Review

Nature Reviews Drug Discovery 5, 123-132 (February 2006) | doi:10.1038/nrd1955

Article series: Case Histories

Pegaptanib, a targeted anti-VEGF aptamer for ocular vascular disease

Eugene W. M. Ng1, David T. Shima1, Perry Calias1, Emmett T. Cunningham, Jr.1, David R. Guyer1  About the authors & Anthony P. Adamis1

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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.

Author affiliations

  1. Eyetech Pharmaceuticals, Inc., 3 Times Square, 12th Floor, New York, New York 10036, USA

Correspondence to: Anthony P. Adamis1 Email: Tony.Adamis@eyetech.com

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