An Efficient Conjugation Approach for Coupling Drugs to Native Antibodies via the PtII Linker Lx for Improved Manufacturability of Antibody–Drug Conjugates

The PtII linker [ethylenediamineplatinum(II)]2+, coined Lx, has emerged as a novel non‐conventional approach to antibody–drug conjugates (ADCs) and has shown its potential in preclinical in vitro and in vivo benchmark studies. A crucial improvement of the Lx conjugation reaction from initially...

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Bibliographic Details
Published in:Angewandte Chemie 2021-02, Vol.133 (6), p.3045-3052
Main Authors: Merkul, Eugen, Muns, Joey A., Sijbrandi, Niels J., Houthoff, Hendrik‐Jan, Nijmeijer, Bart, Rheenen, Gerro, Reedijk, Jan, Dongen, Guus A. M. S.
Format: Article
Language:English
Subjects:
Antibodies
antibody–drug conjugates
Chemistry
Conjugates
Conjugation
Efficiency
In vivo methods and tests
Inorganic salts
Iodides
linkers
Manufacturability
platinum
Selectivity
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Summary:The PtII linker [ethylenediamineplatinum(II)]2+, coined Lx, has emerged as a novel non‐conventional approach to antibody–drug conjugates (ADCs) and has shown its potential in preclinical in vitro and in vivo benchmark studies. A crucial improvement of the Lx conjugation reaction from initially
ISSN:0044-8249
1521-3757
DOI:10.1002/ange.202011593