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FAR02 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 ring and incorporating an additional methylene group to enhance molecular flexibility. FAR02 is intended for the treatment of prostate cancer, including castration-resistant prostate cancer (CRPC), where AR signaling continues to drive tumor growth despite androgen deprivation therapy. Preclinical studies have evaluated its antagonistic activity in vitro using the androgen-dependent LNCaP prostate cancer cell line.
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