drug_type
RELEVANT_DRUG
intervention_type
Antibody–drug conjugate (ADC)
drug_description
An anti-HER2 antibody–drug conjugate (T-DXd, Enhertu) composed of trastuzumab linked via a cleavable linker to a DXd topoisomerase I inhibitor payload; binds HER2, is internalized, releases DXd to induce DNA damage and cell death with a bystander effect, and the antibody component also inhibits HER2 signaling and mediates ADCC.
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 mAb (trastuzumab) targets HER2 on tumor cells and is internalized; a cleavable linker releases the DXd payload (a topoisomerase I inhibitor), causing DNA damage, replication arrest, and apoptosis. The membrane‑permeable payload enables a bystander killing effect, and the antibody component also inhibits HER2 signaling and mediates ADCC.
drug_name
Trastuzumab deruxtecan
nct_id_drug_ref
NCT05744375