Source of information: Drugbank (External Link). Last updated on: 3rd July 18
*Trade Name used in the content below may not be the same as the HSA-registered product.
Active Ingredient / Synonyms
Cabozantinib | Cabozantinib |
Cabozantinib was approved in 2012 and is a non-specific tyrosine kinase inhibitor. It is marketed as Cometriq, which is indicated for the treatment of metastatic medullary thyroid cancer. It's label includes a black box warning of gastrointestinal perforations, fistulas, and hemorrhage. The FDA approved cabozantinib as Cabometyx for patients with advanced renal cell carcinoma in April 2016.
For the treatment of metastatic medullary thyroid cancer and for the treatment of patients with advanced renal cell carcinoma (RCC) who have received prior anti-angiogenic therapy.
Mechanism of Action
Cabozantinib inhibits specific receptor tyrosine kinases such as VEGFR-1, -2 and -3, KIT, TRKB, FLT-3, AXL, RET, MET, and TIE-2.
Cabozantinib suppresses metastasis, angiogenesis, and oncognesis by inhibiting receptor tyrosine kinases.
After oral administration, peak plasma concentration was achieved in 2-5 hours.
The volume of distribution is 349L.
Cabozantinib is metabolized mostly by CYP3A4 and, to a minor extent, by CYP2C9. Both enzyme produce an N-oxide metabolite.
Cabozantinib is eliminated mostly by the feces (54%) and also by the urine (27%).
Cabozantinib has a long half-life of 55 hours.
At steady state, the clearance is 4.4 L/hr.
Cabozantinib has a black box warning of serious gastrointestinal fistulas and perforations, and potentially fatal hemoptysis and gastrointestinal hemorrhage.
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