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| Other names | EPI-506 |
| Routes of administration | By mouth |
| Drug class | Nonsteroidal antiandrogen |
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| Formula | C27H33ClO8 |
| Molar mass | 521.00 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.[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 derivativeofbisphenol A[5] and a prodrugofralaniten (EPI-002), one of the four stereoisomersofEPI-001, and was developed as a successor 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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| ARTooltip Androgen receptor |
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