 | |
| Clinical data | |
|---|---|
| Other names | EPI-506 |
| Routes of administration | By mouth |
| Drug class | Nonsteroidal antiandrogen |
| Identifiers | |
| |
| CAS Number | |
| UNII | |
| KEGG | |
| Chemical and physical data | |
| Formula | C27H33ClO8 |
| Molar mass | 521.00 g·mol−1 |
Ralaniten acetate (developmental code nameEPI-506) is a first-in-classantiandrogen that targets theN-terminal domain (NTD) of theandrogen receptor (AR) developed by ESSA Pharmaceuticals and was under investigation for the treatment ofprostate cancer.[1][2] Thismechanism of action is believed to allow the drug to block signaling from the AR and itssplice variants.[3][4] EPI-506 is aderivative ofbisphenol A[5] and aprodrug ofralaniten (EPI-002), one of the fourstereoisomers ofEPI-001, and was developed as a successor of EPI-001.[6] The drug reachedphase I/II prior to the discontinuation of its development.[1] It showed signs of efficacy in the form ofprostatic specific antigen (PSA) decreases (4–29%) predominantly at higher doses (≥1,280 mg) in some patients but also causedside effects and was discontinued by its developer in favor of next-generation AR NTD inhibitors with improvedpotency andtolerability.[7]
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