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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Authors
Dates
2019-07-02—Published
2014-12-29—Filed