NCI Drug Dictionary

The NCI Drug Dictionary contains technical definitions and synonyms for drugs/agents used to treat patients with cancer or conditions related to cancer. Each drug entry includes links to check for clinical trials listed in NCI's List of Cancer Clinical Trials.

anti-HER2 antibody-drug conjugate MEDI4276
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 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. Check for active clinical trials using this agent. (NCI Thesaurus)

Synonym:ADC MEDI4276
Code name:MEDI4276