Selective Androgenic Receptor Modulators
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
- ↑ Thevis, M. and Schänzer, W., 2018. Detection of SARMs in doping control analysis. Molecular and Cellular Endocrinology, 464, pp.34-45.
- ↑ 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.
- ↑ Hackney, A., 2018. Doping, performance-enhancing drugs, and hormones in sport. Waltham, Massachusetts: Elsevier.
- ↑ 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.
- ↑ 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.
- ↑ 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>
- ↑ 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
- ↑ 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
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Last edited:
4 July 2022 19:52:17
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