Ostarine (MK-2866) Catalog Description 25mg/ml, 60ml
Enobosarm (also called ostarine, MK-2866, and GTx-024) is a selective androgen receptor modulator (SARM) developed by Merck and later acquired by GTx Inc. The principal characteristic of a SARM is to “elicit muscle-anabolic effects while only sparingly affecting reproductive tissues”. Enobosarm (ostarine) is under clinical investigation for sarcopenia (age-related muscle-wasting), cancer cachexia (cancer-related muscle-wasting), and other muscle wasting diseases
Enobosarm (ostarine) has the same efficacy for increasing skeletal muscle mass as the androgen dihydrotestosterone (DHT), and also causes expression of many of the same “muscle-specific and androgen-sensitive genes”. Unlike DHT enobosarm elicits only muscle-specific effects or affects other tissues sparingly. And unlike related testosterone, because enobosarm is not a hormone it does not convert (through aromatization or 5-AR activity) to other bioactive compounds through enzymatic pathways.
According to Furuya (2010), SARMs possess “significant potential” to stimulate bone formation, justifying various studies going on worldwide into SARM efficacy for building bone density as well as muscle mass. This makes SARMs such as ostarine candidates for two conditions associated with the elderly, bone wasting and sarcopenia (age-related muscle-wasting).
The availability of approved drugs for cancer cachexia is very slim, meaning that if enobosarm or other SARMs are approved, they will be a first-in-class; Madeddu and Montovani have suggested that for patients outside of clinical trials, a multi-prong approach incorporating more than one therapy, even more than one cutting-edge therapy, would be appropriate .
In 2015 enobosarm was entered into phase 2 proof-of-concept trials as a therapy for stress urinary incontinence in post-menopausal women under the rationale that “the androgen receptor rich environment of the pelvic floor muscles...are potentially sensitive to relatively low doses of enobosarm”; the trials will gather data from over 1500 women.
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;156(12):4522-33. doi: 10.1210/en.2015-1479.
 “GTx Presents Phase II Ostarine (MK-2866) Cancer Cachexia Clinical Trial Results At Endocrine Society Annual Meeting.” Medical News TODAY. 6/14/2009. http://www.medicalnewstoday.com/articles/153779.php; Accessed 2/15/2016.
 Furuya K. [Translated title from Japanese: Bone and Men's Health. Bone selective androgen receptor modulators]. Clin Calcium. 2010 Feb;20(2):225-33.
 Madeddu C, Mantovani G. An update on promising agents for the treatment of cancer cachexia. Curr Opin Support Palliat Care. 2009 Dec;3(4):258-62.
”GTx Receives FDA Clearance to Initiate Clinical Trial in Stress Urinary Incontinence”. Business Wire. 10-13-2015 http://www.businesswire.com/news/home/20151013005315/en/#.VhzuYflVhBc Accessed 2/15/2016.