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Raludotatug deruxtecan is an investigational antibody-drug conjugate (ADC) specifically engineered to target cadherin-6 (CDH6), a tumor-associated antigen highly expressed in several cancer types, including ovarian and renal cell carcinoma. The drug consists of a humanized anti-CDH6 IgG1 monoclonal antibody linked via tetrapeptide-based cleavable linkers to multiple molecules of DXd, a potent DNA topoisomerase I inhibitor payload derived from exatecan. Upon binding to CDH6 on the surface of cancer cells, the ADC is internalized and trafficked to lysosomes where the cytotoxic payload is released. This results in inhibition of cell replication and induction of apoptosis; additionally, the membrane-permeable DXd can exert bystander effects on neighboring tumor cells with heterogeneous CDH6 expression. Raludotatug deruxtecan has demonstrated strong antitumor activity in preclinical models and is currently being evaluated in clinical trials for advanced ovarian cancer. It is being developed by Daiichi Sankyo and Merck and utilizes proprietary DXd ADC technology developed by Daiichi Sankyo. It remains investigational as of April 2025.
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