"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).
References
1. K. Holt-Tiffin et al., "Nitrilase-Catalyzed Desymmetrization of 3-Hydroxyglutaronitrile: Preparation of a Statin Side-Chain Intermediate," Org. Process Res. Dev. 10 (3), 661–665 (2006).
2. P. Van Arnum, "Achieving Enantioselectivity in Synthesizing APIs and Intermediates," Pharm. Technol. 30
Technology Outlook: APIs, Intermediates, and Formulation suppl. s20–s25 (2006).
3. P. Van Arnum, "Optimizing Strategies for API Synthesis and Formulation Development," Pharm. Technol. 30 (11), 44–48 (2006).
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.
5. Drugs@FDA,
http://www.fda.gov/cder/foi/label/2006/021756s006,s007lbl.pdf (accessed June 4, 2007).
|
