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Therapy Name | Tegavivint |
Synonyms | |
Therapy Description |
Tegavivint (BC2059) binds to beta-catenin (CTNNB1) and interferes with binding to TBL1 and TBLR1, resulting in increased degradation of beta-catenin and potentially leading to increased apoptosis of tumor cells with activated canonical Wnt signaling (PMID: 28500235, PMID: 30793158). |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
Tegavivint | BC-2059|BC 2059|Tegatrabetan|BC2059 | CTNNB1 Inhibitor 27 | Tegavivint (BC2059) binds to beta-catenin (CTNNB1) and interferes with binding to TBL1 and TBLR1, resulting in increased degradation of beta-catenin and potentially leading to increased apoptosis of tumor cells with activated canonical Wnt signaling (PMID: 28500235, PMID: 30793158). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
CTNNB1 act mut | hepatocellular carcinoma | predicted - sensitive | Tegavivint | Phase Ib/II | Actionable | In a Phase I/II trial, Tegavivint (BC2059) treatment was tolerated and demonstrated preliminary efficacy with 1 partial response (PR) and stable disease (SD) in 8 of 15 evaluable patients with advanced hepatocellular carcinoma, 6 of the 7 patients harboring CTNNB1 activation mutations achieved a best response of PR or SD, comparing to 3 in 8 of the CTNNB1 wild-type patients (Cancer Res (2025) 85 (8_Supplement_2): CT032; NCT05797805). | detail... |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
---|---|---|---|---|---|---|
NCT04851119 | Phase Ib/II | Tegavivint | Tegavivint for the Treatment of Recurrent or Refractory Solid Tumors, Including Lymphomas and Desmoid Tumors | Recruiting | USA | 0 |
NCT05755087 | Phase I | Tegavivint | Tegavivint for Treating Patients With Relapsed or Refractory Large B-Cell Lymphoma | Recruiting | USA | 0 |
NCT03459469 | Phase I | Tegavivint | Phase I, Open-label, Non-randomized Study to Evaluate Safety of BC2059 | Completed | USA | CAN | 0 |
NCT05797805 | Phase Ib/II | Tegavivint Lenvatinib + Tegavivint Cabozantinib + Tegavivint | A Study of Tegavivint (BC2059) in Patients With Advanced Hepatocellular Carcinoma | Recruiting | USA | CAN | 0 |