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. 2013 Jun 11;5:103–115. doi: 10.2147/CMAR.S45193

Table 1.

Biological anti-VEGF agents: currently approved and/or under phase III evaluation

Agent What it is What it binds/inhibits Rationale for use as an antiangiogenic agent? Approved indications (potential indications)
Bevacizumab Humanized monoclonal antibody VEGF-A Inhibition of VEGF-A will prevent pathological angiogenesis by inhibiting its interaction with VEGFR-2 mCRC, glioblastoma, NSCLC, RCC
Aflibercept Soluble decoy receptor VEGF-A
VEGF-B
PlGF
Targeting multiple VEGF ligands will allow for a broader inhibition of proangiogenic processes and inhibit possible resistance mechanisms mCRC (melanoma, prostate cancer, glioblastoma, pancreatic cancer, NSCLC)
Regorafenib Tyrosine kinase inhibitor VEGFR-1, -2, -3
PDGFR
c-kit
FGFR
Inhibition of VEGFR tyrosine kinase activity to prevent pathological angiogenesis in tumors mCRC (RCC, breast cancer)
Ramucirumab Fully human monoclonal antibody VEGFR-2 extracellular domain Inhibition of signaling by VEGFR-2 (receptor for VEGF-A) will prevent pathological angiogenesis by inhibiting VEGF-A activity Currently investigational (mCRC, breast cancer, NSCLC)

Abbreviations: FGFR, fibroblast growth factor receptor; mCRC, metastatic colorectal cancer; NSCLC, non-small-cell lung cancer; PDGFR, platelet-derived growth factor receptor; PlGF, placental growth factor; RCC, renal cell carcinoma; VEGF, vascular endothelial growth factor; VEGFR, vascular endothelial growth factor receptor.