Ralaniten_acetate
Ralaniten acetate
Chemical compound
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.[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]