The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
May. 24, 2022
Filed:
Feb. 08, 2017
Synaffix B.v., AB Oss, NL;
Sander Sebastiaan Van Berkel, HR Lent, NL;
Jorge Merijn Mathieu Verkade, NC Eindhoven, NL;
Maria Antonia Wijdeven, HR Lent, NL;
Ryan Heesbeen, CM Nijmegen, NL;
Petrus Josephus Jacobus Maria Van De Sande, BE Eindhoven, NL;
Remon Van Geel, CM Lithoijen, NL;
Brian Maria Gerardus Janssen, MJ Eindhoven, NL;
Inge Catharina Josephina Hurkmans, DG Asten, NL;
Floris Louis Van Delft, KZ Nijmegen, NL;
SYNAFFIX B.V., Oss, NL;
Abstract
The present invention concerns novel and improved antibody-conjugates for targeting HER2. The inventors found N 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(F)-P in the presence of a catalyst, wherein S(F)is a sugar derivative comprising x functional groups F1 capable of reacting with a functional group Q, x is 1 or 2 and P is a nucleoside mono- or diphosphate, and wherein the catalyst is capable of transferring the S(F)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 Qcapable of reacting with functional group Fand a target molecule D connected to Qvia a linker Lto obtain the antibody-conjugate wherein linker L comprises S—Z-Land wherein Zis a connecting group resulting from the reaction between Qand F. The invention also relates to a use for improving the therapeutic index of an antibody-conjugate and to a method for targeting HER2-expressing cells.