A Review on Steroidal 5α-Reductase Inhibitors for Treatment of Benign Prostatic Hyperplasia

    August 2011 in “ Current Medicinal Chemistry ”
    Jiaqian Sun, Hua Xiang, Lin Yang, J.-B. Chen
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    TLDR New treatments for enlarged prostate are being developed, some of which may be more effective than current medications.
    The document reviewed the effectiveness of steroidal 5α-reductase inhibitors, particularly finasteride and dutasteride, in treating benign prostatic hyperplasia (BPH). It detailed the role of the enzyme 5α-reductase in converting testosterone to dihydrotestosterone (DHT), a key factor in BPH development, and the significance of targeting the enzyme's two isozymes. The review highlighted dutasteride as a potent dual inhibitor, reducing DHT levels by over 90%, compared to finasteride's 65-80% reduction. It also discussed the importance of structural modifications, such as the C17-substituent, in enhancing inhibitory activity, with new compounds showing up to five times the potency of finasteride. The document concluded by mentioning the synthesis of new inhibitors, like compound 66, with comparable potency to finasteride, indicating ongoing efforts to improve treatment options for BPH.
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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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