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  • A human immunoglobulin G1 (IgG1) monoclonal antibody-drug conjugate (ADC) targeting the extracellular domain of T-cell immunoglobulin mucin-1 (TIM-1) (clone CR014) and linked, via a valine-citrulline (vc) peptide linker, to the potent cytotoxic agent monomethyl auristatin E (MMAE), with potential antineoplastic activity. Upon administration of ADC Anti-TIM-1-vcMMAE CDX-014, the monoclonal antibody moiety targets and binds to TIM-1. Upon internalization and proteolytic cleavage, MMAE is released into the cytosol of TIM-1-expressing tumor cells, binds to tubulin and inhibits its polymerization, resulting in G2/M phase arrest and tumor cell apoptosis. TIM-1 is upregulated in a variety of cancer cell types while only minimally expressed in healthy tissue. The linkage system in CDX-014 is highly stable in plasma, resulting in cytotoxic specificity for TIM-1-positive cells. Check for \'https://www.cancer.gov/about-cancer/treatment/clinical-trials/intervention/C129401\' active clinical trials using this agent. (\'http://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI%20Thesaurus&code=C129401\' NCI Thesaurus)
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