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NT-0231 is a small molecule inhibitor of the Bromodomain and Extra-Terminal (BET) family of proteins, specifically designed to be selective for the second bromodomain (BD2). Developed by Nuvation Bio, NT-0231 aims to provide therapeutic benefit in various oncology indications, including solid tumors, by disrupting the epigenetic reading of acetylated histones. By selectively targeting the BD2 pocket of BET proteins such as BRD4, the drug modulates the expression of key oncogenes like MYC while potentially minimizing the dose-limiting toxicities, such as thrombocytopenia and gastrointestinal issues, often associated with non-selective BET inhibitors that target both BD1 and BD2. NT-0231 is part of a broader pipeline of epigenetic modulators intended to treat advanced malignancies through precise transcriptional regulation.
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