Precise Control of Drug-to-Antibody Ratio (DAR) via Pyridazinedione- Based Site-Selective Conjugation

  • Summarizing the current pyridazinedione (PD)-based linkers that enable precise and programmable control over drug-to-antibody ratio (DAR), including DARs of 8, 4, 2 and 1, generating highly homogeneous antibody conjugates from native antibodies
  • Discussing recent advances that enable modular access to DARs 1, 2, 3, 4, 5, 6, 7 and 8 on THIOMAB-based scaffolds, by using the versatility of the PD core, p-anisidine derivatives and various click chemistries