Products
Cabozantinib is commercially available in the form of film-coated tablets (Cabometyx). It was approved in the United States in 2012, in the EU in 2013, and in many countries in 2017. In some countries, Cometriq capsules are additionally on the market for the treatment of medullary thyroid carcinoma. This article relates to renal cell carcinoma therapy.
Structure and properties
Cabozantinib (C28H24FN3O5, Mr = 501.5 g/mol) is present in the drug as cabozantinibmalate, a white substance that is practically insoluble in water. It is a dicarboxamide and a quinoline derivative.
Effects
Cabozantinib (ATC L01XE26) has antitumor, antiproliferative, and antiangiogenic properties. The effects are due to inhibition of several tyrosine kinases (RET, MET, VEGFR-1, -2, -3, KIT, TRKB, FLT-3, AXL, TIE-2) involved in tumorigenesis and growth and vascularization. The half-life is in the range of 99 hours.
Indications
For the treatment of advanced renal cell carcinoma.
Dosage
According to the SmPC. Tablets are taken once daily. Nothing should be eaten 2 hours before taking and until 1 hour after taking.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
Cabozantinib is a substrate of CYP344 isozymes and corresponding interactions are possible.
Adverse effects
The most common potential adverse effects include diarrhea, fatigue, nausea, poor appetite, weight loss, palmar-plantar erythrodysesthesia syndrome, hypertension, vomiting, and constipation.
