Relamorelin

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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
PubChem CID
ChemSpider
KEGG
Chemical and physical data
FormulaC43H50N8O5S
Molar mass790.9727 g/mol 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 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 Rhythm Pharmaceuticals for the treatment of diabetic gastroparesis, chronic idiopathic constipation, and anorexia nervosa.[1][2][3] It is a pentapeptide and 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]

See also

References

  1. ^ 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.
  2. ^ a b c Camilleri, M.; Acosta, A. (2015). "Emerging treatments in Neurogastroenterology: relamorelin: a novel gastrocolokinetic synthetic ghrelin agonist". Neurogastroenterology & Motility. 27 (3): 324–332. doi:10.1111/nmo.12490. ISSN 1350-1925.
  3. ^ a b Acosta, Andres; Camilleri, Michael; Kolar, Gururaj; Iturrino, Johanna; Szarka, Lawrence A.; Boldingh, Amy; Burton, Duane; Ryks, Michael; Rhoten, Deborah; Zinsmeister, Alan R.; Spence, Sharon C.; Gottesdiener, Keith; Bouras, Ernest P.; Vazquez-Roque, Maria I. (2015). "Relamorelin Relieves Constipation and Accelerates Colonic Transit in a Phase 2, Placebo-Controlled, Randomized Trial". Clinical Gastroenterology and Hepatology. doi:10.1016/j.cgh.2015.04.184. ISSN 1542-3565.
  4. ^ Shin, A.; Camilleri, M.; Busciglio, I.; Burton, D.; Stoner, E.; Noonan, P.; Gottesdiener, K.; Smith, S. A.; Vella, A.; Zinsmeister, A. R. (2012). "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): 41–48. doi:10.2337/dc12-1128. ISSN 0149-5992.
  5. ^ Valentin, Nelson; Acosta, Andres; Camilleri, Michael (2015). "Early investigational therapeutics for gastrointestinal motility disorders: from animal studies to Phase II trials". Expert Opinion on Investigational Drugs. 24 (6): 769–779. doi:10.1517/13543784.2015.1025132. ISSN 1354-3784.
  6. ^ Rhythm Pharmaceuticals (2014). "Rhythm Presents Positive Phase 2 Study Results for Relamorelin for Chronic Constipation". PRNewsire. Retrieved June 10, 2015.

External links

Template:Neuropeptidergics


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