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：
NO20160175
公开号：
NO20160175A1
申请日:
2016.02.03
申请国别(地区):
NO
年份:
2016
代理人:
摘要：
The present invention relates to: a long-acting pharmaceutical composition containing a conjugate comprising a physiologically active polypeptide linked to an immunoglobulin Fc fragment, wherein the composition contains a monomeric conjugate comprising one molecule of the physiologically active polypeptide linked to a single immunoglobulin Fc fragment, and optionally contains a multimeric conjugate comprising two or more molecules of the same physiologically active polypeptide linked to a single immunoglobulin Fc fragment, provided that the molar ratio of the monomeric conjugate to the multimeric conjugate in the composition is at least 19； a physiologically active polypeptide monomer-immunoglobulin Fc fragment conjugate that comprises a physiologically active polypeptide monomer linked via a non-peptidyl linker to an immunoglobulin Fc fragment, wherein the physiologically active polypeptide is linked via the non-peptidyl linker to the immunoglobulin Fc fragment in a monomeric form, the conjugate showing reduced receptor-mediated internalization or receptor-mediated clearance compared to either a dimeric conjugate comprising two molecules of the physiologically active polypeptide linked via the non-peptidyl linker to a single immunoglobulin Fc fragment, or a conjugate comprising a physiologically active polypeptide dimer linked in-frame to the immunoglobulin Fc fragment； and a method for preparing the long-acting pharmaceutical composition.
