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Review
. 2020 Oct;30(10):781-794.
doi: 10.1080/13543776.2020.1811851. Epub 2020 Sep 11.

GLP-1R agonists for the treatment of obesity: a patent review (2015-present)

Affiliations
Review

GLP-1R agonists for the treatment of obesity: a patent review (2015-present)

Chunxia Liu et al. Expert Opin Ther Pat. 2020 Oct.

Abstract

Introduction: Glucagon-like peptide-1 (GLP-1) is an endogenous peptide which is secreted by enteroendocrine L cells, GLP-1 receptor agonists (GLP-1 RAs) can exhibit glucoregulation by stimulating insulin release, promote satiety, delay gastric emptying, and reduce energy intake. Liraglutide is the only GLP-1 RA approved for the treatment of obesity. The phase III clinical study of semaglutide has completed and the result showed significant weight loss effect. GLP-1 RAs have been proven to be safe and effective in clinical trials, they are considered to be promising anti-obesity drugs.

Areas covered: This review provides an overview of recently published patents describing modified GLP-1 RAs, multi-agonists in the treatment or prevention of obesity from January 2015 to April 2020. Moreover, small molecule GLP-1 RAs, recombinant fusion proteins, combination of GLP-1 RAs with other drugs and the preparation of GLP-1 RAs are also covered.

Expert opinion: Currently, research on anti-obesity effect of modified GLP-1 RAs has grown significantly, liraglutide accounts for approximately 56% of the global obesity drug market. Long-acting analogues and multifunctional peptides showed good weight loss activity. As more and more clinical trials are carried out, we believe that GLP-1 RAs will occupy an important position in the market of obesity treatment.

Keywords: Glucagon-like peptide-1 receptor agonists; glucagon; glucose-dependent insulinotropic polypeptide; obesity.

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