Abstract
Introduction:
Apatinib, a small-molecule inhibitor of vascular endothelial growth factor receptor 2, has demonstrated encouraging anti-cancer activity in gastric cancer within both in vitro and in vivo models.
Areas covered:
Apatinib's efficacy, tolerability and safety have been evaluated in one Phase II and one Phase III study in metastatic/advanced gastric cancer. In this review, we focus on the mechanism of action of apatinib, its pharmacokinetic profile and its clinical activity in the treatment of advanced/metastatic gastric cancer. Expert commentary: Unfortunately, as yet, there is no definitive biomarker data for apatinib in gastric cancer.
Keywords:
Gastric cancer; VEGFR2; angiogenesis; apatinib; chemotherapy.
MeSH terms
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Angiogenesis Inhibitors / adverse effects
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Angiogenesis Inhibitors / pharmacokinetics
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Angiogenesis Inhibitors / therapeutic use*
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Animals
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Humans
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Molecular Targeted Therapy
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Neovascularization, Pathologic*
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Protein Kinase Inhibitors / adverse effects
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Protein Kinase Inhibitors / pharmacokinetics
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Protein Kinase Inhibitors / therapeutic use*
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Pyridines / adverse effects
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Pyridines / pharmacokinetics
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Pyridines / therapeutic use*
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Signal Transduction / drug effects
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Stomach Neoplasms / blood supply
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Stomach Neoplasms / drug therapy*
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Stomach Neoplasms / enzymology
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Stomach Neoplasms / pathology
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Treatment Outcome
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Vascular Endothelial Growth Factor Receptor-2 / antagonists & inhibitors*
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Vascular Endothelial Growth Factor Receptor-2 / metabolism
Substances
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Angiogenesis Inhibitors
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Protein Kinase Inhibitors
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Pyridines
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apatinib
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KDR protein, human
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Vascular Endothelial Growth Factor Receptor-2