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Information about Sunitinib

Sunitinib is multi-specific tyrosine kinase receptor inhibitor that is used in the therapy of gastrointestinal stromal tumors and advanced renal cell carcinoma.

Liver safety of Sunitinib

Sunitinib therapy is associated with transient elevations in serum aminotransferase and bilirubin levels and rare instances of clinically apparent acute liver injury

Mechanism of action of Sunitinib

Sunitinib (soo ni' ti nib) is an inhibitor of several tyrosine kinase receptors which are associated with tumor growth and angiogenesis.  The tyrosine kinase receptors of cancer cells are often mutated and can cause unregulated cell growth and proliferation.  Sunitinib is one of several tyrosine kinase receptor inhibitors that have been introduced into cancer chemotherapy and are specially directed at molecular abnormalities that occur in cancer cells.  Inhibition of the receptor can lead to dramatic reversal of progression the cancer, although sometimes limited by the development of tumor resistance caused by mutations in the kinase.  Sunitinib has special activity against the abnormal tyrosine kinase (cKit) that is found in gastrointestinal stromal tumors (GIST).  Sunitinib also has activity against the receptors for platelet derived growth factor (PDGF) and vascular endothelial growth factor (VEGF). 

FDA approval information for Sunitinib

Sunitinib received approval for use in the United States in 2006.  Current indications are for unresectable or metastatic GIST with positive cKit (CD117), advanced renal cell carcinoma and advanced pancreatic neuroendocrine tumors.  Sunitinib is also used in patients who are intolerant or become resistant to imatinib, the initial tyrosine kinase receptor inhibitor that has special activity against chronic myelogenous leukemia (CML) bearing the Philadelphia chromosome. 

Dosage and administration for Sunitinib

Sunitinib is available in capsules of 12.5, 25 and 50 mg under the brand name Sutent.  The typical dose of sunitinib is in cycles of 4 weeks, followed by a rest period of 2 weeks, using a starting dose of 37.5 or 50 mg daily and increasing or decreasing in 12.5 mg increments, with each cycle based upon tolerance and response. 

Side effects of Sunitinib

Side effects include fatigue, diarrhea, anorexia, skin discoloration, rash, hand-foot syndrome, edema, muscle cramps, arthralgias, headache, abdominal discomfort, anemia, cough, and pruritus.  Uncommon side effects include heart failure, pancreatitis and renal failure.


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