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Tegavivint + gemcitabine is an investigational combination therapy being developed by Iterion Therapeutics for the treatment of relapsed or refractory pediatric osteosarcoma. Tegavivint is a first-in-class small molecule inhibitor of Transducin beta-like protein 1 (TBL1), a critical transcriptional regulator in the Wnt/β-catenin signaling pathway. By binding to TBL1, tegavivint disrupts the interaction between TBL1 and β-catenin, promoting the degradation of nuclear β-catenin and preventing the transcription of oncogenic genes. Gemcitabine is a nucleoside analogue chemotherapy agent that inhibits DNA synthesis and ribonucleotide reductase. The combination is currently being evaluated in Phase 2 clinical trials, and tegavivint has received Orphan Drug and Pediatric Rare Disease designations from the U.S. FDA for the treatment of osteosarcoma.
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