Cabozantinib Chemical Properties
density 1.396
Safety Information
MSDS Information
Cabozantinib Usage And Synthesis
Anti-cancer drugs Cabozantinib is a kind of a novel type of molecular targeted drugs developed by the United States Exelixis biopharmaceutical company. On November 29, 2012, the US Food and Drug Administration (FDA) approved the use of cabozantinib for the treatment of unresectable malignant local advanced or metastatic medullary thyroid carcinoma.
In addition, Sorafenib, Vandernib and Levotinib have been approved by the Food and Drug Administration (FDA) for the treatment of advanced thyroid cancer.
Mechanism of action In vitro biochemical and/or cytological analysis have shown that cabozantinib can inhibit the tyrosine kinase activity of RET, human hepatocyte growth factor receptor (MET), vascular endothelial growth factor receptor 1 (VEGFR-1, VEGFR-2, VEGFR-3, stem cell factor receptor (KIT), receptor kinase receptor (TRKB), FMS-like tyrosine kinase-3, FLT-3), AXL and human tyrosine kinase with immunoglobulinlike and EGF-like domains 2, TIE-2. All the above kinase receptors play an important role in the growth of normal cells and tumor cells. The abnormal expression of these receptors is critical in the development and progression of many kinds of tumors, including the inhibition of tumor cell apoptosis, participating into the tumor angiogenesis and invasion and other pathological processes. Cabozantinib exerts its antitumor effect by inhibiting the above kinase activity, killing tumor cells, reducing metastasis and inhibiting tumor angiogenesis.
Pharmacokinetics The pharmacokinetic analysis showed that the half-life of this drug was about 55 h with the volume of distribution (V/F) being about 349L, and the clearance rate of CLL being about 4.4 L • h-1. Upon oral administration of this drug, the time for reaching plasma concentration peak time (tmax) is 2~5h. Compared with a single dose of oral administration of 140 mg • d ^ (-1) for 19 days, the exposure amount in vivo was increased t