Selective Androgen Receptor Modulators (SARMs)
Selective androgen receptor modulators (SARMs) are synthetic, nonsteroidal small molecules that act as agonists and antagonists at the androgen receptor with reported tissue-selective activity. [1] SARMs are often marketed for “research” or as dietary supplements despite regulatory status as unapproved drugs. [2]
Pharmacologic Properties
SARMs are designed to produce anabolic effects through androgen receptor signaling while minimizing “classic” anabolic-steroid effects in off-target tissues. [1]
Key observed pharmacodynamic effects in human reports and clinical/experimental work include:
- Increased lean body mass in preclinical and clinical studies. [1]
- Suppression of endogenous testosterone reported across SARMs described in preclinical and clinical studies. [1]
- Androgenic downstream effects reported beyond muscle, including prostate enlargement and bone remodeling. [1]
Approved Medical Indications
No SARM has an FDA-approved indication for use in humans. [2] Systematic review evidence likewise reports that SARMs have no FDA-approved use. [1]
Use for Performance Enhancement or Doping
SARMs are prohibited substances in sport and are included under the WADA Prohibited List category of anabolic agents. WADA Prohibited List (entry includes SARMs) USADA educational materials state SARMs are prohibited at all times. USADA prohibited-class page
Documented reasons doping-related use is unsafe include:
- Product mislabeling and contamination risk with other substances in gray-market SARMs. [1]
- Typical athlete dosing patterns that exceed clinically studied exposures in reviewed reports, increasing risk of adverse events. [1]
Potential Health Risks (Recreational/Doping Use)
SARMs have been associated with multi-organ toxicity in reported cases and synthesized literature. [1]
Health risks reported in the literature include:
- Hepatotoxicity, including drug-induced liver injury cases described in the sports medicine literature review. [1]
- Cardiovascular toxicity signals, including reported myocarditis in case reports summarized in the systematic review. [1]
- Tendon injury, including tendon rupture described in case reports summarized in the systematic review. [1]
- Endocrine and androgenic effects, including testosterone suppression and prostate enlargement. [1]
- Metabolic risk signals such as impaired insulin sensitivity reported in athlete-use literature. [1]
In a 2025 systematic review of athlete SARM abuse, contamination was emphasized as a contributing factor to adverse outcomes. [1]
Evidence of Athlete-Use Prevalence and Clinical Case Burden
Prevalence estimates synthesized in a 2025 systematic review suggested SARM use among athletes at approximately 1% to 3%. [1] The review identified 13 case reports describing 15 abuse cases, with reported mean course length around 8 weeks in those cases. [1]