Chemistry:Sermorelin
Sermorelin acetate (INN; brand names Geref, Gerel), also known as GHRH (1-29), is a peptide analogue of growth hormone-releasing hormone (GHRH) which is used as a diagnostic agent to assess growth hormone (GH) secretion for the purpose of diagnosing growth hormone deficiency.[1][2][3] It is a 29-amino acid polypeptide representing the 1–29 fragment from endogenous human GHRH, thought to be the shortest fully functional fragment of GHRH.[1]
Sermorelin was approved by the US Food and Drug Administration (FDA) in 1997 for use as a treatment for children with growth hormone deficiency or growth failure.[4] However, as of 2008, the manufacturer discontinued the production of Sermorelin for commercial reasons, and it is no longer available as an FDA-approved drug.[5][6] Despite this, it may still be used in some off-label contexts or obtained through compounding pharmacies.[7]
Medical usage
Sermorelin was used to treat children with growth hormone deficiency or growth failure by stimulating the pituitary gland to release growth hormone (GH), thereby increasing plasma GH levels.[1]
Mechanism of action
Sermorelin binds to the growth hormone-releasing hormone receptor (GHRHR), mimicking the effects of the full-length GHRH in promoting growth hormone secretion.[8]
Sermorelin's effects are regulated by negative feedback through the inhibitory hormone somatostatin, making it difficult to overdose, unlike exogenous rhGH (a synthetic version of human GH). This interaction with somatostatin prompts the pituitary to release hGH in bursts, which mirrors natural hormone rhythms rather than the constant levels produced by rhGH injections. As a result, sermorelin avoids tachyphylaxis by promoting a more physiological pattern of hGH release. Additionally, sermorelin stimulates the pituitary to enhance hGH gene transcription, thereby maintaining the growth hormone neuroendocrine system axis, which is the first to deteriorate with age. By supporting pituitary function, sermorelin helps slow the decline of pituitary hormones during aging, thereby preserving both youthful anatomy and physiology.[2]
Research potential
GHRH naturally declines with age. No conclusive results are known whether sermorelin could yield potential benefits for adults, such as to enhance pituitary function or mimic growth hormone secretion patterns. Oral active growth hormone-releasing peptides may be under development. Sermorelin may be an alternative to rhGH for growth hormone replacement therapy (GHRT) in aging adults.
Sermorelin can be prescribed for off-label use without the legal restrictions that apply to rhGH. To support evidence-based GHRT in clinical age management, the Society for Applied Research in Aging is offering sermorelin free of charge to practitioners willing to study its effects under protocol conditions and publish their findings in peer-reviewed journals.[2]
See also
- List of growth hormone secretagogues
References
- ↑ 1.0 1.1 1.2 "Sermorelin: a review of its use in the diagnosis and treatment of children with idiopathic growth hormone deficiency". BioDrugs 12 (2): 139–157. August 1999. doi:10.2165/00063030-199912020-00007. PMID 18031173.
- ↑ 2.0 2.1 2.2 "Sermorelin: a better approach to management of adult-onset growth hormone insufficiency?". Clinical Interventions in Aging 1 (4): 307–308. 2006. doi:10.2147/ciia.2006.1.4.307. PMID 18046908.
- ↑ Pharmacology (5th ed.). Edinburgh: Churchill Livingstone. 2003. ISBN 0-443-07145-4.
- ↑ "Growth hormone-releasing hormone.". Handbook of Hormones. Academic Press. January 2016. pp. 144-145, e18B-2-e18B-4. doi:10.1016/B978-0-12-801028-0.00143-4. ISBN 978-0-12-801028-0.
- ↑ "Geref (Sermorelin acetate)". fda.gov. US Food and Drug Administration. https://www.accessdata.fda.gov/scripts/cder/daf/index.cfm?event=overview.process&ApplNo=020443.
- ↑ "Determination That GEREF (Sermorelin Acetate) Injection, 0.5 Milligrams Base/Vial and 1.0 Milligrams Base/Vial, and GEREF (Sermorelin Acetate) Injection, 0.05 Milligrams Base/Amp, Were Not Withdrawn From Sale for Reasons of Safety or Effectiveness". Federal Register. US Food and Drug Administration. 4 March 2013. https://www.federalregister.gov/documents/2013/03/04/2013-04827/determination-that-geref-sermorelin-acetate-injection-05-milligrams-basevial-and-10-milligrams.
- ↑ "Assessing safety and efficacy of growth hormone replacement in aging by community physicians.". Journal of Anti-Aging Medicine 5 (1): 41–55. March 2002. doi:10.1089/10945450231762928. https://www.liebertpub.com/doi/abs/10.1089/109454502317629282?journalCode=rej.1.
- ↑ "Growth hormone secretagogues: history, mechanism of action, and clinical development". JCSM Rapid Communications 3 (1): 25–37. January 2020. doi:10.1002/rco2.9.
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