1637573-04-6

Ralaniten triacetate (EPI-506), the pro-agent of Ralaniten, is a first-in-class, orally active androgen receptor (AR) N-terminal domain (NTD) inhibitor. Ralaniten triacetate shows activity against both full length and resistance-related AR species, including AR-v7[1][2].

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[1] Obst JK, et al. Revealing Metabolic Liabilities of Ralaniten To Enhance Novel Androgen Receptor Targeted Therapies. ACS Pharmacol Transl Sci. 2019;2(6):453-467. Published 2019 Sep 26. DOI:10.1021/acsptsci.9b00065
[2] Chi, Kim Nguyen et al. Efficacy, safety, tolerability, and pharmacokinetics of EPI-506 (ralaniten acetate), a novel androgen receptor (AR) N-terminal domain (NTD) inhibitor, in men with metastatic castration-resistant prostate cancer (mCRPC) progressing after enzalutamide and/or abiraterone. Journal of Clinical Oncology 35 (2017): 5032-5032.