"Macugen" (pegaptanib sodium), which was approved by FDA in 2004, is an example of a commercial aptamer. The drug was developed
by Eyetech Pharmaceuticals, which was acquired by OSI Pharmaceuticals (Melville, NY) in 2005. Pegaptanib is a covalent conjugate of a 28-mer oligonucleotide that terminates in a pentylamino
linker, to which two 20-kilodalton monomethoxy polyethylene glycol units are covalently attached via the two amino groups
on a lysine residue (5).
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Technology Outlook: APIs, Intermediates, and Formulation suppl. s20–s25 (2006).
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4. M. Stanek et al., "Preparation of Alkylated N- or Amino, Ammonium or Spirobicyclic Ammonium Group-containing, Cross-linked Polymers," US Patent
7105631, Sept. 12, 2006.
http://www.fda.gov/cder/foi/label/2006/021756s006,s007lbl.pdf (accessed June 4, 2007).