Factor VIII conjugates

摘要

This invention relates to Factor VIII muteins that are covalently bound, at a predefined site that is not an N-terminal amine, to one or more biocompatible polymers such as polyethylene glycol. The mutein conjugates retain FVIII procoagulant activity and have improved pharmacokinetic properties.

主权项

1. A pharmaceutical composition comprising pharmaceutically acceptable adjuvants and a therapeutically effective amount of factor VIII conjugates;
wherein the factor VIII conjugates have factor VIII procoagulant activity and consist of a functional factor VIII polypeptide having a heavy and a light chain in which one or more biocompatible polymers are covalently attached to the functional factor VIII polypeptide at only the heavy chain; wherein the functional factor VIII polypeptide comprises the amino acid sequence of SEQ ID NO: 4 or an allelic variant thereof; and wherein the one or more biocompatible polymers comprise polyalkylene oxide.