Axitinib: from preclinical development to future clinical perspectives in renal cell carcinoma

Expert Opin Drug Discov. 2015;10(8):925-35. doi: 10.1517/17460441.2015.1045411. Epub 2015 Jun 3.

Abstract

Introduction: Based on extensive preclinical data and abundant evidence for clinical activity, vascular endothelial growth factor receptor (VEGFR) inhibitors are currently standard of care for metastatic renal cell carcinoma (mRCC). Axitinib is one of the most selective molecules in the class of anti-angiogenic agents, which confers an optimal profile between its safety and anti-cancer activity spectrum.

Area covered: In this review, the authors discuss the different stages that lead to the approval of axitinib in the clinic as well as the current perspectives for its clinical use with other promising therapies in mRCC such as immune checkpoint inhibitors and vaccines.

Expert opinion: In 2015, axitinib has emerged as one of the major agents used in mRCC. Based on robust preclinical data, this highly specific VEGFR inhibitor continues to be evaluated in different indications, including the adjuvant setting but also sequential administration with other molecularly targeted agents or combinations with immune therapies.

Keywords: axitinib; clinical; preclinical; renal cancer.

Publication types

  • Review

MeSH terms

  • Angiogenesis Inhibitors / adverse effects
  • Angiogenesis Inhibitors / pharmacology
  • Angiogenesis Inhibitors / therapeutic use
  • Animals
  • Antineoplastic Agents / adverse effects
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use
  • Axitinib
  • Carcinoma, Renal Cell / drug therapy*
  • Carcinoma, Renal Cell / pathology
  • Humans
  • Imidazoles / adverse effects
  • Imidazoles / pharmacology
  • Imidazoles / therapeutic use*
  • Indazoles / adverse effects
  • Indazoles / pharmacology
  • Indazoles / therapeutic use*
  • Kidney Neoplasms / drug therapy*
  • Kidney Neoplasms / pathology
  • Protein Kinase Inhibitors / adverse effects
  • Protein Kinase Inhibitors / pharmacology
  • Protein Kinase Inhibitors / therapeutic use
  • Receptors, Vascular Endothelial Growth Factor / antagonists & inhibitors

Substances

  • Angiogenesis Inhibitors
  • Antineoplastic Agents
  • Imidazoles
  • Indazoles
  • Protein Kinase Inhibitors
  • Axitinib
  • Receptors, Vascular Endothelial Growth Factor