Relamorelin

Ghrelin Receptor Agonist (growth Hormone Secretagogue)Rx: InvestigationalCompound: Investigational

Also known as: relamorelin acetate, RM-131, Ulimorelin analog

Educational Only — Not medical advice. Consult a qualified clinician before using any peptide.

Summary

Relamorelin (RM-131) is a synthetic pentapeptide ghrelin receptor agonist developed primarily for the treatment of diabetic gastroparesis. It accelerates gastric emptying and reduces gastroparesis symptoms including nausea, vomiting, bloating, and early satiety. It has been evaluated in Phase 2 and Phase 3 clinical trials.

Mechanism of Action

Selective agonist of the ghrelin receptor (GHS-R1a), stimulating gastric motility by accelerating gastric emptying through prokinetic effects on the gastrointestinal tract, mimicking the actions of endogenous ghrelin on gut motility without significant GH release at therapeutic doses.

Routes of Administration

Subcutaneous

Goals & Uses

  • Reduction of nausea and vomitingSymptom ManagementModerate
  • Chronic idiopathic gastroparesisGastrointestinal MotilityLow
  • Acceleration of gastric emptyingGastrointestinal MotilityModerate
  • Improvement in postprandial fullness and bloatingSymptom ManagementLow
  • Diabetic gastroparesis symptom reliefGastrointestinal MotilityModerate

Contraindications

  • Mechanical gastrointestinal obstructionGastrointestinalHigh
  • Hypersensitivity to relamorelin or excipientsAllergy/ImmunologyHigh
  • Gastrointestinal perforation or hemorrhageGastrointestinalHigh

Adverse Effects

  • Injection site reactionsLocalCommon
  • Abdominal pain or crampingGastrointestinalUncommon
  • Transient hyperglycemiaMetabolic/EndocrineUncommon
  • Growth hormone elevationEndocrineUncommon
  • DiarrheaGastrointestinalUncommonLoose or frequent stools

Drug Interactions

  • OpioidsModerate
  • Anticholinergic agentsModerate
  • Insulin and antidiabetic medicationsModerate

Population Constraints

  • PregnancyReproductive SafetyRelative
  • Severe renal impairmentOrgan ImpairmentRelative
  • Pediatric patientsAgeRelative
  • Severe hepatic impairmentOrgan ImpairmentRelative

Regulatory Status

  • European UnionInvestigationalNot approved by EMA. Investigated under EU clinical trial frameworks.
  • United StatesInvestigationalNot FDA approved. Received Fast Track designation for diabetic gastroparesis. Phase 3 DIGEST trials completed; NDA not approved as of available data.
  • United KingdomInvestigationalNot approved by MHRA. Status follows EU investigational classification.

Not approved by FDA or EMA as of the latest available data. Was under investigation by Allergan (later AbbVie) for diabetic gastroparesis. Phase 3 trials (DIGEST program) were conducted but regulatory approval has not been granted.

Evidence & Sources

No sources recorded yet.

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