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The target of cabozantinib
In vitro biochemical and/or cellular assays show that Cabozantinibinhibits the tyrosine kinase activity of MET, VEGFR-1, -2 and -3, AXL, RET, ROS1, TYRO3, MER, KIT, TRKB, FLT-3 and TIE-2. These receptor tyrosine kinases are involved in normal cellular functions and pathological processes, such as tumorigenesis, metastasis, tumor angiogenesis, drug resistance, and maintenance of the tumor microenvironment. Cabozantinib inhibits metastasis, angiogenesis, and tumorigenesis by inhibiting receptor tyrosine kinases. After 19 days of repeated daily administration of cabozantinib, the mean accumulation of cabozantinib was 4 to 5 times higher than that after a single dose; a steady state was reached on day 15.
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