Tivozanib CAS# 475108-18-0 替沃扎尼

Tivozanib (AV-951) is a potent, selective, orally bioavailable inhibitor of vascular endothelial growth factor receptors (VEGFR) 1, 2, and 3. In preclinical kinase assays, it inhibited VEGFR2 with an IC50 of ~0.16 nM and showed >100-fold selectivity over other tyrosine kinases. In endothelial cell models, tivozanib blocked VEGF-induced proliferation and tube formation at low nanomolar concentrations. In tumor xenograft models, oral administration significantly inhibited angiogenesis and tumor growth across multiple cancer types, including renal and colon carcinomas. Pharmacokinetic studies demonstrated good oral bioavailability, sustained plasma exposure, and strong correlation between VEGFR inhibition and antitumor efficacy, supporting its clinical development.