ZEN3694

ZEN3694 is an orally bioavailable small molecule inhibitor of the Bromodomain and Extra-Terminal (BET) family of proteins, including BRD2, BRD3, and BRD4. As an epigenetic modulator, it prevents the binding of BET proteins to acetylated lysine residues on histones, thereby disrupting the assembly of transcriptional complexes required for the expression of key oncogenes such as MYC and the androgen receptor (AR). Developed by Zenith Epigenetics, ZEN3694 is primarily investigated for its potential to overcome resistance to standard-of-care therapies in solid tumors, including metastatic castration-resistant prostate cancer (mCRPC) and triple-negative breast cancer (TNBC). It is often studied in combination with other targeted agents, such as the CDK9 inhibitor VIP152 or androgen receptor signaling inhibitors like enzalutamide, to enhance therapeutic efficacy and reverse acquired resistance mechanisms.

Other names

BET bromodomain inhibitor ZEN-3694