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pegaptanib

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Also known as Pegaptanib Octasodium, NX1838, Pegaptanib sodium, EYE 001, NX 1838

Pegaptanib sodium injection (brand name Macugen) is an anti-angiogenic medicine for the treatment of neovascular (wet) age-related macular degeneration (AMD). It was discovered by NeXstar Pharmaceuticals (which merged with Gilead Sciences in 1999) and licensed in 2000 to EyeTech Pharmaceuticals, now OSI Pharmaceuticals, for late stage development and marketing in the United States. Gilead Sciences continues to receive royalties from the drugs licensing. Outside the US pegaptanib is marketed by Pfizer. Approval was granted by the U.S. Food and Drug Administration (FDA) in December 2004.

Wikidata facts

Mass
536.2349
Show 4 more facts
chemical formula
C₂₀H₄₀N₃NaO₁₀P
canonical SMILES
COCCOC(=O)NCCCCC(C(=O)NCCCCCOP(=O)(C)O)NC(=O)OCCOC.[Na]
NCI Thesaurus ID
C90657
isomeric SMILES
COCCOC(=O)NCCCC[C@@H](C(=O)NCCCCCOP(=O)(C)O)NC(=O)OCCOC.[Na]
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~7 min read

Article

12 sections
Contents
  • Mechanism of action
  • Means of administration
  • Preclinical trials
  • Animal toxicology studies
  • Clinical studies
  • Phase I
  • Phase II
  • Phase III
  • Regulatory approval information
  • Side effects
  • Commercialization
  • References

Pegaptanib sodium injection (brand name Macugen) is an anti-angiogenic medicine for the treatment of neovascular (wet) age-related macular degeneration (AMD). It was discovered by NeXstar Pharmaceuticals (which merged with Gilead Sciences in 1999) and licensed in 2000 to EyeTech Pharmaceuticals, now OSI Pharmaceuticals, for late stage development and marketing in the United States. Gilead Sciences continues to receive royalties from the drugs licensing. Outside the US pegaptanib is marketed by Pfizer. Approval was granted by the U.S. Food and Drug Administration (FDA) in December 2004.

==Mechanism of action== Pegaptanib is a pegylated anti-vascular endothelial growth factor (VEGF) aptamer, a single strand of nucleic acid that binds with specificity to a particular target. Pegaptanib specifically binds to the 165 isoform of VEGF, a protein that plays a critical role in angiogenesis (the formation of new blood vessels) and increased permeability (leakage from blood vessels), two of the primary pathological processes responsible for the vision loss associated with neovascular AMD.

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