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-LP-NH-(CH2)n1-La-(CH2)n2-C(=O)-(NH-DX) or (maleimide-N-yl)-(CH2)n3-C(=O)-L2-LP-(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, LP 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, La 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
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Authors
Dates
2023-08-23—Published
2015-04-10—Filed