Polymer conjugates with decreased antigenicity, methods of preparation and uses thereof
First Claim
1. A composition comprising a conjugate 95% or more pure, said conjugate comprising a peptide, protein or glycoprotein covalently attached to at least one linear or branched polyalkylene glycol(s),wherein said linear or branched polyalkylene glycol(s) is or are attached to said peptide, protein or glycoprotein at a single site on said linear or branched polyalkylene glycol(s),wherein a hydroxyl group is present on all of the distal polyalkylene glycol termini in said pure conjugate, andwherein said pure conjugate exhibits reduced antigenicity compared to a second conjugate comprising the same peptide, protein or glycoprotein linked at the same site or sites on the peptide, protein or glycoprotein to the same number of polyalkylene glycol(s) of the same size and the same linear or branched structure, wherein an alkoxyl or an aryloxyl group is present on the distal polyalkylene glycol termini in said second conjugate.
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Abstract
Methods are provided for the preparation of conjugates of a variety of bioactive components, especially proteins, with water-soluble polymers (e.g., poly(ethylene glycol) and derivatives thereof), which conjugates have reduced antigenicity and immunogenicity compared to similar conjugates prepared using poly(ethylene glycol) containing a methoxyl or another alkoxyl group. The invention also provides conjugates prepared by such methods, compositions comprising such conjugates, kits containing such conjugates or compositions and methods of use of the conjugates and compositions in diagnostic and therapeutic protocols.
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94 Claims
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1. A composition comprising a conjugate 95% or more pure, said conjugate comprising a peptide, protein or glycoprotein covalently attached to at least one linear or branched polyalkylene glycol(s),
wherein said linear or branched polyalkylene glycol(s) is or are attached to said peptide, protein or glycoprotein at a single site on said linear or branched polyalkylene glycol(s), wherein a hydroxyl group is present on all of the distal polyalkylene glycol termini in said pure conjugate, and wherein said pure conjugate exhibits reduced antigenicity compared to a second conjugate comprising the same peptide, protein or glycoprotein linked at the same site or sites on the peptide, protein or glycoprotein to the same number of polyalkylene glycol(s) of the same size and the same linear or branched structure, wherein an alkoxyl or an aryloxyl group is present on the distal polyalkylene glycol termini in said second conjugate.
Specification