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Selective Androgen Receptor Modulators (SARMs) as Function Promoting Therapies
Purpose of review
The last decade has witnessed unprecedented discovery effort to develop selective androgen receptor modulators (SARMs) that improve physical function and bone health without adversely affecting the prostate and cardiovascular outcomes. This review describes the historical evolution, the rationale for SARM development, and the mechanisms of testosterone action and SARM selectivity.
While steroidal SARMs have been around since the 1940s, a number of nonsteroidal SARMs that do not serve as substrates for CYP19 aromatase or 5α-reductase, act as full agonists in muscle and bone and as partial agonists in prostate are in development. The differing interactions of steroidal and nonsteroidal compounds with AR contribute to their unique pharmacologic actions. Ligand binding induces specific conformational changes in the ligand binding domain, which could modulate surface topology and protein-protein interactions between AR and coregulators, resulting in tissue-specific gene regulation. Preclinical studies have demonstrated the ability of SARMs to increase muscle and bone mass in preclinical rodent models with varying degree of prostate sparing. Phase I trials of SARMs in humans have reported modest increments in fat-free mass.
promise as a new class of function promoting anabolic therapies for a number of
clinical indications, including functional limitations associated with aging
and chronic disease, frailty, cancer cachexia, and osteoporosis.
Where to Buy SARMs
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Every batch of their SARMs are 3rd party verified, so you know that they’re at least 99% pure, verified by an independent laboratory.
When ordering SARMs online, you need to be very
careful—only get them from a reputable vendor, as many vendors sell fake SARMs
laced with dangerous prohormones, or even worse.