Degrader Antibody–Drug Conjugates (DACs): Redefining Payload Design for Precision-Engineered Biotherapeutics
- Chimeric degraders, by leveraging the ubiquitin–proteasome system, can substantially enhance the potency of traditional small-molecule inhibitors, advancing from sub-micromolar to sub-nanomolar efficacy. This capability significantly broadens the accessible payload target space and enables the precision engineering of novel therapeutic payloads
- DACs exhibit internalization-dependent cellular target degradation and robust inhibition of cell proliferation in vitro, demonstrating a powerful mechanism of action that couples targeted delivery with intracellular protein degradation
- DACs are able to display favorable ADME characteristics, potent in vivo antitumor activity with reduced toxicities, underscoring their potential as next-generation precision therapeutics