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EPI-506 (developed by Essa Pharma; structure undisclosed as of 2015)[1] is an experimental antiandrogen in phase I/II development for prostate cancer.[2] It is the successor of EPI-001 and targets the N-terminal domain of the androgen receptor (AR). This mechanism of action is believed to allow the drug to block signaling from the AR and its splice variants.[3][4] EPI-506 is a prodrug of EPI-002, one of the four stereoisomers of EPI-001.[5]


  1. Martinez-Ariza, Guillermo; Hulme, Christopher (2015). "Recent advances in allosteric androgen receptor inhibitors for the potential treatment of castration-resistant prostate cancer". Pharmaceutical Patent Analyst. 4 (5): 387–402. doi:10.4155/ppa.15.20. ISSN 2046-8954.
  2. "Safety and Anti-Tumor Study of Oral EPI-506 for Patients With Metastatic Castration-Resistant Prostate Cancer - Full Text View - ClinicalTrials.gov". clinicaltrials.gov. Retrieved 2016-02-27.
  3. "A phase 1/2 open-label study of safety and antitumor activity of EPI-506, a novel AR N-terminal domain inhibitor, in men with metastatic castration-resistant prostate cancer (mCRPC) with progression after enzalutamide or abiraterone.". Journal of Clinical Oncology. ISSN 0732-183X.
  4. Silberstein, John L.; Taylor, Maritza N.; Antonarakis, Emmanuel S. (2016-02-23). "Novel Insights into Molecular Indicators of Response and Resistance to Modern Androgen-Axis Therapies in Prostate Cancer". Current Urology Reports. 17 (4): 1–10. doi:10.1007/s11934-016-0584-4. ISSN 1527-2737.
  5. Myung, Jae-Kyung; Banuelos, Carmen A.; Fernandez, Javier Garcia; Mawji, Nasrin R.; Wang, Jun; Tien, Amy H.; Yang, Yu Chi; Tavakoli, Iran; Haile, Simon; Watt, Kate; McEwan, Iain J.; Plymate, Stephen; Andersen, Raymond J.; Sadar, Marianne D. (2013). "An androgen receptor N-terminal domain antagonist for treating prostate cancer". Journal of Clinical Investigation. 123 (7): 2948–2960. doi:10.1172/JCI66398. ISSN 0021-9738.

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