Morphogenesis

The CREB-binding protein (CBP)/beta-catenin inhibitor E7386, co-created by Eisai and PRISM BioLab, achieved the clinical POC (Proof of Concept)

Retrieved on: 
Monday, November 1, 2021

The E7386 targets, beta-catenin, is considered to be one of the undruggable targets that are particularly difficult to develop into drug discovery.

Key Points: 
  • The E7386 targets, beta-catenin, is considered to be one of the undruggable targets that are particularly difficult to develop into drug discovery.
  • E7386 is a CBP / beta-catenin inhibitor that inhibits CBP and beta-catenin protein-protein interactions and regulates the Wnt signal-dependent gene expression.
  • (1)
    Based on the POC achievement, Eisai has initiated a phase Ib/II clinical trial (Study 201) of E7386 in combination with anti-PD-1 therapy pembrolizumab for solid tumors in Japan.
  • E7386 is a CBP / beta-catenin inhibitor that inhibits protein-protein interactions between the transcription coactivator CBP and beta-catenin, and regulates the Wnt signaling-dependent gene expression.