BISPECIFIC ANTI-HAPTEN/ANTI-BLOOD BRAIN BARRIER RECEPTOR ANTIBODIES, COMPLEXES THEREOF AND THEIR USE AS BLOOD BRAIN BARRIER SHUTTLES Russian patent published in 2019 - IPC A61K47/68 A61K39/395 C07K19/00 

Abstract RU 2693438 C2

FIELD: biotechnology.

SUBSTANCE: disclosed is a conjugate and use thereof for targeted delivery of a haptenilised pharmaceutically active load through a blood-brain barrier. Also disclosed is a pharmaceutical composition containing said conjugate for treating a brain disease. Conjugate of the present invention comprises a haptenylated load and a bispecific antibody which has a first antigen-binding fragment, specifically bound to a haptenilated load, and a second antigen-binding fragment specifically binding to blood-brain barrier receptor, where the first antigen-binding fragment is covalently bonded to the haptenylated load using a cysteine residue at position 52b or 53 of the heavy chain according to Kabat numbering. Covalent bond with hapten provides stabilization of pharmaceutically active load, and presence of second antigen-binding fragment - its transportation through blood-brain barrier.

EFFECT: present invention can find further application in therapy.

14 cl, 63 dwg, 8 tbl, 38 ex

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RU 2 693 438 C2

Authors

Brinkmann Ulrikh

Georges Gaj

Mundigl Olaf

Nivener Ens

Dates

2019-07-02Published

2014-12-29Filed