CONJUGATES OF ANTIBODIES AND DRUGS CHARACTERIZED IN HIGH IN VIVO TOLERANCE Russian patent published in 2022 - IPC A61K39/395 A61K47/68 C07K16/00 A61P35/00 

FIELD: medicine; pharmaceutics.

SUBSTANCE: group of inventions relates to the field of medicine and pharmaceutics; it can be used for the treatment of cancer. An antibody-drug conjugate contains an antibody or an antibody fragment or derivative preserving properties of binding to a target, containing at least one C-end of a constant region of a light chain, and a small molecule based on anthracycline. The antibody, the antibody fragment or derivative preserving properties of binding to a target are aimed at an antigen expressed on tumor cells, and the molecule(s) of anthracycline is(are) bound to exceptionally C-end(s) of the constant region of the light chain of the antibody, fragment or derivative by a linker containing a peptide sequence, including: (i) a peptide motif, which is the result of the cleavage of the motif of sortase enzyme recognition, and (ii) an oligoglycin sequence Gly_n, where the specified motif of sortase enzyme recognition is pentapeptide, and where n in the specified oligoglycin sequence is 1, 2, 3, 4 or 5. The small molecule based on anthracycline is selected from PNU-159682 or from its derivatives containing a structure according to the formula (i)

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The group of inventions also relates to conjugate options, its production method, a pharmaceutical composition containing the conjugate, and the use of the conjugate for manufacturing a drug for the treatment of a neoplastic disease.

EFFECT: conjugate has an improved in vivo tolerance.

23 cl, 9 dwg, 12 tbl, 10 ex