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Tschöp, M.H. ; Nogueiras, R.* ; Ahrén, B.*

Gut hormone-based pharmacology: Novel formulations and future possibilities for metabolic disease therapy.

Diabetologia 66, 1796-1808 (2023)
Publ. Version/Full Text DOI PMC
Open Access Gold (Paid Option)
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Glucagon-like peptide-1 (GLP-1) receptor agonists are established pharmaceutical therapies for the treatment of type 2 diabetes and obesity. They mimic the action of GLP-1 to reduce glucose levels through stimulation of insulin secretion and inhibition of glucagon secretion. They also reduce body weight by inducing satiety through central actions. The GLP-1 receptor agonists used clinically are based on exendin-4 and native GLP-1 and are available as formulations for daily or weekly s.c. or oral administration. GLP-1 receptor agonism is also achieved by inhibitors of dipeptidyl peptidase-4 (DPP-4), which prevent the inactivation of GLP-1 and glucose-dependent insulinotropic polypeptide (GIP), thereby prolonging their raised levels after meal ingestion. Other developments in GLP-1 receptor agonism include the formation of small orally available agonists and compounds with the potential to pharmaceutically stimulate GLP-1 secretion from the gut. In addition, GLP-1/glucagon and GLP-1/GIP dual receptor agonists and GLP-1/GIP/glucagon triple receptor agonists have shown the potential to reduce blood glucose levels and body weight through their effects on islets and peripheral tissues, improving beta cell function and stimulating energy expenditure. This review summarises developments in gut hormone-based therapies and presents the future outlook for their use in type 2 diabetes and obesity.
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Publication type Article: Journal article
Document type Review
Corresponding Author
Keywords Diabetes ; Double Receptor Agonists ; Gip ; Glp-1 Receptor Agonists ; Glucagon ; Obesity ; Review ; Triple Receptor Agonists; Glucagon-like Peptide-1; Glp-1 Receptor Agonist; Beta-cell Function; Type-2 Diabetic-patients; Glycemic Control; Weight-loss; Body-weight; Gip; Fat; Analog
ISSN (print) / ISBN 0012-186X
e-ISSN 1432-0428
Journal Diabetologia
Quellenangaben Volume: 66, Issue: 10, Pages: 1796-1808 Article Number: , Supplement: ,
Publisher Springer
Publishing Place Berlin ; Heidelberg [u.a.]
Non-patent literature Publications
Reviewing status Peer reviewed
Grants Faculty of Medicine, Lund University, Lund, Sweden
Lund University