Drug intelligence / Profile preview

sunitinib

Development stage
Approved
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Sunitinib is an orally administered small-molecule multi-targeted receptor tyrosine kinase (RTK) inhibitor developed for the treatment of various cancers. It inhibits cellular signaling by targeting multiple RTKs, including platelet-derived growth factor receptors (PDGFRα and PDGFRβ), vascular endothelial growth factor receptors (VEGFR1, VEGFR2, VEGFR3), stem cell factor receptor (KIT), Fms-like tyrosine kinase-3 (FLT3), colony stimulating factor receptor type 1 (CSF-1R), and glial cell-line derived neurotrophic factor receptor (RET). By blocking these kinases, sunitinib interferes with tumor growth, pathologic angiogenesis, and metastatic progression. Sunitinib is primarily indicated for advanced renal cell carcinoma (RCC), imatinib-resistant gastrointestinal stromal tumor (GIST), adjuvant treatment of RCC at high risk of recurrence following nephrectomy, and progressive well-differentiated pancreatic neuroendocrine tumors in adults with unresectable locally advanced or metastatic disease[5][7][8].

Brand names
Sutent
Other names
sunitinib malate
02

Targets

MET (Mesenchymal-epithelial transition factor receptor)KIT (c-KIT proto-oncogene receptor tyrosine kinase)ABL2 (ABL proto-oncogene 2, non-receptor tyrosine kinase)PDGFRB (Platelet-derived growth factor receptor beta)VEGFR2 (Vascular endothelial growth factor receptor 2)CSF1R (Macrophage colony-stimulating factor receptor)PDGFRA (Platelet-derived growth factor receptor alpha)EGFR T790M (Epidermal growth factor receptor T790M mutant)VEGFR3 (Vascular endothelial growth factor receptor 3)VEGFR-1 (Vascular endothelial growth factor receptor 1)FGFR1 (Fibroblast growth factor receptor 1)RET (Rearranged during transfection receptor tyrosine kinase)FLT3 (Fms related receptor tyrosine kinase 3)

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