Cabozantinib

Cabozantinib is a potent multi-targeted receptor tyrosine kinase (RTK) inhibitor of endothelial growth factor receptor 2 (VEGFR2) (IC50=0.035nM), the hepatocyte growth factor receptor c-Met (IC50=1.3nM), AXL (IC50=7nM), fms like tyrosine kinase 3 (FLT3) (IC50=11.3nM), mast/stem cell growth factor (KIT) (IC50=4.6nM), RET (IC50=5.2nM), tyrosine-protein kinase receptor (TIE-2) (IC50=14.3nM) and RON (IC50=124nM). Cabozantinib reduces cell proliferation and vascular density. It also induces apoptosis and intratumoral hypoxia. Cabozantinib exhibits dose-related tumor growth inhibition, tumor regression, angiogenesis and/or metastasis inhibition in a broad range of preclinical tumor models. The anticancer compound cabozantinib has undergone clinical trial in a broad number of cancers, including thyroid carcinoma, prostate cancer, ovarian cancer, melanoma, breast cancer, non-small cell lung cancer, hepatocellular cancer, renal cell carcinoma and glioblastoma.