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SARMs

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Steroidal Selective Androgen Receptor Modulators have existed since the 1940s, while nonsteroidal SARMs, currently in development, act as full agonists in muscle and bone and partial agonists in prostate. These compounds induce specific conformational changes in androgen receptors, impacting gene regulation and tissue specific actions. Preclinical research has shown that SARMs can help increase both muscle and bone mass while minimizing effects on the prostate. Phase I human trials show modest fat-free mass gains. Current substances are a new class of function-promoting anabolic therapies with potential clinical applications for aging, chronic disease and frailty. They may also help manage conditions such as cancer cachexia and osteoporosis, by improving physical function and addressing limitations caused by these health issues. The ability of SARMs to promote both muscle strength and bone mechanical strength constitutes a unique advantage over other therapies for osteoporosis that only increase bone density. Two approaches for achieving tissue selectivity of androgen action are: developing SARMs with specific activity profiles and tissue selectivity, and identifying downstream signaling molecules that activate skeletal muscle hypertrophy without affecting the prostate.

References:

Bhasin, S. and Jasuja, R., 2009. Selective androgen receptor modulators as function promoting therapies. Current Opinion in Clinical Nutrition and Metabolic Care.