AMATOXIN ANTIBODY-DRUG CONJUGATES AND USE THEREOF Russian patent published in 2024 - IPC C07K7/64 A61K38/12 A61K47/68 A61P35/00 

Abstract RU 2826004 C2

FIELD: chemistry.

SUBSTANCE: invention relates to amatoxins of general formula (An), where n is 2, 3, 4, 5, 6, 7, 8 or 9. Invention also relates to an antibody-drug conjugate (ADC) consisting of an antibody conjugated to amatoxin through a linker, wherein the ADC has structural formula (Ia), where Q is S; L is -(CH2)n, wherein n is integer from 1 to 6; Z is a maleimide group; and Ab is an antibody which specifically binds to Her2 or PSMA. Invention also relates to an antibody-drug conjugate (ADC), wherein the antibody specifically binds to human PSMA and contains heavy and light chain amino acid sequences and which is conjugated with HDP30.2867 compound. Invention also relates to the use of ADC for treating cancer. (HDP30.2867).

EFFECT: providing amatoxins which can be used in antibody-drug conjugates (ADC) for delivering amatoxin to a target cell, which have high plasma stability and tolerance in vivo.

16 cl, 15 tbl, 48 dwg, 22 ex

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RU 2 826 004 C2

Authors

Makdonakh, Sharlott Fenton

Panvar, Radzhiv

Khekhler, Torsten

Kulke, Mikhael

Sarma, Ganapati N.

Pal, Andreas

Myuller, Kristof

Simon, Verner

Lutts, Kristian

Gallo, Francheska

Dates

2024-09-03Published

2020-04-24Filed