VOTRIENT (Pazopanib) – an antitumor agent, tyrosine kinase inhibitor. Actively affects many target receptors.
Pazopanib binds to receptors for vascular endothelial growth factor isolated from growth factor platelets and stem cell factor receptor, with inhibitory concentrations of 50% (IC 50 ) of 10, 30, 47, 71, 84 and 74 nmol / L, respectively.
Pazopanib is an inhibitor of a variety of tyrosine kinases, including tyrosine kinase receptor for endothelial growth factors-1, 2, 3 (VEGFR-1, VEGFR-2, VEGFR-3), platelet growth factor receptor alpha and beta (PDGFR-α and PDGFR-β), fibroblast growth factor receptor-1 and – 3 (FGFR-1, -3), cytokine receptor (Kit), interleukin-2 receptor, induced by T-cell kinase (Itk), leukocyte-specific protein tyrosine kinase (Lck) and transmembrane glycoprotein tyrosine kinase receptor (c-Fms). In vitro, pazopanib inhibits ligand-induced autophosphorylation of VEGFR-2, Kit and PDGFR-β. In vivo, pazopanib inhibits VEGF-induced phosphorylation of VEGFR-2, angiogenesis, and the growth of some human tumor xenografts in mice.