Tivozanib, an oral formulation, is a selective tyrosine kinase inhibitor that targets all three VEGFR isoforms and has a long half-life. Tivozanib showed good drug activity and tolerability in phase II trials. The overall response rate was 24.0% (95% CI, 19% to 30%) and median progression-free survival was 11.7 months (95% CI, 8.3-14.3 months). The most common grade 3 or 4 treatment-related adverse event was hypertension (12.0%). 2012 American Society of Clinical Oncology (ASCO) meeting reported a phase III clinical trial comparing tivozanib with sorafenib in untreated or previously treated metastatic non-VEGF-targeted therapy or mammalian target of rapamycin (mTOR) inhibitor Patients with renal cancer, but results are not yet fully published. 70.0% of untreated patients were treated with a median progression-free survival of 12.7 months in the Tivozanib group and 9.1 months in the sorafenib group (HR= 0.756; 95% CI: 0.580 to 0.985). For all patient groups, the objective response rates were 33.0% and 23.0% in the Tivozanib and sorafenib groups, respectively. the most common adverse events (all grades ≥3) with Tivozanib were hypertension (46.0%/26.0%), diarrhea (22.0%/2.0%), malaise 18.0%/5.0%), and neutropenia ( 10.0%/2.0%). However, a subsequent final overall survival analysis showed that the overall survival of patients in the Tivozanib-treated group did not exceed that of patients treated with sorafenib; therefore, the FDA ultimately failed to approve Tivozanib for the treatment of metastatic kidney cancer.