CAS Insight

molecules of the month


oral, selective beta-catenin/CBP PPI inhibitor

synergy w/ PD-1i in model, in Ph. I for cancer

opt. of prior peptidomimetic candidate

Cancer Res., Jan. 6, 2021

Eisai Co., Ltd., Tsukuba, JP

Chemical structure of molecule E7386 modulator
1 min read

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.

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