SARMs (abbreviation for Selective androgen receptor modulator) are selective androgen receptor modulators. By the same principle as SERMs – selective modulators of estrogen receptors, which include the well-known clomiphene and tamoxifen, SARMs are able to attach to the receptors of sex hormones, only not female, but male androgens and interact with them. But not having the same structure as anabolic steroids, SARMs are not affected by enzymes that convert testosterone into other compounds with unwanted health effects.
In creating this class of drugs, scientists hoped to reduce the adverse effects of testosterone on the prostate. As is customary, first of all any substances and compounds are tested on animals; in the case of positive effects and having made sure that they are safe to take, clinical studies are conducted on humans, after which they are put into production. Often the positive results in experiments on rats alone are enough to get the drug in the field of view of “chemical” athletes, who began to test it on themselves.
About the same situation was with SARMs – as soon as they started to be written about this brainchild of James Dalton in the accessible literature, saying that taking them leads to muscle mass growth, they immediately, illegally, found their way into the hands of bodybuilders. One of the first, despite controversial research findings, was Andarine, better known in the sports world as ‘S4′. And Ostarine known as GTX-024 came right after it. Both products were already being sold in Internet stores before it was officially confirmed that Ostarine really helps people to gain muscle mass and is relatively safe in use. However, in high-performance sports and when antidoping controls are threatened, Ostarine is extremely risky and undesirable because its metabolites are detected for three months or more – depending on the dose and the individual athlete’s metabolic patterns. No data on other SARMs are available yet.
For example, in September 2011, the Journal Cachexia Sarcopenia Muscle (‘Journal Cachexia Sarcopenia Muscle’), pp. 153 – 161, appeared an article with the self-speaking title “The selective androgen receptor modulator GTx-024 improves muscle mass and physical function in healthy older men and postmenopausal women: results from a double-blind, placebo-controlled phase II study.” The results of GTx-024, which were statistically significant: a 12-week course of 3 mg oral administration resulted in 1.4 kg of lean muscle mass gain and 300 g of fat mass loss in the absence of any physical activity, were presented in this paper. Lower dosages resulted in less pronounced results. The official conclusion of the researchers was that GTx-024 showed a dose-dependent improvement in overall muscle mass and physical function and was well tolerated. GTx-024 may be useful for the prevention and/or treatment of muscle mass catabolism associated with cancer and other chronic diseases.” Maybe 1.4 kg of muscle mass in 12 weeks is not much, but it is an officially obtained and documented result.
At the moment, pharmaceutical companies have several types of SARMs for which the first stages of human clinical trials have been successfully completed and may soon appear in the legal sale, and by then, the practice of their use for sports purposes will have already formed, but at the moment, even based on the small amount of information above, you can get an idea of the dosage, duration of administration and side effects.
Research Evidence
No selective androgen receptor modulator is truly selective at this time. They only show a higher anabolic index, with a ratio of anabolic to androgenic activity ranging from 3:1 to 10:1 (testosterone has a ratio of 1:1)
Virtually all selective androgen receptor modulators are available in tablet form and do not cause liver damage.
They are the optimal choice for women because they have minimal effects on libido, sex characteristics, blood cholesterol levels, liver, etc.
SARM’S legal status.
Most SARM’S have legal status. SARM’s are very likely to be recognized as drugs in court practice.
Stages of SARMs trials
Clinical trials:
- Ostarine (MK-2866, GTx-024) – acts on bone and muscle tissue
- BMS-564,929 – acts primarily on muscle tissue
- Ligandrol – Ligandrol or Anablicum (lab code LGD-4033) – similar to Ostarine
Preclinical testing:
- AC-262,356 (Accadine, Sarmastol)
- JNJ-28330835
- LGD-2226 – effects on bone and muscle, study suspended due to high toxicity
- LGD-3303
- S-40503- acts primarily on bone (treatment of osteoarthritis)
- S-23 (Mastorin, Mastorin) – as a male contraceptive
- YK-11 (Myostan, Myostine, Myostan, Miostop)[16] – a Japanese SARM in development, which is also a myostatin inhibitor
- RAD140 (Radarine, Radium) – developed by Radius, suitable for oral administration, in addition to its anabolic effect causes an increase in endurance and has neuroprotective effects
Suspended:
- Andarin – Andarine (lab code S-4, S-40503, GTx-007) – development is no longer supported
- Cardarin – (Cardarin, Endurobol, Peroximod, Hennos, laboratory code number GW-501516) – development is no longer supported due to carcinogenic effects
Other (not related to SARMs):
- Reverol (Reverol, edrophonium, Endorol, Stenabol, or SR9009) – Oral-eligible compound being developed by Scripps Research Institute. The main effects are the increase of endurance (due to the formation of new mitochondria), treatment of obesity, muscle hypertrophy. The mechanism of action is to bind to the Rev-ErbA alpha molecule in the body, which performs various regulatory functions.
- Recardin (Recardin or SR9011) is an analog of SR9009.
- Ibutamoren – Ibutamoren, Nutrobal (MK-677) is a growth hormone secretion stimulant taken orally.
- Laxogenin (5a-hydroxy-laxogenin or Anogenin) – A plant steroid sapogenin, studied by the Japanese as early as 1960. It has now begun to be actively promoted in sports, although no positive effects in humans have been proven.
- AICAR- an endurance drug
