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Selective Androgen Receptor Modulators - Bodybuilding Supplements

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At this time, SARMS are NOT RECOMMENDED for human use. These drugs are still in the research and testing stages of development. In addition, some experimental drugs that are not SARMs are being marketed as or along with SARMs.
The development of Andarine (S-4) was halted because the use of this compound caused serious disturbances in vision

In 2013, the original developer discontinued GW501516 due to the discovery that during animal testing it rapidly caused cancer in multiple organs
Until such issues are resolved, DO NOT USE SARMs.

SARMs Research and Information Articles

  1. Dalton, J; “Discovery of Nonsteroidal Androgens”;  Biochemical and Biophysical Research Communications; Volume 244, Issue 1, 6 March 1998, Pages 1–4; Retrievedf rom http://www.sciencedirect.com/science/article/pii/S0006291X98982092
  2. Chen, Jiyun, Juhyun Kim, and James T. Dalton. “Discovery AND Therapeutic Promise OF Selective Androgen Receptor Modulators.” Molecular interventions 5.3 (2005): 173–188; http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2072877/
  3. Gao, W; Expanding the therapeutic use of androgens via selective androgen receptor modulators (SARMs); Drug Discovery Today; Volume 12, Issues 5–6, March 2007, Pages 241–248; Retrieved from http://www.sciencedirect.com/science/article/pii/S1359644607000359
  4. Cadilla, R; Selective androgen receptor modulators in drug discovery: medicinal chemistry and therapeutic potential.; Curr Top Med Chem. 2006;6(3):245-70; Retrieved from http://www.ncbi.nlm.nih.gov/pubmed/16515480
  5. World Anti-Doping Agency; The 2015 Prohibited List; September 20, 2014; Retrieved from http://www.uefa.org/MultimediaFiles/Download/EuroExperience/uefaorg/Anti-doping/02/14/00/26/2140026_DOWNLOAD.pdf
  6. Hurst, M; Designer drug SRAMS sweeping world sport; The daily Telegraph; February 9, 2012; Retrieved from http://www.dailytelegraph.com.au/sport/designer-drug-srams-sweeping-world-sport/story-fn9dirj0-1226266138458
  7. Singer, E; Next-Generation Sports Doping; MIT Technology Review; October 26, 2007; Retrieved from http://www.technologyreview.com/news/408954/next-generation-sports-doping/
  8. Donzé, F; WADA Executive Committee Approves the 2008 Prohibited List; September 23, 2007; Retrieved from https://www.wada-ama.org/en/media/news/2007-09/wada-executive-committee-approves-the-2008-prohibited-list-0
  9. Carroll, W; “Under the Knife”; Baseball Prospectus; February 5, 2009; Retrieved from http://www.baseballprospectus.com/article.php?articleid=8470
  10. Ligand Pharmaceuticals; Ligand Initiates Clinical Trial with the Selective Androgen Receptor Modulator LGD-4033, a Potential Treatment of Muscle and Bone Disorders; Retrieved from http://investor.ligand.com/press-releases/detail/45/ligand-initiates-clinical-trial-with-the-selective-androgen
  11. Ligand Pharmaceuticals; Ligand Presents New Preclinical Data on its Lead SARM Molecule LGD-4033 at the Gerontological Society of America Annual Meeting; November 20, 2009; Retrieved from http://investor.ligand.com/press-releases/detail/150/ligand-presents-new-preclinical-data-on-its-lead-sarm
  12. Ligand Pharmaceuticals; Ligand Presents First-in-Human Phase I Data on Lead SARM Molecule LGD-4033 at the International Congress of Endocrinology; March 29, 2010; Retrieved from http://investor.ligand.com/press-releases/detail/134/ligand-presents-first-in-human-phase-i-data-on-lead-sarm
  13. Ligand Pharmaceuticals; Ligand Presents Multi-Dose Phase I Data on Lead SARM Molecule LGD-4033 at the Endocrine Society Annual Meeting; June 6, 2011; Retrieved from http://investor.ligand.com/press-releases/detail/166/ligand-presents-multi-dose-phase-i-data-on-lead-sarm
  14. Basaria, S; Safety and Tolerability of LGD-4033, a Novel Non-Steroidal Oral Selective Androgen Receptor Modulator (SARM), in Healthy Men; Endocrine Reviews; Vol. 32 (03_MeetingAbstracts): P3-207; Retrieved from https://www.google.com/url?sa=t&rct=j&q=&esrc=s&source=web&cd=9&cad=rja&uact=8&ved=0CFAQFjAIahUKEwiRxtSxkNHHAhXIGpIKHSUfA-A&url=http%3A%2F%2Fphx.corporate-ir.net%2FExternal.File%3Fitem%3DUGFyZW50SUQ9NDI5Njk5fENoaWxkSUQ9NDQ3MDcyfFR5cGU9MQ%3D%3D%26t%3D1&ei=CyLjVdGUA8i1yASlvoyADg&usg=AFQjCNH8sv_qb1P0WO1-VQTZU9ZLNlDrGQ&sig2=DnF09muc2TglU-_Lj0bqQw (backup abstract at https://archive.is/LAt17#selection-331.1-331.125)
  15. Merck; GTx Presents Phase II Ostarine (MK-2866) Cancer Cachexia Clinical Trial Results at Endocrine Society Annual Meeting: Ostarine Improved Lean Body Mass and Muscle Performance in Patients with Cancer Cachexia; June 11, 2009; Retrieved from http://www.merck.com/licensing/news-and-events/gtx-press-release.html
  16. McLaughlin, K; Johnson & Johnson; Janssen to Showcase Data from Five Compounds Including Daratumumab and IMBRUVICA at the 2015 American Society of Clinical Oncology (ASCO) Annual Meeting; May 13, 2015; Retrieved from http://www.jnj.com/news/all/Janssen-to-Showcase-Data-from-Five-Compounds-Including-Daratumumab-and-IMBRUVICA-at-the-2015-American-Society-of-Clinical-Oncology-ASCO-Annual-Meeting
  17. Narayanan, Ramesh et al. “Selective Androgen Receptor Modulators in Preclinical and Clinical Development: Peer-reviewed SARMs from Johnson & Johnson (J&J) and subsidiaries.” Nuclear Receptor Signaling 6 (2008): e010; 30 Aug. 2015; Retrieved from http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2602589/figure/fig6/
  18. GlaxoSmithKline; “GSK Product Development Pipeline”; March 2015; Retrieved from https://www.gsk.com/media/712057/product-pipeline-2015.pdf
  19. Narayanan, Ramesh et al. “Selective Androgen Receptor Modulators in Preclinical and Clinical Development.” Nuclear Receptor Signaling 6 (2008): e010; http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2602589/
  20. GTx Inc; enobosarm (Ostarine; GTx-024); Retrieved from http://www.gtxinc.com/Pipeline/OstarineMK2866.aspx?Sid=4
  21. He Y, Yin D, Perera M, Kirkovsky L, Stourman N, Li W, Dalton JT, Miller DD. Novel nonsteroidal ligands with high binding affinity and potent functional activity for the androgen receptor; European journal of medicinal chemistry. 2002; 37:619–634; Retrieved from http://www.researchgate.net/profile/Minoli_Perera/publication/11225682_Novel_nonsteroidal_ligands_with_high_binding_affinity_and_potent_functional_activity_for_the_androgen_receptor/links/0046351c49845bf4cc000000.pdf?inViewer=true&disableCoverPage=true&origin=publication_detail
  22. Marhefka, Craig A. et al. “Design, Synthesis, and Biological Characterization of Metabolically Stable Selective Androgen Receptor Modulators.” Journal of medicinal chemistry 47.4 (2004): 993–998; http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2040239/
  23. Dalton, J; US Patent 8853266: “Selective androgen receptor modulators for treating diabetes”; April 13, 2007; https://www.google.com/patents/US8853266
  24. US Food and Drug Administration; “Dietary Supplement Health and Education Act of 1994”; October 25, 1994; Retrieved from http://www.fda.gov/RegulatoryInformation/Legislation/SignificantAmendmentstotheFDCAct/ucm148003.htm
  25. United States Congress; “Anabolic Steroid Control Act of 2004”; October 22, 2004; Retrieved from  http://www.gpo.gov/fdsys/pkg/BILLS-108s2195enr/pdf/BILLS-108s2195enr.pdf
  26. Zambrana, I; Food and Drug Administration; Warning Letter to BioGenix USA, LLC; December 11, 2014; Retrieved from http://www.fda.gov/ICECI/EnforcementActions/WarningLetters/ucm434928.htm
  27. Kloner, R; “Time course of the interaction between tadalafil and nitrates”; Journal of the American College of Cardiology; Volume 42, Issue 10, 19 November 2003, Pages 1855–1860; Retrieved from http://www.sciencedirect.com/science/article/pii/S0735109703012932
  28. Zhi, L; “Selective androgen receptor modulators (SARMs) and uses thereof”; US Patent and Trademark Office; US Patent #8354446; Retrieved from https://www.google.com/patents/US8354446
  29. Bigge, C; “Antidiabetic agents”; US Patent and Trademark Office; US Patent #20030171377; Retrieved from https://www.google.com/patents/US20030171377
  30. Schacht, W; Patent Law and Its Application to the Pharmaceutical Industry: An Examination of the Drug Price Competition and Patent Term Restoration Act of 1984 (“The Hatch-Waxman Act”); Congressional Research Report for Congress; January 10, 2005; Retrieved from http://www.law.umaryland.edu/marshall/crsreports/crsdocuments/rl3075601102005.pdf
  31. Dalton, James T. et al. “The Selective Androgen Receptor Modulator GTx-024 (enobosarm) Improves Lean Body Mass and Physical Function in Healthy Elderly Men and Postmenopausal Women: Results of a Double-Blind, Placebo-Controlled Phase II Trial.” Journal of Cachexia, Sarcopenia and Muscle 2.3 (2011): 153–161; Retrieved from http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3177038/
  32. Narayanan, Ramesh et al. “Selective Androgen Receptor Modulators in Preclinical and Clinical Development.” Nuclear Receptor Signaling 6 (2008); Retrieved from http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2602589/
  33. GTx, Inc; Form 10-Q Quarterly Report for the Quarterly Period Ended June 30, 2014; United States Securities and Exchange Commission; Retrieved from https://www.sec.gov/Archives/edgar/data/1260990/000110465914056983/a14-14015_110q.htm
  34. GTx, Inc; Income Statement; Google Finance; Retrieved from https://www.google.com/finance?q=NASDAQ%3AGTXI&fstype=ii
  35. Geiger, L; “Rat Carcinogenicity with GW501516, a PPAR Delta Agonist”; Society of Toxicology 48th Annual Meeting and ToxExpo; The Toxicologist Supplement to Toxicological Sciences; Oxford University Press; Volume 108, Number 1, March 2009; pp. 189; Retrieved from  https://web.archive.org/web/20150504013406/http://www.toxicology.org/AI/PUB/Tox/2009Tox.pdf
  36. Sahebkar, A; “New peroxisome proliferator-activated receptor agonists: potential treatments for atherogenic dyslipidemia and non-alcoholic fatty liver disease.”; Expert Opin Pharmacother. 2014 Mar;15(4):493-503; Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/24428677
  37. World Anti-Doping Agency; “WADA issues alert on GW501516”; March 21, 2013; Retrieved from https://web.archive.org/web/20130602050612/http://playtrue.wada-ama.org/news/wada-issues-alert-on-gw501516/
  38. New Scientist; Anti-doping Agency Warns Athletes of Black Market Drug; March 26, 2013; Retrieved from https://www.newscientist.com/article/mg21729103-400-anti-doping-agency-warns-athletes-of-black-market-drug/
  39. Rossen, J; “A New Class of Unapproved Supplements Has Mass Appeal”; Maxim Magazine; April 14, 2015; Retrieved from http://www.maxim.com/maxim-man/fitness/article/new-class-unapproved-supplements-has-mass-appeal


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