Ghrelin Receptor Antagonists
Overview
Ghrelin receptor antagonists are a class of peptides and peptidomimetics designed to block the growth hormone secretagogue receptor (GHSR), also known as the ghrelin receptor. Ghrelin is a 28-amino acid orexigenic peptide that stimulates appetite and promotes food intake.
Mechanism of Action
By antagonizing GHSR, these agents aim to reduce hunger signals and promote satiety, with therapeutic potential in obesity and metabolic disorders. The class includes both peptide-based molecules and small-molecule antagonists targeting the same receptor..
Research Summary & Key Findings
Early-phase clinical trials have explored various ghrelin receptor antagonists for obesity and cachexia, though no agent has achieved regulatory approval to date. Preclinical models have demonstrated reduced food intake and body weight in rodents treated with peptide antagonists. Clinical development has been limited by challenges in demonstrating sustained weight loss and acceptable safety profiles.
Clinical 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.
Administration Routes
Related Peptides in Gastrointestinal
Octreotide (Sandostatin)
FDA ApprovedA synthetic octapeptide analog of somatostatin with a substantially longer half-life (90 minutes IV, 6 hours subcutaneou...
View detailsLanreotide (Somatuline Depot)
FDA ApprovedA synthetic octapeptide analog of somatostatin with high affinity for SSTR2 and moderate affinity for SSTR5 receptors. L...
View detailsPasireotide (Signifor)
FDA ApprovedA multireceptor-targeted somatostatin analog with high binding affinity for SSTR1, SSTR2, SSTR3, and SSTR5, particularly...
View detailsPlecanatide (Trulance)
FDA ApprovedA synthetic 16-amino acid peptide structurally related to uroguanylin, an endogenous intestinal peptide that regulates f...
View detailsFind a Provider
Find a verified provider who offers Ghrelin Receptor Antagonists therapy in your area.
Browse Provider MapFind a Pharmacy
Browse PCAB-accredited and FDA 503B-registered compounding pharmacies that supply Ghrelin Receptor Antagonists.
Pharmacy DirectoryJoin the Association
Access exclusive peptide protocols, provider resources, and community support.
List Your PracticeDisclaimer: This information is provided for educational and research purposes only. It is not intended as medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider before starting any peptide therapy. The Peptide Association does not endorse or recommend any specific treatment protocol.