ANTI-CD138 IMMUNOCONJUGATES AND USING THEM Russian patent published in 2015 - IPC C07K16/28 A61K39/395 A61P35/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to immunology. What is described is an immunoconjugates targeting CD138-expressing cells containing: IgG4 anti-CD138 antibody containing a heavy chain having CDRs from SEQ ID NO: 1 presented in the description and at least 70% identical to SEQ ID NO: 1, and a light chain having CDRs from SEQ ID NO: 2 presented in the description and at least 70% identical to SEQ ID NO: 2; and an effector molecule presenting a tubulin polymerisation inhibitor, and wherein the effector molecule is attached to the above engineered target antibody through a cleaved linker containing a disulphide bond. Besides, disclosed are a pharmaceutical composition and a kit for inhibition, delaying and/or prevention of tumour growth and/or CD138-expressing tumour cell propagation, wherein the composition contains the above immunoconjugate in an effective amount, and one or more pharmaceutically acceptable excipients; the kit comprises pharmaceutical compositions in independent containers, wherein one container comprises an effective amount of the pharmaceutical composition according to the present invention, while the other container contains a second pharmaceutical composition containing an effective amount of a co-drug, preferentially a cytotoxic agent, and one or more pharmaceutically acceptable excipients. There are presented the following methods implying administering the above immunoconjugate: a) a method of treating multiple myeloma in an individual; b) a method for immunoconjugate-mediated drug delivery; c) a method for inhibition, delaying and/or prevention of CD138-expressing tumour cell growth in a cell culture; d) a method for inhibition, delaying and/or prevention of the growth of a tumour containing CD138 tumour cells, and/or propagation of the tumour cells of this tumour in the patient; e) a method for inhibition, delaying and/or prevention of the tumour growth and/or propagation of CD138-expressing tumour cells in the patient; f) a method of treating the individual suffering a condition expected to be improved by suppressing myeloma cell survival; g) a method for inhibition, delaying and/or prevention of the growth of the tumour containing CD138 tumour cells, and/or propagation of the tumour cells in the individual; h) a method for reducing a cell count in a direct or mediated contact to the CD138-expressing tumour cells in the individual; i) a method for reducing a cell count in a direct or mediated contact to the CD138-expressing tumour cells.

EFFECT: invention enables preparing a homogenously targeted agent for treating the CD138-related diseases.

45 cl, 13 dwg, 5 tbl, 1 ex