INTRODUCTION: Advanced understanding of the pathogenesis of renal cell carcinoma 
(RCC) has led to development and approval of several molecularly targeted 
therapies since 2005. Axitinib is a potent and selective inhibitor of vascular 
endothelial growth factor receptors 1, 2 and 3. In the randomized Phase III AXIS 
trial, axitinib significantly prolonged progression-free survival compared with 
sorafenib, respectively (6.7 vs 4.7 months; p < 0.0001), and improved objective 
response rate (19 vs 9%; p = 0.0001), resulting in its approval for advanced or 
metastatic RCC after failure of one systemic therapy. However, overall survival 
was similar with axitinib and sorafenib. Common adverse events associated with 
axitinib include diarrhea, hypertension and fatigue.
AREAS COVERED: The properties, clinical efficacy, adverse events, 
pharmacokinetics and pharmacodynamics of axitinib are summarized and its 
position in the overall therapeutic landscape for metastatic RCC among several 
targeted therapies is described.
EXPERT OPINION: Axitinib is generally well-tolerated and provides definitive 
clinical benefits in patients with advanced or metastatic RCC as second-line 
therapy. However, as with other tyrosine kinase inhibitors of the same class, 
axitinib does not prolong overall survival; therefore, selection of second-line 
tyrosine kinase inhibitor therapy, including axitinib, must be carefully 
considered to maximize outcomes for each patient.