The progress of anabolic steroid therapy as a medical treatment has been hampered due to its dose-limiting side effects. Its constant abuse by athletes and bodybuilders did not make it easy to advocate its use for medical benefits.

Over the last decade, researchers have been busy finding alternative treatments – one that can perform the anabolic activities of synthetic testosterone without harboring the negative effects of its androgenic function. With increased efforts, science has been able to tap the potential of androgen receptors or AR.   

The androgenic effect of synthetic steroids is responsible for the feminine characteristics that appear in men who regularly use it. Possible side effects include reduced sperm count, development of breast tissue, impotence, and shrinking of testicles (read more). For women, it accounts for the appearance of hair throughout the body, voice maturation, breast reduction, and irregular menstrual cycle.

In the search for ways to eliminate the adverse androgenic effects of steroids, they were able to stumble upon something that might be fundamental in advanced medicine. That is the discovery of SARMs or Selective Androgen Receptor Modulators.

What are SARMs?

Selective androgen receptor modulators are synthetic drugs that mimic the anabolic effect of steroids without triggering its negative effects such as prostate cancer, heart disease, and those mentioned above. The drug can be non-steroidal and steroidal. Its non-steroidal version is more medically favored than the latter.

During the early nineties, Dalton and Miller’s quest to find a cure for prostate cancer made them accidentally discover SARMs. Since these pioneering efforts, pharmaceutical manufacturers worked to engineer and improve this new nonsteroidal drug.

Despite great efforts, SARMs are currently not approved by the FDA for human consumption. It is also prohibited by the World Anti-Doping Agency for athletic and sports-related use.

How do SARMs work?

The therapeutic applications of anabolic steroids are off the charts. Several studies have already proven its health benefits to people with muscle and bone disorder, anemia, endometriosis, and other chronic conditions. It just did not thrive in the medical field because the risk was greater than the reward. With its tissue-selective properties, SARMs were able to produce favorable pharmacokinetic abilities than its predecessor.

Selective androgen receptor modulators are tissue-selective ligands, which bind to their respective androgen receptors to activate their tissue-specific anabolic effects such as increased muscle mass and fat reduction. Their specificity reduces the chance of the negative androgenic effects from being expressed. Thus, making it a potential treatment for several chronic and terminal conditions.

Potential therapeutic use

SARMs are still under preclinical trials, meaning that it is still being tested on animals. Nevertheless, preclinical results are already promising and are set to advance towards clinical phases.

Cancer-related muscle wasting

Cancer patients undergoing chemotherapy usually suffer from muscle wasting as the disease progresses. It lessens their quality of life as well as their survival rate.

Doctors believed that the administration of SARMs would increase patient’s fat-free muscle mass, size, and strength. The synthetic drug acts by increasing protein synthesis in the muscle cells, thus increasing its number and enhancing its flexibility. Preclinical evidence showed that anabolic effects on the skeletal muscle did not bring about any androgenic effects on the tissue.

SARMs as a treatment for muscle wasting are also applicable for hypogonadal men and the elderly.

Male osteoporosis

According to studies, 50 percent of male osteoporosis is due to the treatment of an underlying condition such as endocrine-related disease, alcoholism, and hypogonadism. It is usually underdiagnosed and will only present itself after a fracture happens. By then, it is already in its severe stages, proving treatments to be worthless.

Based on the present studies, researchers believed SARMs to be a promising treatment for male osteoporosis. Its tissue-specific action stimulates androgenic organs to perform bone formation. This restores bone mass and strength for a patient with severe osteoporosis. Additionally, the action can prevent male osteoporosis in its early stages. Another beneficial action is its anabolic effect. SARMs anabolic effects increase the patient’s bone cell production and reduce the risk of fracture.

Lastly, male patients with hypogonadism can avoid osteoporosis completely by using SARMs as their primary treatment.

Benign prostate hyperplasia

Benign prostate hyperplasia or BPH is a disease characterized by enlargement of the prostate glands. As the disease progresses, it will affect and weaken the urinary bladder, causing it to retain small amounts of urine in the bladder. This can cause urinary tract infection, bladder damage, and kidney damage.

Its usual cause is aging. It develops in men between 51 to 60 years old. During the senior years, the amount of endogenous testosterone decreases, which leaves estrogen to dominate the circulation. When this happens, estrogen will exert its androgenic effects by influencing the prostate cells to grow in numbers.

SARMs were found to potentiate the usual treatment of BPH which is a 5alpha reductase inhibitor. In combination, the two treatments fully inactivates the 5alpha reductase enzyme, causing the suppression of prostate cell hyperplasia. The partial agonistic effect of SARMs also contributes to the suppression of prostate size.

What are its adverse effects?

Its therapeutic use was eventually overshadowed by the authorities’ growing concern of unapproved companies marketing it to the public. Many manufacturers illegally marketed it as “dietary supplements”, which is the reason why the FDA banned its use in the country.

Reported adverse effects of the drug include hypertension, heart disease, and skin rashes. There are also common reports of visual disturbances characterized by a tinge of yellow or green color. These side effects are only based on anecdotal reports. Scientific studies are yet to be published.