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Selective Androgen Receptor Modulators (SARMs) – A Prohibited Class of Anabolic Agents

usada_logo_high_resolutionWhat are SARMs?

Selective Androgen Receptor Modulators (SARMs) are a class of therapeutic compounds that have similar properties to anabolic agents, but with reduced androgenic properties. This property allows SARMs the advantage of androgen-receptor specificity, tissue selectivity, and the lack of steroid-related side effects. Some potential side effects of anabolic steroid use include acne, liver damage, breast tissue development, and shrinking of the testicle in males, and deepening of the voice, growth of hair on the face, stomach, upper back, and abnormal menstrual cycles in females. SARMs have the ability to differentiate between anabolic and androgenic activities, and this provides the potential for therapeutic opportunities in a variety of medical conditions including muscle-wasting diseases, osteoporosis, cancer, and hypogonadism. [1] [2]

What is the current status of SARMs on the WADA Prohibited List?

SARMs have been prohibited by the World Anti-Doping Agency (WADA) since 2008. SARMs have the potential to be misused for performance enhancement in sport due to their anabolic properties as well as ability to stimulate androgen receptors in muscle and bone. They are currently prohibited at-all-times in the category of “other anabolic agents” under section S1.2 of the WADA Prohibited List. Some examples of SARMs are Ostarine and Andarine. [3]

Is there a list of clinically-approved SARMs?

The first non-steroidal SARMs were introduced in 1998 and since then there has been a growing list of drug candidates in this new class of therapeutics. [3] Many SARM drug candidates have been subject to pre-clinical and clinical trials by global pharmaceutical companies. However, full clinical approval for human consumption as prescription drugs has not yet been accomplished for any of the substances. Published scientific literature, reviews on recent developments and clinical trials of SARM drug candidates are available.

What are the number of Adverse Analytical Findings for SARMs?

SARMs were added to the WADA Prohibited List in 2008. The first Adverse Analytical Finding (AAF) with a SARM drug candidate was reported in 2010. [3] Since then, there has been a steady increase in the number of AAFs reported globally. As per the WADA Anti-Doping Testing Figures report, over 30 AAFs have been reported for SARMs between 2012 and 2014.

What is the detection strategy for SARMs?

Due to the recent increase in the number of SARMs-related AAFs in doping control samples, anti-doping agencies have taken a proactive approach to tackle SARMs abuse in sport. Potential SARM drug candidates are investigated even though clinical trials for these drugs are not yet complete. This allows anti-doping agencies to integrate testing strategies for SARMs, in an efficient and timely manner, to routine testing procedures. [4] Demonstration and effectivity of this strategy was in 2010, when an AAF was reported with the non-approved and officially discontinued SARM drug candidate, Andarine. [3]

As a more recent example of preventive doping research, metabolites of LG121071, a potential SARM drug candidate, were generated in vitro and a detection method was established for urine samples based on liquid-chromatography-tandem mass spectrometry. This assay serves as a detection method in sport drug testing. [4]

Can SARMs be found in dietary supplements?

SARMs are not legal ingredients for dietary supplements. However, there have been instances of products containing SARMs being sold illegally as dietary supplements. These products could pose significant health risks to athletes. Since SARMs are prohibited at-all-times on the WADA Prohibited List, consumption of these dietary supplements could also lead to an Anti-Doping Rule Violation (ADRV) in sport. Athletes should be aware that SARMs ingredients could be listed on dietary supplement product labels under various names, and should be cautious when consuming such products. [5]

As an example, in 2014, the U.S. Food and Drug Administration (FDA) issued a warning letter to a dietary supplement company as one of their products contained an unapproved SARM ingredient, Ostarine. According to the letter, a dietary supplement cannot include a substance that is being investigated as a new drug candidate; in this case, Ostarine. [6]

 

Pictured:

Chemical structures of selected selective androgen receptor modulator drug candidates: andarine (A), ostarine (B). Photo credit: Figure 6, p. 5 of Geyer H , Schänzer W, Thevis M. Anabolic agents: recent strategies for their detection and protection from inadvertent doping. Br J Sports Med 2014;48:820-826. http://bjsm.bmj.com/content/48/10/820.full.

 

Resources:

[1] Zhang X, Sui Z. Deciphering the selective androgen receptor modulators paradigm. Expert Opin Drug Discov. 2013;8(2):191-218. http://www.ncbi.nlm.nih.gov/pubmed/23231475

[2] Chen J, Kim J, Dalton J. Discovery and therapeutic promise of selective androgen receptor modulators. Mol Interv. 2005;5(3):173-188.  http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2072877/

[3] Geyer H , Schänzer W, Thevis M. Anabolic agents: recent strategies for their detection and protection from inadvertent doping. Br J Sports Med 2014;48:820-826. http://bjsm.bmj.com/content/48/10/820.full. Photo credit to this article, Figure 6, p. 5.

[4] Knoop A, Krug O, Voncenti M, Schanzer W, Thevis M. In vetro metabolism studies on the selective androgen receptor modulator (SARM) LG121071 and its implementation into human doping controls using liquid chromatography-mass spectrometry. Eur J Mass Spectrom 2015;21(1):27-36. http://www.ncbi.nlm.nih.gov/pubmed/25906032 

[5] U.S. Department of Defense, Human Performance Resource Center. What are SARMs and are they safe to use as dietary supplements? Retrieved November 12, 2015, from http://hprc-online.org/dietary-supplements/opss/operation-supplement-safety-OPSS/opss-frequently-asked-questions-faqs-1/what-are-sarms-and-are-they-safe-to-use-as-dietary-supplements

[6] U.S. Food and Drug Administration, Department of Health and Human Services. Biogenix USA, LLC warning letter, December 11, 2014. Retrieved November 12, 2015, from http://www.fda.gov/ICECI/EnforcementActions/WarningLetters/ucm434928.htm

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