Drug intelligence / Profile preview

SU014813

Development stage
Phase 2
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

SU014813 is an orally-active, small molecule multitargeted tyrosine kinase inhibitor with potential antitumor activity. It binds to and inhibits the phosphorylation of several receptor tyrosine kinases including vascular endothelial growth factor receptor 2 (VEGFR2), platelet-derived growth factor receptors (PDGFR) alpha and beta, c-Kit (KIT), and Fms-like tyrosine kinase 3 (FLT3). This inhibition leads to reduced cellular proliferation and angiogenesis as well as induction of apoptosis in tumor cells. Developed as a next-generation agent following sunitinib, it was designed for improved pharmacokinetic and tolerability profiles. Clinical studies have evaluated its use in combination with docetaxel for advanced solid tumors such as melanoma and gastrointestinal stromal tumors refractory to other TKIs[1][2][5][7].

Other names
1H-Pyrrole-3-carboxamide, 5-((5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl)-N-((2S)-2-hydroxy-3-(4-morpholinyl)propyl)-2,4-dimethyl-
02

Targets

FLT3 (Fms related receptor tyrosine kinase 3)VEGFR2 (Vascular endothelial growth factor receptor 2)PDGFRB (Platelet-derived growth factor receptor beta)VEGFR4 (Vascular endothelial growth factor Receptor-3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)VEGFR-1 (Vascular endothelial growth factor receptor 1)PDGFRA (Platelet-derived growth factor receptor alpha)

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