FAR03

FAR03 is an experimental small molecule androgen receptor (AR) antagonist developed as part of a series (FAR01-FAR11) for the treatment of prostate cancer, including castration-resistant prostate cancer (CRPC). It is structurally derived from the second-generation AR antagonist enzalutamide, featuring a modification where the rigid thiohydantoin pharmacophore is replaced by a more flexible 4,4-dimethylimidazolidin-2-one moiety. Additionally, the structure incorporates a methylene group between the pharmacophore and one of the aromatic rings to increase molecular flexibility. FAR03 was designed to inhibit AR signaling, which remains fundamental to tumor growth even in castration-resistant stages of the disease. The compound was evaluated in vitro using the androgen-dependent LNCaP prostate cancer cell line to assess its antagonistic activity relative to established therapies.