Vandetanib is a multi-kinase inhibitor targeting primarily receptor tyrosine kinases, such as vascular endothelial growth factor receptors (VEGFR1, KDR, and FLT4), epidermal growth factor receptor (EGFR), and fibroblast growth factor receptor (FGFR; Morabito et al.) It most potently inhibits KDR with an IC50 of 40 nM
It also inhibits non-receptor tyrosine kinases such as RET, ABL, and SRC as well as several serine/threonine kinases (Carlomagno et al.; Hennequin et al.; Kiselyov et al.; Levinson & Boxer)
Inhibits tumor growth in mouse xenograft models, including RET/PTC papillary thyroid carcinoma and lung carcinoma (Hennequin et al.; Carlomagno et al.)
Inhibits angiogenesis, cell growth, and metastasis in numerous cancer cell lines (Morabito et al.; Wedge et al.)