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US 12,605,458 B2Granted
Antibody-drug conjugate having acidic self-stabilization junction
AssigneeSystimmune, Inc.
InventorsYi Zhu, Yiqian Wang, Jie Li, Shi Zhuo, Weili Wan
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Abstract
The present invention provides a special drug conjugate having a hydrophilic acidic stabilization junction. Compared with a conjugate having a lower drug loading, due to the introduction of the acidic stabilization junction, the conjugate in the present invention can also have a higher drug loading (that is, each targeted reagent has more hydrophilic drug junctions), keeps a desired PK property and has a same or better activity in a body.
Claims18
An antibody-drug conjugate or its pharmaceutically acceptable salt thereof as shown in Formula I:
- wherein:
- the circle represents a scaffold, wherein the scaffold comprises a C1-8 alkylidene group, a C1-8 heteroalkylidene group, a C6-10 arylidene group, or a C4-10 heteroarylidene group;
- L comprises an antibody, an antibody fragment or a protein;
- M comprises a succinimide group;
- Ac is connected to the scaffold through an amino group, wherein Ac comprises an acidic unit that serves to stabilize the antibody-drug conjugate, and wherein Ac comprises a fragment consisting of at least one amino group and at least one acidic group or an oligopeptide group consisting of a plurality of amino acid units;
- D comprises a drug unit;
- A comprises a linker;
- m is an integer selected from 1 to 20;
- and
- n is 1 or 2.
7 more elements
Dependencies are inferred from the claim text.