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NEV-801 is a conjugated multi-inhibitor small molecule drug developed by Neovia Oncology for the treatment of advanced, drug-resistant cancers. It acts as a multi-targeted antineoplastic agent, selectively inhibiting both topoisomerase I and II enzymes, which are essential for DNA replication and gene expression. In addition to its topoisomerase inhibition, NEV-801 inhibits hypoxia-inducible factor 1 (HIF-1) transcriptional activation and the hypoxic induction of vascular endothelial growth factor (VEGF) mRNA. The compound also targets RecQ helicase Werner syndrome protein (WRN), aiming to overcome multidrug resistance mediated by MDR genes. By simultaneously blocking these cancer pathways, NEV-801 is designed to induce tumor cell stress that leads to increased expression of target antigens on tumor cells, thereby enhancing immune recognition and potentially improving the efficacy of immunotherapies. Preclinical studies have shown promising results in models of chronic myeloid leukemia and advanced colon cancer resistant to standard therapies, with minimal bone marrow or gastrointestinal toxicity observed[2][5][7][9].
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