Background:

Peroxisome proliferator-activated receptor gamma (PPARγ) agonists and PPARg/a dual agonists are used in the treatment of type 2 diabetes mellitus. Troglitazone is a prototypical sarcomagenic PPARg agonist.

In vitro: Troglitazone PPARγ ligands showed potent inhibitory effect on proliferation, and could induce RCC cell apoptosis, suggesting that the PPARγ ligands have potential antitumor effects on renal carcinoma cells [1].

In vivo: Troglitazone increased EC proliferation in brown and white adipose tissue and liver in mice at sarcomagenic doses (400 and 800 mg/kg) after four weeks of treatment [2].

Clinical trial: Several clinical trials have been conducted to investigate the efficacy, safety and pharmacokinetics of troglitazone in the liposarcoma and diabtes mellitus patients [3].

参考文献:
[1] Yang FG, Zhang ZW, Xin DQ, Shi CJ, Wu JP, Guo YL, Guan YF.  Peroxisome proliferator-activated receptor gamma ligands induce cell cycle arrest and apoptosis in human renal carcinoma cell lines. Acta Pharmacol Sin. 2005;26(6):753-61.
[2] Kakiuchi-Kiyota S, Arnold LL, Yokohira M, Koza-Taylor P, Suzuki S, Varney M, Pennington KL, Cohen SM.  Evaluation of direct and indirect effects of the PPARγ agonist troglitazone on mouse endothelial cell proliferation. Toxicol Pathol. 2011;39(7):1032-45.