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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)

General

  • 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

Pharmacology

  • 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


References


  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