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  • Title: Pegaptanib, a targeted anti-VEGF aptamer for ocular vascular disease.
    Author: Ng EW, Shima DT, Calias P, Cunningham ET, Guyer DR, Adamis AP.
    Journal: Nat Rev Drug Discov; 2006 Feb; 5(2):123-32. PubMed ID: 16518379.
    Abstract:
    Aptamers are oligonucleotide ligands that are selected for high-affinity binding to 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. After nearly a decade of preclinical development to optimize and characterize its biological effects, pegaptanib was shown in clinical trials to be effective in treating choroidal neovascularization associated with age-related macular degeneration. Pegaptanib therefore has the notable distinction of being the first aptamer therapeutic approved for use in humans, paving the way for future aptamer applications.
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