With the development of metastatic renal cell carcinoma(mRCC) treatment,several new drugs have been approved in recent years,but mRCC remains incurable.Axitinib,a potent vascular endothelial growth factor receptor tyrosine kinase inhibitor,has been demonstrated to be effective in treatment of mRCC by phase Ⅰ and Ⅱ clinical trials,and its toxicity is mild to moderate and manageable.Recently compared with sorafenib,the phase HI randomized clinical trial demonstrated an improvement in progression-free survival for patients with mRCC who were treated with axitinib as second-line therapy.The US Food and Drug Administration(FDA) approved axitinib for use in patients with mRCC who had failed to respond to a previous treatment.This article reviewed the preclinical and clinical evolution of axitinib,with a emphasis on its role in mRCC.