Definition: "An ergogenic aid is any substance or phenomenon that enhances performance "
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30.01.2018 |
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GSK2881078 - SARM star rising
SARMs are the successors of the good, old anabolic steroids. A number of these, such as RAD140 and LGD4033, have already become established in pharmacological bodybuilding. GlaxoSmithKline (GSK) researchers are researching another SARM, about which they release remarkably little. But what we have learned about GSK2881078 so far suggests that this could be a more-than-average effective muscle builder.
We'll say it right away
The only thing we could find about the anabolic effect of GSK2881078 is this sentence, hidden in a publication published in 2017 in the British Journal of Clinical Pharmacology:
"GSK2881078 at 0.3 mg/kg/d dosed orally once daily for 28 days restored the weight of the levator ani muscle in orchiectomized rats to that of sham-operated rats but produced only a minor increase in prostate weight compared with vehicle-treated orchiectomized rats (unpublished data on file, GlaxoSmithKline, 709 Swedeland Road, King of Prussia, PA, USA 19406)."
Study
The researchers gave GSK2881078 in doses of 0.05, 0.08, 0.24, 0.48 and 0.75 milligrams per day to adult men, and in doses of 0.24 and 0.35 milligrams to postmenopausal women for up to 14 days. The mode of administration was, as in the animal study we mentioned above, oral.
Results
The doses tested reduced total testosterone levels, but this decrease was mainly due to SHBG-bound - and inactive - testosterone. (GSK2881078 lowered the SHBG level.) In men, the concentration of free testosterone did not decrease.
Click on the figure below for a larger version.
Conclusion
"Negro-Vilar [J Clin Endocrinol Metab. 1999 Oct;84(10):3459-62.] defined an ideal SARM for the treatment of male hypogonadism as one that is orally active, suitable for once daily administration, and capable of enhancing fat-free mass, muscle mass and strength, bone growth and libido, with lesser but stimulatory effects on the prostate, seminal vesicles and other sex accessory tissues", Dalton wrote.
"Like other SARMs ahead of it in development, GSK2881078 appears to meet most of these criteria."
"Although it has been 2 decades since the initial discovery of a SARM, much work remains to be done before they can be used for muscle wasting or another condition. GSK2881078 has taken the earliest steps down this winding road."
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