Drug Overview Cabometyx (cabozantinib; Exelixis/Ipsen/Takeda) is an orally available small molecule inhibitor which has been shown to suppress tumor growth and metastasis by inhibiting the activity of multiple tyrosine kinases including MET, AXL, and vascular endothelial growth factor receptor (VEGFR). VEGF production is upregulated in renal cell carcinoma and results in increased tumor vascularization and disease progression. Standard first-line therapies such as Sutent (sunitinib; Pfizer) work by targeting VEGF/VEGFR signaling; however, tumors often develop resistance to these anti-angiogenic treatments. Aberrant expression of MET and AXL tyrosine kinases is associated with drug resistance and poor disease prognosis; by targeting MET and AXL, as well as VEGF/VEGFR signaling, Cabometyx may provide an alternative treatment option for patients in the relapsed setting.
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