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Selective Androgenic Receptor Modulators

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Other Names

  • Selective Androgenic Receptor Modulators (SARMs)

Compound Names

  • Ostarine
  • Andarine
  • LGD-4033 (Ligandrol)
  • LGD-3033
  • RAD140 (Testolone)
  • S23
  • S4 (Andarine)


  • Discovered in the late 90s
  • Chemically engineered molecule drugs that can selectively activate androgen receptors in muscles and bones
  • Anabolic properties similar to steroids but with reduced androgenic properties
  • Not FDA approved for any medical use in humans
  • Lack estrogenic activity
  • Potential therapeutic applications include treatment of muscle loss seen in sarcopenia, cancer-associated cachexia, and muscular dystrophy [1]
  • Can only be administered orally
  • Ostarine, Ligandrol, and andarine are the most abused SARMs [2]

Performance Enhancing Effects

  • Animal data support the consumption of physiologic and performance enhancement by SARMs [3]
    • Human data less conclusive
    • Enhancing effects include increased muscle mass, strength, and recovery from exercise training

Medical Indications

  • There are no FDA-cleared medical indications for the use of SARMs
  • SARMs have been investigated in triple-negative breast cancer and have been shown to reduce tumor growth and tumor weight by greater than 90% [4]
  • They also have shown promise in the treatment of cachexia, BPH, hypogonadism, and prostate cancer [5]

Adverse Effects

  • Liver toxicity [6]
  • Increase risk for MI and stroke 2
  • Case report of acute myocarditis in 32 year old male [7]
  • Mood swings
  • decreased testicular size
  • Acne


  • SARMs bind to androgen receptors > complex translocates to nucleus > recruits cofactors and regulates gene transcription involved in muscle building
  • They are receptor ligands and act as full agonists in anabolic organs (muscle and bone) [8]
    • Similar AR binding affinity to testosterone
    • Mechanism of tissue selectivity (bones and muscles) remains unclear
    • Results in less androgenic properties when compared to testosterone/anabolic steroids
  • Partial agonists in androgenic tissues (prostate and seminal vesicles)
  • Most SARMs have a half-life of 24 hours

WADA Considerations

  • Banned by WADA and commonly contain other banned substances not on the label
  • Added to the WADA's prohibited list in 2008

See Also


  1. Thevis, M. and Schänzer, W., 2018. Detection of SARMs in doping control analysis. Molecular and Cellular Endocrinology, 464, pp.34-45.
  2. Kintz, P., Ameline, A., Gheddar, L. and Raul, J., 2019. LGD-4033, S-4 and MK-2866 – Testing for SARMs in hair: About 2 doping cases. Toxicologie Analytique et Clinique, 31(1), pp.56-63.
  3. Hackney, A., 2018. Doping, performance-enhancing drugs, and hormones in sport. Waltham, Massachusetts: Elsevier.
  4. Narayanan R, Ahn S, Cheney MD, Yepuru M, Miller DD, Steiner MS, Dalton JT. Selective androgen receptor modulators (SARMs) negatively regulate triple-negative breast cancer growth and epithelial:mesenchymal stem cell signaling. PLoS One. 2014 Jul 29;9(7):e103202. doi: 10.1371/journal.pone.0103202. PMID: 25072326; PMCID: PMC4114483.
  5. Solomon ZJ, Mirabal JR, Mazur DJ, Kohn TP, Lipshultz LI, Pastuszak AW. Selective Androgen Receptor Modulators: Current Knowledge and Clinical Applications. Sex Med Rev. 2019 Jan;7(1):84-94. doi: 10.1016/j.sxmr.2018.09.006. Epub 2018 Nov 30. PMID: 30503797; PMCID: PMC6326857.
  6. U.S. Food and Drug Administration. 2022. FDA In Brief: FDA warns against using SARMs in body-building products. [online] Available at: <https://www.fda.gov/news-events/fda-brief/fda-brief-fda-warns-against-using-sarms-body-building-products>
  7. Padappayil R, Chandini Arjun A, Vivar Acosta J, et al. (January 27, 2022) Acute Myocarditis From the Use of Selective Androgen Receptor Modulator (SARM) RAD-140 (Testolone). Cureus 14(1): e21663. doi:10.7759/cureus.21663
  8. Chen J, Kim J, Dalton JT. Discovery and therapeutic promise of selective androgen receptor modulators. Mol Interv. 2005;5(3):173-188. doi:10.1124/mi.5.3.7
Created by:
Khashayar ( Khash ) Farzam on 12 July 2019 02:54:19
Last edited:
4 July 2022 19:52:17