ABT-869

ABT-869 (Linifanib) is an ATP-competitive, multi-targeted RTK inhibitor that is completely effective against all members of the vascular endothelial growth factor (VEGF) and platelet derived growth factor (PDGF) receptor families. ABT-869 (Linifanib) showed potent antiproliferative and apoptotic properties in vitro and in animal cancer xenograft models. The kinase inhibition profile of ABT-869 is evident in cellular assays of RTK phosphorylation (IC₅₀ values of 2, 4 and 7 nM for PDGFRβ, KDR and CSF-1R, respectively) and VEGF-stimulated proliferation (0.2 nM IC₅₀ for human endothelial cells). ABT-869 is active in advanced non-small cell lung cancer as second- or third-line therapy. Increased adverse event rates were observed at the high dose of linifanib.