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Relamorelin

From Wikipedia, the free encyclopedia
Chemical compound

Pharmaceutical compound
Relamorelin
Clinical data
Routes of
administration
Subcutaneous
ATC code
  • None
Identifiers
  • 4-[[(2S)-2-[[(2R)-2-[[(2R)-3-(1-Benzothiophen-3-yl)-2-(piperidine-3-carbonylamino)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-phenylpropanoyl]amino]piperidine-4-carboxamide
CAS Number
PubChemCID
ChemSpider
UNII
KEGG
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC43H50N8O5S
Molar mass790.98 g·mol−1
3D model (JSmol)
  • c1ccc(cc1)C[C@@H](C(=O)NC2(CCNCC2)C(=O)N)NC(=O)[C@@H](Cc3c[nH]c4c3cccc4)NC(=O)[C@@H](Cc5csc6c5cccc6)NC(=O)C7CCNCC7
  • InChI=1S/C43H50N8O5S/c44-42(56)43(16-20-46-21-17-43)51-41(55)34(22-27-8-2-1-3-9-27)49-39(53)35(23-29-25-47-33-12-6-4-10-31(29)33)50-40(54)36(48-38(52)28-14-18-45-19-15-28)24-30-26-57-37-13-7-5-11-32(30)37/h1-13,25-26,28,34-36,45-47H,14-24H2,(H2,44,56)(H,48,52)(H,49,53)(H,50,54)(H,51,55)/t34-,35+,36+/m0/s1
  • Key:KUBPNVYPKPWGRJ-LIVOIKKVSA-N

Relamorelin (INN,USAN) (developmental code namesRM-131,BIM-28131,BIM-28163) is asyntheticpeptide,centrally penetrant, selectiveagonist of theghrelin/growth hormone secretagogue receptor (GHSR) which is under development byAllergan pharmaceuticals for the treatment ofdiabetic gastroparesis,chronic idiopathic constipation, andanorexia nervosa.[1][2][3] It is apentapeptide and ananalogue ofghrelin with improvedpotency andpharmacokinetics.[1][2] In humans, relamorelin produces increases inplasmagrowth hormone,prolactin, andcortisol levels,[2][4] and, like other GHSR agonists, increasesappetite.[3] As of June 2015, relamorelin is inphase IIclinical trials for diabetic gastroparesis and constipation.[5] The United StatesFood and Drug Administration (FDA) has grantedFast Track designation to relamorelin for diabetic gastroparesis.[6] The development of the drug is uncertain as the most recent mention of it was in a 2019 SEC filing from the drug manufacturer lists the drug's expected launch year as 2024, but not in subsequent filings or press releases.[7][8]

See also

[edit]

References

[edit]
  1. ^abHaddley K (2014). "Relamorelin. Ghrelin receptor agonist, treatment of constipation, treatment of anorexia nervosa, treatment of diabetic gastroparesis".Drugs of the Future.39 (11): 775.doi:10.1358/dof.2014.039.011.2231856.ISSN 0377-8282.
  2. ^abcCamilleri M, Acosta A (March 2015)."Emerging treatments in Neurogastroenterology: relamorelin: a novel gastrocolokinetic synthetic ghrelin agonist".Neurogastroenterology and Motility.27 (3):324–32.doi:10.1111/nmo.12490.PMC 4424792.PMID 25545036.
  3. ^abAcosta A, Camilleri M, Kolar G, Iturrino J, Szarka LA, Boldingh A, et al. (December 2015)."Relamorelin Relieves Constipation and Accelerates Colonic Transit in a Phase 2, Placebo-Controlled, Randomized Trial".Clinical Gastroenterology and Hepatology.13 (13): 2312–9.e1.doi:10.1016/j.cgh.2015.04.184.PMID 26001337.
  4. ^Shin A, Camilleri M, Busciglio I, Burton D, Stoner E, Noonan P, et al. (January 2013)."Randomized controlled phase Ib study of ghrelin agonist, RM-131, in type 2 diabetic women with delayed gastric emptying: pharmacokinetics and pharmacodynamics".Diabetes Care.36 (1):41–8.doi:10.2337/dc12-1128.PMC 3526234.PMID 22961573.
  5. ^Valentin N, Acosta A, Camilleri M (June 2015)."Early investigational therapeutics for gastrointestinal motility disorders: from animal studies to Phase II trials".Expert Opinion on Investigational Drugs.24 (6):769–79.doi:10.1517/13543784.2015.1025132.PMC 4578705.PMID 25971881.
  6. ^Rhythm Pharmaceuticals (2014)."Rhythm Presents Positive Phase 2 Study Results for Relamorelin for Chronic Constipation". PRNewsire. RetrievedJune 10, 2015.
  7. ^"AbbVie Inc SEC filing 2019".AbbVie. November 7, 2019.
  8. ^"AbbVie Reports First-Quarter 2023 Financial Results".

External links

[edit]
Drugs for constipation (laxatives andcathartics) (A06)
Stool softeners
Stimulant laxatives
Bulk-forming laxatives
Lubricant laxatives
Osmotic laxatives
Enemas
Opioid antagonists
Others
GH
(somatotropin)
GHIH
(somatostatin)
GHRH
(somatocrinin)
GHS
(ghrelin)
IGF-1
(somatomedin)
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