Table 1.
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.