Background:

Pioglitazone HCl is a potent and highly selective agonist of PPARγ with IC50 value of 3μM[1].

Pioglitazone HCl can increase both insulin-stimulated glucose uptake in peripheral tissues and insulin sensitivity in hepatic and adipose tissue. It is treated for hyperglycemia and Type 2 diabetes (T2D). Pioglitazone needs insulin as a co-factor for PPAR agonism so it is not effect when being treated to late stages of T2D with developed insulinopenia. In clinical trials, 15mg pioglitazone produces significant improvements in HbA1c and fasting plasma glucose (FPG) [2].

Pioglitazone is also reported to have multiple beneficial effects on lipid metabolism. It produces significant decreases in TG and significant increases in high density lipoprotein (HDL) in clinical studies [2].

参考文献:
[1] Saad S, Agapiou DJ, Chen XM, Stevens V, Pollock CA. The role of Sgk-1 in the upregulation of transport proteins by PPAR-{gamma} agonists in human proximal tubule cells. Nephrol Dial Transplant. 2009 Apr;24(4):1130-41.
[2] Dorkhan M, Frid A. A review of pioglitazone HCL and glimepiride in the treatment of type 2 diabetes. Vasc Health Risk Manag. 2007;3(5):721-31.