ZEN003694 + enzalutamide

This is a **combination therapy of ZEN003694 (also known as ZEN-3694), a pan-bromodomain and extra-terminal domain inhibitor (BET inhibitor), and enzalutamide, an androgen receptor inhibitor**. ZEN003694 disrupts the function of BET proteins, which regulate the transcription of genes involved in cancer cell proliferation and survival, including *MYC* and androgen receptor (AR) signaling genes. Enzalutamide blocks the AR signaling pathway, which is implicated in the growth of castration-resistant prostate cancer (CRPC). The combination is studied in metastatic castration-resistant prostate cancer (mCRPC), especially in tumors with resistance to prior androgen-signaling inhibitors. Mechanistically, the combination aims to abrogate AR pathway resistance and re-sensitize tumors to AR inhibition, with robust down-regulation of BET-dependent gene expression and AR pathway activity[1][7][3][9]. Both ZEN003694 and enzalutamide are administered orally. ZEN003694 is developed by Zenith Epigenetics, and enzalutamide is developed by Pfizer/Astellas. Current research supports further clinical development of this combination, with evidence of additive or potentially synergistic efficacy in AR-signaling inhibitor-resistant mCRPC[1][7][9].

Other names

ZEN-3694 + enzalutamideZEN003694 + enzalutamide