Relamorelin
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Routes of administration | Subcutaneous |
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Formula | C43H50N8O5S |
Molar mass | 790.98 g·mol−1 |
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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 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]
See also[]
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.
External links[]
- Drugs not assigned an ATC code
- Amines
- Appetite stimulants
- Benzothiophenes
- Carboxamides
- Drugs acting on the gastrointestinal system and metabolism
- Experimental drugs
- Ghrelin receptor agonists
- Growth hormone secretagogues
- Motility stimulants
- Piperidines
- Systemic hormonal preparation stubs
- Gastrointestinal system drug stubs