Yi ZHU,Yixi WANG,Shi ZHUO,Jie LI,Lan CHEN,Weili WAN,Yongguo YU
申请号:
US16339719
公开号:
US20200129635A1
申请日:
2017.09.30
申请国别(地区):
US
年份:
2020
代理人:
摘要:
By inserting cysteine (C) into a heavy chain and/or a light chain of a target antibody at specific insertion site, and performing a site-specific conjugation through a free thiol group (—;SH) from the site-specific inserted cysteine and a linker conjugated with a highly potent small molecule cytotoxin, a cysteine modified antibody-drug conjugate with good homogeneity is provided. The specific insertion sites of cysteine are position 205 and/or position 206 (Kabat numbering scheme) of the light chain of the antibody, and/or position 439 (Kabat numbering scheme) of the heavy chain