drug_type
RELEVANT_DRUG
intervention_type
Drug - antibody-drug conjugate
drug_description
An anti-HER2 antibody–drug conjugate (Enhertu) composed of humanized IgG1 trastuzumab linked to a topoisomerase I inhibitor payload (DXd). It binds HER2 on tumor cells, is internalized, and releases DXd to inhibit topoisomerase I, causing DNA damage and bystander killing; it also retains trastuzumab functions such as ADCC and HER2 signaling blockade.
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
Humanized anti-HER2 monoclonal antibody (trastuzumab) linked to a topoisomerase I inhibitor (DXd). Binds HER2 on tumor cells, is internalized, and releases DXd to inhibit topoisomerase I, causing DNA damage, replication arrest, and apoptosis with a bystander-killing effect; retains trastuzumab functions including HER2 signaling blockade and antibody-dependent cell-mediated cytotoxicity (ADCC).
drug_name
Trastuzumab deruxtecan
nct_id_drug_ref
NCT05480384