ANTIBODY-DRUG CONJUGATES AND THEIR USE Russian patent published in 2023 - IPC A61K47/68 A61K47/65 A61P35/00 

FIELD: pharmaceutics.

SUBSTANCE: invention relates to an antibody-drug conjugate (hereinafter – ADC) having increased drug loading, which is obtained using one or more cysteine residues or cysteine derivative residue as carriers bound to a drug and due to conjugation of one or more drugs at the same time by a limited number of antibody binding sites, or it can be obtained with a drug with low toxicity in such a way that ADC product with a wider therapeutic window is obtained. In addition, since a set of drug molecules can be conjugated by one binding site, when ADC is obtained having the same DAR value, the resulting ADC product has better homogeneity. The used amount of an antibody required for preparation can also be significantly reduced.

EFFECT: resulting ADC still can achieve the same inhibitory or destructive effect on tumor cells, while the total number of conjugated drug molecules is significantly reduced compared to ADC capable of binding only one drug molecule by the same site.

14 cl, 2 tbl, 9 ex