drug_type
RELEVANT_DRUG
intervention_type
Antibody–drug conjugate
drug_description
An antibody–drug conjugate consisting of patritumab (anti-HER3 monoclonal antibody) linked to the deruxtecan topoisomerase I inhibitor payload (DXd). It binds HER3 on tumor cells, is internalized, and releases DXd to inhibit Topo 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
Human anti-HER3 monoclonal antibody (patritumab) linked via a cleavable linker to a deruxtecan (DXd) topoisomerase I inhibitor payload. Binds HER3 (ERBB3) on tumor cells, is internalized, and releases DXd intracellularly; DXd inhibits Topo I by stabilizing the Topo I–DNA cleavage complex and blocking religation, causing DNA damage, replication arrest, and apoptosis. The membrane-permeable payload can produce a bystander effect.
drug_name
Patritumab deruxtecan
nct_id_drug_ref
NCT06596694