Compact hydrophilic electrophiles enable highly efficacious high DAR ADCs with excellent <i>in vivo</i> PK profile
Philipp Ochtrop, Jahaziel Jahzerah, Paul Machui, Isabelle Mai, Dominik Schumacher, Jonas Helma, Marc‐André Kasper, Christian P. R. Hackenberger
Abstract
stability and increased antitumor activity in tumour xenograft models relative to the established FDA approved VC-PAB-MMAE ADC Adcetris, clearly showing the benefit of the phosphonamidate based building-blocks as a general tool for the efficient and stable antibody-based delivery of highly hydrophobic linker-payload systems.
Topics & Concepts
In vivoElectrophilePharmacologyChemistryCombinatorial chemistryMaterials scienceNanotechnologyMedicineOrganic chemistryBiologyCatalysisBiotechnologyChemical Synthesis and AnalysisHER2/EGFR in Cancer ResearchClick Chemistry and Applications