DGN549

DGN549 is a cytotoxic payload belonging to the indolino-benzodiazepine (IGN) class, specifically designed for incorporation into antibody-drug conjugates (ADCs). Developed by ImmunoGen, DGN549 is a mono-imine DNA alkylator that binds to the minor groove of DNA and covalently alkylates it. This mechanism of action distinguishes it from diimine IGN versions, which function as DNA cross-linkers. Preclinical research indicates that DGN549-based ADCs, often utilizing protease-cleavable peptide linkers like alanine-alanine, demonstrate potent anti-tumor activity with enhanced bystander killing effects and a wider therapeutic index compared to cross-linking IGN ADCs. It has been evaluated in preclinical models targeting folate receptor-alpha (FRα) and EpCAM-expressing malignancies.

Other names

indolino-benzodiazepine DNA-alkylatorIGN DNA-alkylatormono-imine IGN