Iterion Therapeutics is developing Tegavivint, a first-in-class small molecule that shuts down oncogenic Wnt/β-catenin signaling by targeting TBL1, a key nuclear co-activator required for β-catenin–driven transcription. By selectively degrading nuclear β-catenin, Tegavivint blocks oncogenic activity while avoiding the toxicities seen with upstream Wnt inhibitors. It is the most advanced Wnt/β-catenin inhibitor in development, with relevance across 500,000+ cancers annually.
Iterion’s lead focus is advanced HCC, where ~40% of patients harbor Wnt-pathway mutations and no targeted therapies exist. In Phase 1, Tegavivint showed partial responses, durable disease control, ctDNA declines, and liver function improvement in heavily pre-treated, Wnt-mutated HCC patients, with strong safety and tolerability. Tegavivint is positioned to become the first targeted therapy for Wnt-mutated HCC, with expansion opportunities in CRC and other Wnt-driven tumors.
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