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Datopotamab deruxtecan is a Trop-2-directed antibody-drug conjugate (ADC) composed of a humanized monoclonal antibody targeting the tumor-associated antigen TROP2 linked to a topoisomerase I inhibitor payload (deruxtecan). Upon binding to TROP2 on cancer cells, the ADC is internalized and releases its cytotoxic payload inside lysosomes. The released drug inhibits topoisomerase I, causing DNA damage and apoptosis in tumor cells. Datopotamab deruxtecan is approved for the treatment of hormone receptor positive (HR+), HER2-negative unresectable or metastatic breast cancer in adults who have received prior endocrine therapy and chemotherapy. It is also being studied for other cancers including non-small cell lung cancer (NSCLC). The drug was developed jointly by Daiichi Sankyo and AstraZeneca
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