Drugs of interest to pathologists
Drugs related to surgical pathology
Sunitinib malate

Topic Completed: 1 October 2011

Minor changes: 22 August 2019

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PubMed Search: Sunitinib malate [title] "loattrfree full text"[sb]

Him G. Kwee, M.D.
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Cite this page: Kwee HG. Sunitinib malate. PathologyOutlines.com website. http://www.pathologyoutlines.com/topic/drugssunitinib.html. Accessed August 14th, 2020.
Definition / general
  • 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: Article Sunitinib [Accessed 14 December 2018])
Trade name
  • Sutent®
Clinical information
Approved by U.S. Food and Drug Administration for:
Uses by pathologists
  • Imatinib mesylate is approved by U.S. 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 possesses 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)
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