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

被引：42
作者：
Bae, Jaehyun [1 ]
Park, Taegyun [2 ]
Kim, Hyeyoung [3 ]
Lee, Minyoung [4 ]
Cha, Bong-Soo [4 ]
机构：
[1] Catholic Kwandong Univ, Dept Internal Med, Div Endocrinol & Metab, Coll Med,Int St Marys Hosp, Incheon, South Korea
[2] Sungkyunkwan Univ, Samsung Adv Inst Hlth Sci & Technol, Dept Clin Res Design & Evaluat, Seoul, South Korea
[3] CKD Pharmaceut Corp, Med Informat & Pharmacovigilance Team, Seoul, South Korea
[4] Yonsei Univ, Dept Internal Med, Div Endocrinol & Metab, Coll Med, 50 Yonsei Ro, Seoul 03722, South Korea
来源：
DIABETES & METABOLISM JOURNAL | 2021年 / 45卷 / 03期
关键词：
Diabetes mellitus; type; 2; Lobeglitazone; Thiazolidinediones; RECEPTOR-GAMMA AGONIST; BONE-MINERAL DENSITY; DOUBLE-BLIND; GLYCEMIC CONTROL; PPAR-GAMMA; PHARMACOKINETIC INTERACTION; PARALLEL-GROUP; BLADDER-CANCER; CLINICAL-TRIAL; OPEN-LABEL;
D O I：
10.4093/dmj.2020.0272
中图分类号：
R5 [内科学];
学科分类号：
1002 ; 100201 ;
摘要：
Type 2 diabetes mellitus (T2DM) is characterized by insulin resistance and beta-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 gamma. 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.
引用
收藏
页码：326 / 336
页数：11
相关论文
共 57 条
[1]   Rosiglitazone causes bone loss in mice by suppressing osteoblast differentiation and bone formation [J].
Ali, AA ;
Weinstein, RS ;
Stewart, SA ;
Parfitt, AM ;
Manolagas, SC ;
Jilka, RL .
ENDOCRINOLOGY, 2005, 146 (03) :1226-1235
[2]   Pioglitazone hydrochloride monotherapy improves glycemic control in the treatment of patients with type 2 diabetes - A 6-month randomized placebo-controlled dose-response study [J].
Aronoff, S ;
Rosenblatt, S ;
Braithwaite, S ;
Egan, JW ;
Mathisen, AL ;
Schneider, RL .
DIABETES CARE, 2000, 23 (11) :1605-1611
[3]   Lobeglitazone, a Novel Peroxisome Proliferator-Activated Receptor γ Agonist, Attenuates Renal Fibrosis Caused by Unilateral Ureteral Obstruction in Mice [J].
Bae, Kwi-Hyun ;
Seo, Jung Beom ;
Jung, Yun-A ;
Seo, Hye-Young ;
Kang, Sun Hee ;
Jeon, Hui-Jeon ;
Lee, Jae Man ;
Lee, Sungwoo ;
Kim, Jung-Guk ;
Lee, In-Kyu ;
Jung, Gwon-Soo ;
Park, Keun-Gyu .
ENDOCRINOLOGY AND METABOLISM, 2017, 32 (01) :115-123
[4]   Rosiglitazone Decreases Bone Mineral Density and Increases Bone Turnover in Postmenopausal Women With Type 2 Diabetes Mellitus [J].
Bilezikian, John P. ;
Josse, Robert G. ;
Eastell, Richard ;
Lewiecki, E. Michael ;
Miller, Colin G. ;
Wooddell, Margaret ;
Northcutt, Allison R. ;
Kravitz, Barbara G. ;
Paul, Gitanjali ;
Cobitz, Alexander R. ;
Nino, Antonio J. ;
Fitzpatrick, Lorraine A. .
JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM, 2013, 98 (04) :1519-1528
[5]   Efficacy and tolerability of vildagliptin vs. pioglitazone when added to metformin: a 24-week, randomized, double-blind study [J].
Bolli, G. ;
Dotta, F. ;
Rochotte, E. ;
Cohen, S. E. .
DIABETES OBESITY & METABOLISM, 2008, 10 (01) :82-90
[6]   The Diagnosis and Management of Non-alcoholic Fatty Liver Disease: Practice Guideline by the American Association for the Study of Liver Diseases, American College of Gastroenterology, and the American Gastroenterological Association [J].
Chalasani, Naga ;
Younossi, Zobair ;
Lavine, Joel E. ;
Diehl, Anna Mae ;
Brunt, Elizabeth M. ;
Cusi, Kenneth ;
Charlton, Michael ;
Sanyal, Arun J. .
AMERICAN JOURNAL OF GASTROENTEROLOGY, 2012, 107 (06) :811-826
[7]   A long-term comparison of pioglitazone and gliclazide in patients with Type 2 diabetes mellitus: a randomized, double-blind, parallel-group comparison trial [J].
Charbonnel, BH ;
Matthews, DR ;
Schernthaner, G ;
Hanefeld, M ;
Brunetti, P .
DIABETIC MEDICINE, 2005, 22 (04) :399-405
[8]   Therapeutic Effects of Targeted PPAR. Activation on Inflamed High-Risk Plaques Assessed by Serial Optical Imaging In Vivo [J].
Choi, Jah Yeon ;
Ryu, Jiheun ;
Kim, Hyun Jung ;
Song, Joon Woo ;
Jeon, Joo Hee ;
Lee, Dae-Hee ;
Oh, Dong Joo ;
Gweon, Dae-Gab ;
Oh, Wang-Yuhl ;
Yoo, Hongki ;
Park, Kyeongsoon ;
Kim, Jin Won .
THERANOSTICS, 2018, 8 (01) :45-60
[9]   Treatment with Lobeglitazone Attenuates Hepatic Steatosis in Diet-Induced Obese Mice [J].
Choung, Sorim ;
Joung, Kyong Hye ;
You, Bo Ram ;
Park, Sang Ki ;
Kim, Hyun Jin ;
Ku, Bon Jeong .
PPAR RESEARCH, 2018, 2018
[10]  
Goke Burkhard, 2002, Treat Endocrinol, V1, P329
123456