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DGN549
- Development stage
- Preclinical
- Lead developer
- AbbVie
- Modality
- Small Molecules
- Administration
- Intravenous
01
Overview
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
02
Targets
DNA
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