Drug intelligence / Profile preview

tegavivint + lenvatinib

Development stage
Phase 2
Lead developer
Iterion Therapeutics
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination therapy consisting of **tegavivint**, a small molecule targeting the Wnt/β-catenin signaling pathway, and **lenvatinib**, an orally available multi-targeted tyrosine kinase inhibitor. Tegavivint inhibits β-catenin-mediated transcription by disrupting its interaction with TBL1 and triggers a unique TECR-dependent, nonapoptotic cell death mechanism in cancer cells, particularly active in sarcomas and other solid tumors. Lenvatinib inhibits vascular endothelial growth factor receptors (VEGFR1, VEGFR2, VEGFR3), fibroblast growth factor receptors (FGFR1-4), platelet-derived growth factor receptor alpha (PDGFRα), KIT, and RET, impeding angiogenesis and tumor proliferation. This combination is currently under clinical investigation for solid tumors, including advanced hepatocellular carcinoma and recurrent or refractory solid tumors[2][4][5][6][8].

02

Targets

TBL1X (Transducin beta-like protein 1)CTNNB1 (Beta-catenin)FGFR1 (Fibroblast growth factor receptor 1)FGFR2 (Keratinocyte growth factor receptor)FGFR3 (Fibroblast growth factor receptor 3)FGFR4 (Fibroblast growth factor receptor 4)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFRA (Platelet-derived growth factor receptor alpha)RET (Rearranged during transfection receptor tyrosine kinase)TECR (Trans-2,3-enoyl-CoA reductase)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)

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