In Vivo Time-Dependent Inhibition of Human Steroid 5a-Reductase by Finasteride

    January 1996 in “Journal of Pharmaceutical Sciences
    Gaochao Tian
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    TLDR Finasteride poorly inhibits type 1 5AR, affecting its effectiveness.
    The paper discusses the time-dependent inhibition of human steroid 5a-reductase by finasteride, a specific 5AR inhibitor used to treat benign prostatic hyperplasia. The study found that the limited efficacy of finasteride in vivo is due to poor inhibition of type 1 5AR. The rate of inhibition is important for both potency and selectivity, and the document analyzes the in vivo factors affecting these rates. The study concludes that time-dependent inhibitors have potential for potent inhibition of target enzymes, but their potency may not be observed in vivo unless the rate of inhibition is faster than the rate of inhibitor elimination.
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