ZEN-019

ZEN-019 is a potent, small-molecule inhibitor specifically targeting the second bromodomain (BD2) of the Bromodomain and Extra-Terminal (BET) family proteins, which include BRD2, BRD3, and BRD4. Developed by Zenere Therapeutics, ZEN-019 is designed to provide more selective epigenetic modulation compared to first-generation pan-BET inhibitors, with the goal of reducing dose-limiting toxicities such as thrombocytopenia and gastrointestinal distress. By selectively binding to the BD2 pocket, ZEN-019 disrupts the recruitment of BET proteins to chromatin, thereby downregulating the transcription of key oncogenic drivers such as MYC, BCL2, and CDK6. The compound is primarily being investigated for the treatment of advanced solid tumors and hematological malignancies that are dependent on BET-mediated transcriptional programs, including NUT midline carcinoma and other MYC-driven cancers.