FTX-6746
/ Flare Therap
- LARVOL DELTA
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September 03, 2022
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
October 26, 2022
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
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