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.
    Epristeride, a novel inhibitor of Type II 5α‐reductase, is being studied for its potential use in treating benign prostatic hyperplasia and its implications for doping control. This study used in vitro microsome models to explore epristeride's metabolic pathways, identifying three primary metabolites: two Phase I oxidation products (M1 and M2) and one Phase II glucuronidation product (M3). The research highlighted the dominant role of the CYP3A4 isoform in epristeride metabolism and identified five key target proteins with which the Phase I metabolites showed significant binding potential. These findings enhance the understanding of epristeride's pharmacokinetics and its potential impact on steroid metabolism, providing crucial insights for its monitoring in doping tests.
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      FCE 28260: A Forgotten 5α-Reductase Inhibitor

      community FCE 28260: A Forgotten 5α-Reductase Inhibitor

      in Research  330 upvotes 1 year ago
      FCE 28260 (PNU 156765), an under-explored 5α-reductase inhibitor, showcases promising results in research by Giudici et al., outperforming well-known treatments like Finasteride in reducing the conversion of testosterone to DHT. Its superior efficacy, demonstrated through lower IC50 values in both natural and human recombinant enzyme studies, suggests it could offer more effective management of DHT-related conditions. Additionally, its lower molecular weight hints at better potential for topical application, potentially offering advantages in treating conditions such as androgenic alopecia. Despite its potential, it has not advanced in development, possibly due to financial limitations, leaving its therapeutic prospects and side effect profile largely unexplored.

      community We need actual hair loss studies on Epristeride

      in Research/Science  6 upvotes 1 year ago
      Epristeride is a selective 5 alpha reductase type 2 inhibitor that may reduce scalp DHT similarly to finasteride, with potentially fewer side effects. It is suggested that combining epristeride with finasteride or dutasteride could enhance hair loss treatment effectiveness.

      community Research behind RU-58642? Has anyone heard of this?

      in Research/Science  1 upvotes 6 months ago
      RU-58642 is a powerful anti-androgen that was not developed further, possibly due to safety concerns or financial reasons. RU58841 is a topical alternative, but it is less effective than finasteride and dutasteride, and its long-term effects are not well-studied.

      community How to reduce scalp DHT as much as possible?

      in Finasteride/Dutasteride  16 upvotes 2 months ago
      The conversation discusses reducing scalp DHT to prevent hair loss, with a focus on using dutasteride, finasteride, and other treatments like RU58841 and minoxidil. It highlights the challenges of managing hair loss while on high testosterone levels, suggesting that dutasteride may be more effective than finasteride in such cases.

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