Therapeutic Androgen Receptor Ligands

    January 2003 in “ Nuclear Receptor Signaling
    George F. Allan, Zhihua Sui
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    TLDR Androgens and SARMs play a role in body mass, frailty, skin health, and hair growth, and are used in treating prostate cancer, acne, and hair loss, with potential for new uses and improved versions in the future.
    In 2002, George F. Allan and Zhihua Sui reviewed the role of androgens and selective androgen receptor modulators (SARMs) in various physiological functions and diseases. They noted that declining androgen levels with age can lead to decreased lean body mass and increased frailty. They also discussed the potential link between androgens and prostate cancer, and the use of androgen antagonists in treating prostate cancer and benign prostatic hyperplasia, despite their side effects. The authors also highlighted the role of androgens in skin health and hair growth, and how excess androgens can cause acne and alopecia. They predicted that androgen antagonists would continue to be used in treating prostate cancer and would likely be approved for new uses, such as treating hirsutism in women, alopecia in men, and acne in both sexes. They also foresaw the emergence of new SARMs with improved tissue specificity. The authors were optimistic about the potential of SARM agonists to increase lean body mass and muscle strength in hypogonadal men and in patients with cancer and immunodeficiency, thereby counteracting frailty associated with aging.
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