Relamorelin

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]

Relamorelin
Clinical data
Routes of
administration		Subcutaneous
ATC code
  • None
Identifiers
CAS Number
PubChem CID
ChemSpider
KEGG
Chemical and physical data
FormulaC43H50N8O5S
Molar mass790.9727 g/mol g·mol−1
3D model (JSmol)

See also

References
  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.
  2. 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. PMC 4424792.
  3. 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. 13: 2312–2319.e1. 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. PMC 3526234. PMID 22961573.
  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. PMC 4578705.
  6. Rhythm Pharmaceuticals (2014). "Rhythm Presents Positive Phase 2 Study Results for Relamorelin for Chronic Constipation". PRNewsire. Retrieved June 10, 2015.



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