FTX-6746

FTX-6746 is a potent, highly selective, and orally bioavailable small molecule inhibitor of peroxisome proliferator-activated receptor gamma (PPARG, PPARγ). Developed by Flare Therapeutics, it functions as an inverse agonist that drives robust silencing of PPARG target genes. The compound demonstrates significant anticancer activity, particularly in urothelial carcinoma (UC) models characterized by PPARG amplification or RXRA mutations, where it has been shown to drive tumor regression in xenograft models. FTX-6746 exhibits high potency with a cellular IC50 of 5 nM and maintains greater than 100-fold selectivity over other PPAR isoforms, specifically PPARA and PPARD.