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US 11,141,465 B2Granted
Method of making a water-soluble polymer-factor VIII moiety conjugate
AssigneeNektar Therapeutics
InventorsMary J. Bossard, Michael D. Bentley, Ping Zhang
Life of this patent
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Abstract
Conjugates of a Factor VIII moiety and one or more water-soluble polymers are provided. Typically, the water-soluble polymer is poly(ethylene glycol) or a derivative thereof. Also provided are compositions comprising the conjugates, methods of making the conjugates, and methods of administering compositions comprising the conjugates to a patient.
Claims12
A method of making a conjugate, the method comprising:
- (i) contacting, at ambient temperature, a Factor VIII moiety comprised in a buffer solution, wherein the Factor VIII moiety comprises amino groups and is selected from the group consisting of Factor VIII, Factor Villa, Factor VIII:C and B-domain deleted Factor VIII, with a methoxypoly(ethylene glycol) (mPEG) butryaldehyde reagent having a nominal average molecular weight in a range of 6,000 Daltons to about 90,000 Daltons, to thereby form a Schiff base resulting from reaction of amino groups of the Factor VIII moiety with the mPEG butryaldehyde reagent,
- (ii) reducing the Schiff base from (i) to thereby form a reaction mixture comprising methoxypoly(ethylene glycol)—Factor VIII moiety conjugates comprising one or more methoxypoly(ethylene) glycol polymer(s) covalently attached to the Factor VIII moiety via a secondary butamine linkage, and
- (iii) purifying the reaction mixture from (ii) to isolate mono-mPEGylated Factor VIII moiety conjugates having one methoxypoly(ethylene glycol) polymer covalently attached to the Factor VIII moiety via a secondary butamine linkage.
Dependencies are inferred from the claim text.