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The importance of tumor angiogenesis in tumor biology is now widely accepted and has emerged as a valid therapeutic target in oncology. Vascular endothelial growth factor (VEGF) represents a key mediator of tumor-initiated angiogenesis and the first target of antiangiogenesis agents introduced in clinical practice. VEGF and VEGF receptor antagonists have revolutionized therapy of cancer which is reflected by their outstanding commercial success: 2008 sales of US$ 6.4 bln only in oncology. VEGF blockers found further use in inhibiting or even reversing angiogenesis in neovascular (wet) age-related macular degeneration (AMD). This market already reached US$ 1.8 bln in 2008.
The total market size of US$ 8.2 bln for VEGF and VEGF receptor (VEGF-R) antagonists has attracted many companies to invest in follow-up and next generation molecules targeting VEGF and VEGF-R. The clinically validated target provides a low risk opportunity for new technologies with proteins, RNA, antibodies and vaccines for validation of the technologies. Multi-target receptor tyrosine kinase (RTK) inhibitors are another possibility to further increase the efficacy of VEGF-R antagonists by adding anti-proliferative or anti-migration effects. In contrast to antagonism of angiogenesis, the growth factor activity of VEGF has created a high level of interest for neuroprotection and several approaches are in clinical evaluation.