Preferred Label : Datopotamab Deruxtecan;
NCIt synonyms : ADC DS-1062a; Anti-TROP2/DXd Antibody-drug Conjugate DS-1062a; Dato-DXd;
NCIt definition : An antibody-drug conjugate (ADC) composed of a humanized monoclonal antibody against
tumor-associated antigen (TAA) trophoblast cell surface protein 2 (calcium signal
transducer 2; TROP2; TROP-2; TACSTD2) conjugated, via an enzymatically cleavable tetrapeptide-based
linker, to the cytotoxic DNA topoisomerase I inhibitor and exatecan (DX-8951) derivative
DXd (MAAA-1181a; MAAA-1181), with potential antineoplastic activity. Upon administration
of the datopotamab deruxtecan, the anti-TROP2 antibody targets and binds to TROP2
expressed on 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 tumor cell proliferation of TROP2-expressing tumor cells.
TROP2 is a transmembrane protein overexpressed in various tumors while its expression
is low and/or restricted in normal, healthy tissues. Its expression is associated
with enhanced tumor aggressiveness, metastasis, drug resistance and increased tumor
cell survival. The ADC allows for reduced systemic exposure and enhanced delivery
of the cytotoxic agent DXd.;
UNII : GD2OWY1DTK;
CAS number : 2238831-60-0; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 2238831-60-0
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G-SRS /a ;
Molecule name : DS-1062a; DS-1062;
NCI Metathesaurus CUI : CL553190;
Origin ID : C151967;
UMLS CUI : C5432272;
Semantic type(s)
- concept_is_in_subset
- has_target
