| 摘要 |
PROBLEM TO BE SOLVED: To provide a blood coagulation factor VII (FVIIa molecule) which has an increased half-life, and an improved pharmacokinetics (PK) and pharmacodynamics (PD).SOLUTION: The invention relates to a biocompatible polymer conjugated to FVIIa via one or more cysteine residues (properly a linker of a reduced disulfide bond of FVIIa), such as the following structure, and a drug composition comprising FVIIa of such a conjugated form. [R1 is a direct bond, an alkylene group (preferably C1-10 alkylene group) or an optionally-substituted aryl or heteroaryl group; the aryl groups include phenyl, benzoyl and naphthyl groups; suitable heteroaryl groups include pyridine, pyrrole, furan, pyran, imidazole, pyrazole, oxazole, pyridazine, pyrimidine and purine; linkage to the polymer is by a hydrolytically labile bond, or by a non-labile bond.] |
