Prostate cancer enzalutamide

Pal SK, Stain CA, Sartor O. Enzalutamide for the treatment of prostate cancer. Expert Opin Pharmacother. 2013 14 679-85. 

Enzalutamide (Xtandi) An Androgen Receptor Antagonist for Late-Stage Prostate Cancer... 

Enzalutamide (1, marketed as Xtandi and formerly known as MDV3100) was developed by the pharmaceutical company Medivation and was approved by the US FDA on August 31, 2012, for men with docetaxel-pretreated, metastatic castration-resistant prostate cancer (CRPC). The current market price for enzalutamide treatment is approximately 7000/month with treatments lasting 5-8 months. 

In phase I/II trials for enzalutamide 1, 140 men with progressive castration-resistant prostate cancer (CRPC) were enrolled across the United States. In a majority of those enrolled, the cancer was metastasized, and approximately half of the patients had received prior chemotherapy. Anti-tumor activity was observed at all doses and the maximum tolerated dose of enzalutamide was determined to be 240 mg daily, and no additional anti-tumor effects were... 

Current ongoing trials are intended to explore the possibility of using enzalutamide in earlier stages of the disease and to investigate the optimal sequencing and combination of enzalutamide with other standard and novel therapies for prostate cancer. 

Enzalutamide is an oral inhibitor of AR signalling that blocks AR interaction, inhibits translocation of the AR to the nucleus, impairs AR binding to DNA and inhibits co-activator recruitment and receptor-mediated DNA transcription. In the United Kingdom, enzalutamide is licensed for the treatment of men wi metastatic, castrate-resistant prostate cancer whose disease has progressed on or after docetaxel-based chemotherapy. 

Hoffman-Censits J, Kelly WK. Enzalutamide a novel antiandrogen for patients with castrate-resistant prostate cancer. Clin Cancer Res 2013 19(6) 1335-9. 

Scher HI, Fizazi K, Saad F, TaplinME, Sternberg CN, Miller K, et al. AFFIRM investigators. Increased survival with enzalutamide in prostate cancer after chemotherapy. N Engl J Med 2012 367(13) 1187-97. 

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