Multi-receptor tyrosine kinase (VEGFR1-3, FGFR1-4, PDGFRα, RET, KIT) (RTK (Multi-target))

This target profile represents a specific cluster of receptor tyrosine kinases (RTKs) that are central to tumor growth, angiogenesis, and lymphangiogenesis. It includes the Vascular Endothelial Growth Factor Receptors (VEGFR1, VEGFR2, and VEGFR3), which are the primary drivers of blood and lymphatic vessel formation in the tumor microenvironment [FDA Lenvima Label]. The Fibroblast Growth Factor Receptors (FGFR1, FGFR2, FGFR3, and FGFR4) are also included, which play critical roles in cell proliferation, survival, and the development of resistance to anti-angiogenic therapies [PubChem CID 9823820]. Additionally, the profile covers Platelet-Derived Growth Factor Receptor alpha (PDGFRα), the RET proto-oncogene, and the KIT receptor (c-Kit), all of which contribute to oncogenic signaling and the maintenance of the tumor stroma [UniProt P07949, P10721]. Drugs targeting this specific combination, most notably the multi-kinase inhibitor lenvatinib, are utilized in the treatment of advanced malignancies such as differentiated thyroid cancer, hepatocellular carcinoma, and renal cell carcinoma [NCI Drug Dictionary]. By simultaneously inhibiting these diverse pathways, these therapies aim to disrupt the tumor's blood supply while directly inhibiting the signaling cascades that drive cancer cell division and survival.

Other names

Vascular endothelial growth factor receptor 1 (FLT1)Vascular endothelial growth factor receptor 2 (KDR)Vascular endothelial growth factor receptor 3 (FLT4)Fibroblast growth factor receptor 1 (FGFR1)Fibroblast growth factor receptor 2 (FGFR2)Fibroblast growth factor receptor 3 (FGFR3)Fibroblast growth factor receptor 4 (FGFR4)Platelet-derived growth factor receptor alpha (PDGFRA)Proto-oncogene tyrosine-protein kinase receptor Ret (RET)Mast/stem cell growth factor receptor Kit (KIT)Lenvatinib target profile

Inhibition of the adenosine triphosphate (ATP) binding site of multiple receptor tyrosine kinases, preventing phosphorylation and downstream signaling.