Identification of Metabolites for the Novel 5α-Reductase Inhibitor Epristeride In Vitro and Its Potential Impact on Doping Testing

    November 2025 in “ Drug Testing and Analysis ”
    Zhongquan Li, Bing Liu, Yirang Wang, Jiahui Cheng, Rodrigo Aguilera, Xiaojun Deng, Qing Chen, Peijie Chen
    TLDR Epristeride's metabolism involves key metabolites and proteins, affecting its use in doping tests.
    The study investigates the metabolic pathways of epristeride, a novel noncompetitive inhibitor of Type II 5α-reductase, using in vitro microsome models. Epristeride is considered a potential therapeutic alternative for benign prostatic hyperplasia and its metabolites were analyzed using liquid chromatography–high resolution mass spectrometry. The research identified three primary metabolites: two Phase I oxidation products (M1 and M2) and one Phase II glucuronidation product (M3). Among the five CYP450 isoforms examined, CYP3A4 was found to play a dominant role in epristeride metabolism. The study also identified five key target proteins (ESR1, CYP19A1, STAT3, AKR1C3, and CYP17A1) with which the Phase I metabolites showed significant binding potential, while the Phase II metabolite exhibited lower binding stability. These findings enhance the understanding of epristeride's metabolic pathways and its potential impact on doping control.
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