Deruxtecan (MC-GGFG-DXD) is a cleavable antibody-drug conjugate (ADC) linker used in the synthesis of ADCs such as fam-trastuzumab deruxtecan-nxki (ENHERTU®), which is approved for the treatment of certain types of HER2-positive breast cancer and gastroesophageal junction cancer. The MC (maleimide) moiety enables selective conjugation to thiol groups on antibodies, while the GGFG peptide sequence serves as a protease-cleavable linker that is degraded intracellularly, enabling the release of the cytotoxic payload DXD within target cells.
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