Archive for January 2016

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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