ANTI-HER3 CONJUGATE ANTIBODY-DRUG Russian patent published in 2023 - IPC A61K31/535 A61K47/64 A61K39/395 C07K16/28 

FIELD: antitumor drugs.

SUBSTANCE: method of producing an antibody-drug conjugate includes the interaction of the compound (maleimid-N-yl)-(CH₂)n³-C(=O)-L²-L^P-NH-(CH₂)n¹-L^a-(CH₂)n²-C(=O)-(NH-DX) or (maleimide-N-yl)-(CH₂)n³-C(=O)-L²-L^P-(NH-DX) with an anti-HER3 antibody or a reactive derivative thereof; and conjugating the drug-linker fragment with the antibody in a manner to form a thioether bond at the disulfide bond site present in the hinge portion of the antibody, where n³ is an integer having a value of 2 to 8, L² represents -NH-(CH₂CH₂-O)n⁴-CH₂CH₂-C(=O)- or a single bond, where n⁴ is an integer having a value from 1 to 6, L^P represents a peptide residue consisting of 2–7 amino acids selected from phenylalanine, glycine, valine, lysine, citrulline, serine, glutamic acid and aspartic acid, n¹ is an integer having a value from 0 to 6, n² is an integer having a value from 0 to 5, L^a represents either -O- or a single bond. Also another option for obtaining an antibody-drug conjugate is disclosed.

EFFECT: group of inventions provides antitumor effect and safety.

26 cl, 30 dwg, 2 tbl, 23 ex