review and meta-analysis" 10 : 1627-1638, 2018

      20 Aronoff S, "Pioglitazone hydrochloride monotherapy improves glycemic control in the treatment of patients with type 2diabetes : a 6-month randomized placebo-controlled dose-response study. The Pioglitazone 001 Study Group" 23 : 1605-1611, 2000

      21 Waugh J, "Pioglitazone : a review of its use in type 2 diabetes mellitus" 66 : 85-109, 2006

      22 Kim SY, "Pharmacokinetics of a lobeglitazone/metformin fixed-dose combination tablet(CKD-3950. 5/1000 mg)versus concomitant administration of single agents and the effect of food on the metabolism of CKD-395 in healthy male subjects" 8 : 576-584, 2019

      23 Kim CO, "Pharmacokinetic interaction between amlodipine and lobeglitazone, a novel peroxisome proliferator-activated receptor-γ agonist, in healthy subjects" 37 : 1999-2006, 2015

      24 Tseng CH, "Peroxisome proliferator-activated receptor agonists and bladder cancer : lessons from animal studies" 30 : 368-402, 2012

      25 Jiang C, "PPAR-gamma agonists inhibit production of monocyte inflammatory cytokines" 391 : 82-86, 1998

      26 이용호, "Lobeglitazone, a Novel Thiazolidinedione, Improves Non-Alcoholic Fatty Liver Disease in Type 2 Diabetes: Its Efficacy and Predictive Factors Related to Responsiveness" 대한의학회 32 (32): 60-69, 2017

      27 배기현, "Lobeglitazone, a Novel Peroxisome Proliferator-Activated Receptor γ Agonist, Attenuates Renal Fibrosis Caused by Unilateral Ureteral Obstruction in Mice" 대한내분비학회 32 (32): 115-123, 2017

      28 Shin NR, "Lobeglitazone attenuates airway inflammation and mucus hypersecretion in a murine model of ovalbumin-induced asthma" 9 : 906-, 2018

      29 Jin SM, "Lobeglitazone and pioglitazone as add-ons to metformin for patients with type 2 diabetes : a 24-week, multicentre, randomized, double-blind, parallel-group, active-controlled, phase III clinical trial with a 28-week extension" 17 : 599-602, 2015

      30 Jung JA, "Lack of the effect of lobeglitazone, a peroxisome proliferator-activated receptor-γ agonist, on the pharmacokinetics and pharmacodynamics of warfarin" 9 : 737-743, 2015

      31 Park S, "Labelfree tomographic imaging of lipid droplets in foam cells for machine-learning-assisted therapeutic evaluation of targeted nanodrugs" 14 : 1856-1865, 2020

      32 Goke B, "Improved glycemic control and lipid profile in a randomized study of pioglitazone compared with acarbose in patients with type 2 diabetes mellitus" 1 : 329-336, 2002

      33 Kohlroser J, "Hepatotoxicity due to troglitazone : report of two cases and review of adverse events reported to the United States Food and Drug Administration" 95 : 272-276, 2000

      34 Kahn SE, "Glycemic durability of rosiglitazone, metformin, or glyburide monotherapy" 355 : 2427-2443, 2006

      35 Hanefeld M, "Glycemic control and treatment failure with pioglitazone versus glibenclamide in type 2 diabetes mellitus : a 42-month, open-label, observational, primary care study" 22 : 1211-1215, 2006

      36 Law RE, "Expression and function of PPARgamma in rat and human vascular smooth muscle cells" 101 : 1311-1318, 2000

      37 Jang K, "Evaluation of the pharmacokinetic interaction between lobeglitazone and dapagliflozin at steady state" 42 : 295-304, 2020

      38 Bolli G, "Efficacy and tolerability of vildagliptin vs. pioglitazone when added to metformin : a 24-week, randomized, double-blind study" 10 : 82-90, 2008

      39 Schernthaner G, "Efficacy and safety of pioglitazone versus metformin in patients with type 2 diabetes mellitus : a double-blind, randomized trial" 89 : 6068-6076, 2004

      40 Kim SG, "Efficacy and safety of lobeglitazone versus sitagliptin as an add-on to metformin in patients with type 2 diabetes with two or more components of metabolic syndrome over 24weeks" 22 : 1869-1873, 2020

      41 Kim SG, "Efficacy and safety of lobeglitazone monotherapy in patients with type 2 diabetes mellitus over 24-weeks : a multicenter, randomized, double-blind, parallel-group, placebo controlled trial" 9 : e92843-, 2014

      42 Tan M, "Effects of pioglitazone and glimepiride on glycemic control and insulin sensitivity in Mexican patients with type 2 diabetes mellitus : a multicenter, randomized, double-blind, parallel-group trial" 26 : 680-693, 2004

      43 Kim G, "Effects of lobeglitazone, a novel thiazolidinedione, on adipose tissue remodeling and brown and beige adipose tissue development in db/db mice" 42 : 542-551, 2018

      44 손지형, "Effects of Three Thiazolidinediones on Metabolic Regulation and Cold-Induced Thermogenesis" 한국분자세포생물학회 41 (41): 900-908, 2018

      45 임수, "Effects of Lobeglitazone, a Novel Thiazolidinedione, on Bone Mineral Density in Patients with Type 2 Diabetes Mellitus over 52 Weeks" 대한당뇨병학회 41 (41): 377-385, 2017

      46 김경민, "Effects of Lobeglitazone, a New Thiazolidinedione, on Osteoblastogenesis and Bone Mineral Density in Mice" 대한내분비학회 32 (32): 389-395, 2017

      47 Nissen SE, "Effect of rosiglitazone on the risk of myocardial infarction and death from cardiovascular causes" 356 : 2457-2471, 2007

      48 Oh ES, "Effect of ketoconazole on lobeglitazone pharmacokinetics in Korean volunteers" 36 : 1064-1071, 2014

      49 Lim S, "Effect of a new PPAR-gamma agonist, lobeglitazone, on neointimal formation after balloon injury in rats and the development of atherosclerosis" 243 : 107-119, 2015

      50 Chong Kun Dang Pharmaceutical Corp, "Data on file"

      51 Lee JY, "Clinical efficacy of the novel thiazolidinedione lobeglitazone in patients with type 2 diabetes" 44 : 452-455, 2018

      52 Lee HS, "Carcinogenicity study of CKD-501, a novel dual peroxisome proliferator-activated receptors α and γ agonist, following oral administration to Sprague Dawley rats for 94-101 weeks" 69 : 207-216, 2014

      53 Moon KS, "CKD-501, a novel selective PPARγ agonist, shows no carcinogenic potential in ICR mice following oral administration for 104 weeks" 34 : 1271-1284, 2014

      54 Shin D, "Assessment of the pharmacokinetics of co-administered metformin and lobeglitazone, a thiazolidinedione antihyperglycemic agent, in healthy subjects" 28 : 1213-1220, 2012

      55 Moon SJ, "An assessment of pharmacokinetic interaction between lobeglitazone and sitagliptin after multiple oral administrations in healthy men" 42 : 1047-1057, 2020

      56 Lehmann JM, "An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor gamma(PPAR gamma)" 270 : 12953-12956, 1995

      57 Herz M, "A randomized, double-blind, placebo-controlled, clinical trial of the effects of pioglitazone on glycemic control and dyslipidemia in oral antihyperglycemic medication-naïve patients with type 2 diabetes mellitus" 25 : 1074-1095, 2003

      58 Charbonnel BH, "A long-term comparison of pioglitazone and gliclazide in patients with type 2 diabetes mellitus : a randomized, double-blind, parallel-group comparison trial" 22 : 399-405, 2005

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      2020-01-01 평가 등재학술지 유지 (해외등재 학술지 평가) KCI등재
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      2011-05-30 학술지명변경 한글명 : KOREAN DIABETES JOURNAL -> Diabetes and Metabolism Journal KCI등재
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