drug_type
RELEVANT_DRUG
intervention_type
Drug
drug_description
An antibody–drug conjugate (HER3-DXd; U3-1402) consisting of a fully human anti-HER3 (ERBB3) IgG1 monoclonal antibody linked via a cleavable linker to DXd, a membrane-permeable topoisomerase I inhibitor. It binds HER3 on tumor cells, is internalized, and releases DXd intracellularly to inhibit topoisomerase I, causing DNA damage and cell death with a potential bystander effect.
nci_thesaurus_concept_id
C136987
nci_thesaurus_preferred_term
Patritumab Deruxtecan
nci_thesaurus_definition
An antibody-drug conjugate (ADC) composed of patritumab, a monoclonal antibody directed against the human epidermal growth factor receptor HER3 (ErbB3),linked to the topoisomerase I inhibitor DX 8951, a semisynthetic, water-soluble derivative of camptothecin, with potential antineoplastic activity. Upon administration of patritumab deruxtecan, the patritumab moiety targets and binds to HER3. After internalization, DX 8951 inhibits topoisomerase I activity by stabilizing the complex between topoisomerase I and DNA and inhibiting religation of DNA breaks, thereby inhibiting DNA replication and triggering apoptotic cell death. HER3, a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases, is frequently overexpressed in tumors.
drug_mesh_term
patritumab deruxtecan
drug_category
ANTIBODY DRUG CONJUGATE
drug_class
Conjugate
drug_delivery_route
Intravenous
drug_mechanism_of_action
Patritumab deruxtecan is a HER3-targeted antibody–drug conjugate. The patritumab antibody binds HER3 (ERBB3) on tumor cells, is internalized, and a cleavable linker releases the DXd payload intracellularly. DXd inhibits topoisomerase I by stabilizing the Topo I–DNA complex and preventing religation of DNA breaks, leading to DNA damage and apoptotic cell death. The membrane-permeable payload can exert a bystander effect on neighboring tumor cells.
drug_name
patritumab deruxtecan
nct_id_drug_ref
NCT06172478