Enzalutamide is a 2nd generation androgen receptor antagonist. It binds to the intracellular androgen receptor and prevents it from translocating into the nucleus and promoting gene transcription. Enzalutamide (Xtandi®) has been approved for use in the treatment of metastatic castration-resistant prostate cancer. More importantly, the co-crystal structure of bicalutamide, a 1st generation androgen receptor inhibitor, and mutant androgen receptor provided binding mechanism insights that facilitated the discovery and development of 2nd generation inhibitors (Tran et al. 2009).

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Tran C, Ouk S, Clegg NJ, Chen Y, Watson PA, Arora V, Wongvipat J, Smith-Jones PM, Yoo D, Kwon A, Wasielewska T, Welsbie D, Chen CD, Higano CS, Beer TM, Hung DT, Scher HI, Jung ME, Sawyers CL. Development of a second-generation antiandrogen for treatment of advanced prostate cancer. Science. 2009 May 8;324(5928):787-90. doi: 10.1126/science.1168175. Epub 2009 Apr 9. PMID: 19359544; PMCID: PMC2981508.