A small-molecule inverse agonist of PPARγ for advanced solid tumors: a phase 1 trial - PubMed
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- #Urothelial carcinoma
- #PPARγ inverse agonist
- #Phase 1 trial
- FX-909 is a first-in-class oral small-molecule PPARγ inverse agonist.
- Phase 1A trial enrolled 56 patients with advanced solid tumors, including 46 with urothelial carcinoma.
- Primary endpoint was safety and tolerability; secondary endpoints included pharmacokinetics and antitumor activity.
- FX-909 showed acceptable safety profile with grade ≥3 adverse events like anemia (26.8%) and thrombocytopenia (21.4%).
- Doses of 30 mg and 50 mg daily were selected for phase 2 dose optimization.
- Objective responses observed in 17.5% of urothelial carcinoma patients across all dose levels.
- Tumor responses were enriched in patients with high PPARγ expression.
- Supports further clinical development in urothelial cancer.