Axitinib for the treatment of advanced renal cell carcinoma

Expert Opin Pharmacother. 2014 Feb;15(2):283-97. doi: 10.1517/14656566.2014.868436. Epub 2013 Dec 13.

Abstract

Introduction: Advanced understanding of the pathogenesis of renal cell carcinoma (RCC) has led to development and approval of several molecularly targeted therapies since 2005. Axitinib is a potent and selective inhibitor of vascular endothelial growth factor receptors 1, 2 and 3. In the randomized Phase III AXIS trial, axitinib significantly prolonged progression-free survival compared with sorafenib, respectively (6.7 vs 4.7 months; p < 0.0001), and improved objective response rate (19 vs 9%; p = 0.0001), resulting in its approval for advanced or metastatic RCC after failure of one systemic therapy. However, overall survival was similar with axitinib and sorafenib. Common adverse events associated with axitinib include diarrhea, hypertension and fatigue.

Areas covered: The properties, clinical efficacy, adverse events, pharmacokinetics and pharmacodynamics of axitinib are summarized and its position in the overall therapeutic landscape for metastatic RCC among several targeted therapies is described.

Expert opinion: Axitinib is generally well-tolerated and provides definitive clinical benefits in patients with advanced or metastatic RCC as second-line therapy. However, as with other tyrosine kinase inhibitors of the same class, axitinib does not prolong overall survival; therefore, selection of second-line tyrosine kinase inhibitor therapy, including axitinib, must be carefully considered to maximize outcomes for each patient.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / adverse effects
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use
  • Axitinib
  • Carcinoma, Renal Cell / drug therapy*
  • Carcinoma, Renal Cell / pathology
  • Disease-Free Survival
  • Humans
  • Imidazoles / adverse effects
  • Imidazoles / pharmacology
  • Imidazoles / therapeutic use*
  • Indazoles / adverse effects
  • Indazoles / pharmacology
  • Indazoles / therapeutic use*
  • Kidney Neoplasms / drug therapy*
  • Kidney Neoplasms / pathology
  • Molecular Targeted Therapy
  • Niacinamide / analogs & derivatives
  • Niacinamide / therapeutic use
  • Phenylurea Compounds / therapeutic use
  • Protein Kinase Inhibitors / adverse effects
  • Protein Kinase Inhibitors / pharmacology
  • Protein Kinase Inhibitors / therapeutic use
  • Sorafenib
  • Survival Rate

Substances

  • Antineoplastic Agents
  • Imidazoles
  • Indazoles
  • Phenylurea Compounds
  • Protein Kinase Inhibitors
  • Niacinamide
  • Sorafenib
  • Axitinib