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Best Peptides for Gastroparesis: Mechanism Comparison
Ghrelin Analogs (Relamorelin, TZP-101) GHS-R1a receptors on enteric neurons Stimulates vagal nerve activation and ICC pacemaker frequency, increasing antral peristalsis 35–50% reduction in gastric retention time in Phase 2 diabetic gastroparesis trials Subcuta
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- Ghrelin Analogs (Relamorelin, TZP-101)
- GHS-R1a receptors on enteric neurons
- Stimulates vagal nerve activation and ICC pacemaker frequency, increasing antral peristalsis
- 35–50% reduction in gastric retention time in Phase 2 diabetic gastroparesis trials
- Subcutaneous injection twice daily
- Strongest evidence for diabetic gastroparesis with intact vagal pathways. Requires injection compliance
- Motilin Agonists (Camicinal, Mitemcinal)
- Motilin receptors (GPR38) on gastric smooth muscle
- Initiates phase III migrating motor complex, triggering coordinated antral contractions
- 28% increase in gastric emptying rate at 4 weeks in Phase 2 trials
- Oral, three times daily
- Mechanistically sound but prone to receptor desensitisation. Intermittent dosing critical
- 5-HT4 Agonists (Velusetrag, Prucalopride)
- Serotonin 5-HT4 receptors on enteric neurons
- Stimulates acetylcholine release, coordinating smooth muscle peristalsis
- 15–20% improvement in gastric emptying (prucalopride); 18 percentage point reduction in retention (velusetrag)
- Oral, once daily
- Safer cardiac profile than older agents. Moderate efficacy, works best with intact enteric neurons