Sunitinib

DB01268ApprovedInvestigationalSmall moleculeKinase Inhibitor

Sunitinib is a receptor tyrosine kinase inhibitor and chemotherapeutic agent used for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST). For these purposes, sunitinib is generally available as an orally administered formulation.

Mechanism: Sunitinib is a small molecule that inhibits multiple RTKs, some of which are implicated in tumor growth, pathologic angiogenesis, and metastatic progression of cancer. Sunitinib was evaluated for its inhibitory activity against a variety of kinases (>80 kinases) and was identified as an inhibitor of platelet-derived growth factor receptors (PDGFRa and PDGFRb), vascular endothelial growth factor receptors (VEGFR1, VEGFR2 and VEGFR3), stem cell factor receptor (KIT), Fms-like tyrosine kinase-3 (FLT3), colony stimulating factor receptor Type 1 (CSF-1R), and the glial cell-line derived neurotrophic factor receptor (RET). Sunitinib inhibition of the activity of these RTKs has been demonstrated in biochemical and cellular assays, and inhibition of function has been demonstrated in cell proliferation assays. The primary metabolite exhibits similar potency compared to sunitinib in biochemical and cellular assays.
Curator reviewed
Primary indication: Sunitinib is indicated for the following conditions: - Treatment of adult patients with gastrointestinal stromal tumor (GIST) following disease progression on (or intolerance to) imatinib mesylate - Treatment of adult patients with advanced renal cell...Curator reviewed · 5 structured indications
Formula / weight: C₂₂H₂₇FN₄O₂ · 398.4738 g/mol (avg)
First approval: Canada, 2006 · United States, 2006 · European Union, 2016
Code names: SU-011248 · SU-11248
Brand names: Sunitinib Accord
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