ralaniten

**Ralaniten** (EPI-002) is a first-in-class small molecule inhibitor that directly targets the intrinsically disordered N-terminal domain (NTD) of the androgen receptor (AR), specifically binding covalently to the activation function-1 (AF-1) region, including the transactivation Tau-5 domain. Unlike traditional antiandrogens that target the ligand-binding domain (LBD), ralaniten inhibits the transcriptional activity of both full-length AR and constitutively active AR splice variants lacking the LBD—a relevant mechanism for castration-resistant prostate cancer (CRPC). Ralaniten blocks essential protein-protein interactions required for AR-driven gene expression and has demonstrated preclinical efficacy in reducing tumor growth and disrupting AR-driven transcriptional programs in CRPC models. Ralaniten (EPI-002) was studied in humans as the active metabolite of its prodrug, ralaniten acetate (EPI-506). Clinical development was terminated after phase I due to insufficient potency and poor metabolic properties[1][2][3][5][7][9].

Brand names

ralaniten

Other names

ralanitenbisphenol-A derivative