Anti-her3 antibody drug conjugate, composition thereof, and use thereof
AssigneeChia Tai Tianqing Pharmaceutical Group Co., Ltd.
InventorsTianxi Chen, Tongjie Xu, Xiaoqi Tang, Weiwei Feng, Zhengping Zhang
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Abstract
Provided is an anti-HER3 antibody drug conjugate, specifically comprising an antibody moiety, an intermediate linker moiety, and a cytotoxic drug moiety which are linked together. The provided antibody drug conjugate achieves excellent anti-tumor activity or/and better safety. The provided antibody drug conjugate can be used for the treatment of cancer.
Claims21
An antibody-drug conjugate having general formula Ab-(L-U)n or a pharmaceutically acceptable salt or a solvate thereof, wherein Ab represents an antibody moiety, L represents a linker moiety, U represents a cytotoxic drug moiety, and n is an integer or a decimal selected from numbers from 1 to 10, wherein the antibody-drug conjugate comprises a structure of formula IIa below:
- wherein,
- Ra is selected from a hydrogen atom, a deuterium atom, optionally substituted C1-6 alkyl, optionally substituted C3-7 cycloalkyl, optionally substituted C3-7 heterocyclyl, optionally substituted C6-10 aryl, and optionally substituted C5-12 heteroaryl;
- Rb is selected from a hydrogen atom, a deuterium atom, optionally substituted C1-6 alkyl, optionally substituted C3-7 cycloalkyl, optionally substituted C3-7 heterocyclyl, optionally substituted C6-10 aryl, and optionally substituted C5-12 heteroaryl;
- or,
- Ra and Rb, together with an atom to which they are attached, form optionally substituted 5-8 membered heterocyclyl.
(canceled)
A linker-drug intermediate compound having a structure of formula III:
- wherein,
- Ra is selected from a hydrogen atom, a deuterium atom, optionally substituted C1-6 alkyl, optionally substituted C3-7 cycloalkyl, optionally substituted C3-7 heterocyclyl, optionally substituted C6-10 aryl, and optionally substituted C5-12 heteroaryl;
- Rb is selected from a hydrogen atom, a deuterium atom, optionally substituted C1-6 alkyl, optionally substituted C3-7 cycloalkyl, optionally substituted C3-7 heterocyclyl, optionally substituted C6-10 aryl, and optionally substituted C5-12 heteroaryl;
- or Ra and Rb, together with an atom to which they are attached, form optionally substituted 5-8 membered heterocyclyl.
Dependencies are inferred from the claim text.