Discovery and Clinical Development of Dutasteride, a Potent Dual 5α-Reductase Inhibitor

    Stephen V. Frye
    TLDR Dutasteride effectively treats benign prostatic hyperplasia and may reduce prostate cancer risk.
    The review described the discovery and clinical development of dutasteride, a dual inhibitor of type 1 and type 2 5α-reductase, for treating prostatic diseases. Dutasteride was optimized through structure-activity relationship studies to inhibit both forms of human 5α-reductase. Clinical results from three randomized, placebo-controlled, Phase III studies over 2 years showed that dutasteride improved symptoms of benign prostatic hyperplasia (BPH). Additionally, dutasteride was being studied for its potential to reduce prostate cancer incidence in high-risk men, with its dual inhibition, half-life, and tolerability being significant factors for treatment success.
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