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US 12,318,455 B2Granted
Anti-HER2 antibody-drug conjugate and application thereof
AssigneeHangzhou Adcoris Biopharma Co., Ltd
InventorsZhenwei Miao, Tong Zhu, B. Khasanov Alisher, Gang Chen, Zhaohui Li, Sheldon Cao
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Abstract
An anti-human epidermal growth factor receptor 2 (anti-HER2) antibody-drug conjugate or a pharmaceutically acceptable salt thereof, and an application of the anti-HER2 antibody-drug conjugate for preparing an antitumor 5 pharmaceutical product.
Claims14
An antibody-drug conjugate or a pharmaceutically acceptable salt thereof, wherein the structure of the antibody-drug conjugate is as shown in formula I:
- Ab-(L-D)n I
- wherein:
- Ab is an antibody, wherein the antibody is pertuzumab;
- L is a linker connecting the antibody and the drug;
- wherein L has a structure of L-1:
- wherein L21 is a linker moiety independently selected from the group consisting of Val-Cit, —(CH2)n-, —(CH2CH2O)n-, Ala-Ala-Asn, and a combination thereof, and the wavy line indicates the connection position with antibody
- D is a small molecule drug that inhibits tumor cells, and the structure of D is as shown in formula II:
- wherein in formula II, Y is O or NH, and the wavy line indicates the connection position with L,
- X is CH2N3 or
- n is an average number of coupled drugs in the antibody-drug, and n is from 1.8 to 2;
- the dash marks represent bonds;
- wherein the light chain constant region of the antibody comprises a EKH motif and the drug molecule is linked to a lysine (K) residue of the motif.
9 more elements
Dependencies are inferred from the claim text.