Tegavivint Targets β-Catenin in aHCC with Promising Safety and Activity

In this Phase 1/2 study, weekly intravenous tegavivint—a TBL1 inhibitor disrupting Wnt/β-catenin signaling—demonstrated manageable safety across dose levels (3–5 mg/kg) with some Grade 3 bilirubin elevations resolving without liver injury, and among 15 evaluable advanced HCC patients, one partial response and stable disease in eight patients—with notably enhanced responses among those with β-catenin activating mutations.

These early findings indicate that tegavivint could be an effective targeted approach for aHCC, particularly for patients harboring β-catenin pathway mutations, potentially addressing a critical need in this challenging population.