Aptamers are oligonucleotide ligands that are selected for their high-affinity to bind molecular targets.

Pegaptanib sodium (Macugen^®; Eyetech Pharmaceuticals/Pfizer) is an RNA Aptamer directed against vascular endothelial growth factor (VEGF)-165, the VEGF isoform primarily responsible for pathological ocular neovascularization and vascular permeability.

“Pegaptanib therefore has the notable distinction of being the first aptamer therapeutic approved for use in humans, paving the way for future aptamer applications.”⁽¹⁾

Like the use of Lucentis^® and Avastin^® future prospects with the use of Macugen^® are essentially made by process innovation, with adoption of optimized therapeutic schemes of combined therapy.