Releasable PEGylation
Biobetters and prodrugs
Intellectual Property Rights

Releasable Pegylation

PEGylation, i.e. conjugation of polyethylene glycol (PEG) to biopharmaceutical molecules is known to enhance pharmacologic and pharmaceutical properties of peptides, proteins and other large molecules, including prolonged blood circulation half-life and improved drug solubility and stability.

The improved pharmacokinetic properties of the pegylated molecule are due to one or more factors, e.g:

  • Reduced renal elimination as a consequence of increased molecular weight and larger hydrodynamic radius
  • Reduced proteolytic degradation due to steric hindrance from the PEG-chain impeding access for proteases and peptidases.
  • These advantages have made PEGylation a common technique in the pharmaceutical industry. On the other hand, the same properties can greatly reduce a drug's potency, e.g. by reducing the affinity of the PEGylated substance for its biological receptor.

    Benefits of QuiaPEG’s proprietary technology 

    QuiaPEG’s releasable pegylation technology harnesses the benefits of pegylation while eliminating the potential drawbacks. By developing customized scaffolds, it is possible to adjust the half-life at physiological pH of the bond between the PEG-chain and the active drug. Alternatively, the release mechanism can be tailor-made to enable enzyme-specific digestion. These controlled processes result in the release of the original, unmodified active substance.

    Benefits of pH-dependent release include stable blood concentrations between dose administrations, thus potentially avoiding adverse drug reactions from high drug concentrations immediately after dosing, and an increased dosing interval, increasing patient convenience.

    QuiaPEG’s releasable chemistry is compatible with both linear and branched-chain PEG reagents irrespective of molecular size.

    Clinical benefits of releasable pegylation  

    • Controlled release of the unmodified drug allowing full potency
    • Increased dosing interval
    • Stable blood concentrations
    • May qualify for section 505(b)(2) approval pathway

    QuiaPEG Pharmaceuticals Holding AB

    Virdings Allé 32 B
    754 54 Uppsala
    +46 (0) 70 693 12 53

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