PEGYLATION OF FGF21

The present disclosure provides an additive system for use in protein PEGylation. The additive system includes />aminobenzoic hydrazide used either alone or in combination with aromatic amines, such as 3,5-diaminobenzoic acid, or with ammonium sals such as ammonium chloride or ammonium acetate. T...

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Bibliographic Details
Main Authors HICKEY, Matthew R, RAMIREZ, Antonio
Format Patent
LanguageEnglish
French
German
Published 10.03.2021
Subjects
CHEMISTRY
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PEPTIDES
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
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Summary:The present disclosure provides an additive system for use in protein PEGylation. The additive system includes />aminobenzoic hydrazide used either alone or in combination with aromatic amines, such as 3,5-diaminobenzoic acid, or with ammonium sals such as ammonium chloride or ammonium acetate. The disclosed additive combination provides several benefits including increased reaction rates, higher yields and reduction in the aminoxy-PEG equivalents required to complete the conjugation reaction. Typical reactions can be run by combining the additive or additive system with a solution of a protein and aminoxy-PEG reagent. The solution is adjusted to pH 4 and held at 20-25 °C without stirring until completion, typically within 24 hours.
Bibliography:Application Number: EP20200189107