Preferred Label : Trastuzumab Envedotin;
NCIt synonyms : Antibody-drug Conjugate DP303c; ADC DP303c; Anti-HER2 Antibody-drug Conjugate DP303c;
NCIt definition : An antibody-drug conjugate (ADC) composed of trastuzumab, a humanized immunoglobulin
G1 (IgG1) a monoclonal antibody targeting human epidermal growth factor receptor 2
(EGFR2; HER2; ErbB2) and site-specifically conjugated, via a cleavable linker, to
the microtubule-disrupting cytotoxic agent monomethyl auristatin E (MMAE), with potential
antineoplastic activity. Upon administration of trastuzumab envedotin, the trastuzumab
moiety targets and binds to HER2 on the surface of tumor cells. Following internalization,
MMAE targets and binds to tubulin, and inhibits microtubule polymerization. This results
in G2/M phase cell cycle arrest and apoptosis in HER2-expressing tumor cells. HER2,
a tyrosine kinase receptor, is overexpressed by many cancer cell types. Trastuzumab
envedotin has an average drug-to-antibody (DAR) ratio of 2.0; the two MMAE molecules
are attached site-specifically through transamidation to residue Q295 in the antibody
heavy chain's constant region.;
UNII : 37DMF82G1F;
CAS number : 2865132-89-2;
Molecule name : DP-303c; DP 303c;
NCI Metathesaurus CUI : CL1407846;
Origin ID : C173962;
UMLS CUI : C5418040;
Currated CISMeF NLP mapping
Semantic type(s)
concept_is_in_subset