Relamorelin Explained

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. In humans, relamorelin produces increases in plasma growth hormone, prolactin, and cortisol levels,^[4] and, like other GHSR agonists, increases appetite. 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]}

See also

• List of growth hormone secretagogues

External links

• Relamorelin (RM-131): Ghrelin Peptide Agonist: A New Drug Class for the Treatment of GI Functional Disorders – Rhythm Pharmaceuticals
• Relamorelin – AdisInsight

Notes and References

1. Haddley K . Relamorelin. Ghrelin receptor agonist, treatment of constipation, treatment of anorexia nervosa, treatment of diabetic gastroparesis. Drugs of the Future. 39. 11. 2014. 775. 0377-8282. 10.1358/dof.2014.039.011.2231856.
2. Camilleri M, Acosta A . Emerging treatments in Neurogastroenterology: relamorelin: a novel gastrocolokinetic synthetic ghrelin agonist . Neurogastroenterology and Motility . 27 . 3 . 324–32 . March 2015 . 25545036 . 4424792 . 10.1111/nmo.12490 .
3. Acosta A, Camilleri M, Kolar G, Iturrino J, Szarka LA, Boldingh A, Burton D, Ryks M, Rhoten D, Zinsmeister AR, Spence SC, Gottesdiener K, Bouras EP, Vazquez-Roque MI . 6 . Relamorelin Relieves Constipation and Accelerates Colonic Transit in a Phase 2, Placebo-Controlled, Randomized Trial . Clinical Gastroenterology and Hepatology . 13 . 13 . 2312–9.e1 . December 2015 . 26001337 . 10.1016/j.cgh.2015.04.184 . free .
4. Shin A, Camilleri M, Busciglio I, Burton D, Stoner E, Noonan P, Gottesdiener K, Smith SA, Vella A, Zinsmeister AR . 6 . 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 . January 2013 . 22961573 . 3526234 . 10.2337/dc12-1128 .
5. Valentin N, Acosta A, Camilleri M . Early investigational therapeutics for gastrointestinal motility disorders: from animal studies to Phase II trials . Expert Opinion on Investigational Drugs . 24 . 6 . 769–79 . June 2015 . 25971881 . 4578705 . 10.1517/13543784.2015.1025132 .
6. Web site: Rhythm Presents Positive Phase 2 Study Results for Relamorelin for Chronic Constipation . Rhythm Pharmaceuticals . PRNewsire . 2014 . June 10, 2015.
7. Web site: November 7, 2019 . AbbVie Inc SEC filing 2019 . AbbVie.
8. Web site: AbbVie Reports First-Quarter 2023 Financial Results .