Chemistry:Ibutamoren

From HandWiki

Ibutamoren (INN; developmental code 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,[1][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.[1]

Effect on sleep architecture

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

Growth hormone deficiency

In a study of children with growth hormone deficiency, ibutamoren performed better than other growth hormone secretagogues at improving growth hormone levels.[16] An ongoing study compares ibutamoren directly to injectable hGH in terms of height velocity in this population.[17] Topline data from Phase 2 OraGrowtH210 and OraGrowtH212 Trials of LUM-201 in PGHD met all primary and secondary endpoints.

Non-research use

Since ibutamoren is still an Investigational New Drug, it has not yet been approved to be marketed for consumption by humans in the United States.[1] However, it has been used experimentally by some in the bodybuilding community. The use of ibutamoren is banned in most sports.[18]

See also

  • List of growth hormone secretagogues
  • Ghrelin

References

  1. ↑ 1.0 1.1 1.2 1.3 "Ibutamoren - Lumos Pharma/Merck". https://adisinsight.springer.com/drugs/800007434. 
  2. ↑ "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. doi:10.1073/pnas.92.15.7001. PMID 7624358. Bibcode: 1995PNAS...92.7001P. 
  3. ↑ "Identification of a new G-protein-linked receptor for growth hormone secretagogues". Molecular Endocrinology 10 (1): 57–61. January 1996. doi:10.1210/mend.10.1.8838145. PMID 8838145. 
  4. ↑ "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. doi:10.1210/jcem.86.4.7402. PMID 11297611. 
  5. ↑ "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. doi:10.1124/mol.108.049189. PMID 18923064. 
  6. ↑ "Effects of an oral ghrelin mimetic on body composition and clinical outcomes in healthy older adults: a randomized trial". Annals of Internal Medicine 149 (9): 601–611. November 2008. doi:10.7326/0003-4819-149-9-200811040-00003. PMID 18981485. 
  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. doi:10.1210/jcem.81.12.8954023. PMID 8954023. 
  8. ↑ "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. doi:10.1210/jcem.81.12.8954023. PMID 8954023. 
  9. ↑ "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. PMID 9238854. 
  10. ↑ "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. doi:10.1210/jcem.82.10.4297. PMID 9329386. 
  11. ↑ "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. doi:10.1359/jbmr.1999.14.7.1182. PMID 10404019. 
  12. ↑ "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. doi:10.1210/jcem.86.3.7294. PMID 11238495. 
  13. ↑ "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. doi:10.1196/annals.1404.023. PMID 18056963. Bibcode: 2007NYASA1119..147S. 
  14. ↑ "An Anti-frailty Pill For Seniors? New Drug Increases Muscle Mass In Arms And Legs Of Older Adults.". 5 November 2008. https://www.sciencedaily.com/releases/2008/11/081104132902.htm. 
  15. ↑ 15.0 15.1 "Prolonged oral treatment with MK-677, a novel growth hormone secretagogue, improves sleep quality in man" (in english). Neuroendocrinology 66 (4): 278–286. October 1997. doi:10.1159/000127249. PMID 9349662. 
  16. ↑ "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. doi:10.1159/000524244. PMID 35354138. 
  17. ↑ "Phase 2 Study of LUM-201 in Children With Growth Hormone Deficiency (OraGrowtH210 Trial) - Full Text View" (in en). https://classic.clinicaltrials.gov/ct2/show/NCT04614337. 
  18. ↑ "Ibutamoren (MK 677) not OK - Don't be fooled by marketing!" (in en-AU). 23 May 2022. https://www.sportintegrity.gov.au/news/integrity-blog/2022-05/ibutamoren-mk-677-not-ok-dont-be-fooled-marketing. 



Retrieved from "https://handwiki.org/wiki/index.php?title=Chemistry:Ibutamoren&oldid=4175697"