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Information about Cabozantinib

  Cabozantinib is orally available kinase inhibitor and antineoplastic agent that is used in treatment of advanced, metastatic medullary thyroid cancer and refractory renal cell carcinoma.


Liver safety of Cabozantinib

Cabozantinib is associated with a low rate of serum enzyme elevations during treatment and has been implicated with rare instances of clinically apparent, acute liver injury, some of which have been severe. 

Mechanism of action of Cabozantinib

Cabozantinib (ka" boe zan' ti nib) is an orally available, small molecule, multi-kinase inhibitor with activity against hepatocyte growth factor receptor (MET), vascular endothelial growth factor receptor 2 (VEGFR-2), and rearranged during transfection (RET), cell surface tyrosine kinase receptors which are overexpressed in several forms of cancer.  Cabozantinib has been evaluated as therapy of several forms of advanced and metastatic carcinomas and has shown efficacy in medullary thyroid and renal cell carcinoma. 

FDA approval information for Cabozantinib

Cabozantinib received accelerated approval for use in the United States in 2012 for therapy of medullary thyroid cancer after failure of other therapies. 

Clinical use of Cabozantinib

Indications were expanded in 2016 to include advanced renal cell carcinoma in addition to medullary thyroid cancer

Dosage and administration for Cabozantinib

For therapy of medullary thyroid cancer, cabozantinib is available as capsules of 20 and 80 mg under the brand name Cometriq, and the recommended dose is 140 mg orally once daily.  For treatment of advanced renal cell carcinoma, cabozantinib is available as tablets of 20, 40 and 60 mg under the brand name Cabometyx, and the recommended dose is 60 mg orally once daily. 

Side effects of Cabozantinib

Common side effects include diarrhea, fatigue, nausea, constipation, anorexia, weight loss, hand-foot syndrome, stomatitis, hypertension, change in hair color, thrombocytopenia, neutropenia, anemia, rash and fever.  Other uncommon, but potentially severe side effects include thrombotic events including myocardial infarction, stroke and arterial thromboses, osteonecrosis of the jaw, posterior leukoencephalopathy and fetal toxicity.

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