e7386

E7386 is a first-in-class, orally bioavailable small molecule that selectively inhibits the interaction between CREB-binding protein (CBP) and β-catenin. By disrupting this protein-protein interaction at the most downstream point of the Wnt/β-catenin signaling pathway, E7386 modulates Wnt-dependent gene expression. This mechanism suppresses tumor growth driven by aberrant Wnt signaling—including tumors with mutations in APC or β-catenin—and may also enhance immune cell infiltration into tumors and synergize with immune checkpoint inhibitors such as anti-PD‑1 antibodies. Preclinical studies have demonstrated antitumor activity both as monotherapy and in combination regimens. Clinical trials are ongoing for advanced solid tumors and endometrial cancer[1][3][5][7].

Other names

CBP/beta-catenin Modulator E7386(6S,9aS)-N-benzyl-8-[[6-[3-(4-ethylpiperazin-1-yl)azetidin-1-yl]pyridin-2-yl]methyl]-6-[(2-fluoro-4-hydroxyphenyl)methyl]-4,7-dioxohexahydro-pyrazino[2,1-c][1,2,4]triazine carboxamide