drug_type
RELEVANT_DRUG
intervention_type
Drug (antibody–drug conjugate)
drug_description
An intravenous anti-HER2 antibody–drug conjugate (trastuzumab linked via a cleavable linker to the topoisomerase I inhibitor payload deruxtecan [DXd]); binds HER2 (including HER2-low), internalizes, and releases DXd to inhibit topoisomerase I causing DNA damage and apoptosis; retains trastuzumab-mediated HER2 blockade and ADCC with bystander killing.
nci_thesaurus_concept_id
C128799
nci_thesaurus_preferred_term
Trastuzumab Deruxtecan
nci_thesaurus_definition
An antibody-drug conjugate (ADC) composed of trastuzumab, a monoclonal antibody targeting human epidermal growth factor receptor 2 (ERBB2; EGFR2; HER2) conjugated to deruxtecan, a derivative of the camptothecin analog exatecan (DXd; DX-8951 derivative), a DNA topoisomerase 1 (topoisomerase I; Top1) inhibitor, with antineoplastic activity. Upon administration of trastuzumab deruxtecan, trastuzumab targets and binds to HER2 on tumor cells. Upon antibody/antigen binding and internalization, deruxtecan binds to and inhibits Top1-DNA complexes, which results in an inhibition of DNA replication, cell cycle arrest and tumor cell apoptosis. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types. In addition, trastuzumab deruxtecan induces antibody-dependent cell-mediated cytotoxicity (ADCC) and causes a bystander killing effect.
drug_mesh_term
Trastuzumab deruxtecan
drug_category
ANTIBODY DRUG CONJUGATE
drug_class
Conjugate
drug_delivery_route
Intravenous
drug_mechanism_of_action
Anti-HER2 antibody–drug conjugate: trastuzumab targets HER2 (including HER2-low), is internalized, and releases the topoisomerase I–inhibiting payload deruxtecan (DXd), causing DNA damage, cell-cycle arrest, and apoptosis. Retains trastuzumab-mediated HER2 blockade and Fc-dependent ADCC, with a membrane-permeable payload enabling bystander killing.
drug_name
Trastuzumab deruxtecan
nct_id_drug_ref
NCT06210776