CALICHEAMICIN DERIVATIVE-CARRIER CONJUGATES Russian patent published in 2019 - IPC A61K31/175 A61K39/395 A61P35/00 

FIELD: medicine.

SUBSTANCE: group of inventions relates to medicine, specifically to oncology, and can be used to obtain a conjugate for the treatment of a subject with a proliferative disorder. Conjugate ʺderivative of monomeric N-acetyl-gamma calicheamicin / anti-CD22 antibodyʺ is represented by formula Pr(-X-W)_m, where: Pr is an anti-CD22 antibody. Antibody contains SEQ ID NO: 1 for CDR-H1, SEQ ID NO: 2 or SEQ ID NO: 13, or SEQ ID NO: 15, or SEQ ID NO: 16, or the sequence GINPGNQYTTYKRNLKG, or the sequence GINPGNNYATYRRKFQG for CDR-H2, SEQ ID NO: 3 for CDR-H3, SEQ ID NO: 4 for CDR-L1, SEQ ID NO: 5 for CDR-L2 and SEQ ID NO: 6 for CDR-L3. X is a bifunctional linker containing 4-(4-acetylphenoxy)butanoic acid (AcBut). W is N-acetyl-gamma calicheamicin, m is the average load for the purified conjugation product, such that calicheamicin is 4–10 % by weight of the conjugate and (-X-W)_m is a dimethyl hydrazide of AcBut-acetyl-gamma-calicheamicin. Group of inventions also relates to a method of treating a subject with a proliferative disorder.

EFFECT: use of this group of inventions allows to obtain a conjugate ʺderivative of monomeric N-acetyl-gamma calicheamicin / anti-CD22 antibodyʺ with a high drug load and with a low content of low-conjugated fraction (LCF).

32 cl, 8 ex, 13 tbl, 29 dwg