The Sound of Evolution
Lobeglitazone
Mechanism of action:
Lobeglitazone is a thiazolidinedione derivative and acts as a peroxisome proliferator-activated receptor gamma (PPAR-γ) agonist. After entering the cell, lobeglitazone binds to the nuclear PPAR-γ receptor. PPAR-γ then forms a complex with the retinoid X receptor, and this complex binds to PPAR response elements (PPREs) on DNA to regulate the transcription of multiple metabolism-related genes. This increases insulin sensitivity in adipocytes, promotes GLUT4-related expression, and reduces the release of free fatty acids.
Reference(s):
1. Lee YH et al. (2017). Lobeglitazone, a Novel Thiazolidinedione, Improves Non-Alcoholic Fatty Liver Disease in Type 2 Diabetes: Its Efficacy and Predictive Factors Related to Responsiveness. J Korean Med Sci.
2. Lee JH et al. (2015). Kinetics of the Absorption, Distribution, Metabolism, and Excretion of Lobeglitazone, a Novel Activator of Peroxisome Proliferator-Activated Receptor Gamma in Rats. J Pharm Sci.
3. Jin SM et al. (2015). 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. Diabetes Obes Metab.