Relamorelin - Misplaced Pages

Chemical compound

Pharmaceutical compound

Relamorelin
Clinical data

Routes of administration	Subcutaneous
ATC code	None
Identifiers
IUPAC name 4-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
3D model (JSmol)	Interactive image
SMILES c1ccc(cc1)C(C(=O)NC2(CCNCC2)C(=O)N)NC(=O)(Cc3cc4c3cccc4)NC(=O)(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. It is a pentapeptide and an analogue of ghrelin with improved potency and pharmacokinetics. In humans, relamorelin produces increases in plasma growth hormone, prolactin, and cortisol levels, and, like other GHSR agonists, increases appetite. As of June 2015, relamorelin is in phase II clinical trials for diabetic gastroparesis and constipation. The United States Food and Drug Administration (FDA) has granted Fast Track designation to relamorelin for diabetic gastroparesis. 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.

References

^ 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.
^ 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.
^ 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

v t e Drugs for constipation (laxatives and cathartics) (A06)
Stool softeners	Docusate
Stimulant laxatives	Bisacodyl Bisoxatin Cascara Castor oil Dantron Oxyphenisatine Phenolphthalein Senna glycosides Sodium picosulfate
Bulk-forming laxatives	Dietary fiber Ethulose Ispaghula Methylcellulose Polycarbophil calcium Sterculia Triticum Syrup of figs
Lubricant laxatives	Liquid paraffin Mineral oil
Osmotic laxatives	Lactitol Lactulose Laminarid Magnesium carbonate Magnesium citrate Magnesium hydroxide (milk of magnesia) Magnesium oxide Magnesium peroxide Magnesium sulfate Mannitol Pentaerythritol Polyethylene glycol (macrogol) Sodium phosphate Sodium sulfate Sodium tartrate Sorbitol
Enemas	Bisacodyl Dantron Glycerol Oil Sodium laurilsulfate Sodium lauryl sulfoacetate Sodium phosphate Sorbitol
Opioid antagonists	Naloxone (Oxycodone/naloxone) PAMORAs Alvimopan Axelopran Bevenopran Methylnaltrexone Naldemedine Naloxegol
Others	Linaclotide Lubiprostone Oxyphenisatine Plecanatide Prucalopride Tegaserod Tenapanor Ulimorelin

v t e GH/IGF-1 axis signaling modulators
GH (somatotropin)	Agonists: Albusomatropin Bovine somatotropin Efpegsomatropin Eftansomatropin alfa Growth hormone Human placental lactogen Lonapegsomatropin Placental growth hormone (growth hormone variant) Somagrebove Somapacitan Somatosalm Somatotropin Somatropin pegol Somatrem Sometribove Somatrogon (MOD-4023; hGH-CTP) Somavaratan Somavubove Somidobove Antagonists: G120K-hGH Pegvisomant Antisense oligonucleotides: Atesidorsen Binding proteins: GHBPTooltip Growth hormone-binding protein
GHIH (somatostatin)	Agonists: BIM-23052 CH-275 Cortistatin-14 Depreotide Edotreotide Ilatreotide L-803,087 L-817,818 Lanreotide NNC 26-9100 Octreotate Octreotide Pasireotide Pentetreotide RC-160 Seglitide Somatostatin (GHIH) Somatostatin (1-28) SRIF-14 SRIF-28 TT-232 Vapreotide Veldoreotide Antagonists: BIM-23056 Cyclosomatostatin CYN-154806 Satoreotide
GHRH (somatocrinin)	Agonists: Peptide: ALRN-5281 CJC-1295 Dumorelin GHRH Modified GRF (1-29) Rismorelin Sermorelin Somatorelin Tesamorelin Antagonists: MZ-5-156
GHS (ghrelin)	Agonists: Peptide: Alexamorelin Cortistatin-14 EP-51216 Examorelin (hexarelin) Ghrelin GHRP-1 GHRP-3 GHRP-4 GHRP-5 GHRP-6 Ipamorelin Lenomorelin Livoletide LY-444711 Pralmorelin (GHRP-2) Relamorelin Tabimorelin Ulimorelin; Non-peptide: Adenosine Anamorelin Capromorelin CP-464709 Ibutamoren (MK-677) L-692,585 Macimorelin SM-130686; Unsorted: LY-426410 LY-444711 Antagonists: A-778193 Cortistatin-8 (D-Lys³)-GHRP-6 JMV2959 YIL-781
IGF-1 (somatomedin)	See here instead.

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