Linker for antibody-drug conjugates and its use
AssigneeRemegen Co., Ltd.
InventorsChangjiang Huang, Hui Ye, Hu Chen, Xiuzhi Zhan, Nan Shen, Wenting Luo, Qiaohua Hou, Jianmin Fang
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Abstract
The present invention provides a linker for preparing antibody-drug conjugates and antibody-drug conjugates prepared by the linker, as well as use of the antibody-drug conjugates in a medicament for treating tumor. The linker is capable of coupling simultaneously with the thiol group or amino group on the antibody or functional fragment of the antibody, especially it is capable of coupling with 2, 3 or 4 thiol groups on the antibody or functional fragment of the antibody. A coupled product is uniform and structurally stable.
Claims11
Use of the linker in the preparation of antibody-drug conjugates, the linker has the structure:
An antibody-drug conjugate, which has the structure represented by Formula II:
- Ab-(A-L-D)n (II)
- wherein,
- Ab is an antibody or functional fragment of the antibody;
- A and L are linker moiety, and A as a first linker moiety A, L as a second linker moiety L;
- D is a drug moiety;
- n is 1, 2, 3 or 4;
- wherein:
- the first linker moiety A may have the structure:
- the second linker moiety L may be:
- C1-C9 alkyl, C2-C9 alkenyl, C2-C9 alkynyl, aryl, heteroaryl, C3-C9 cycloalkyl, C3-C9 heterocyclyl,
- Val-Val-PAB, Val-Cit-PAB, Val-Ala-PAB, Val-Lys (Ac)-PAB, Phe-Lys-PAB, Phe-Lys (Ac)-PAB, D-Val-Leu-Lys, Gly-Gly-Arg, Ala-Ala-Asn-PAB, Ala-PAB, PAB and any combination thereof or is absent, wherein, R6, R7 each are independently selected from H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, aryl, heteroaryl, C3-C9 cycloalkyl, C3-C9 heterocyclyl, e is 0, 1, 2, 3, 4, 5, 6, 7 or 8.
Dependencies are inferred from the claim text.