from Section 5 - Medical and Surgical Management of Issues of Male Health
Published online by Cambridge University Press: 06 December 2023
The androgen receptor (AR) is part of a superfamily of nuclear receptors. The AR has a diverse set of downstream effects on male phenotype and sexual function, muscle mass and strength, bone density, hematopoiesis, cognition, and metabolism. Testosterone replacement therapy (TRT) to treat male hypogonadism utilizes exogenously administered testosterone to activate the AR. However, TRT is known to have potential risks, including erythrocytosis, dyslipidemia, prostatic hypertrophy, hepatotoxicity, impaired fertility, aromatization of testosterone to estrogen, and testicular atrophy. Selective androgen receptor modulators, also known as SARMs, are compounds that have shown tissue-selective activation of the AR. These compounds potentially offer the ability to treat hypogonadal conditions where activating the AR in the bone, muscle, or brain is desired while sparing undesired effects in tissues such as the prostate, liver, or bone marrow. Currently, there is a dearth of data in human subjects regarding the treatment of male hypogonadism with SARMs. However, from animal models and preliminary studies of SARMs in humans, there appears to be a possible role for SARMs in the hypogonadal man, and their efficacy and safety warrant further study.
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