The Sound of Evolution
Lobeglitazone
洛貝格列酮
Mechanism of action:
Lobeglitazone 是一種噻唑烷二酮類（thiazolidinedione）衍生物，屬於過氧化物酶體增殖物活化受體γ（PPAR-γ）促效劑。Lobeglitazone 進入細胞後，會與細胞核內的 PPAR-γ 受體結合，之後 PPAR-γ 與視網酸 X 受體（retinoid X receptor）形成複合體，再結合至 DNA 上的 PPAR 反應元件（PPRE），調控多個代謝相關基因的轉錄，能提升脂肪細胞對胰島素的敏感性、促進葡萄糖轉運蛋白 GLUT4 相關表達、降低游離脂肪酸的釋放。
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.