VOTRIENT (Pazopanib) – antineoplastic agent, tyrosine kinase inhibitor. Actively affects many target receptors.
Pazopanib binds to receptors of vascular endothelial growth factor isolated from platelet growth factor and receptor of stem cell factor, while the inhibitory concentration of 50% (IC 50 ) is 10, 30, 47, 71, 84 and 74 nmol / L, respectively.
Pazopanib is an inhibitor of many tyrosine kinases, incl. tyrosine kinases of endothelial growth factor receptor-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 VEGFR-2 phosphorylation, angiogenesis, and the growth of certain human tumor xenografts in mice.