CONJUGATE OF BIOLOGICALLY ACTIVE POLYPEPTIDE MONOMER AND IMMUNOGLOBULIN FC FRAGMENT WITH REDUCED RECEPTOR-MEDIATED CLEARANCE, AND THE METHOD FOR PREPARING THE SAME
PARK, SUNG HEE,KIM, MIN YOUNG,LIM, HYUNG KYU,BAE, SUNG MIN,JUNG, SUNG YOUB,KWON, SE CHANG
申请号：
PH12016500075
公开号：
PH12016500075A1
申请日:
2016.01.11
申请国别(地区):
PH
年份:
2016
代理人:
摘要：
The present invention relates to: a composition containing a conjugate having a bioactive polypeptide linked to an immunoglobulin Fc fragment, wherein the composition is a sustained pharmaceutical composition containing a monomer conjugate having one molecule of bioactive polypeptide linked to one immunoglobulin Fc fragment, and optionally a multimer conjugate having two or more molecules of identical bioactive polypeptide linked to one immunoglobulin Fc fragment, wherein the molar ratio of the monomer conjugate to the multimer conjugate in the composition is 19 or greater； a bioactive polypeptide monomer-immunoglobulin Fc fragment conjugate in which a bioactive polypeptide monomer and an immunoglobulin Fc fragment are linked via a non-peptide linker, wherein the bioactive polypeptide is linked, in a monomer form, to one immunoglobulin Fc fragment via the non-peptide linker, and demonstrates a lower receptor-mediated internalization or receptor-mediated clearance, compared to a dimer conjugate having two molecules of bioactive polypeptide linked to one immunoglobulin Fc fragment via a non-peptide polymer, or a bioactive polypeptide-immunoglobulin Fc fragment inframe conjugate； and a method for preparing the sustained pharmaceutical composition.
