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

• Published in: Diabetes & metabolism journal Vol. 45; no. 3; pp. 326 - 336
• Main Authors: Bae, Jaehyun, Park, Taegyun, Kim, Hyeyoung, Lee, Minyoung, Cha, Bong-Soo
• Format: Journal Article
• Language: English
• Published: Korea (South) Korean Diabetes Association / Daehan Dangnyobyeong Hakoe 01.05.2021; Korean Diabetes Association; 대한당뇨병학회
• Subjects: Adipocytes; Atherosclerosis; Bladder cancer; Clinical significance; Cytochrome; Diabetes; diabetes mellitus, type 2; Diabetes Mellitus, Type 2 - drug therapy; Drug dosages; FDA approval; Humans; Hypoglycemic Agents - adverse effects; Insulin resistance; Kinases; Lipids; lobeglitazone; Males; Metabolism; Metabolites; Pharmacokinetics; Plasma; Pyrimidines; Review; thiazolidinediones; Thiazolidinediones - adverse effects; 내과학; Diabetes mellitus, type 2; Lobeglitazone; Thiazolidinediones
• ISSN: 2233-6079; 2233-6087; 2233-6087
• DOI: 10.4093/dmj.2020.0272

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.