EP 3413916 A1 20181219 - ANTIBODY-CONJUGATES WITH IMPROVED THERAPEUTIC INDEX FOR TARGETING CD30 TUMOURS AND METHOD FOR IMPROVING THERAPEUTIC INDEX OF ANTIBODY-CONJUGATES
Title (en)
ANTIBODY-CONJUGATES WITH IMPROVED THERAPEUTIC INDEX FOR TARGETING CD30 TUMOURS AND METHOD FOR IMPROVING THERAPEUTIC INDEX OF ANTIBODY-CONJUGATES
Title (de)
ANTIKÖRPERKONJUGATE MIT VERBESSERTEM THERAPEUTISCHEM INDEX ZUR ABZIELUNG AUF CD30-TUMOREN UND VERFAHREN ZUR VERBESSERUNG DES THERAPEUTISCHEN INDEX VON ANTIKÖRPERKONJUGATEN
Title (fr)
CONJUGUÉS D'ANTICORPS À INDICE THÉRAPEUTIQUE AMÉLIORÉ POUR LE CIBLAGE DE TUMEURS DE CD30 ET MÉTHODE D'AMÉLIORATION DE L'INDICE THÉRAPEUTIQUE DE CONJUGUÉS D'ANTICORPS
Publication
Application
Priority
- EP 16154712 A 20160208
- EP 16154739 A 20160208
- EP 16173599 A 20160608
- JP 2016155927 A 20160808
- EP 2017052791 W 20170208
Abstract (en)
[origin: WO2017137458A1] The present invention concerns novel and improved antibody-conjugates for targeting CD30. The inventors found that when antibody-conjugates were prepared using a specific mode of conjugation, they exhibit an improved therapeutic index. The mode of conjugation comprises a first step (i) of contacting a glycoprotein comprising 1 - 4 core N-acetylglucosamine moieties with a compound of the formula S(F1)x-P in the presence of a catalyst, wherein S(F1)x is a sugar derivative comprising x functional groups F1 capable of reacting with a functional group Q1, x is 1 or 2 and P is a nucleoside mono- or diphosphate, and wherein the catalyst is capable of transferring the S(F1)X moiety to the core-GlcNAc moiety, to obtain a modified antibody; and a second step (ii) of reacting the modified antibody with a linker-conjugate comprising a functional group Q1 capable of reacting with functional group F1 and a target molecule D connected to Q1 via a linker L2 to obtain the antibody-conjugate wherein linker L comprises S-Z3-L2 and wherein Z3 is a connecting group resulting from the reaction between Q1 and F1. The invention also relates to a use for improving the therapeutic index of an antibody-conjugate and to a method for targeting CD30-expressing cells.
IPC 8 full level
A61K 47/34 (2017.01); A61K 47/42 (2017.01); A61K 47/59 (2017.01); A61K 47/68 (2017.01); A61P 35/00 (2006.01); A61P 35/02 (2006.01)
CPC (source: EP)
A61K 47/549 (2017.07); A61K 47/68031 (2023.08); A61K 47/6817 (2017.07); A61K 47/6849 (2017.07); A61K 47/6851 (2017.07); A61K 47/6889 (2017.07); A61P 35/00 (2017.12); A61P 35/02 (2017.12)
Citation (search report)
See references of WO 2017137458A1
Designated contracting state (EPC)
AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
Designated extension state (EPC)
BA ME
DOCDB simple family (publication)
WO 2017137458 A1 20170817; CN 108883191 A 20181123; CN 108883191 B 20221014; EP 3413916 A1 20181219
DOCDB simple family (application)
EP 2017052791 W 20170208; CN 201780022004 A 20170208; EP 17703994 A 20170208