Ralaniten acetate explained

Ralaniten acetate (developmental code name EPI-506) is a first-in-class antiandrogen that targets the N-terminal domain (NTD) of the androgen receptor (AR) developed by ESSA Pharmaceuticals and was under investigation for the treatment of prostate cancer.[1] [2] 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, and was developed as a successor of EPI-001.[6] The drug reached phase I/II prior to the discontinuation of its development. 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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Notes and References

  1. Web site: Ralaniten acetate - ESSA Pharma . AdisInsight . Springer Nature Switzerland AG .
  2. Martinez-Ariza G, Hulme C . Recent advances in allosteric androgen receptor inhibitors for the potential treatment of castration-resistant prostate cancer . Pharmaceutical Patent Analyst . 4 . 5 . 387–402 . 2015 . 26389532 . 10.4155/ppa.15.20 .
  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 . 0732-183X . 2016-02-27 . 2016-03-06 . https://web.archive.org/web/20160306055024/http://meetinglibrary.asco.org/content/146857-156 . dead .
  4. Silberstein JL, Taylor MN, Antonarakis ES . Novel Insights into Molecular Indicators of Response and Resistance to Modern Androgen-Axis Therapies in Prostate Cancer . Current Urology Reports . 17 . 4 . 29 . April 2016 . 26902623 . 4888068 . 10.1007/s11934-016-0584-4 .
  5. Monaghan AE, McEwan IJ . 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 . 2016 . 27212126 . 5000789 . 10.4103/1008-682X.181081 . free .
  6. Myung JK, Banuelos CA, Fernandez JG, Mawji NR, Wang J, Tien AH, Yang YC, Tavakoli I, Haile S, Watt K, McEwan IJ, Plymate S, Andersen RJ, Sadar MD . 6 . An androgen receptor N-terminal domain antagonist for treating prostate cancer . The Journal of Clinical Investigation . 123 . 7 . 2948–60 . July 2013 . 23722902 . 3696543 . 10.1172/JCI66398 .
  7. ESSA Pharma Announces Results from the Phase 1 Clinical Trial of EPI-506 for Treatment of mCRPC and Updates Clinical and Strategic Plans . ESSA Pharma.

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