Products
Axitinib was approved in many countries in 2012 in film-coated tablet form (Inlyta).
Structure and properties
Axitinib (C22H18N4OS, Mr = 386.5 g/mol) is a benzamide and benzindazole derivative. It exists as a white to slightly yellow powder.
Effects
Axitinib (ATC L01XE17) has antitumor properties. The effects are due to inhibition of VEGFR-1, -2, and -3 (vascular endothelial growth factor receptors). These are involved in new vessel formation and tumor growth.
Indications
For the treatment of patients with advanced renal cell carcinoma (RCC) after failure of prior systemic therapy.
Dosage
According to the SmPC. Axitinib is usually taken twice daily, 12 hours apart, with or without food.
Contraindications
- Hypersensitivity
Full details of precautions and interactions can be found in the drug label.
Interactions
Axitinib is metabolized primarily by CYP3A4/5 and to a lesser extent by CYP1A2, CYP2C19, and UGT1A1. Corresponding interactions with CYP inhibitors and inducers are possible.
Adverse effects
The most common possible adverse effects include diarrhea, high blood pressure, fatigue, lack of appetite, nausea, voice disorders, hand-foot syndrome, reduced body weight, vomiting, and constipation.
