umbrellalabs MK-2866 OSTARINE 25MG 1OZ 30ML

Ostarine is an orally-available, non-steroidal SARM that has demonstrated fascinating results in animal, lab studies and trials, and it is currently being explored for a number of different indications. It is being researched for a variety of benefits: increased lean body mass and muscle strength; prevention of muscle loss; prevention of osteoporosis; urinary incontinence due to stress; and treatment of prostate cancer.

CAS: 841205-47-8

 
Clinical Data

Ostarine has been the subject of two different Phase 2 clinical trials each of which produced positive data regarding its ability to increase strength.
Study 1

The first was a study of cachexia—also known as muscle wasting—which is a complex musculoskeletal condition characterized by loss of appendicular skeletal muscle and a complementary decline in physical function with respect to strength. In this study, which was a 12‐week randomized, double‐blind, placebo‐controlled trial, Ostarine was evaluated in 120 healthy men (60 years of age) and postmenopausal women, all healthy volunteers without evidence of disease recruited from the general population around the phase I study units in in the UK, Northern Ireland, and Germany 1.  The primary goal of the study was to assess changes in total lean body mass (as assessed by dual energy X‐ray absorptiometry) while the secondary goal was to assess broad physical function, body weight, insulin resistance, and pharmacological safety and tolerability. The volunteers were not allowed to initiate dietary modification or initiate or discontinue any exercise program during the study. No additional dietary supplementation was provided.

Volunteers were randomly assigned to one of five different dose groups (doses of 0.1, 0.3, 1.0 and 3.0 mg of Ostarine or placebo) and were instructed to consume the medication every day for 80-90 days at approximately the same time each day, which included a period of approximately 70 days on an outpatient basis. These doses were chosen from the pharmacokinetic, safety and tolerability data from the previous trials with Ostarine, and the clinical trial material was provided by the manufacturer, GTx, Inc. Each dose group contained 24 volunteers and was randomized in equal fashion. Randomization was done in such a way that each dose group contained equivalent numbers of both gender.

A baseline pre‐study assessment of the volunteers was completed within 3 days of the first administered dose, and the final assessments were conducted at day 86. Body composition, including bone mineral density, was assessed at baseline, day 30, and day 86 by Xray. Physical function was evaluated using the Stair Climb Test at baseline, day 30, and day 86. Volunteers were asked to climb the stairs, one step at a time as quickly as possible without assistance, and were asked to only use the handrail if they felt like they were losing their balance.

Figure 1. Ostarine increases lean body mass in a dose-dependent fashion.

Percentage change from baseline end of study in total lean body mass: entire study population, *P  0.001 3 mg vs. placebo (T test).

Adapted from J. T. Dalton et al., The selective androgen receptor modulator 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., J. Cachexia. Sarcopenia Muscle, vol. 2, no. 3, pp. 153–161, Sep. 2011.

Figure 2. Ostarine increases lean body mass, decreases fat mass, and increases power as measured in stair climb challenge.

A statistically significant decrease in total fat mass was also observed at the 3‐mg dose, with the 1‐mg dose approaching statistical significance (P = 0.085). The differences in changes in fat mass from baseline were similar in males and females with a loss of 0.6 kg relative to placebo. No differences in total body weight were observed.

 

Adapted from: Adapted from J. T. Dalton et al., The selective androgen receptor modulator 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.,” J. Cachexia. Sarcopenia Muscle, vol. 2, no. 3, pp. 153–161, Sep. 2011.

 
Discussion

The risk profile of TRT (testosteronee replacement therapy) and anabolic steroid use limits their clinical utility for a variety of health conditions that would otherwise benefit from increasing lean mass, improving physical function, and improving insulin resistance. Ostarine is the first SARM to reach advanced clinical trials and demonstrate excellent efficacy and safety [2]. In this randomized, double‐blind, placebo‐controlled study, Ostarine increased total lean body mass and improved physical function with no evidence of androgenic side effects in healthy men and postmenopausal women. The increase in total lean body mass with Ostarine was accompanied by a vast improvement in physical function as evidenced by a clinically-meaningful improved score in the Stair Climb Test.

Ostarine at 3.0 mg also significantly reduced fasting glucose levels, and a trend toward reduction in blood insulin was observed. These effects resulted in a decrease in insulin resistance from baseline in the 1.0 mg and 3.0 mg treatment groups. Of note, such decrease in insulin resistance was similar to that observed with metformi and glipizidee, which are drugs used in the treatment of diabetes [3], [4]. Low levels of testosteronee in men are associated with insulin resistance and type II diabetes, while testosteronee therapy is known to improve metabolic parameters 5–7. This observation may have potential implications for the use of SARMs in pre-diabetic or diabetic individuals, as commonly seen in patients with chronic kidney disease, chronic obstructive pulmonary disease, or metabolic syndrome 8–10.

Ostarine was well tolerated with similar adverse events compared to placebo during the 3 months of daily treatment. Compared to placebo, Ostarine decreased total cholesterol, HDL, and triglycerides. These findings are consistent with previous reports that oral anabolic therapy influences serum lipid profiles 11, 12. Furthermore, the beneficial effects of Ostarine on insulin sensitivity and triglycerides, combined with the known associations of hypogonadism with metabolic syndrome and cardiovascular risk, as well as the low cardiovascular risk observed in randomized clinical trials of testosteronee supplementation [13], all point to one conclusion: the overall cardiovascular risk/benefit ratio for Ostarine is very favorable.