2. Academic Validation
  3. Small-Molecule GLP-1 Receptor Agonists: A Promising Pharmacological Approach

Small-Molecule GLP-1 Receptor Agonists: A Promising Pharmacological Approach

  • Medicina (Kaunas). 2025 Oct 23;61(11):1902. doi: 10.3390/medicina61111902.
Oana Cristina Șeremet 1,  Ciprian Pușcașu 1,  Corina Andrei 1,  Georgiana Nițulescu 2,  Cristina Elena Zbârcea 1,  Octavian Tudorel Olaru 3
Affiliations

Affiliations

  • 1 Department of Pharmacology and Clinical Pharmacy, Faculty of Pharmacy, Carol Davila University of Medicine and Pharmacy, 6 Traian Vuia Street, 020945 Bucharest, Romania.
  • 2 Department of Pharmaceutical Technology and Biopharmacy, Faculty of Pharmacy, Carol Davila University of Medicine and Pharmacy, 6 Traian Vuia Street, 020945 Bucharest, Romania.
  • 3 Department of Pharmaceutical Botany and Cell Biology, Faculty of Pharmacy, Carol Davila University of Medicine and Pharmacy, 6 Traian Vuia Street, 020945 Bucharest, Romania.
PMID: 41303737 DOI: 10.3390/medicina61111902
Abstract

Glucagon-like peptide-1 receptor (GLP-1R) agonists are injectable peptide-based therapies that have become a focal point in the medical community due to their significant therapeutic efficacy in type 2 diabetes and obesity treatment. Recent advancements in medicinal chemistry have enabled the development of small-molecule GLP-1R agonists, presenting advantages such as oral administration, improved patient adherence, and cost-effectiveness. These compounds demonstrate promising efficacy in enhancing Insulin secretion and promoting weight loss, in a similar way to peptide agonists. This narrative review focuses on the pharmacodynamic profiles and the current progress in clinical and preclinical research on small-molecule GLP-1R agonists. As this class of agents continues to evolve, it represents a compelling therapeutic alternative with the potential to reshape the treatment for metabolic disorders.

Keywords

obesity; small-molecule GLP-1 receptor agonists; type 2 diabetes.

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