The acronym SARMs stands for “Selective Androgen Receptor Modulators.” They bind with androgens and act in a similar manner as androgenic drugs like anabolic steroids (ex., testosterone). However, they are more selective than anabolic steroids; thus, they have less uses than these steroids. On the other hand, their selectivity means that they are safer to use than steroids.
The Science behind the Molecule
Selective Androgen Receptor Modulators refer to a group of androgen receptor ligands. This means that they bind with androgens. The ligand/androgen pair then travels to the cell’s nucleus and signals it to start gene transcription. This gene transcription may result in increased production of proteins and certain molecules, depending on which genes are stimulated.
Steroidal versions of this molecule were first studied in the 1940s and were based on a testosterone model. Today, non-steroidal versions of this group have been produced by independent pharmaceutical companies. These include cyclic quinolinones and aryl propinoamides, which exhibit anabolic activity on skeletal muscles as well as tissue selectivity.
Anabolic activity refers to the synthesis of complex molecules from simpler molecules while storing energy (“anabolism”). Anabolic steroids and hormones help produce proteins in cells, which contribute to muscle building.
Drugs that are able to stimulate or block hormone receptors in specific conditions are called “selective receptor modulators.” This mimics the beneficial effects of synthetic and natural steroids in a specific tissue without causing unwanted harm to other tissues. One such drug is SARMs. They give the same benefits as Anabolic Androgenic Steroids (like testosterone) but are less likely to produce unwanted side effects. They can cause fat loss, increased muscle mass, or increased bone density in particular tissues without affecting others.
Steroids are often prescribed for muscle degeneration or for hormone replacement therapy. However, there could be several unwanted side-effects to steroid intake. This is why alternative molecules are being researched by pharmaceutical companies.
Anabolic Androgenic Steroids can cause following:
• Prostate cancer stimulation
• Over-stimulation of hair growth
• Breast development in males
• Male pattern baldness
• High blood pressure
• Cholesterol imbalance
• Liver toxicity
• Growth of the left ventricle of the heart
• Impairment of the body’s natural testosterone production
In comparison, stimulating the androgen receptors in muscle or bone only can prevent these side effects.
The benefits associated with these selective androgen receptors are:
• Can be taken orally
• Prevention of muscle loss during weight loss
• Growth of lean muscles
• Rehabilitation after injury
• Post-cycle therapy after anabolic use (they can restore normal testosterone levels in the body)
• Anabolic effects even with low dosage
• Help in aerobic and anaerobic endurance
• Heals joint injuries
• Doesn’t significantly damage the liver
• Ideal for Androgen Replacement Therapy, especially in cases of osteoporosis and muscle wasting
Androgen Replacement Therapy
Currently, oral androgen replacements are rather limited. There are two commonly used forms: Andriol, which is considered expensive and ineffective, and Methyl testosterone, which can damage the liver. SARMs can be a good alternative to these, since it can also be taken orally and still produce beneficial effects without resulting in liver toxicity.
Many types of SARMs are presently undergoing development. They have different androgenic and anabolic activity, as well as varying potential side effects. Generally, though, most produce few side effects and have anabolic profiles similar to testosterone. The one furthest along, Ostarine, is at the third and final stage for clinical development.
SARMs were banned for a few years by the World Anti-Doping Agency, but efforts are underway for developing testing protocols for them. They have a relatively short half life, unique structures, and a short research history. These characteristics present a complex problem to many doping authorities.