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{{Short description|Pharmaceutical drug}} |
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{{cs1 config|name-list-style=vanc}} |
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{{Drugbox |
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{{Drugbox |
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| Verifiedfields = changed |
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| verifiedrevid = 408742257 |
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| Watchedfields = changed |
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| IUPAC_name = |
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| verifiedrevid = 409589124 |
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| image = |
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| IUPAC_name = <small>L</small>-Tyrosyl-<small>L</small>-alanyl-<small>L</small>-α-aspartyl-<small>L</small>-alanyl-<small>L</small>-isoleucyl-<small>L</small>-phenylalanyl-<small>L</small>-threonyl-<small>L</small>-asparaginyl-<small>L</small>-seryl-<small>L</small>-tyrosyl-<small>L</small>-arginyl-<small>L</small>-lysyl-<small>L</small>-valyl-<small>L</small>-leucylglycyl-<small>L</small>-glutaminyl-<small>L</small>-leucyl-<small>L</small>-seryl-<small>L</small>-alanyl-<small>L</small>-arginyl-<small>L</small>-lysyl-<small>L</small>-leucyl-<small>L</small>-leucyl-<small>L</small>-glutaminyl-<small>L</small>-α-aspartyl-<small>L</small>-isoleucyl-<small>L</small>-methionyl-<small>L</small>-seryl-<small>L</small>-argininamide |
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| CAS_number = 86168-78-7 |
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| image = Sermorelin.svg |
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| ATC_prefix = H01 |
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| width = 300px |
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| ATC_suffix = AC04 |
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<!--Clinical data--> |
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| tradename = Geref, Gerel |
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| Drugs.com = {{drugs.com|CONS|sermorelin}} |
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| pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X --> |
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| pregnancy_US = C |
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| pregnancy_category = |
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| legal_AU = <!-- S2, S3, S4, S5, S6, S7, S8, S9 or Unscheduled--> |
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| legal_CA = <!-- Schedule I, II, III, IV, V, VI, VII, VIII --> |
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| legal_UK = <!-- GSL, P, POM, CD, or Class A, B, C --> |
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| legal_US = Discontinued<ref name = "NDA_020443" /> |
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| legal_status = |
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| routes_of_administration = Injection |
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<!--Pharmacokinetic data--> |
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| bioavailability = |
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| protein_bound = |
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| metabolism = |
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| elimination_half-life = |
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| excretion = |
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<!--Identifiers--> |
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| CAS_number_Ref = {{cascite|correct|??}} |
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| CAS_number = 86168-78-7 |
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| ATC_prefix = H01 |
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| ATC_suffix = AC04 |
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| ATC_supplemental = {{ATC|V04|CD03}} |
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| ATC_supplemental = {{ATC|V04|CD03}} |
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| PubChem = 16132413 |
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| PubChem = 16132413 |
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| DrugBank_Ref = {{drugbankcite|changed|drugbank}} |
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| DrugBank = |
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| DrugBank = DB00010 |
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| ChEBI = 9118 |
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| ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}} |
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| ChemSpiderID = 17289071 |
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| UNII_Ref = {{fdacite|changed|FDA}} |
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| UNII = 89243S03TE |
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| KEGG_Ref = {{keggcite|correct|kegg}} |
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| KEGG_Ref = {{keggcite|correct|kegg}} |
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| KEGG = D08509 |
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| KEGG = D08509 |
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| ChEMBL_Ref = {{ebicite|changed|EBI}} |
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| C = 149 | H = 246 | N = 44 | O = 42 | S = 1 |
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| ChEMBL = 1201490 |
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| molecular_weight = 3357.882 |
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| synonyms = GRF 1–29 |
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| smiles = CC(C)(C(=O)N(CC1=CC=CC=C1)C(=O)N((C)O)C(=O)N(CC(=O)N)C(=O)N(CO)C(=O)N(CC2=CC=C(C=C2)O)C(=O)N(CCCNC(=N)N)C(=O)N(CCCCN)C(=O)N(C(C)C)C(=O)N(CC(C)C)C(=O)NCC(=O)N(CCC(=O)N)C(=O)N(CC(C)C)C(=O)N(CO)C(=O)N(C)C(=O)N(CCCNC(=N)N)C(=O)N(CCCCN)C(=O)N(CC(C)C)C(=O)N(CC(C)C)C(=O)N(CCC(=O)N)C(=O)N(CC(=O)O)C(=O)N((C)CC)C(=O)N(CCSC)C(=O)N(CO)C(=O)N(CCCNC(=N)N)C(=O)N)NC(=O)(C)NC(=O)(CC(=O)O)NC(=O)(C)NC(=O)(CC3=CC=C(C=C3)O)N |
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| bioavailability = |
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<!--Chemical data--> |
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| protein_bound = |
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| metabolism = |
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| C=149 | H=246 | N=44 | O=42 | S=1 |
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| smiles = CC(C)(C(=O)N(CC1=CC=CC=C1)C(=O)N((C)O)C(=O)N(CC(=O)N)C(=O)N(CO)C(=O)N(CC2=CC=C(C=C2)O)C(=O)N(CCCNC(=N)N)C(=O)N(CCCCN)C(=O)N(C(C)C)C(=O)N(CC(C)C)C(=O)NCC(=O)N(CCC(=O)N)C(=O)N(CC(C)C)C(=O)N(CO)C(=O)N(C)C(=O)N(CCCNC(=N)N)C(=O)N(CCCCN)C(=O)N(CC(C)C)C(=O)N(CC(C)C)C(=O)N(CCC(=O)N)C(=O)N(CC(=O)O)C(=O)N((C)CC)C(=O)N(CCSC)C(=O)N(CO)C(=O)N(CCCNC(=N)N)C(=O)N)NC(=O)(C)NC(=O)(CC(=O)O)NC(=O)(C)NC(=O)(CC3=CC=C(C=C3)O)N |
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| elimination_half-life = |
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| StdInChI_Ref = {{stdinchicite|changed|chemspider}} |
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| excretion = |
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| StdInChI=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 |
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| pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X --> |
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| StdInChIKey_Ref = {{stdinchicite|changed|chemspider}} |
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| pregnancy_US = <!-- A / B / C / D / X --> |
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| StdInChIKey = WGWPRVFKDLAUQJ-MITYVQBRSA-N |
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| pregnancy_category= |
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| legal_AU = <!-- S2, S3, S4, S5, S6, S7, S8, S9 or Unscheduled--> |
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| legal_CA = <!-- Schedule I, II, III, IV, V, VI, VII, VIII --> |
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| legal_UK = <!-- GSL, P, POM, CD, or Class A, B, C --> |
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| legal_US = <!-- OTC / Rx-only / Schedule I, II, III, IV, V --> |
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| legal_status = |
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| routes_of_administration = |
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}} |
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}} |
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'''Sermorelin''', sometimes called '''GRF 1-29''', is a ] releasing hormone analogue. It is a 29-] ] representing the 1-29 fragment from endogenous human ], and is thought to be the shortest fully functional fragment of GHRH.<ref name="pmid18031173">{{cite journal |author=Prakash A, Goa KL |title=Sermorelin: a review of its use in the diagnosis and treatment of children with idiopathic growth hormone deficiency |journal=BioDrugs : Clinical Immunotherapeutics, Biopharmaceuticals and Gene Therapy |volume=12 |issue=2 |pages=139–57 |year=1999 |month=August |pmid=18031173 |doi= |url= |issn=}}</ref> It is used as a test for growth hormone secretion.<ref>Pharmacology (Rang, Dale, Ritter & Moore, ISBN 0443071454, 5:th ed., Churchill Livingstone 2003).</ref> It is also used as doping substance in sports. |
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Used extensively in Anti-aging Therapy often in conjunction with Testosterone in men. Safer alternative to Human Growth Hormone.{{Citation needed|date=January 2011}} |
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'''Sermorelin acetate''' ({{abbrlink|INN|International Nonproprietary Name}}; brand names '''Geref''', '''Gerel'''), also known as '''GHRH (1-29)''', is a ] ] of ] (GHRH) which is used as a ] to assess ] (GH) ] for the purpose of diagnosing ].<ref name="Prakash_1999">{{cite journal | vauthors = Prakash A, Goa KL | title = Sermorelin: a review of its use in the diagnosis and treatment of children with idiopathic growth hormone deficiency | journal = BioDrugs | volume = 12 | issue = 2 | pages = 139–157 | date = August 1999 | pmid = 18031173 | doi = 10.2165/00063030-199912020-00007 | s2cid = 195690081 }}</ref><ref name="Walker_2006">{{cite journal | vauthors = Walker RF | title = Sermorelin: a better approach to management of adult-onset growth hormone insufficiency? | journal = Clinical Interventions in Aging | volume = 1 | issue = 4 | pages = 307–308 | date = 2006 | pmid = 18046908 | pmc = 2699646 | doi = 10.2147/ciia.2006.1.4.307 | doi-access = free }}</ref><ref>{{cite book | vauthors = Rang HP, Dale MM, Ritter JM, Moore PK |title=Pharmacology |date=2003 |publisher=Churchill Livingstone |location=Edinburgh |isbn=0-443-07145-4 |edition=5th}}</ref> It is a 29-] ] representing the 1–29 fragment from ] human GHRH, thought to be the shortest fully functional fragment of GHRH.<ref name="Prakash_1999" /> |
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==See also== |
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*] |
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*] |
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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.<ref>{{cite book | vauthors = Xu Z | chapter = Growth hormone-releasing hormone. | title = Handbook of Hormones | date = January 2016 | pages = 144-145, e18B-2-e18B-4 | publisher = Academic Press | doi = 10.1016/B978-0-12-801028-0.00143-4 | isbn = 978-0-12-801028-0 }}</ref> 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.<ref name = "NDA_020443">{{cite web | title = Geref (Sermorelin acetate) | work = Drugs@FDA: FDA-Approved Drugs | publisher = U.S. Food and Drug Administration | id = NDA 020443 | url = https://www.accessdata.fda.gov/scripts/cder/daf/index.cfm?event=overview.process&ApplNo=020443 }}</ref><ref>{{cite web | title = 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 | work = U.S. Food and Drug Administration | date = 4 March 2013 | publisher = Federal Register | id = Docket No. FDA-2012-P-1071 | url = https://www.federalregister.gov/documents/2013/03/04/2013-04827/determination-that-geref-sermorelin-acetate-injection-05-milligrams-basevial-and-10-milligrams}}</ref> Despite this, it may still be used in some off-label contexts or obtained through compounding pharmacies.<ref>{{cite journal | vauthors = Walker RF | title = Assessing safety and efficacy of growth hormone replacement in aging by community physicians. | journal = Journal of Anti-Aging Medicine | date = March 2002 | volume = 5 | issue = 1 | pages = 41–55 | doi = 10.1089/10945450231762928 | doi-broken-date = 1 November 2024 | url = https://www.liebertpub.com/doi/abs/10.1089/109454502317629282?journalCode=rej.1 }}</ref> |
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==References== |
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<references/> |
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== 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.<ref name="Prakash_1999" /> |
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== Mechanism of action == |
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Sermorelin binds to the ] (GHRH), mimicking the effects of the full-length GHRH in promoting growth hormone secretion.<ref>{{cite journal | vauthors = Ishida J, Saitoh M, Ebner N, Springer J, Anker SD, von Haehling S | title = Growth hormone secretagogues: history, mechanism of action, and clinical development. | journal = JCSM Rapid Communications | date = January 2020 | volume = 3 | issue = 1 | pages = 25–37 | doi = 10.1002/rco2.9 | doi-access = free }}</ref> |
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Sermorelin's effects are regulated by negative feedback through the inhibitory hormone ], 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 ] by promoting a more physiological pattern of hGH release. Additionally, sermorelin stimulates the pituitary to enhance hGH ], thereby maintaining the growth hormone ] 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.<ref name="Walker_2006" /> |
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== Research == |
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Sermorelin is a synthetic form (]) 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 ] for GHRT in aging adults. It was originally marketed as a growth-promoting agent for children with growth deficiencies.<ref name="Prakash_1999" /> |
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Sermorelin can be prescribed for ] 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 ]. This effort aims to develop a more evidence-based approach to GHRT.<ref name="Walker_2006" /> |
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== See also == |
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* ] |
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== References == |
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{{Reflist}} |
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{{Pituitary and hypothalamic hormones and analogues}} |
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{{Neuropeptide agonists and antagonists}} |
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{{Diagnostic agents}} |
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{{Diagnostic agents}} |
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{{GH/IGF-1 axis signaling modulators}} |
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{{biology-stub}} |
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{{Systemic-hormonal-drug-stub}} |
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