ZEN-017

ZEN-017 is a small molecule inhibitor of the Bromodomain and Extra-Terminal (BET) family of proteins, which includes BRD2, BRD3, and BRD4. Developed by Zenith Epigenetics, ZEN-017 functions as an epigenetic modulator by competitively binding to the acetyl-lysine recognition site (bromodomain) of BET proteins. This action prevents the recruitment of BET proteins to chromatin, thereby inhibiting the transcription of key oncogenic drivers such as MYC, BCL2, and CDK6 that are critical for the survival and proliferation of various cancer cells. ZEN-017 has been investigated in early-stage clinical research for the treatment of solid tumors and hematological malignancies, including NUT midline carcinoma and acute myeloid leukemia. By targeting these epigenetic readers, the drug aims to disrupt the transcriptional programs that maintain the malignant phenotype in sensitive tumor types.