公开(公告)号：US20180169262A1

公开(公告)日：2018-06-21

申请号：US15830272

申请日：2017-12-04

Applicant: Industrial Technology Research Institute

Inventor： 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

IPC: A61K47/68 ,  A61K31/4745 ,  A61K47/64 ,  C07K16/30

CPC classification number: A61K47/6889 ,  A61K31/4745 ,  A61K47/64 ,  A61K47/65 ,  A61K47/6803 ,  A61K47/6817 ,  A61K47/6851 ,  A61K47/6855 ,  A61P35/00 ,  C07K16/30

Abstract: 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.