deruxtecan

Deruxtecan is a novel, potent topoisomerase I inhibitor that functions as a cytotoxic payload in antibody-drug conjugates (ADCs). It is an exatecan derivative. In ADCs, deruxtecan is linked to a monoclonal antibody (e.g., trastuzumab, patritumab, datopotamab) via a cleavable linker. The antibody targets specific proteins on cancer cells, leading to the internalization of the ADC. Once inside the cell, deruxtecan is released, enters the nucleus, and induces DNA damage, leading to apoptotic cell death. A key feature of ADCs containing deruxtecan is their "bystander effect," where the released payload can diffuse out of the targeted cell and kill neighboring tumor cells, even those with low target antigen expression. It was developed by Daiichi Sankyo.

Other names

exatecan derivative