Sermorelin

Sermorelin
Clinical data
Trade namesGeref, Gerel
Other namesGRF 1–29
AHFS/Drugs.comMicromedex Detailed Consumer Information
Routes of
administration		Injection
ATC code
Legal status
Legal status
  • US: Discontinued[1]
Identifiers
  • L-Tyrosyl-L-alanyl-L-α-aspartyl-L-alanyl-L-isoleucyl-L-phenylalanyl-L-threonyl-L-asparaginyl-L-seryl-L-tyrosyl-L-arginyl-L-lysyl-L-valyl-L-leucylglycyl-L-glutaminyl-L-leucyl-L-seryl-L-alanyl-L-arginyl-L-lysyl-L-leucyl-L-leucyl-L-glutaminyl-L-α-aspartyl-L-isoleucyl-L-methionyl-L-seryl-L-argininamide
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC149H246N44O42S
Molar mass3357.93 g·mol−1
3D model (JSmol)
  • CC[C@H](C)[C@@H](C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC2=CC=C(C=C2)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CC3=CC=C(C=C3)O)N
  • InChI=1S/C149H246N44O42S/c1-20-77(13)116(191-122(211)81(17)168-132(221)104(66-113(204)205)178-121(210)79(15)167-123(212)88(152)62-84-39-43-86(198)44-40-84)145(234)185-102(63-83-32-23-22-24-33-83)138(227)193-118(82(18)197)146(235)186-103(65-111(155)202)137(226)189-108(71-196)142(231)182-101(64-85-41-45-87(199)46-42-85)136(225)175-93(38-31-56-165-149(161)162)126(215)174-91(35-26-28-53-151)131(220)190-115(76(11)12)143(232)184-97(58-72(3)4)124(213)166-68-112(203)170-94(47-49-109(153)200)128(217)180-100(61-75(9)10)135(224)188-106(69-194)140(229)169-80(16)120(209)172-92(37-30-55-164-148(159)160)125(214)173-90(34-25-27-52-150)127(216)179-99(60-74(7)8)134(223)181-98(59-73(5)6)133(222)176-95(48-50-110(154)201)129(218)183-105(67-114(206)207)139(228)192-117(78(14)21-2)144(233)177-96(51-57-236-19)130(219)187-107(70-195)141(230)171-89(119(156)208)36-29-54-163-147(157)158/h22-24,32-33,39-46,72-82,88-108,115-118,194-199H,20-21,25-31,34-38,47-71,150-152H2,1-19H3,(H2,153,200)(H2,154,201)(H2,155,202)(H2,156,208)(H,166,213)(H,167,212)(H,168,221)(H,169,229)(H,170,203)(H,171,230)(H,172,209)(H,173,214)(H,174,215)(H,175,225)(H,176,222)(H,177,233)(H,178,210)(H,179,216)(H,180,217)(H,181,223)(H,182,231)(H,183,218)(H,184,232)(H,185,234)(H,186,235)(H,187,219)(H,188,224)(H,189,226)(H,190,220)(H,191,211)(H,192,228)(H,193,227)(H,204,205)(H,206,207)(H4,157,158,163)(H4,159,160,164)(H4,161,162,165)/t77-,78-,79-,80-,81-,82+,88-,89-,90-,91-,92-,93-,94-,95-,96-,97-,98-,99-,100-,101-,102-,103-,104-,105-,106-,107-,108-,115-,116-,117-,118-/m0/s1 ☒N
  • Key:WGWPRVFKDLAUQJ-MITYVQBRSA-N ☒N
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Sermorelin acetate (INNTooltip International Nonproprietary Name; 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.[2][3][4] 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.[2]

Sermorelin was approved by the U.S. Food and Drug Administration (FDA) in 1997 for use as a treatment for children with growth hormone deficiency or growth failure.[5] 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.[1][6] Despite this, it may still be used in some off-label contexts or obtained through compounding pharmacies.[7]

Medical uses

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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.[2]

Mechanism of action

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Sermorelin binds to the growth hormone-releasing hormone receptor (GHRH), 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. 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.[3]

Research

[edit]

Sermorelin is a synthetic form (GHRH) that naturally declines with age. Potential benefits of sermorelin in adults lie in its ability to enhance pituitary function and mimic youthful growth hormone secretion patterns. Other options include orally active growth hormone-releasing peptides currently under development. Sermorelin, however, offers a more immediate and potentially better alternative to RHGH for GHRT in aging adults. It was originally marketed as a growth-promoting agent for children with growth deficiencies.[2]

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. This effort aims to develop a more evidence-based approach to GHRT.[3]

See also

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References

[edit]
  1. ^ a b "Geref (Sermorelin acetate)". Drugs@FDA: FDA-Approved Drugs. U.S. Food and Drug Administration. NDA 020443.
  2. ^ a b c d Prakash A, Goa KL (August 1999). "Sermorelin: a review of its use in the diagnosis and treatment of children with idiopathic growth hormone deficiency". BioDrugs. 12 (2): 139–157. doi:10.2165/00063030-199912020-00007. PMID 18031173. S2CID 195690081.
  3. ^ a b c Walker RF (2006). "Sermorelin: a better approach to management of adult-onset growth hormone insufficiency?". Clinical Interventions in Aging. 1 (4): 307–308. doi:10.2147/ciia.2006.1.4.307. PMC 2699646. PMID 18046908.
  4. ^ Rang HP, Dale MM, Ritter JM, Moore PK (2003). Pharmacology (5th ed.). Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4.
  5. ^ Xu Z (January 2016). "Growth hormone-releasing hormone.". Handbook of Hormones. Academic Press. pp. 144–145, e18B-2-e18B-4. doi:10.1016/B978-0-12-801028-0.00143-4. ISBN 978-0-12-801028-0.
  6. ^ "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". U.S. Food and Drug Administration. Federal Register. 4 March 2013. Docket No. FDA-2012-P-1071.
  7. ^ Walker RF (March 2002). "Assessing safety and efficacy of growth hormone replacement in aging by community physicians". Journal of Anti-Aging Medicine. 5 (1): 41–55. doi:10.1089/10945450231762928 (inactive 1 November 2024).{{cite journal}}: CS1 maint: DOI inactive as of November 2024 (link)
  8. ^ Ishida J, Saitoh M, Ebner N, Springer J, Anker SD, von Haehling S (January 2020). "Growth hormone secretagogues: history, mechanism of action, and clinical development". JCSM Rapid Communications. 3 (1): 25–37. doi:10.1002/rco2.9.
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