FAR04

FAR04 is a small molecule androgen receptor (AR) antagonist developed as part of a series of 4,4-dimethylimidazolidin-2-one derivatives (FAR01-FAR11). It was designed as a structural analog of the second-generation AR antagonist enzalutamide, specifically replacing the rigid thiohydantoin pharmacophore with a more flexible 4,4-dimethylimidazolidin-2-one moiety. This modification was intended to explore the impact of molecular flexibility and electronic effects on the inhibition of AR signaling, which is a primary driver of prostate cancer progression. Preclinical research has evaluated FAR04 for its potential in treating androgen-dependent prostate cancer and castration-resistant prostate cancer (CRPC) by competitively binding to the AR and preventing its activation by endogenous androgens.