Gastrointestinal · In Clinical Trials
Ghrelin Receptor Antagonists
No lawful US pathway
01 · Overview
Ghrelin receptor antagonists are peptides, peptidomimetics, and small molecules designed to block the growth hormone secretagogue receptor (GHSR), also known as the ghrelin receptor. Ghrelin is a 28-amino acid hormone secreted mainly by the gastric fundus; its acylated form activates GHSR and is the only known peripheral hormone that stimulates appetite (PMID 27376422).
By blocking GHSR, these agents aim to reduce hunger signals, with potential uses in obesity and metabolic disease. The endogenous peptide LEAP2 acts as a natural GHSR antagonist and inverse agonist (PMID 41911360).
02 · Research summary & key findings
In mice, peptide GHSR antagonists reduced food intake and gastric emptying, and repeated dosing reduced weight gain and improved glucose control in obese ob/ob mice (PMID 12801949). In randomized crossover studies, intravenous LEAP2 lowered post-meal glucose and reduced food intake in healthy men (PMID 35492241) and reduced ad libitum food intake by about 12% in men with obesity (PMID 41911360). In a phase 2a study in alcohol use disorder, the oral GHSR blocker PF-5190457 did not reduce cue-induced alcohol craving but reduced calories selected in a virtual food task (PMID 39704175). None has been approved.
03 · Regulatory status
Ghrelin Receptor Antagonists is currently undergoing clinical trials. It is not yet FDA-approved and is available only through clinical research settings or investigational protocols.
No lawful pathway today
Ghrelin Receptor Antagonists is not FDA-approved and does not currently have a lawful prescription or compounding pathway in the United States, so we do not sell it and will not book a consultation for it. That can change: in 2026 FDA began reviewing several peptides for compounding.
See the 7 FDA-approved compounds in Gastrointestinal
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04 · Administration routes
- Subcutaneous injection
- Oral
References
- [1]Antagonism of ghrelin receptor reduces food intake and body weight gain in mice Gut, 2003. PMID 12801949
- [2]Effects of ghrelin in energy balance and body weight homeostasis Hormones (Athens), 2016. PMID 27376422
- [3]LEAP2 reduces postprandial glucose excursions and ad libitum food intake in healthy men Cell Rep Med, 2022. PMID 35492241
- [4]A randomized, double-blind, placebo-controlled study of a GHSR blocker in people with alcohol use disorder JCI Insight, 2024. PMID 39704175
- [5]LEAP2 Reduces Ad Libitum Food Intake and Attenuates Postprandial Glucose Excursions in Men With Obesity Diabetes, 2026. PMID 41911360
Primary literature
- PubMed: "Ghrelin Receptor Antagonists"
Peer-reviewed literature indexed by the National Library of Medicine.
- ClinicalTrials.gov: "Ghrelin Receptor Antagonists"
Registered interventional and observational studies, including status and phase.
- PubChem: "Ghrelin Receptor Antagonists"
Chemical structure, molecular properties, and bioactivity data.
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