tegavivint

Tegavivint is a potent and specific small molecule inhibitor of the Wnt/beta-catenin signaling pathway with potential antineoplastic activity. It binds to transducin beta-like protein 1 (TBL1), disrupting the interaction between beta-catenin and TBL1. This leads to degradation of beta-catenin and reduced transcriptional activity of TCF4 and its downstream oncogenic targets such as cyclin D1, c-MYC, and survivin. The Wnt/beta-catenin pathway is implicated in cell proliferation and survival; its dysregulation is associated with various cancers. Tegavivint is being developed primarily for solid tumors (including desmoid tumors), Ewing sarcoma, osteosarcoma, liver cancer (hepatocellular carcinoma), Wilms tumor, lymphomas (including B-cell lymphoma), fibroma/desmoid tumor (orphan drug status for fibroma), and other malignancies characterized by aberrant Wnt signaling[1][3][5][7].

Brand names

tegavivint

Other names

Tegatrabetan9,10-anthracenedione, 2,7-bis(((3r,5s)-3,5-dimethyl-1-piperidinyl)sulfonyl)-, 9,10-dioxime, rel-SCHEMBL13366899SCHEMBL-13366899SCHEMBL 13366899BCP32893BCP-32893BCP 32893