CAPPED AND UNCAPPED CYSTEINES OF ANTIBODY AND THEIR USE IN ANTIBODY-DRUG CONJUGATION Russian patent published in 2021 - IPC A61K47/64 A61K47/68 C07K16/00 

Abstract RU 2742260 C2

FIELD: pharmaceuticals.

SUBSTANCE: present invention relates to creation of therapeutic agents. Disclosed is a method for preparing a conjugate of a drug with an antibody (ADC), comprising the steps of producing a capped antibody in a cell culture, where the capping fragments are selected from 5-thio-2-nitrobenzoic acid (TNB), 2-mercaptopyridine and dithiodipyridine (DTDP); subjecting the capped antibody to the action of a reducing agent which is three (3-sulphophenyl) phosphine (TSPP); and without introduction of oxidising agent conjugation of reduced sulfur bonds on antibody with payload by binding fragment, wherein said payload is auristatin, splice statin or calicheamicin.

EFFECT: conjugates obtained in this way have higher efficacy and can be used in therapy.

6 cl, 16 dwg, 1 tbl, 8 ex

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RU 2 742 260 C2

Authors

Chzhun, Syaotyan

Prashad, Amarnaut Shastri

Kriz, Ronald Uilyam

Khi, Tao

Somers, Uill

Van, Venge

Letendre, Leo Dzhozef

Dates

2021-02-04Published

2016-08-09Filed