KIM, YONG ZU,金容柱,金容柱,OH, YEONG SOO,吴英秀,吳英秀,CHAE, JEIWOOK,蔡济旭,蔡濟旭,SONG, HO YOUNG,宋昊永,宋昊永,CHUNG, CHUL-WOONG,郑哲雄,鄭哲雄,PARK, YUN HEE,朴允姬,朴允姬,CHOI, HYO JUNG,崔孝汀,崔孝汀,PARK, KYUNG EUN,朴庆恩,朴慶恩,KIM, HYOUNGRAE,金炯
申请号：
TW105138777
公开号：
TW201720466A
申请日:
2016.11.25
申请国别(地区):
TW
年份:
2017
代理人:
摘要：
The present invention relates to antibody-drug conjugates (ADCs) wherein a plurality of active agents are conjugated to an antibody through at least one branched linker. The branched linker may comprise a branching unit, and two active agents are coupled to the branching unit through a secondary linker and the branching unit is coupled to the antibody by a primary linker. The active agents may be the same or different. In certain such embodiments, two or more such branched linkers are conjugated to the antibody, e.g., 2-4 branched linkers, which may each be coupled to a different C-terminal cysteine of a heavy or light chain of the antibody. The branched linker may comprise one active agent coupled to the branching unit by a first branch and a second branch that comprises a polyethylene glycol moiety coupled to the branching unit. In certain such embodiments, two or more such branched linkers are conjugated to the antibody, e.g., 2-4 branched linkers, which may each be coupled to a different C-terminal cysteine of a heavy or light chain of the antibody.本發明係關於抗體-藥物結合物(ADC),其中複數種活性劑經由至少一個分支連接子結合於抗體。分支連接子可包含分支單元,且兩種活性劑經由次要連接子偶合於分支單元,且分支單元藉由主要連接子偶合於抗體。活性劑可相同或不同。在某些此類實施例中,兩個或更多個此類分支連接子結合於抗體,例如2-4個分支連接子,其可各偶合於抗體重鏈或輕鏈之不同C端半胱胺酸。分支連接子可包含藉由第一分支偶合於分支單元之一種活性劑及包含偶合於分支單元之聚乙二醇部分的第二分支。在某些此類實施例中,兩個或更多個此類分支連接子結合於抗體,例如2-4個分支連接子,其可各偶合於抗體重鏈或輕鏈之不同C端半胱胺酸。無
