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Home > A. Molecular pathology > Targeted therapy > Small molecules > apatinib


Tuesday 1 November 2016



Apatinib is a VEGFR2 tyrosine kinase inhibitor (VEGFR2 TKI) that selectively inhibits the vascular endothelial growth factor receptor-2 (VEGFR2, also known as KDR).

Apatinib is an orally bioavailable, small molecule agent which is thought to inhibit angiogenesis in cancer cells.

Specifically apatinib inhibits VEGF-mediated endothelial cell migration and proliferation thus blocking new blood vessel formation in tumor tissue. This agent also mildly inhibits c-Kit and c-SRC tyrosine kinases, as a TKI.

Apatinib is an investigational cancer drug currently undergoing clinical trials as a potential targeted treatment in:
- metastatic gastric carcinomas,
- metastatic mammary carcinomas
- advanced hepatocellular carcinoma (HCC)