Tivozanib is an orally available, selective VEGFR inhibitor with IC50 values of 0.21, 0.16, and 0.24 nM for VEGFR1, VEGFR2, and VEGFR3, respectively. It can also inhibit c-Kit and PDGFRβ with IC50 values of 1.63 and 1.72 nM, respectively. When administered to athymic rats, tivozanib was shown to decrease the microvessel density within tumor xenografts and attenuate VEGFR2 phosphorylation levels in tumor endothelium. It also displays antitumor activity against a wide variety of human tumor xenografts, including lung, breast, colon, ovarian, pancreas, and prostate cancer.
