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US 12,723,058 B2Granted
Processes for preparing conjugates of the IL-2 protein
AssigneeMerck Sharp & Dohme Corp.
InventorsJoshua Lee, Gregory F. Pirrone, Michael J. Iammarino, David J. Roush
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Abstract
Disclosed herein are novel processes for preparing IL-2 conjugates with one or more water-soluble polymers. In one embodiment, the IL-2 conjugate comprises five poly(ethylene glycol) polymers each of which is covalently attached to the IL-2 moiety via a releasable linkage to an amino group of the IL-2 moiety.
Claims3
A process for preparing a conjugate of an interleukin-2 (IL-2) moiety comprising:
- providing a water solution comprising an IL-2 moiety comprising the amino acid sequence set forth in SEQ ID NO:
- 1 and adding PEG fluorene NHS ester having the following formula:
- wherein each of n1 and n2 is independently selected from 150-300 in a water solution to react with the IL-2 moiety to form an IL-2 conjugate, in which the IL-2 conjugate comprises five poly(ethylene glycol) polymers each of which is covalently attached to an amino group of a lysine residue of the IL-2 moiety in a releasable linkage;
- and
- wherein the conjugation reaction is carried out at a pH of about 8.4.
2 more elements
Dependencies are inferred from the claim text.