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drug_type
RELEVANT_DRUG
intervention_type
Antibody–drug conjugate
drug_description
HER3-directed antibody–drug conjugate targeting ERBB3; internalization after receptor binding with subsequent release of a cytotoxic payload to kill HER3-expressing tumor cells.
nci_thesaurus_concept_id
C202278
nci_thesaurus_definition
An antibody-drug conjugate (ADC) composed of an immunoglobulin G1 (IgG1) human monoclonal antibody directed against human epidermal growth factor receptor 3 (HER3; ErbB3) conjugated via a cleavable peptide linker to a cytotoxic DNA topoisomerase I inhibitor, with potential antineoplastic activity. Upon administration of anti-HER3 ADC SHR-A2009, the anti-HER3 antibody moiety targets and binds to HER3 expressed on tumor cells. Upon binding, internalization and linker cleavage, the topoisomerase I inhibitor targets and binds to DNA topoisomerase I, thereby stabilizing the cleavable complex between topoisomerase I and DNA and resulting in DNA breaks, inhibition of DNA replication and apoptosis in HER3-expressing tumor cells. HER3, a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases, is frequently overexpressed in tumors.
drug_category
ANTIBODY DRUG CONJUGATE
drug_class
Conjugate
drug_delivery_route
Intravenous
drug_mechanism_of_action
HER3 (ERBB3)-targeted IgG1 ADC that binds HER3 on tumor cells, undergoes internalization and cleavable-linker processing to release a topoisomerase I inhibitor payload, stabilizing Topo I–DNA complexes and inducing DNA breaks, replication arrest, and apoptosis in HER3-expressing cells.
drug_name
SHR-A2009
nct_id_drug_ref
NCT06649331