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tegavivint + cabozantinib
- Development stage
- Phase 2
- Lead developer
- Iterion Therapeutics
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
**Tegavivint + cabozantinib** is an investigational combination therapy comprised of tegavivint, a selective inhibitor of the TBL1–beta-catenin interaction that disrupts Wnt/beta-catenin signaling, and cabozantinib, a multi-targeted tyrosine kinase inhibitor (TKI) approved for several solid tumors. Tegavivint has demonstrated the ability to induce nonapoptotic cancer cell death via mechanisms involving TECR-dependent lipid metabolism and directly disrupts tumor-promoting Wnt/beta-catenin signaling[2][4][6]. Cabozantinib targets a range of receptor tyrosine kinases including VEGFR, MET, and AXL, leading to inhibition of tumor angiogenesis, growth, invasion, and metastasis[3][5]. The combination is being investigated for synergistic antitumor activity, particularly in advanced hepatocellular carcinoma (HCC) and other solid tumors, aiming to overcome resistance pathways and enhance efficacy through complementary mechanisms[1].
- Other names
- tegavivint plus cabozantinib
02
Targets
AXL (AXL receptor tyrosine kinase)CTNNB1 (Beta-catenin)FLT3 (Fms related receptor tyrosine kinase 3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)MET (Mesenchymal-epithelial transition factor receptor)RET (Rearranged during transfection receptor tyrosine kinase)TEK (Tie2)VEGFR2 (Vascular endothelial growth factor receptor 2)MERTK (MER proto-oncogene, tyrosine kinase)NTRK2 (Tropomyosin-related kinase receptor type B)ROS1 (Proto-oncogene tyrosine-protein kinase ROS)TBL1X (Transducin beta-like protein 1)TECR (Trans-2,3-enoyl-CoA reductase)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR4 (Vascular endothelial growth factor Receptor-3)
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