Emerging treatments in Neurogastroenterology: Relamorelin: A novel gastrocolokinetic synthetic ghrelin agonist

Research output: Contribution to journalReview article

32 Scopus citations

Abstract

Background: Synthetic ghrelin agonists, predominantly small molecules, are being developed as prokinetic agents that may prove useful in the treatment of gastrointestinal motility disorders. Relamorelin (RM-131) is a pentapeptide synthetic ghrelin analog that activates the growth hormone secretagogue (GHS)-1a (also called the ghrelin) receptor with approximately sixfold greater potency than natural ghrelin. The ability of relamorelin to stimulate growth hormone (GH) release is comparable to that of native ghrelin. Relamorelin has enhanced efficacy and plasma stability compared to native ghrelin. Purpose: In this review, we discuss the pharmacokinetics, pharmacodynamics and potential indications for relamorelin. Relamorelin is administered subcutaneously, dosed daily or twice daily. Relamorelin is being studied for the treatment of patients with gastrointestinal motility disorders. Phase IIA pharmacodynamic studies have demonstrated acceleration of gastric emptying in patients with type 1 diabetes mellitus (T1DM) and type 2 DM (T2DM) and upper gastrointestinal symptoms. In a phase IIA study in patients with diabetic gastroparesis, relamorelin accelerated gastric emptying and significantly improved vomiting frequency compared to placebo and improved other symptoms of gastroparesis in a prespecified subgroup of patients with vomiting at baseline. In patients with chronic idiopathic constipation with defined transit profile at baseline, relamorelin relieved constipation and accelerated colonic transit compared to placebo. These characteristics suggest that this new ghrelin analog shows great promise to relieve patients with upper or lower gastrointestinal motility disorders. Synthetic ghrelin agonists, predominantly small molecules, are being developed as prokinetic agents that may prove useful in the treatment of GI motility disorders. Relamorelin (RM-131) is a pentapeptide synthetic ghrelin analog that activates the growth hormone secretagogue (GHS)-1a (also called the ghrelin) receptor with approximately sixfold greater potency than natural ghrelin. In this review, we discuss the pharmacokinetics, pharmacodynamics, and potential indications for relamorelin. This new ghrelin analog shows great promise to relieve patients with upper or lower GI motility disorders.

Original languageEnglish (US)
Pages (from-to)324-332
Number of pages9
JournalNeurogastroenterology and Motility
Volume27
Issue number3
DOIs
StatePublished - Mar 1 2015

Keywords

  • Constipation
  • Gastroparesis
  • RM-131

ASJC Scopus subject areas

  • Physiology
  • Endocrine and Autonomic Systems
  • Gastroenterology

Fingerprint Dive into the research topics of 'Emerging treatments in Neurogastroenterology: Relamorelin: A novel gastrocolokinetic synthetic ghrelin agonist'. Together they form a unique fingerprint.

  • Cite this