Relamorelin
Also known as: BIM-28131, Relamorelin, relamorelin acetate, RM-131, Ulimorelin analog
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Summary
Relamorelin is an investigational synthetic analogue of the hunger hormone ghrelin that activates the ghrelin (growth‑ hormone secretagogue) receptor. It is being evaluated primarily for gastroparesis, including diabetic gastroparesis, where delayed gastric emptying causes nausea, vomiting, bloating and early satiety. Early clinical studies suggest it can speed gastric emptying and relieve several core symptoms, positioning it as a potential new prokinetic therapy for these difficult‑to‑treat gastrointestinal motility disorders.
Mechanism of Action
Relamorelin binds to the GHSR1a (ghrelin) receptor on endocrine and enteric cells, mimicking endogenous ghrelin. Activation of this receptor triggers intracellular signaling that increases growth‑ hormone release and enhances smooth‑muscle contractility in the stomach. The resulting coordinated gastric contractions promote faster emptying of gastric contents, while central effects on appetite and nausea pathways may also contribute to symptom improvement.
What the Research Shows
Review articles from 2017‑2019 identify relamorelin as a novel ghrelin‑receptor agonist entering the therapeutic landscape for gastroparesis, alongside other prokinetics. Phase IIA trials reported superiority to placebo for symptom relief in diabetic gastroparesis and chronic idiopathic constipation. Phase IIB data showed accelerated gastric emptying and reductions in nausea, fullness, bloating and abdominal pain, though vomiting frequency was not significantly altered. A 2023 meta‑analysis of five randomized controlled trials (1,033 participants) confirmed a statistically significant shortening of gastric emptying time (≈‑11 minutes overall, ‑8 minutes in diabetic patients). Safety signals were modest, with more frequent headaches, dizziness and gastrointestinal complaints but no cardiac or neurologic adverse events reported. Ongoing phase III studies aim to confirm efficacy and long‑term safety.
Reported Benefits
Clinical evidence indicates that relamorelin can markedly speed gastric emptying, which correlates with improvements in key gastroparesis symptoms such as nausea, early satiety, bloating and abdominal pain. The meta‑analysis demonstrated a mean reduction of about 11 minutes in emptying time versus placebo, and subgroup analysis showed benefit in diabetic gastroparesis. Early trials also reported symptom relief in chronic idiopathic constipation. Across studies, the drug has been described as well tolerated, with no serious cardiac or neurologic toxicity observed.
Limitations of the Evidence
Evidence to date is limited to phase II trials and a meta‑analysis of five studies; no phase III results have been published, leaving long‑term efficacy and safety uncertain. Benefit on vomiting frequency was not demonstrated, and adverse events such as headache, dizziness and mild gastrointestinal upset were more common than with placebo. The drug is not FDA‑approved and remains investigational, so its use is confined to clinical trials. Data on chronic idiopathic constipation are sparse and derived from small cohorts.
Safety Considerations
Relamorelin has been generally well tolerated in trial participants. Reported adverse events include headaches, dizziness and transient gastrointestinal symptoms, occurring more often than with placebo. Importantly, studies to date have not identified cardiac arrhythmias, hypotension, or neurologic toxicity. Nevertheless, the safety profile is based on relatively short‑term exposure in phase II trials, and comprehensive long‑term safety data are still pending.
How It Is Administered
In clinical studies relamorelin has been administered by subcutaneous injection, typically as an acetate formulation. The route and dosing schedule are determined by trial protocols; the drug is not available as an oral or over‑the‑counter product.
Routes of Administration
Goals & Uses
- Reduction of nausea and vomitingSymptom ManagementModerate
- Chronic idiopathic gastroparesisGastrointestinal MotilityLow
- Acceleration of gastric emptyingGastrointestinal MotilityModerate
- Post‑operative ileusGastrointestinal MotilityLow
- Chronic constipationGastrointestinal MotilityModerate
- Improvement in postprandial fullness and bloatingSymptom ManagementLow
- Diabetic gastroparesis symptom reliefGastrointestinal MotilityModerate
- Diabetic gastroparesisGastrointestinal MotilityHigh
Contraindications
- Mechanical gastrointestinal obstructionGastrointestinalHigh
- Hypersensitivity to relamorelin or excipientsAllergy/ImmunologyHigh
- PregnancyPopulationModeratePotential fetal risk or insufficient safety data
- Known hypersensitivity to relamorelin or excipientsAllergyHigh
- Gastrointestinal perforation or hemorrhageGastrointestinalHigh
Adverse Effects
- Injection site reactionsLocalCommon
- HeadacheNeurologicCommonPain in the head or upper neck
- Abdominal pain or crampingGastrointestinalUncommon
- Transient hyperglycemiaMetabolic/EndocrineUncommon
- NauseaGastrointestinalCommonFeeling of sickness or urge to vomit
- Growth hormone elevationEndocrineUncommon
- DiarrheaGastrointestinalCommonLoose or frequent stools
- Abdominal painGastrointestinalUncommonPain or discomfort in the abdomen
Drug Interactions
- Other ghrelin agonists or GH secretagoguesModerate
- CYP450 substratesLow
- OpioidsModerate
- Anticholinergic agentsModerate
- Insulin and antidiabetic medicationsModerate
Population Constraints
- PregnancyReproductive SafetyRelative
- Severe renal impairmentOrgan ImpairmentRelative
- Pediatric patientsAgeAbsolute
- Severe hepatic impairmentOrgan ImpairmentRelative
Regulatory Status
- European UnionInvestigationalNo marketing authorization; clinical studies in progress.
- United StatesInvestigationalPhase III trials ongoing; Fast Track for diabetic gastroparesis.
- United KingdomInvestigationalUnder MHRA review for trial use.
Granted Fast Track designation by the FDA for diabetic gastroparesis; not approved for any indication in the US, EU, or UK as of 2026.
Evidence & Sources
- Journal ArticleModerateTack J, Van den Houte K, Carbone F2018-01-01T00:00:00.000000Z
- Journal ArticleModerateTack J, Carbone F2017-01-01T00:00:00.000000Z
- Journal ArticleModerateGrover M, Farrugia G, Stanghellini V2019-01-01T00:00:00.000000Z
- Journal ArticleModeratePatel A, et al.2023-01-01T00:00:00.000000Z
- Journal ArticleModerateChedid V, Camilleri M2017-01-01T00:00:00.000000Z
- Journal ArticleModerateAcosta A, Camilleri M2015-01-01T00:00:00.000000Z
Frequently Asked Questions
What condition is relamorelin being developed to treat?
Relamorelin is under investigation as a prokinetic agent for gastroparesis, especially diabetic gastroparesis, and has also been studied in chronic idiopathic constipation.
How does relamorelin work to improve gastric emptying?
It activates the ghrelin (GHSR1a) receptor, stimulating hormonal and enteric pathways that increase gastric smooth‑muscle contractility and coordinate motility, thereby accelerating the movement of stomach contents into the intestine.
What evidence supports its effectiveness?
Phase IIA and IIB trials showed faster gastric emptying and reductions in nausea, fullness, bloating and abdominal pain. A 2023 meta‑analysis of five randomized trials (1,033 patients) found a mean 11‑minute improvement in emptying time compared with placebo.
What side effects are most commonly reported?
The most frequently reported adverse events are headache, dizziness and mild gastrointestinal symptoms such as abdominal discomfort. No serious cardiac or neurologic side effects have been identified in the published trials.
Is relamorelin currently approved for clinical use?
No. Relamorelin remains an investigational drug in clinical trials and has not received regulatory approval for any indication.
What is Relamorelin?
Relamorelin is an investigational synthetic analogue of the hunger hormone ghrelin that activates the ghrelin (growth‑ hormone secretagogue) receptor. It is being evaluated primarily for gastroparesis, including diabetic gastroparesis, where delayed gastric emptying causes nausea, vomiting, bloating and early satiety. Early clinical studies suggest it can speed gastric emptying and relieve several core symptoms, positioning it as a potential new prokinetic therapy for these difficult‑to‑treat gastrointestinal motility disorders.
What is Relamorelin used for?
Relamorelin is educationally associated with: Reduction of nausea and vomiting, Chronic idiopathic gastroparesis, Acceleration of gastric emptying, Post‑operative ileus, Chronic constipation, Improvement in postprandial fullness and bloating, Diabetic gastroparesis symptom relief, Diabetic gastroparesis. Educational only — not medical advice.
How is Relamorelin administered?
Recorded routes of administration: Intravenous, Subcutaneous.
What are the potential side effects of Relamorelin?
Reported adverse effects include: Injection site reactions, Headache, Abdominal pain or cramping, Transient hyperglycemia, Nausea, Growth hormone elevation, Diarrhea, Abdominal pain. This list is not exhaustive — consult a qualified clinician.
Who should avoid Relamorelin?
Recorded contraindications: Mechanical gastrointestinal obstruction, Hypersensitivity to relamorelin or excipients, Pregnancy, Known hypersensitivity to relamorelin or excipients, Gastrointestinal perforation or hemorrhage. Consult a qualified clinician before use.