Therapeutic potentials of Apatinib in cancer treatment: Possible mechanisms and clinical relevance

Life Sci. 2020 Jan 15:241:117106. doi: 10.1016/j.lfs.2019.117106. Epub 2019 Nov 28.

Abstract

Metastasis is one of the main issues in cancer treatment and it has been documented that angiogenesis plays an important role in this process. Studies showed that vascular endothelial growth factor (VEGF) and its receptor (VEGFR) have elevated expression in tumors and are involved in tumor progression and metastasis; suggesting their potential for being a therapeutic target. In this regard, Apatinib or YN968D1, a specific inhibitor of VEGFR-2 has been suggested as a promising therapeutic agent for cancer that can prevent tumor angiogenesis and metastasis. Furthermore, this drug can sensitize resistant tumor cells to chemotherapy drugs and increase the effectiveness of conventional chemotherapy drugs. Recent studies have shown that Apatinib has beneficial implications as a post-second and third-line therapy agent in a variety of cancers. Furthermore, Apatinib has the capacity to promote the overall survival and progression-free survival of cancer patients. This review discussed about, the molecular mechanisms and clinical relevance underlying the therapeutic potential of Apatinib in cancer treatment.

Keywords: Apatinib; Cancer treatment; Vascular endothelial growth factor; Vascular endothelial growth factor receptor.

Publication types

  • Review

MeSH terms

  • Angiogenesis Inhibitors / pharmacology
  • Angiogenesis Inhibitors / therapeutic use
  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / therapeutic use*
  • Apoptosis / drug effects
  • Cell Proliferation / drug effects
  • Chemotherapy, Adjuvant
  • Clinical Trials as Topic
  • Drug Resistance, Neoplasm / drug effects
  • Humans
  • Neoplasms / blood supply
  • Neoplasms / drug therapy*
  • Protein Kinase Inhibitors / therapeutic use
  • Pyridines / pharmacology*
  • Pyridines / therapeutic use*
  • Vascular Endothelial Growth Factor Receptor-2 / antagonists & inhibitors

Substances

  • Angiogenesis Inhibitors
  • Antineoplastic Agents
  • Protein Kinase Inhibitors
  • Pyridines
  • apatinib
  • KDR protein, human
  • Vascular Endothelial Growth Factor Receptor-2