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Ostarine

Ostarine, also known as MK-2866 or enobosarm, belongs to the family of selective androgen receptor modulators (SARMs) and is used to treat conditions like muscle wasting and osteoporosis. It exerts its anabolic effects by targeting only bone and muscle androgen receptors, which prevents adverse side effects anabolic steroids can result in. Ostarine is quite safe and its effects are maintainable after use is discontinued. The benefits of ostarine go beyond improving body composition since it has a positive effect in almost every organ system in the body.

Overall Health Benefits of Ostarine

  • Improves Muscle Mass and Strength [1-11]
  • Improves Exercise Performance [12]
  • Strengthens Bones and Fights Osteoporosis [13-15]
  • Promotes Weight Loss [16-18]
  • Improves Heart Health [19-22]
  • Improves Cholesterol Levels [23]
  • Improves Blood Sugar Levels [24]
  • Treats Benign Prostatic Hyperplasia (BPH) [25-27]
  • Boosts Brain Health [28-29]

Muscle Mass and Strength

Studies show that ostarine is quite effective in increasing lean muscle mass in bodybuilders and athletes, as well as patients with muscle wasting secondary to severe diseases:

  1. In elderly men and women, supplementation with ostarine appears to increase muscle mass and physical function. [1]
  2. In patients with muscle wasting related to cancer, ostarine treatment increases lean body mass as well as muscle mass, and improves measurements of physical function and power. [2-10]
  3. In rats, oral ostarine supplementation treats muscle wasting disorders without any adverse side effects. [11]

Exercise Performance

Ostarine supplementation may help athletes and physically active individuals improve their exercise performance. Apart from helping build muscle mass and enhancing strength, studies show that taking ostarine supplements increases exercise endurance, strength, and recovery. [12]

Bone Health

By acting on bone androgen receptors, ostarine helps maintain bone quality and strength. Numerous studies show that ostarine supplementation can be beneficial in osteoporosis and other bone disorders:

  1. In men with osteoporosis, ostarine supplementation stimulates bone formation and strengthens the bones without any adverse side effects. [13]
  2. In patients with fractures, administration of ostarine promotes healthy muscle tissues and accelerates bone healing. [14]
  3. Just like testosterone replacement therapy, ostarine supplementation also increases bone mineral density in patients with osteoporosis. [15]

Weight Loss

Not only does ostarine improves body composition by increasing muscle mass, but it also reduces fat mass. Studies show that ostarine may help overweight and obese individuals lose weight:

  1. Phase I and II clinical trials have shown that ostarine supplementation increases total lean body mass, enhances functional performance, and decreases total tissue percent fat. [16]
  2. In healthy, elderly men and women, ostarine significantly increases lean body mass and decreases fat mass after only 86 days. [17-18]

Heart Health

Ostarine also has cardioprotective effects. Studies show that ostarine may help maintain heart health and prevent cardiovascular diseases through the following important mechanisms:

  1. Ostarine increases muscle mass, thereby improving heart muscle function. Numerous studies show that low muscle mass is highly associated with increased risk of cardiovascular disease. [19-21]
  2. In patients with muscle wasting, ostarine improves muscle quality, which in turn results in better heart function. [22]

Cholesterol Levels

Supplementing with ostarine may also help improve cholesterol to healthy levels. Studies show that ostarine decreases low density lipoprotein (bad cholesterol). [23] This effect also lowers one’s risk of developing chronic illnesses such as heart disease, diabetes, cancer, and other fatal medical conditions.

Blood Sugar Levels

Ostarine may also be beneficial in improving blood sugar levels, thus, lowering one’s risk of diabetes. Studies show that in healthy elderly men and postmenopausal women, ostarine administration at a dose of 3 mg for 12 weeks lowers blood sugar levels by improving insulin resistance. [24] This mechanism enhances the body’s response to the effects of insulin, a hormone that helps stabilize blood sugar levels.

Benign Prostatic Hyperplasia (BPH)

BPH is characterized by prostate enlargement and leads to unpleasant urinary problems such as frequent urination, difficulty passing urine, weak urine stream, and urinary tract infection. Studies show that SARMs such as ostarine may be beneficial in patients with BPH:

  1. Administration of SARMs at varying doses (5, 10, and 25 mg/kg) decreases prostate weight effectively just like finasteride, a medication used mainly to treat BPH. [25]
  2. Repeated treatment with SARMs produces beneficial results such as decreased prostate weight and improved symptoms. [26]
  3. In rats, administration of SARMs either as a single agent or combination therapy, decreases prostate weight via different mechanisms of action. [27]

Brain Health

There is increasing evidence that SARMs such as ostarine also play a crucial role in maintaining brain health, thus, preventing cognitive deficits and other brain disorders:

  1. In mouse models of Alzheimer’s disease (AD), SARMs improve cognitive deficits and decrease the levels of abnormal sticky plaques in the brain known as amyloid beta. [28]
  2. In patients with cognitive impairment, SARMs is equal in efficacy to testosterone replacement therapy in improving various parameters of cognitive function including memory and thinking skills. [29]

References:

  1. Dalton JT, Barnette KG, Bohl CE. 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; 2(3):153-161. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/22031847.
  2. Dalton JT, Taylor RP, Mohler ML, Steiner MS. Selective androgen receptor modulators for the prevention and treatment of muscle wasting associated with cancer. Current opinion in supportive and palliative care. 2013; 7(4):345-51. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/24189892.
  3. Srinath R, Dobs A. Enobosarm (GTx-024, S-22): a potential treatment for cachexia. Future oncology (London, England). 2014; 10(2):187-94. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/24490605.
  4. Madeddu C, Mantovani G. An update on promising agents for the treatment of cancer cachexia. Current opinion in supportive and palliative care. 2009; 3(4):258-62. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/19667995.
  5. Dalton JT, Barnette KG, Bohl CE, 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. 2011;2(3):153-161. doi:10.1007/s13539-011-0034-6. Retrieved from https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3177038/.
  6. Handlon AL, Schaller LT, Leesnitzer LM, et al. Optimizing Ligand Efficiency of Selective Androgen Receptor Modulators (SARMs). ACS Medicinal Chemistry Letters. 2016;7(1):83-88. doi:10.1021/acsmedchemlett.5b00377. Retrieved from https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4716610/.
  7. Dubois V, Simitsidellis I, Laurent MR. Enobosarm (GTx-024) Modulates Adult Skeletal Muscle Mass Independently of the Androgen Receptor in the Satellite Cell Lineage. Endocrinology. 2015; 156(12):4522-33. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/26393303.
  8. Crawford J, Prado CM, Johnston MA. Study Design and Rationale for the Phase 3 Clinical Development Program of Enobosarm, a Selective Androgen Receptor Modulator, for the Prevention and Treatment of Muscle Wasting in Cancer Patients (POWER Trials). Current oncology reports. 2016; 18(6):37. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/27138015.
  9. Zilbermint MF, Dobs AS. Nonsteroidal selective androgen receptor modulator Ostarine in cancer cachexia. Future oncology (London, England). 2009; 5(8):1211-20. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/19852734.
  10. Dobs AS, Boccia RV, Croot CC. 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; 14(4):335-45. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/23499390.
  11. Kim J, Wang R, Veverka KA, Dalton JT. Absorption, distribution, metabolism and excretion of the novel SARM GTx-024 [(S)-N-(4-cyano-3-(trifluoromethyl)phenyl)-3-(4-cyanophenoxy)-2-hydroxy-2-methylpropanamide] in rats. Xenobiotica; the fate of foreign compounds in biological systems. 2013; 43(11):993-1009. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/24074268.
  12. Thevis M, Thomas A, Möller I, Geyer H, Dalton JT, Schänzer W. Mass spectrometric characterization of urinary metabolites of the selective androgen receptor modulator S-22 to identify potential targets for routine doping controls. Rapid communications in mass spectrometry : RCM. 2011; 25(15):2187-95. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/21710598.
  13. Furuya K. [Bone and Men’s Health. Bone selective androgen receptor modulators]. Clinical calcium. 2010; 20(2):225-33. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/20118515.
  14. Girgis CM, Mokbel N, DiGirolamo DJ. Therapies for Musculoskeletal Disease: Can we Treat Two Birds with One Stone? Current osteoporosis reports. 2014;12(2):142-153. doi:10.1007/s11914-014-0204-5.
  15. Cilotti A, Falchetti A. Male osteoporosis and androgenic therapy: from testosterone to SARMs. Clinical Cases in Mineral and Bone Metabolism. 2009;6(3):229-233. Retrieved from https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2811355/.
  16. Zilbermint MF, Dobs AS. Nonsteroidal selective androgen receptor modulator Ostarine in cancer cachexia. Future oncology (London, England). 2009; 5(8):1211-20. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/19852734.
  17. Dalton J. T. Development and Potential Uses of Selective Androgen Receptor Modulators (SARMs). American Society of Andrology. 2007a. Retrieved from https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2602589/.
  18. Dalton J. T. Therapeutic Promise of Selective Androgen Receptor Modulators (SARMs): Preclinical and Clinical Proof-of-Concept Studies. Annual Meeting of The Endocrine Society. 2007b. pp. Abstract #S41–2. Retrieved from https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2072877/.
  19. University of California, Los Angeles (UCLA), Health Sciences. “Higher muscle mass associated with lower mortality risk in people with heart disease.” ScienceDaily. ScienceDaily, 22 April 2016. Retrieved from https://www.sciencedaily.com/releases/2016/04/160422080059.htm.
  20. Srikanthan P, Horwich TB, Tseng CH. Relation of Muscle Mass and Fat Mass to Cardiovascular Disease Mortality. The American journal of cardiology. 2016; 117(8):1355-60. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/26949037.
  21. Retrieved from http://atvb.ahajournals.org/content/atvbaha/early/2016/03/31/ATVBAHA.116.307156.full.pdf.
  22. Anker MS, von Haehling S, Springer J, Banach M, Anker SD. Highlights of the mechanistic and therapeutic cachexia and sarcopenia research 2010 to 2012 and their relevance for cardiology. International journal of cardiology. 2013; 162(2):73-6. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/23174169.
  23. Narayanan R, Mohler ML, Bohl CE, Miller DD, Dalton JT. Selective androgen receptor modulators in preclinical and clinical development . Nuclear Receptor Signaling. 2008;6:e010. doi:10.1621/nrs.06010. Retrieved from https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2602589/.
  24. Dalton JT, Barnette KG, Bohl CE, 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. 2011;2(3):153-161. doi:10.1007/s13539-011-0034-6. Retrieved from https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3177038/.
  25. Omwancha J, Brown TR. Selective androgen receptor modulators: in pursuit of tissue-selective androgens. Current opinion in investigational drugs (London, England : 2000). 2006; 7(10):873-81. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/17086931.
  26. Nejishima H, Yamamoto N, Suzuki M, Furuya K, Nagata N, Yamada S. Anti-androgenic effects of S-40542, a novel non-steroidal selective androgen receptor modulator (SARM) for the treatment of benign prostatic hyperplasia. The Prostate. 2012; 72(14):1580-7. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/22430536.
  27. Gao W, Kearbey JD, Nair VA. Comparison of the pharmacological effects of a novel selective androgen receptor modulator, the 5alpha-reductase inhibitor finasteride, and the antiandrogen hydroxyflutamide in intact rats: new approach for benign prostate hyperplasia. Endocrinology. 2004; 145(12):5420-8. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/15308613/.
  28. George S, Petit GH, Gouras GK, Brundin P, Olsson R. Nonsteroidal Selective Androgen Receptor Modulators and Selective Estrogen Receptor β Agonists Moderate Cognitive Deficits and Amyloid-β Levels in a Mouse Model of Alzheimer’s Disease. ACS Chemical Neuroscience. 2013;4(12):1537-1548. doi:10.1021/cn400133s. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/15308613/.
  29. Negro-Vilar A. Selective androgen receptor modulators (SARMs): a novel approach to androgen therapy for the new millennium. The Journal of clinical endocrinology and metabolism. 1999; 84(10):3459-62. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/10522980.

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