drug_type
RELEVANT_DRUG
intervention_type
Antibody–drug conjugate
drug_description
Antibody–drug conjugate targeting EGFR and c-MET that delivers a topoisomerase I inhibitor payload to induce DNA damage and tumor cell kill.
nci_thesaurus_concept_id
C192091
nci_thesaurus_preferred_term
Tilatamig Samrotecan
nci_thesaurus_definition
An antibody-drug conjugate (ADC) composed of a tilatamig, a bispecific antibody targeting both epidermal growth factor receptor (EGFR) and hepatocyte growth factor receptor (HGFR; c-Met) and conjugated to a topoisomerase-1 inhibitor (TOP1i), with potential antineoplastic activity. Upon administration, tilatamig samrotecan simultaneously targets and binds to the extracellular domains of wild-type (WT) or certain mutant forms of both EGFR and c-Met expressed on cancer cells. Upon binding and internalization, the TOP1i moiety is released, binds to TOP1 and stabilizes cleaved DNA-TOP1 complexes. This prevents DNA re-ligation, induces irreversible DNA strand breaks, prevents DNA repair, and leads to cycle arrest and apoptosis specifically in tumor cells expressing EGFR and c-Met. EGFR and c-Met, both upregulated or mutated in a variety of tumor cell types, play key roles in tumor cell proliferation.
drug_category
ANTIBODY DRUG CONJUGATE
drug_class
Conjugate
drug_delivery_route
Intratumoral
drug_mechanism_of_action
Bispecific anti-EGFR/anti-c-MET antibody-drug conjugate that binds EGFR and c-MET on tumor cells, is internalized, and releases a topoisomerase I inhibitor payload which stabilizes TOP1-DNA cleavage complexes, preventing religation and inducing DNA strand breaks, cell-cycle arrest, and apoptosis in EGFR/c-MET–expressing tumors.
drug_name
AZD9592
nct_id_drug_ref
NCT06366451