Ralaniten acetate

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Ralaniten acetate
Ralaniten acetate.svg
Clinical data
Routes of
By mouth
Drug classNonsteroidal antiandrogen
CAS Number
Chemical and physical data
Molar mass521.00 g·mol−1

Ralaniten acetate (developmental code name EPI-506) is a first-in-class drug that targets the amino-terminal domain of the androgen receptor developed by ESSA Pharmaceuticals and was under investigation for the treatment of prostate cancer.[1][2] It was a successor of EPI-001 and targets the N-terminal domain (NTD) 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 derivative of bisphenol A[5] and a prodrug of ralaniten (EPI-002), one of the four stereoisomers of EPI-001.[6] The drug reached phase I/II prior to the discontinuation of its development.[1] It showed signs of efficacy in the form of prostatic specific antigen (PSA) decreases (4–29%) predominantly at higher doses (≥1,280 mg) in some patients but also caused side effects and was discontinued by its developer in favor of next-generation AR NTD inhibitors with improved potency and tolerability.[7]

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  1. ^ a b "Ralaniten acetate - ESSA Pharma - AdisInsight".
  2. ^ 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. PMID 26389532.
  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): 29. doi:10.1007/s11934-016-0584-4. ISSN 1527-2737. PMC 4888068. PMID 26902623.
  5. ^ McEwan, Iainj; Monaghan, Amye (2016). "A sting in the tail: The N-terminal domain of the androgen receptor as a drug target". Asian Journal of Andrology. 18 (5): 687–94. doi:10.4103/1008-682X.181081. PMC 5000789. PMID 27212126.
  6. ^ 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. PMC 3696543. PMID 23722902.
  7. ^ "ESSA Pharma Announces Results from the Phase 1 Clinical Trial of EPI-506 for Treatment of mCRPC and Updates Clinical and Strategic Plans" (Press release). ESSA Pharma.

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