Preferred Label : Anti-TA-MUC1/DXd Antibody-drug Conjugate DS-3939a;
NCIt synonyms : Anti-TA-MUC1 ADC DS-3939a; Anti-TA-MUC1/DXd ADC DS-3939a;
NCIt definition : An antibody-drug conjugate (ADC) composed of a humanized monoclonal antibody directed
against tumor-associated mucin-1 (TA-MUC1) conjugated to the cytotoxic DNA topoisomerase
I inhibitor and exatecan derivative DXd (MAAA-1181a; MAAA-1181) via an enzymatically
cleavable tetrapeptide-based linker, with potential antineoplastic activity. Upon
administration of anti-TA-MUC1/DXd ADC DS-3939a, the anti-TA-MUC1 antibody targets
and binds to TA-MUC1-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 TA-MUC1-expressing
tumor cells. MUC1, a glycoprotein normally expressed on epithelial cells and overexpressed
on the surface of a variety of cancer cells, plays a key role in tumor cell survival
and proliferation. TA-MUC1 is designated to MUC1 epitopes with carbohydrate-induced
conformational structures that are tumor-specific.;
Molecule name : DS-3939a; DS 3939a;
NCI Metathesaurus CUI : CL1926350;
Origin ID : C204077;
UMLS CUI : C5908022;
Semantic type(s)
concept_is_in_subset
has_target