en Relamorelin

Relamorelin
Clinical data
Routes of; administration	Subcutaneous
ATC code	None;
Identifiers
	IUPAC name 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	661472-41-9;
PubChem CID	85364156;
ChemSpider	32699203;
UNII	BIW199E18V;
KEGG	D10660 ;
CompTox Dashboard (EPA)	DTXSID701032407 ;
Chemical and physical data
Formula	C43H50N8O5S
Molar mass	790.98 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES 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 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 names RM-131, BIM-28131, BIM-28163) is a synthetic peptide, centrally penetrant, selective agonist of the ghrelin/growth hormone secretagogue receptor (GHSR) which is under development by Allergan pharmaceuticals for the treatment of diabetic gastroparesis, chronic idiopathic constipation, and anorexia nervosa.^[1]^[2]^[3] It is a pentapeptide and an analogue of ghrelin with improved potency and pharmacokinetics.^[1]^[2] In humans, relamorelin produces increases in plasma growth hormone, prolactin, and cortisol levels,^[2]^[4] and, like other GHSR agonists, increases appetite.^[3] As of June 2015, relamorelin is in phase II clinical trials for diabetic gastroparesis and constipation.^[5] The United States Food and Drug Administration (FDA) has granted Fast 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]

References

^ ^a ^b Haddley 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.
^ ^a ^b ^c Camilleri 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.
^ ^a ^b Acosta 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.
^ 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.
^ 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.
^ Rhythm Pharmaceuticals (2014). "Rhythm Presents Positive Phase 2 Study Results for Relamorelin for Chronic Constipation". PRNewsire. Retrieved June 10, 2015.
^ "AbbVie Inc SEC filing 2019". AbbVie. November 7, 2019.
^ "AbbVie Reports First-Quarter 2023 Financial Results".

External links

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[Haddley2014-1] Haddley 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.

[CamilleriAcosta2015-2] Camilleri 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.

[AcostaCamilleri2015-3] Acosta 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.

[ShinCamilleri2012-4] 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.

[ValentinAcosta2015-5] 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.

[Rhythm2014-6] Rhythm Pharmaceuticals (2014). "Rhythm Presents Positive Phase 2 Study Results for Relamorelin for Chronic Constipation". PRNewsire. Retrieved June 10, 2015.

[7] "AbbVie Inc SEC filing 2019". AbbVie. November 7, 2019.

[8] "AbbVie Reports First-Quarter 2023 Financial Results".

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Relamorelin

See also

References

External links

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