PNU 157706, A Novel Dual Type I and II 5α-Reductase Inhibitor

    E. Di Salle, D. Giudici, A. Radice, T. Zaccheo, G. Ornati, Marcella Nesi, A. Panzeri, Sylvie Délos, Pierre-Marie Martin
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    TLDR PNU 157706 is a more effective treatment than finasteride for conditions caused by DHT, like enlarged prostate and hair loss.
    PNU 157706 was identified as a potent inhibitor of both type I and II 5α-reductase enzymes, surpassing the efficacy of finasteride, a known inhibitor. It demonstrated IC50 values of 3.9 nM for type I and 1.8 nM for type II 5α-reductase in human recombinant enzymes. In vivo studies showed that PNU 157706 reduced prostatic DHT levels more effectively than finasteride in rats, without binding to the androgen receptor, indicating no anti-androgen activity. The compound also significantly reduced prostate weight in castrated rats implanted with testosterone, but not in those implanted with DHT, suggesting its action is specific to inhibiting 5α-reductase. These results suggest PNU 157706 could be a more efficient therapy for conditions related to DHT, such as benign prostatic hyperplasia and androgenic alopecia.
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      FCE 28260: A Forgotten 5α-Reductase Inhibitor

      community FCE 28260: A Forgotten 5α-Reductase Inhibitor

      in Research  330 upvotes 3 months 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.

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