Axitinib--a selective inhibitor of the vascular endothelial growth factor (VEGF) receptor.
An improved understanding of the molecular biology involved in many solid tumors has led to the development of novel targeted agents. Axitinib is a potent and selective inhibitor of vascular endothelial growth factor (VEGF) receptor tyrosine kinases 1, 2, and 3. This review presents preclinical and clinical data available for axitinib, including findings from key phase II clinical trials in a wide variety of tumors including melanomas and renal, pancreatic, thyroid, breast, lung, and colorectal carcinomas. The differences between axitinib and other VEGFR inhibitors are explored and details of the possible use of blood pressure elevation and erythropoietin blood levels as predictive markers of VEGF/VEGFR pathway inhibition are outlined. Ongoing Phase III studies in pancreatic and metastatic renal cell carcinoma should help to determine the optimum utilization of these agents at the appropriate stage of disease.
Kelly
Ronan J
RJ
National Cancer Institute, Medical Oncology Branch, Center for Cancer Research, Bethesda, MD 20892, USA.
Rixe
Olivier
O
D020533:Angiogenesis Inhibitors / Q000008:administration & dosage* / Q000627:therapeutic use; D000818:Animals; D000970:Antineoplastic Agents / Q000627:therapeutic use; D000077784:Axitinib; D004195:Disease Models, Animal; D016503:Drug Delivery Systems; D007093:Imidazoles / Q000008:administration & dosage* / Q000627:therapeutic use; D007191:Indazoles / Q000008:administration & dosage* / Q000627:therapeutic use; D008175:Lung Neoplasms / Q000188:drug therapy*; D051379:Mice; D008819:Mice, Nude; D009368:Neoplasm Transplantation; D009389:Neovascularization, Pathologic / Q000188:drug therapy*; D040262:Receptors, Vascular Endothelial Growth Factor / Q000037:antagonists & inhibitors*; D015398:Signal Transduction; D042461:Vascular Endothelial Growth Factor A / Q000008:administration & dosage* / Q000037:antagonists & inhibitors; D023041:Xenograft Model Antitumor Assays
D020533:Angiogenesis Inhibitors; D000970:Antineoplastic Agents; D007093:Imidazoles; D007191:Indazoles; D042461:Vascular Endothelial Growth Factor A; D000077784:Axitinib; D040262:Receptors, Vascular Endothelial Growth Factor