EPI-013

EPI-013 is a small molecule inhibitor that specifically targets the N-terminal domain (NTD) of the androgen receptor (AR). It is one of the four stereoisomers (specifically the 2R, 19S form) that constitute EPI-001, a compound discovered by ESSA Pharma. Unlike traditional AR-targeted therapies like enzalutamide or bicalutamide, which bind to the C-terminal ligand-binding domain (LBD), EPI-013 forms a covalent bond with the Tau-5 region of the NTD. This mechanism allows the drug to inhibit the transcriptional activity of both full-length AR and truncated AR splice variants (such as AR-V7) that lack the LBD and are frequently implicated in the development of castration-resistant prostate cancer (CRPC). By blocking the NTD, EPI-013 prevents the recruitment of essential co-activators and the assembly of the transcriptional complex, thereby suppressing the expression of AR-regulated genes and inhibiting tumor cell proliferation.

Other names

(2R, 19S)-EPI-001