PARK, SUNG HEE,朴晟喜,KIM, MIN YOUNG,金玟永,LIM, HYUNG KYU,林亨奎,BAE, SUNG MIN,裵城敏,JUNG, SUNG YOUB,郑圣烨,鄭聖燁,KWON, SE CHANG,权世昌,權世昌
申请号：
TW103124094
公开号：
TW201513884A
申请日:
2014.07.14
申请国别(地区):
TW
年份:
2015
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.本發明係有關：一種含有複合物之長效性醫藥組成物，該複合物包含連接免疫球蛋白質Fc片段之生理活性多肽，其中該組成物含有單體複合物(其包含一個分子的生理活性多肽連接至單一免疫球蛋白質Fc片段)，且可視需要含有多聚體複合物(其包含兩個或多個分子的相同生理活性多肽連接至單一免疫球蛋白質Fc片段)，但其限制條件為該組成物中該單體複合物對該多聚體複合物之莫耳比例為至少19；一種生理活性多肽單體-免疫球蛋白質Fc片段複合物，其包含利用非肽基連接子連接免疫球蛋白質Fc片段之生理活性多肽單體，其中該生理活性多肽以單體型利用非肽基連接子連接免疫球蛋白質Fc片段，該複合物相較於包含兩個分子的生理活性多肽利用非肽基連接子連接單一免疫球蛋白質Fc片段之二聚體複合物或包含生理活性多肽二聚體讀碼框內連接至免疫球蛋白質Fc片段之複合物，顯示降低之受體介導內化或受體介導清除；及一種製備該長效性醫藥組成物之方法。
