Apatinib: a promising oral antiangiogenic agent in the treatment of multiple solid tumors

Drugs Today (Barc). 2015 Apr;51(4):223-9. doi: 10.1358/dot.2015.51.4.2320599.

Abstract

Aberrant proangiogenic pathways have long been implicated in tumorigenesis and metastasis. Antiangiogenic therapies have shown efficacy in the treatment of a variety of solid tumors including lung, breast, colon, glioblastomas, and other solid tumor types. Apatinib, a small-molecule inhibitor of vascular endothelial growth factor receptor-2 (VEGFR-2), is an orally bioavailable agent currently being studied in multiple tumor types. Apatinib has shown a survival benefit in gastric cancer in a phase III trial and non-small cell lung cancer in a phase II trial. With a favorable side effect profile and improved outcomes, apatinib has demonstrated a substantial potential to augment therapeutic options in a variety of tumor types.

Keywords: Antiangiogenic drugs; Apatinib; Solid tumor; VEGF; VEGFR-2.

Publication types

  • Review

MeSH terms

  • Administration, Oral
  • Angiogenesis Inhibitors / administration & dosage
  • Angiogenesis Inhibitors / adverse effects
  • Angiogenesis Inhibitors / pharmacokinetics
  • Angiogenesis Inhibitors / therapeutic use*
  • Clinical Trials as Topic
  • Humans
  • Neoplasms / blood supply
  • Neoplasms / drug therapy*
  • Neoplasms / metabolism
  • Neoplasms / pathology
  • Neovascularization, Pathologic / drug therapy*
  • Pyridines / administration & dosage
  • Pyridines / adverse effects
  • Pyridines / pharmacokinetics
  • Pyridines / therapeutic use*
  • Treatment Outcome
  • Vascular Endothelial Growth Factor Receptor-2 / antagonists & inhibitors*

Substances

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