Products
Sunitinib is commercially available in capsule form (Sutent). It has been approved in many countries since 2006.
Structure and properties
Sunitinib (C22H27FN4O2, Mr = 398.5 g/mol) is present in the drug as sunitinibmalate, a yellow to orange powder that is soluble in water. It is an indolin-2-one and pyrrole derivative. It has an active -desethyl metabolite (SU012662).
Effects
Sunitinib (ATC L01XE04) has antiproliferative, antitumor, and antiangiogenic properties. The effects are due to inhibition of several tyrosine kinases. These include PDGFR, VEGFR, KIT, FLT3, CSF-1R and RET. These kinases are involved in tumor development, growth, vascularization and metastasis. Sunitinib has a long half-life of up to 40-60 hours. The active metabolite is effective for even longer.
Indications
- Renal cell carcinoma
- Malignant gastrointestinal stromal tumor
- Neuroendocrine pancreatic carcinoma
Dosage
According to the professional information. The capsules are taken once a day and independently of meals.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
Sunitinib is metabolized by CYP3A4 and appropriate drug interactions with CYP inhibitors and inducers are possible. It should not be administered with P-gp inhibitors.
Adverse effects
The most common possible adverse effects include fatigue, digestive symptoms such as diarrhea, nausea, oral mucositis, dyspepsia, and vomiting, skin discoloration, hand-foot syndrome, taste changes, poor appetite, and hypertension.
