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

The Pt linker [ethylenediamineplatinum(II)] , 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 <15 % to ca. 75-90 % conjugation efficiency is described, resulting from a systematic screening of all relevant reaction parameters.