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Title:
MONO- AND DI-PEG IL-10 PRODUCTION, AND USES
Document Type and Number:
Japanese Patent JP2018168160
Kind Code:
A
Abstract:
To provide interleukin (IL)-10 having a relatively short half life, and in particular a method of producing, more efficiently with greater production yields, a mixture of mono- and di-PEG (polyethylene glycol)-ylated interleukin (IL)-10 to provide a longer half life and higher biological activity.SOLUTION: A method of producing a mixture of mono- and di-PEGylated IL-10 in which a PEG molecule is covalently attached to an amino acid residue of a subunit of IL-10 comprises: reacting IL-10 with an activated PEG-linker, such as PEG-propylaldehyde or succinimidylcarbonate-PEG, in the presence of a boron reducing agent, such as sodium cyanoborohydride, to produce a mixture of mono-PEGylated IL-10 and di-PEGylated IL-10, where the IL-10 and the reducing agent are present in a molar ratio of 0.0009 to 0.04. The production method may further comprise a purification step using size exclusion chromatography or the like.SELECTED DRAWING: Figure 1

Inventors:
STEVEN J BLAISDELL
COLLETTE M CUTLER
BRITTANY C PAPORELLO
ALEXANDRE AMBROGELLY
Application Number:
JP2018107216A
Publication Date:
November 01, 2018
Filing Date:
June 04, 2018
Export Citation:
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Assignee:
MERCK SHARP & DOHME
International Classes:
A61K38/20; A61K33/243; A61K47/60; A61P3/10; A61P29/00; A61P31/04; A61P37/06; A61P43/00; C07K14/54
Attorney, Agent or Firm:
Hiroshi Kobayashi
Norio Omori
Ohno Reie
Yasuhito Suzuki