Nonsteroidal Selective Androgen Receptors Modulators (SARMs): Designer Androgens with Flexible Structures Provide Clinical Promise

    November 2004 in “ Endocrinology
    Terry R. Brown
    TLDR SARMs may offer benefits by boosting muscle effects without unwanted side effects.
    The document discussed the development and potential of nonsteroidal selective androgen receptor modulators (SARMs) as alternatives to traditional steroidal androgens. These SARMs, specifically S1 and S4, demonstrated tissue-selective activity in male rats, acting as partial agonists in androgen-responsive tissues like the prostate and seminal vesicles, but as full agonists in anabolic tissues such as the levator ani muscle. This selectivity allowed them to suppress prostate growth without affecting muscle mass or altering hormone levels, unlike traditional treatments. The study highlighted the importance of ligand structure in determining androgen receptor function and suggested that SARMs could offer therapeutic benefits by enhancing desirable androgen effects while minimizing adverse outcomes.
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