Axitinib (AG-013736)

Recent Results Cancer Res. 2010;184:33-44. doi: 10.1007/978-3-642-01222-8_3.


The vascular endothelial growth factor (VEGF)/VEGF receptor tyrosine kinase (RTK) signaling pathway plays a pivotal role in tumor angiogenesis. Neovascularization promotes increased tumor cell proliferation, survival and metasasis. Many antiangiogenic agents including multi-RTK inhibitors are either approved or are undergoing testing in clinical trials. Axitinib is a potent and selective inhibitor of VEGF RTK 1, 2, and 3. This chapter discusses the stucture of axitinib as well as its toxicities and drug interactions. Important preclinical and clinical data for axitinib are presented including findings from phase II studies in many tumor types including malignant melanoma and renal, pancreatic, thyroid, breast, lung and colorectal carcinomas. Ongoing phase III studies in pancreatic and metastatic renal cell carcinoma will ultimately define the therapeutic role of this targeted agent.

Publication types

  • Review

MeSH terms

  • Angiogenesis Inhibitors / therapeutic use*
  • Animals
  • Axitinib
  • Biological Availability
  • Breast Neoplasms / drug therapy
  • Clinical Trials as Topic
  • Female
  • Humans
  • Imidazoles / adverse effects
  • Imidazoles / pharmacokinetics
  • Imidazoles / pharmacology
  • Imidazoles / therapeutic use*
  • Indazoles / adverse effects
  • Indazoles / pharmacokinetics
  • Indazoles / pharmacology
  • Indazoles / therapeutic use*
  • Neoplasms / drug therapy*
  • Pancreatic Neoplasms / drug therapy
  • Thyroid Neoplasms / drug therapy


  • Angiogenesis Inhibitors
  • Imidazoles
  • Indazoles
  • Axitinib