Cabozantinib, a potent inhibitor of MET, VEGFR2 and RET, is at present being investigated across several tumor types.
In preclinical studies, cabozantinib has demonstrated tumoricidal, antimetastatic and antiangiogenic effects such as extensive apoptosis of malignant cells, decreased tumor invasiveness and metastasis, decreased tumor and endothelial cell proliferation, blockade of metastatic bone lesion progression and disruption of tumor vasculature.
RET is a receptor tyrosine kinase that is frequently activated by point mutation in medullary thyroid carcinomas and MET is upregulated in many tumor types, thus facilitating tumor cell escape by promoting the formation of more aggressive phenotypes, resulting in metastasis.