drug_type
RELEVANT_DRUG
intervention_type
Antibody-drug conjugate
drug_description
Investigational antibody–drug conjugate (ADC) designed to deliver a cytotoxic payload to tumor antigen–expressing 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
Human IgG1 anti-HER3 antibody linked via a cleavable peptide linker to a DNA topoisomerase I inhibitor. After binding HER3 on tumor cells, the ADC is internalized and the payload is released to inhibit topoisomerase I, causing DNA breaks, blocking DNA replication, and inducing apoptosis in HER3-expressing cells.
drug_name
SHR-A2009
nct_id_drug_ref
NCT06092268