ANTI-HER2 ANTIBODY DRUG CONJUGATE Russian patent published in 2023 - IPC A61K47/68 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a method for producing an antibody-drug conjugate represented by the following formula: (maleimide-N-yl)-(CH₂)n³-C(=O)-L²-L^P-NH-(CH₂)n¹-L^a-(CH₂)n²-C(=O)-(NH-DX) with an anti-HER2 antibody or a reactive derivative thereof, and conjugating the linker-drug group with the antibody in a manner to form a thioether bond at the disulphide bonds site represented in the hinge portion of the antibody, where n¹ is an integer from 0 to 6, n² is an integer from 0 to 5, n³ is an integer from 2 to 8, L² is -NH-(CH₂CH₂-O)n⁴ -CH₂CH₂-C(=O)- or a single bond, where n⁴ is an integer from 1 to 6, L^P is a tetrapeptide residue -GGFG-, L^a is -O- or a single bond, and -(NH-DX) is a group represented by the following formula:

,

where the nitrogen atom of the amino group in position 1 is in the bonding position.

EFFECT: conjugate has excellent antitumor activity.

19 cl, 14 dwg, 49 ex