Available Anti-Vascular Endothelial Growth Factor Agents

Pegaptanib sodium (Macugen) is a 50 kDa pegylated modified oligonucleotide aptamer that adopts a 3-dimensional shape to selectively inhibit extracellular vascular endothelial growth factor (VEGF)165, the major VEGF-A isoform in the eye. 1 Aptamers are single-stranded nucleotides that bind with high affinity and specificity to predetermined target molecules such as proteins and peptides. 2 These aptamers are selected in vitro using the systematic evolution of ligands by exponential enrichment technique to isolate oligonucleotide ligands that bind to a variety of proteins. 3 Because VEGF is a secreted protein that binds to and activates receptors located predominantly on the surface of vascular endothelial cells, a selective antagonist in the form of a modified aptamer mitigates VEGF-induced angiogenesis, vascular permeability, and inflammation.