Apatinib for molecular targeted therapy in tumor

Haijun Zhang, Haijun Zhang

Abstract

As tumor angiogenesis is one of the hallmarks of cancer, the inhibition of vascular endothelial growth factor signaling has become an attractive anticancer approach. Apatinib, a small-molecule inhibitor of vascular endothelial growth factor receptor-2, has demonstrated encouraging anticancer activity across a broad range of malignancies, including gastric cancer, non-small-cell lung cancer, breast cancer, and hepatocellular carcinoma. In this up-to-date review, focus is not only on the structure, mechanisms, and pharmacokinetics of apatinib, but also on summarizing clinical trials and making recommendations of apatinib for patients with advanced solid tumors.

Keywords: angiogenesis; apatinib; molecular targeted therapy; tumor; vascular endothelial growth factor receptor-2.

Figures

Figure 1
Figure 1
Chemical structure of apatinib.
Figure 2
Figure 2
Schematic illustration of the possible mechanism of apatinib as the inhibitor of VEGFR-2. Notes: By specifically binding to the phosphorylation sites of VEGFR-2, apatinib inhibits the subsequent effects on the vascular endothelium, including cell proliferation, migration, permeability, and survival. Through this inhibition, apatinib plays an antiangiogenic role. Abbreviations: VEGFR-2, vascular endothelial growth factor receptor-2; VEGF, vascular endothelial growth factor.

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