Preferred Label : Anti-HER2 Antibody-drug Conjugate MEDI4276;
NCIt synonyms : ADC MEDI4276;
NCIt related terms : MEDI-4276;
NCIt definition : An antibody-drug conjugate (ADC) composed of a bispecific antibody against the extracellular
domain of human epidermal growth factor receptor 2 (HER2; ERBB2) comprised of the
single-chain variable fragment (scFv) of the anti- HER2 monoclonal antibody trastuzumab,
which binds to domain IV of HER2, fused to the heavy chains of the anti-HER2 monoclonal
antibody 39S, which binds to domain II of HER2, and conjugated, via a cleavable linker,
to the cytotoxic anti-microtubule agent tubulysin, with potential antineoplastic activity.
Upon administration of ADC MEDI4276, the anti-HER2 bispecific antibody specifically
targets and binds to HER2 on the surface of certain cancer cells. Upon binding, crosslinking
and internalization of antibody-HER2 complexes occurs and MEDI4276 is transported
to the lysosome where the linker is cleaved, thereby delivering tubulysin inside HER2-expressing
cancer cells. Tubulysin binds to tubulin and inhibits microtubule polymerization,
which blocks cell division. This results in G2/M phase arrest, tumor cell apoptosis,
and decreased proliferation of HER2-expressing tumor cells. HER2, a tyrosine kinase
receptor, is overexpressed by many cancer cell types.;
UNII : ZAM3L34SEW;
Molecule name : MEDI-4276;
NCI Metathesaurus CUI : CL504915;
Origin ID : C126355;
UMLS CUI : C4287735;
Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
- has_target
