Axitinib (AG 013736) is a potent multi-target tyrosine kinase inhibitor (TKI), which inhibits VEGFR1, VEGFR2, VEGFR3, PDGFR?, PDGFR? and c-Kit with IC50 values of 1.2 nM, 0.2 nM, 0.1 nM-0.3 nM, 1.6 nM, 5.0 nM, and 1.7 nM, respectively. [1] In human xenograft tumor models (nude mice), Axitinib (AG 013736) shows consistent antitumor efficacy across various tumor types, which is associated with reduction in vascular angiogenesis and tumor proliferation and increase in tumor apoptosis. [1]

Axitinib (AG 013736) resulted in significantly longer progression-free survival compared with sorafenib and has been approved as a second-line therapy of advanced renal cell carcinoma. [2]