Enzalutamide (915087-33-1) is a clinically useful non-steroidal antiandrogen (IC50 = 36 nM) for the treatment of castration-resistant prostate cancer.1,2 It impairs binding of the androgen receptor to DNA, the recruitment of co-activators, and reduces the efficiency of nuclear translocation.
- Tran et al. (2009), Development of a Second-Generation Antiandrogen for Treatment of Advanced Prostate Cancer; Science 324 787
- Jung et al. (2010), Structure-Activity Relationship for Thiohydantoin Androgen Receptor Antagonist for Castration-Resistant Prostate Cancer (CRPC); J. Med. Chem. 53 2779