Therapeutic Targets of Vandetanib

Vandetanib (Vandetanib) can inhibit the tyrosine kinase activity of members of the EGFR and VEGFR families, RET, BRK, TIE2, and EPH receptor and Src kinase families. These receptor tyrosine kinases are involved in normal cellular functions and pathological processes, such as tumorigenesis, metastasis, tumor angiogenesis, and maintenance of the tumor microenvironment. In vitro, vandetanib inhibits epidermal growth factor (EGF)-stimulated receptor tyrosine kinase phosphorylation in tumor cells and endothelial cells and inhibits VEGF-stimulated tyrosine kinase phosphorylation in endothelial cells. In vivo, vandetanib administration reduced tumor cell-induced angiogenesis, tumor vascular permeability, and inhibited tumor growth and metastasis in mouse models of cancer.