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

The Pt II 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 <15 % to ca. 75–90 % conjugation efficiency is described, resulting from a systematic screening of all relevant reaction parameters. NaI, a...