FAR01

FAR01 is a small molecule androgen receptor (AR) antagonist belonging to a series of 4,4-dimethylimidazolidin-2-one pharmacophore-based compounds. It was designed to inhibit AR signaling, a critical pathway in the progression of prostate cancer and the development of castration-resistant prostate cancer (CRPC). FAR01 was synthesized as a structural modification of second-generation AR antagonists like enzalutamide, replacing the rigid thiohydantoin ring with a more flexible 4,4-dimethylimidazolidin-2-one moiety to explore the impact of molecular flexibility and electronic effects on antagonistic activity. Preclinical evaluation in LNCaP prostate cancer cell lines has been conducted to assess its potency relative to established therapies.