Ibutamoren Explained

Ibutamoren (developmental code names MK-677, MK-0677, LUM-201, L-163,191; former tentative brand name Oratrope) is a potent, long-acting, orally-active, selective, and non-peptide agonist of the ghrelin receptor and a growth hormone secretagogue, mimicking the growth hormone (GH)-stimulating action of the endogenous hormone ghrelin.[1] [2] [3] [4] [5] It has been shown to increase the secretion of several hormones including GH and insulin-like growth factor 1 (IGF-1) and produces sustained increases in the plasma levels of these hormones while also raising cortisol levels.[6]

Effect on lean mass

Ibutamoren has been shown to sustain activation of the GH–IGF-1 axis, increasing growth hormone secretion by up to 97%,[7] and to increase lean body mass with no change in total fat mass or visceral fat. It is under investigation as a potential treatment for reduced levels of these hormones, such as in children or elderly adults with growth hormone deficiency,[8] [9] [10] and human studies have shown it to increase both muscle mass and bone mineral density,[11] [12] making it a promising potential therapy for the treatment of frailty in the elderly.[13] [14] As of June 2017, ibutamoren is in the preclinical stage of development for growth hormone deficiency.

Effect on sleep architecture

In a small study of 14 subjects, MK-677 dosed at 25mg/day at bedtime was shown to increase REM sleep by 20% and 50% in young and older subjects respectively.[15] Treatment with MK-677 also resulted in an approximate 50% increase in deep sleep in young subjects.

Growth hormone deficiency

In a study of children with growth hormone deficiency, MK-677 performed better than other growth hormone secretagogues at improving growth hormone levels.[16] An ongoing study compares MK-677 directly to injectable hGH in terms of height velocity in this population.[17]

Non-research use

Since MK-677 is still an Investigational New Drug, it has not yet been approved to be marketed for consumption by humans in the United States. However, it has been used experimentally by some in the bodybuilding community. The use of MK-677 is banned in most sports [18]

See also

External links

Notes and References

  1. Web site: Ibutamoren - Lumos Pharma/Merck . AdisInsight.
  2. Patchett AA, Nargund RP, Tata JR, Chen MH, Barakat KJ, Johnston DB, Cheng K, Chan WW, Butler B, Hickey G . 6 . Design and biological activities of L-163,191 (MK-0677): a potent, orally active growth hormone secretagogue . Proceedings of the National Academy of Sciences of the United States of America . 92 . 15 . 7001–7005 . July 1995 . 7624358 . 41459 . 10.1073/pnas.92.15.7001 . free . 1995PNAS...92.7001P .
  3. Pong SS, Chaung LY, Dean DC, Nargund RP, Patchett AA, Smith RG . Identification of a new G-protein-linked receptor for growth hormone secretagogues . Molecular Endocrinology . 10 . 1 . 57–61 . January 1996 . 8838145 . 10.1210/mend.10.1.8838145 . free .
  4. Cassoni P, Papotti M, Ghè C, Catapano F, Sapino A, Graziani A, Deghenghi R, Reissmann T, Ghigo E, Muccioli G . 6 . Identification, characterization, and biological activity of specific receptors for natural (ghrelin) and synthetic growth hormone secretagogues and analogs in human breast carcinomas and cell lines . The Journal of Clinical Endocrinology and Metabolism . 86 . 4 . 1738–1745 . April 2001 . 11297611 . 10.1210/jcem.86.4.7402 . free .
  5. Holst B, Frimurer TM, Mokrosinski J, Halkjaer T, Cullberg KB, Underwood CR, Schwartz TW . Overlapping binding site for the endogenous agonist, small-molecule agonists, and ago-allosteric modulators on the ghrelin receptor . Molecular Pharmacology . 75 . 1 . 44–59 . January 2009 . 18923064 . 10.1124/mol.108.049189 . 2218638 .
  6. Nass R, Pezzoli SS, Oliveri MC, Patrie JT, Harrell FE Jr, Clasey JL, Heymsfield SB, Bach MA, Vance ML, Thorner MO . 6 . Effects of an oral ghrelin mimetic on body composition and clinical outcomes in healthy older adults: a randomized trial . 149 . 9 . 601–611 . November 2008 . 18981485 . 10.7326/0003-4819-149-9-200811040-00003 . free .
  7. Chapman, I. M. (1996). Stimulation of the growth hormone (gh)-insulin-like growth factor I axis by Daily Oral Administration of a GH secretogogue (MK-677) in healthy elderly subjects. Journal of Clinical Endocrinology & Metabolism, 81(12), 4249–4257. https://doi.org/10.1210/jc.81.12.4249
  8. Chapman IM, Bach MA, Van Cauter E, Farmer M, Krupa D, Taylor AM, Schilling LM, Cole KY, Skiles EH, Pezzoli SS, Hartman ML, Veldhuis JD, Gormley GJ, Thorner MO . 6 . Stimulation of the growth hormone (GH)-insulin-like growth factor I axis by daily oral administration of a GH secretogogue (MK-677) in healthy elderly subjects . The Journal of Clinical Endocrinology and Metabolism . 81 . 12 . 4249–4257 . December 1996 . 8954023 . 10.1210/jcem.81.12.8954023 . free .
  9. Thorner MO, Chapman IM, Gaylinn BD, Pezzoli SS, Hartman ML . Growth hormone-releasing hormone and growth hormone-releasing peptide as therapeutic agents to enhance growth hormone secretion in disease and aging . Recent Progress in Hormone Research . 52 . 215–44; discussion 244–6 . 1997 . 9238854 .
  10. Chapman IM, Pescovitz OH, Murphy G, Treep T, Cerchio KA, Krupa D, Gertz B, Polvino WJ, Skiles EH, Pezzoli SS, Thorner MO . 6 . Oral administration of growth hormone (GH) releasing peptide-mimetic MK-677 stimulates the GH/insulin-like growth factor-I axis in selected GH-deficient adults . The Journal of Clinical Endocrinology and Metabolism . 82 . 10 . 3455–3463 . October 1997 . 9329386 . 10.1210/jcem.82.10.4297 . free .
  11. Murphy MG, Bach MA, Plotkin D, Bolognese J, Ng J, Krupa D, Cerchio K, Gertz BJ . 6 . Oral administration of the growth hormone secretagogue MK-677 increases markers of bone turnover in healthy and functionally impaired elderly adults. The MK-677 Study Group . Journal of Bone and Mineral Research . 14 . 7 . 1182–1188 . July 1999 . 10404019 . 10.1359/jbmr.1999.14.7.1182 . free .
  12. Murphy MG, Weiss S, McClung M, Schnitzer T, Cerchio K, Connor J, Krupa D, Gertz BJ . 6 . Effect of alendronate and MK-677 (a growth hormone secretagogue), individually and in combination, on markers of bone turnover and bone mineral density in postmenopausal osteoporotic women . The Journal of Clinical Endocrinology and Metabolism . 86 . 3 . 1116–1125 . March 2001 . 11238495 . 10.1210/jcem.86.3.7294 . free .
  13. Smith RG, Sun Y, Jiang H, Albarran-Zeckler R, Timchenko N . Ghrelin receptor (GHS-R1A) agonists show potential as interventive agents during aging . Annals of the New York Academy of Sciences . 1119 . 1 . 147–164 . November 2007 . 18056963 . 10.1196/annals.1404.023 . 3220799 . 2007NYASA1119..147S .
  14. Web site: An Anti-frailty Pill For Seniors? New Drug Increases Muscle Mass In Arms And Legs Of Older Adults. . ScienceDaily . 5 November 2008 .
  15. Copinschi G, Leproult R, Van Onderbergen A, Caufriez A, Cole KY, Schilling LM, Mendel CM, De Lepeleire I, Bolognese JA, Van Cauter E . 6 . Prolonged oral treatment with MK-677, a novel growth hormone secretagogue, improves sleep quality in man . english . Neuroendocrinology . 66 . 4 . 278–286 . October 1997 . 9349662 . 10.1159/000127249 .
  16. Bright GM, Thorner MO . A GH Secretagogue Receptor Agonist (LUM-201) Elicits Greater GH Responses than Standard GH Secretagogues in Subjects of a Pediatric GH Deficiency Trial . Hormone Research in Paediatrics . 95 . 1 . 76–81 . 30 March 2022 . 35354138 . 10.1159/000524244 . 9227666 .
  17. Web site: Phase 2 Study of LUM-201 in Children With Growth Hormone Deficiency (OraGrowtH210 Trial) - Full Text View - ClinicalTrials.gov . clinicaltrials.gov . 4 September 2023 . en.
  18. https://www.sportintegrity.gov.au/news/integrity-blog/2022-05/ibutamoren-mk-677-not-ok-dont-be-fooled-marketing

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