Ralaniten acetate

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Ralaniten acetate
Clinical data
Other namesEPI-506
Routes of
administration		By mouth
Drug classNonsteroidal antiandrogen
Identifiers
  • (2S)-3-phenyl]propan-2-yl)phenoxy]propane-1,2-diyl diacetate
CAS Number
UNII
KEGG
Chemical and physical data
FormulaC27H33ClO8
Molar mass521.00 g·mol−1

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. This mechanism of action is believed to allow the drug to block signaling from the AR and its splice variants. EPI-506 is a derivative of bisphenol A and a prodrug of ralaniten (EPI-002), one of the four stereoisomers of EPI-001, and was developed as a successor of EPI-001. 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.

See also

References

  1. ^ a b "Ralaniten acetate - ESSA Pharma". AdisInsight. Springer Nature Switzerland AG.
  2. ^ Martinez-Ariza G, Hulme C (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. 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. Archived from the original on 2016-03-06. Retrieved 2016-02-27.
  4. ^ Silberstein JL, Taylor MN, Antonarakis ES (April 2016). "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. PMC 4888068. PMID 26902623.
  5. ^ Monaghan AE, McEwan IJ (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 JK, Banuelos CA, Fernandez JG, Mawji NR, Wang J, Tien AH, et al. (July 2013). "An androgen receptor N-terminal domain antagonist for treating prostate cancer". The Journal of Clinical Investigation. 123 (7): 2948–60. doi:10.1172/JCI66398. 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.

External links

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