Definition

An antibody-drug conjugate (ADC) composed of a humanized immunoglobulin G1 (IgG1) monoclonal antibody against the tumor-associated antigen (TAA) cadherin-6 (CDH6; CDH-6) conjugated to deruxtecan, which is comprised of an enzymatically cleavable tetrapeptide-based linker and MAAA-1181a (DXd), the cytotoxic DNA topoisomerase I inhibitor derivative of exatecan, with potential antineoplastic activity. Upon administration of raludotatug deruxtecan, raludotatug targets and binds to CDH6-expressing tumor cells. Upon cellular uptake and lysosomal degradation of the linker, DXd targets and binds to DNA topoisomerase I, thereby stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks, inhibition of DNA replication and apoptosis. This inhibits the proliferation of CDH6-expressing tumor cells. CDH6, a member of the cadherin family and overexpressed by a variety of cancers, plays a key role in tumor cell proliferation.