PEGylation of protein therapeutics : INFa2b & INFb1b

PEGylation of protein therapeutics : INFa2b & INFb1b

INFα2b

  • 165 aa residues – 2 disulphide bridges
  • PEG-Intron® (Schering Plough) has been approved to treatment of Hepatitis C:
    • non-selective PEGylation (12 kDa linear)
    • 14 PEG positional isomers
    • in vitro antiviral activity is 28% of non-modified form

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INFβ1b

  • 165 aa residues – 1 disulphide bridge
  • No PEGylated INFβ1b approved
  • Rapid clearance from blood stream – frequent administration required
  • Neutralizing Abs form in 45% of patients
  • Physical instability

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