drug_type
RELEVANT_DRUG
intervention_type
Drug
drug_description
A first-in-human, intravenous bispecific antibody–drug conjugate that co-engages TROP2 and EGFR on tumor cells to enable receptor-mediated internalization and targeted delivery of a cytotoxic payload; administered every 3 weeks for advanced solid tumors.
nci_thesaurus_concept_id
C211878
nci_thesaurus_preferred_term
Anti-TROP2/EGFR Bispecific Antibody-drug Conjugate DM001
nci_thesaurus_definition
An antibody-drug conjugate (ADC) composed of a bispecific antibody directed against the tumor associated antigens (TAAs) trophoblast cell surface protein 2 (trophoblast antigen 2; calcium signal transducer 2; TROP2; TROP-2; TACSTD2; GA733-1; M1S1) and human epidermal growth factor receptor (EGFR), conjugated, via a protease-cleavable linker, to the auristatin derivative and microtubule-disrupting cytotoxic agent monomethyl auristatin E (MMAE), with potential antineoplastic activity. Upon administration, the antibody moiety of anti-TROP2/EGFR bispecific ADC DM001 targets and binds to TROP2 and EGFR expressed on tumor cells. Upon binding, internalization, proteolytic cleavage of linker, and the release of MMAE, MMAE targets and binds to tubulin, and inhibits microtubule polymerization. This results in G2/M phase cell cycle arrest and apoptosis in TROP2 and EGFR-expressing tumor cells. TROP2 and EGFR are co-expressed in a variety of cancer cells. TROP2, a transmembrane protein overexpressed in various tumors, is associated with enhanced tumor aggressiveness, metastasis, drug resistance and increased tumor cell survival. EGFR, a receptor tyrosine kinase mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization.
drug_mesh_term
Antibody-Drug Conjugates
drug_category
ANTIBODY DRUG CONJUGATE
drug_class
Conjugate
drug_delivery_route
Intravenous
drug_mechanism_of_action
Bispecific antibody–drug conjugate that co-binds TROP2 and EGFR on tumor cells, undergoes receptor-mediated internalization, and releases the cytotoxic payload MMAE via a protease-cleavable linker; MMAE binds tubulin, inhibits microtubule polymerization, and induces G2/M arrest and apoptosis in TROP2/EGFR-expressing tumors.
drug_name
DM001
nct_id_drug_ref
NCT06475937