Ostarine (MK-2866)
Ostarine pills:
In 2005, James T. Dalton, Duane D. Miller and Karen A. Veverka patented the Enobosarm (Ostarine, MK-2866) and since then it has been under development to treat patients with muscle wasting. There are more than 25 studies with Enobosarm that involved over 1700 subjects. In 2007, GTx and Merck announced a three years research and development of Ostarine [1]. The dosage of Ostarine ranged from 1-18 mg in different clinical trials.
Scientific Benefits of Ostarine:
The MK-2866 promotes similar anabolic response compared with Dihydrotestosterone (DHT) through muscle AR activation and its effect may be also intermediated by non-muscle cell pathways that con- tribute to the anabolic response [2]. In a recent with ovariectomized mice, the weight of the musculus gastrocnemius has been shown to be higher in all groups treated with Ostarine as well as bone mineral density and bone biomechanical properties [3]. In [4], the authors showed that Enobosarm (GTx-024, MK-2866) significantly increases the total lean body mass and improvements in physical function. The authors introduce evidences that MK-2866 or GTx-024 provides beneficial anabolic effects on lean body mass and physical function without the adverse consequence that usually seen with testosterone and other steroids. There are several studies to support the same fact that MK-2866 increase the lean body mass [5] [6].
Using Ostarine does not affect other medication as stated in different studies that the results show little risk of interacting with other drugs [7].
Not FDA approved:
Although Ostarine shows a very promising results in different experiments, the mk-2866 is not approved for human use in any country. Since 2008, Ostarine is classified in the prohibited list for competition purpose by the world Anti-Doping Agency [8]. It is available online in the black market [9].
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References:
[1] Ebner N, von Haehling S. Silver linings on the horizon: highlights from the 10th Cachexia Conference.
[2] Dubois V, Simitsidellis I, Laurent MR, Jardi F, Saunders PT, Vanderschueren D, Claessens F. Enobosarm (GTx-024) modulates adult skeletal muscle mass independently of the androgen receptor in the satellite cell lineage. Endocrinology. 2015 Dec 1;156(12):4522-33.
[3] Komrakova M, Furtwängler J, Hoffmann DB, Lehmann W, Schilling AF, Sehmisch S. The selective androgen receptor modulator ostarine improves bone healing in ovariectomized rats. Calcified Tissue International. 2020 Feb;106(2):147-57.
[4] Dalton JT, Barnette KG, Bohl CE, Hancock ML, Rodriguez D, Dodson ST, Morton RA, Steiner MS. 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. 2011 Sep;2(3):153-61.
[5] Dobs AS, Boccia RV, Croot CC, Gabrail NY, Dalton JT, Hancock ML, Johnston MA, Steiner MS. Effects of enobosarm on muscle wasting and physical function in patients with cancer: a double-blind, randomised controlled phase 2 trial. The lancet oncology. 2013 Apr 1;14(4):335-45.
[6] Papanicolaou DA, Ather SN, Zhu H, Zhou Y, Lutkiewicz J, Scott BB, Chandler J. A phase IIA randomized, placebo-controlled clinical trial to study the efficacy and safety of the selective androgen receptor modulator (SARM), MK-0773 in female participants with sarcopenia. The journal of nutrition, health and aging. 2013 Jun;17(6):533-43.
[7] Coss CC, Jones A, Dalton JT. Pharmacokinetic drug interactions of the selective androgen receptor modulator GTx-024 (Enobosarm) with itraconazole, rifampin, probenecid, celecoxib and rosuvastatin. Investigational new drugs. 2016 Aug;34(4):458-67.
[8] Thevis M, Schänzer W. Detection of SARMs in doping control analysis. Molecular and Cellular Endocrinology. 2018 Mar 15;464:34-45.
[9] Thevis M, Geyer H, Thomas A, Schänzer W. Trafficking of drug candidates relevant for sports drug testing: Detection of non‐approved therapeutics categorized as anabolic and gene doping agents in products distributed via the Internet. Drug Testing and Analysis. 2011 May;3(5):331-6.