molecules of the month

The Eisai β-catenin/CBP inhibitor, E7386, is an orally active and selective inhibitor of the β-catenin/CBP protein-protein interaction, a key node in the long studied Wnt/β-catenin pathway in cancer. Prior attempts to drug Wnt directly were met with severe toxicity in clinical trials. The pathway has seen a resurgence in interest due to its potential role in tumor immune evasion, and the Eisei team demonstrates that E7386 synergizes with anti-PD-1 in a syngeneic model. E7386 is currently in a Ph. I study as a monotherapy for solid tumors.