Preferred Label : Anti-TROP2/EGFR Bispecific Antibody-drug Conjugate DM001;
NCIt synonyms : Anti-TROP2/EGFR Bispecific ADC DM001; Anti-TROP2/EGFR ADC DM001; Anti-EGFR/TROP2 ADC DM001; Anti-TROP2/Anti-EGFR/MMAE ADC DM001;
NCIt 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.;
Molecule name : DM-001; DM 001;
Origin ID : C211878;
concept_is_in_subset
- has_target
