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Drugs of interest to pathologists

Drugs related to surgical pathology

Sunitinib malate

Author: Him G. Kwee, M.D. (see Reviewers/Authors page)
Revised: 8 November 2011, last major update October 2011
Copyright: (c) 2011, PathologyOutlines.com, Inc.


● An inhibitor of multiple tyrosine kinase (TK) enzymes such as: KIT (CD 117), PDGFR (platelet-derived growth factor receptors), VEGFR (vascular endothelial growth factor receptors), RET (rearranged during transfection proto-oncogene), CSF-1R (colony stimulating factor 1 receptor ) and flt3 (fms-related tyrosine kinase 3, Wikipedia)

Trade name

● Sutent

Clinical information

Approved by US Food and Drug Administration for:
● Gastrointestinal stromal tumor/GIST resistant to imatinib/Gleevec or for GIST patients that cannot tolerate imatinib (Lancet 2006;368:1329), approved January 2006
● Metastatic renal cell carcinoma (approved January 2006)
● Unresectable or metastatic pancreatic neuroendocrine tumor (approved May 2011, Sutent package insert)

● Cost: in 2006, $4480 per 6 weeks cycle or $17,920 per 6 months (National PBM Drug Monograph on Sunitinib)

Use for pathologists

Imatinib mesylate is approved by US Food and Drug Administration for first line treatment of GIST and sunitinib for second line treatment of GIST
● Both drugs bind to and stabilize the inactivated form of the receptor tyrosine kinases, but they differ in their binding targets as well as inhibitory activity
● Imatinib binds to amino acid residues within the ATP-binding pocket as well as the activation loop, whereas sunitinib interacts with different amino acid residues in the ATP binding pocket
● Sunitinib also posseses activity against VEGFR 1/3 and thus has antiangiogenic properties as well
● Sunitinib can also inhibit KIT-PDGFR wild type GIST including pediatric GIST (Arch Pathol Lab Med 2011;135:1298)

End of Drugs > Drugs related to surgical pathology > Sunitinib malate

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