INTRODUCTION: Tivozanib is a novel tyrosine kinase inhibitor (TKI) which 
inhibits vascular endothelial growth factor (VEGF) receptors-1, -2, and -3 at 
nanomolar concentrations.
AREAS COVERED: A comprehensive MEDLINE and American Society of Clinical Oncology 
abstract search was performed to gather all relevant clinical and translational 
data related to tivozanib. We discuss pre-clinical studies associated with 
tivozanib, and the results of a Phase I assessment in advanced solid tumors. We 
highlight combination studies with tivozanib, including pairings of tivozanib 
with cytotoxic therapy in patients with colorectal cancer and breast cancer. A 
randomized discontinuation Phase II study and a randomized Phase III study 
assessing the activity of tivozanib in metastatic renal cell carcinoma (mRCC) 
are described in detail.
EXPERT OPINION: Tivozanib will face the challenge of entering an already crowded 
therapeutic space in mRCC-emerging combination studies and biomarker assessments 
may distinguish this agent among other VEGF-TKIs. The current review will 
outline the development pathway of tivozanib to date, and offer lessons learned 
and future opportunities.