Tivozanib, a highly potent and selective inhibitor of VEGF receptor tyrosine kinases, for the treatment of metastatic renal cell carcinoma.

The VHL mutation-HIF upregulation-VEGF transcription sequence is the principal pathway in the development of renal cell carcinoma. Tyrosine kinase inhibitors target the VEGF receptors to inhibit further growth of renal cell carcinoma tumors. Tivozanib, originally named AV-951 and KRN-951, is a novel, orally bioavailable VEGF tyrosine kinase inhibitor that is selective for VEGF receptors 1, 2 and 3. Further, only picomolar concentrations of tivozanib are required to target these VEGF receptors and prevent phosphorylation; this potency prevents the debilitating side effects that occur with treatments whose mechanisms of action involve broad-spectrum tyrosine kinase inhibition. This review summarizes the growing body of evidence supporting tivozanib's efficacy and safety in the treatment of advanced renal cell carcinoma.

Future oncology (London, England). 2020 Jul 21 [Epub ahead of print]

Allen Jacob, Jaret Shook, Thomas E Hutson

Department of Internal Medicine, Baylor Scott & White Medical Center-Temple, 2401 South 31st Street, Temple, TX 76508, USA., Ohio Northern University Raabe College of Pharmacy, 525 South Main Street, Ada, OH 45810, USA., Division of Genitourinary Oncology, Charles A Sammons Cancer Center, Baylor University Medical Center, Texas Oncology, 3410 Worth Street STE 400, Dallas, TX 75246, USA.