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US 10,537,644 B2Granted
Covalent linkers in antibody-drug conjugates and methods of making and using the same
AssigneeRc Biotechnologies, Inc.
InventorsChang Jiang Huang, Jianmin Fang, Hui Ye, Lezhi Zhang
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Abstract
The present invention provides novel and advantageous compositions having a linker capable of covalently coupling one or more free thiols of an antibody. Specifically, provided herein are the molecular structures, synthetic pathways, coupling mechanisms, and applications thereof as used in an antibody-drug conjugate (ADC).
Claims7
An antibody-drug conjugate having the following formula:
- or a pharmaceutically acceptable salt thereof,
- wherein:
- L1, and L2 each represent a linker independently selected from C1-C6 alkyls, S, C(═O), and combinations thereof, or can be null;
- M represents a linking group of
- Q represents an active agent selected from tubulin binders, DNA alkylators, DNA intercalators, enzyme inhibitors, immune modalators, visualization agents, peptides, and nucleotides;
- L represents a linker selected from C1-C6 alkyls, S, C(═O), Val-Cit-PAB,
- and combinations thereof;
- m represents an integer from 0 to 6;
- n represents an integer from 0 to 8
- A is an antibody or functional fragment thereof
- S is a sulfur atom of a thiol group of the targeting moiety;
- and
- each of R3 and R4 is
10 more elements
Dependencies are inferred from the claim text.