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Clin Pharmacol Ther. 2012 Jan;91(1):101-8. doi: 10.1038/clpt.2011.275. Epub 2011 Nov 30.

Development and clinical utility of abiraterone acetate as an androgen synthesis inhibitor.

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  • 1Department of Medicine, Mayo Clinic, Scottsdale, Arizona, USA.


In April 2011, abiraterone acetate (AA) was approved by the US Food and Drug Administration (FDA) for the treatment of metastatic castration-resistant prostate cancer (CRPC) after chemotherapy. The development of AA is the direct result of our increased understanding of the intricacies of the androgen receptor (AR) pathway and its natural evolution in prostate cancer cells over the course of treatment. In this paper we review the biology of the AR and how it led to the rational design of AA. We also examine the clinical development of AA, its current use, and questions to be addressed for future development.

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