Maggie Lu,May-Hua Chang,Jenn-Tsang Hwang,Ping-Fu Cheng,Li-Wen Chang,Yi-Ju Ko,Chi-Y Hung,Chun-Min Liu,Chia-Yu Fan
申请号：
US15830272
公开号：
US20180169262A1
申请日:
2017.12.04
申请国别(地区):
US
年份:
2018
代理人:
摘要：
A linker-drug represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof is provided. In formula (I), C is a conjugator, L is a linker unit, D is a toxin unit, and n is an integer ranging from 1 to 4. The structure of the conjugator is represented by formula (II). In formula (II), X is a leaving group, each of R1 and R2 is independently a single bond or —NH—, and Z is substituted aryl, heteroaryl, linear alkyl, cycloalkyl, heterocycloalkyl, or a combination thereof. The antibody is conjugated to the linker unit through a cysteine residue of the antibody. An antibody-drug conjugate (ADC) employing the above linker-drug is also provided.
