Tag Archive for mk-677

Ibutamoren (MK-677)

Ibutamoren (MK-677)

Ibutamoren (MK-0677) is a  non-peptide growth hormone (GH) secretagogue. MK-0677 triggers GH pulse discharge through the pituitary and hypothalamic receptors mimicking the GH stimulating action of the endogenous hormone ghrelin. It has been widely demonstrated to upsurge the release of, and creates sustained increases in plasma levels of several hormones including growth hormone and IGF-1, but without affecting cortisol levels. It is currently under development as a potential treatment for reduced levels of these hormones, such as in growth hormone deficient children or elderly adults, and human studies have shown it to increase both muscle mass and bone mineral density, making it a promising therapy for the treatment of frailty in the elderly. MK-0677 also alters basal metabolism of body fat and so may have application in the future treatment of obesity.

Gao W, Kearbey JD, Nair VA, Chung K, Parlow AF, Miller DD, Dalton JT. 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 Dec;145(12):5420-8.

Adunsky A, Chandler J, Heyden N, Lutkiewicz J, Scott BB, Berd Y, Liu N, Papanicolaou DA.MK-0677 (ibutamoren mesylate) for the treatment of patients recovering from hip fracture: a multicenter, randomized, placebo-controlled phase IIb study.Arch Gerontol Geriatr. 2011 Sep-Oct;53(2):183-9. Epub 2010 Nov 9.

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.

Sevigny JJ, Ryan JM, van Dyck CH, Peng Y, Lines CR, Nessly ML; MK-677 Protocol 30 Study Group.Growth hormone secretagogue MK-677: no clinical effect on AD progression in a randomized trial.Neurology. 2008 Nov 18;71(21):1702-8.

Bennett KA, Langmead CJ, Wise A, Milligan G.Growth hormone secretagogues and growth hormone releasing peptides act as orthosteric super-agonists but not allosteric regulators for activation of the G protein Galpha(o1) by the Ghrelin receptor.Mol Pharmacol. 2009 Oct;76(4):802-11. Epub 2009 Jul 22.

Synonyms: Ibutamoren, CHEMBL13817, S1151_Selleck, MK-677

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MK-677 Restores Muscles, Fountain of Youth?

MK-677 Restores Muscles, Fountain of Youth?

A daily dose of MK-677 has been found to restore muscle mass in the arms and legs of older adults and improve some of their biochemistry to levels found in healthy young adults, suggesting an anti-frailty drug has been found.

The drug, called MK-677, was evaluated for its safety and effectiveness in a study that showed the drug restored 20 percent of muscle mass loss associated with normal aging. In fact, levels of growth hormone (GH) and of insulin-like growth factor I (IGF- I) in healthy seniors who took the drug increased to the levels found in healthy young adults, said Michael O. Thorner, a professor of internal medicine and neurosurgery at the University of Virginia Health System.

“Our study opens the door to the possibility of developing treatments that avert the frailty of aging,” Thorner said. “The search for anti-frailty medications has become increasingly important because the average American is expected to live into his or her 80s, and most seniors want to stay strong enough to remain independent as they age.”

Funded by the National Institutes of Health, the two-year, double-blind, placebo-controlled study involved 65 men and women ranging in age from 60 to 81. The results are detailed in the Nov. 4, 2008, issue of the journal Annals of Internal Medicine.

The MK-677 drug mimics the action of ghrelin, a peptide that stimulates a growth hormone called secretagogue receptor (GHSR). Drug developers are focusing on GHSR because it plays an important role in the regulation of growth hormone and appetite. They think it may prove to be an excellent treatment target for metabolic disorders such as those related to body weight and body composition.

Drugs found to work in early trials don’t always hold up to further testing, however.

The new research was a “proof-of-concept” study that sets the stage for a larger and longer clinical trial to determine whether MK-677 is effective in people who are frail and to assess its long-term safety.

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