Sunitinib malate is an oral, small-molecule, multi-targeted receptor tyrosine kinase (RTK) inhibitor that was approved by the FDA for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST) on January 26, 2006. Sunitinib was the first cancer drug simultaneously approved for two different indications.
Sunitinib inhibits cellular signaling by targeting multiple receptor tyrosine kinases (RTKs).
These include all receptors for platelet-derived (PDGF-Rs) and vascular endothelial receptors (VEGFRs), which play a role in both tumor angiogenesis and tumor cell proliferation.
Sunitinib Malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit
Usage A multi-kinase inhibitor targeting several receptor tyrosine kinases (RTK). Antineoplastic.
Sunitiba Malate is an antineoplastic agent and a potent RTK inhibitor which includes Flk-1 (VEGFR2) as a primary target. It also is a potent, ATP-competitive inhibitor of VEGFR, PDGFR-β and c-Kit (KIT). Sunitiba Malate inhibits cellular receptor phosphorylation of FLT3, RET and CSF-1R. Exhibits antiangiogenic and antitumor activity in multiple xenograft models. Sunitinib Malate is an inhibitor of c-Fms-CSF-1R, Flt-1, Flt-3/Flk-2, Flt-4, PDGFR-α and Ret.
