FTX-6746 / Flare Therap - LARVOL DELTA

Novel inhibitors of the luminal lineage transcription factor peroxisome proliferator-activated receptor gamma (PPARG) durably eradicate tumors in urothelial cancer (UC) animal models (AACR-NCI-EORTC 2022) - "Material and The PPARG inhibitor FTX-6746 was evaluated in UC cell lines including UMUC9 (PPARG amplification) and HT1197 (RXRA-S427F hotspot mutation), which activate PPARG by different genetic mechanisms... These collective results suggest that PPARG is a lineage-defining transcription factor in UC and small molecule PPARG inhibition will be an effective therapy for patients with advanced urothelial cancer harboring the luminal subtype. Model Dose (mg/kg) Schedule %Tumor Growth Inhibition %Target Gene Suppression (D2) UMUC9 3 BID*20 59 16 UMUC9 10 BID*20 70 ND UMUC9 30 BID*20 83 73 UMUC9 30 BID*21 105 80 UMUC9 60 BID*21 108 ND HT1197 30 BID*42 85 46 HT1197 60 BID*42 112 59"

Preclinical • Breast Cancer • Genito-urinary Cancer • Hormone Receptor Breast Cancer • Oncology • Solid Tumor • Urothelial Cancer • ER • PPARA • PPARG • RXRA

Flare Therapeutics Presents Preclinical Data that Show Potential of Novel PPARG Inhibitors to Treat Urothelial Cancer at 2022 EORTC-NCI-AACR Symposium (Businesswire) - "Flare Therapeutics...presented new preclinical data in a poster presentation...at the 34th EORTC-NCI-AACR Symposium in Barcelona, Spain. The data...show that FTX-6746, a potent, selective, small molecule PPARG inhibitor (inverse agonist), drives robust PPARG target gene silencing in UC cell lines and drives tumor regression in PPARG-amplified and RXRA-mutant UC xenograft models....Tumor growth inhibition or regression was observed in PPARG-amplified and RXRA-mutant UC xenograft models, with no tumor regrowth upon cessation of treatment."

Preclinical • Genito-urinary Cancer • Oncology • Solid Tumor • Urothelial Cancer