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/auristatin payload antibody-drug conjugate XMT-1522
An antibody-drug conjugate (ADC) composed of HT-19, a monoclonal antibody directed against the human epidermal growth factor receptor 2 (ERBB2; HER2), conjugated, via a proprietary biodegradable, hydrophilic polymer backbone and various linkers, to proprietary auristatin-derived payload molecules (about 15 per antibody), with potential antineoplastic activity. Upon administration of anti-HER2/auristatin payload ADC XMT-1522, the antibody moiety targets and binds to a unique epitope in the extracellular domain (ECD) of HER2. Upon internalization, cleavage and release of the cytotoxic molecules, the auristatin-derived molecules bind to tubulin and inhibit its polymerization, which results in G2/M phase arrest and induces apoptosis of HER2-expressing tumor cells. The attachment of multiple auristatin molecules to the backbone enables XMT-1522 to effectively kill tumors that express relatively low amounts of the HER2 protein; therefore, this agent shows increased therapeutic potential in tumors with low HER2 expression compared to other anti-HER2 antibody-based therapies. The polymer-based proprietary platform optimizes delivery of the cytotoxic drug payload and improves drug solubility. Check for active clinical trials using this agent. (NCI Thesaurus)
Synonym: ADC XMT-1522
anti-HER2 ADC XMT-1522
Code name: XMT-1522