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EPI-001
EPI-001 is a novel, small molecule drug with potential use for the treatment of prostate cancer. The drug is under investigation by the pharmaceutical company ESSA Pharma Inc (Vancouver, Canada) for the treatment of castration-resistant prostate cancer (CRPC).
EPI-001 is an antagonist of the androgen receptor (AR) that acts by binding covalently to the N-terminal domain (NTD) of the AR and blocking protein-protein interactions required for transcriptional activity of the AR and its splice variants (IC50 for inhibition of AR NTD transactivation ≈ 6 µM).〔〔 This is different from all currently-used antiandrogens, which, conversely, bind to the C-terminal ligand-binding domain (LBD) of the AR and competitively block binding and activation of the receptor by androgens.〔 Due to its unique mechanism of action, EPI-001 may prove to be effective in the treatment of advanced prostate cancer resistant to conventional antiandrogens such as enzalutamide.〔
==Discovery==
EPI-001 was discovered by Marianne Sadar at the British Columbia Cancer Agency and Raymond Andersen at the University of British Columbia. It was derived from bisphenol A diglycidyl ether (BADGE), a known antiandrogenic endocrine disruptor of the bisphenol family.
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