Drugs of interest to pathologists
Drugs related to surgical pathology
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)
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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