Selective Androgen Receptor Modulators

The development of selective androgen receptor modulators (SARMs) that have anabolic effects on the muscle but that do not have adverse effects on the prostate and cardiovascular system has been of considerable interest for the treatment of older men with testosterone deficiency.51-54 The nonsteroidal SARMs differ from testosterone in that they are not converted to active metabolites, such as estradiol and DHT, but they act as agonists in muscle and bone and only partial agonists in prostate and seminal vesicles. More favorable pharmacokinetics and androgen receptor specificity of nonsteroidal SARMs compared to testosterone provide promise for unique pharmacological interactions with the androgen receptor and actions that may allow more specific indications for their clinical use. The proposed mechanisms to explain the tissue selectivity of SARMs as nuclear receptor modulators include ligand binding specific conformational changes in the ligand-binding domain and modulation of surface topology, inducing protein-protein interactions between the androgen receptor and other co-regulators. If the ligand-specific receptor conformation and protein-protein interactions differ in tissues, this could result in tissue-specific gene regulation from interactions with androgen response elements, co-regulators, or transcription factors.

SARMs that promote both muscle strength and bone mechanical strength might have a considerable advantage over other treatments for osteoporosis that only affects bone by increasing bone density.51-54

SARMs that are prostate antagonists, but muscle agonists, might find a use in the treatment of benign prostatic hyperplasia or prostate cancer. Other SARMs with gonadotropin suppression but without prostate stimulation might find application for male contraception. Most of the SARMs research has been conducted in experimental animals. Therefore, the above-mentioned potential applications of SARMs require extensive clinical trials before beneficial use will be a reality.

Whether the absence of both DHT and estrogen action is good or bad is unknown.

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