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GS-4571 is a novel oral small molecule agonist of the glucagon-like peptide 1 receptor (GLP-1R), developed by Gilead Sciences for the treatment of obesity and type 2 diabetes mellitus. As a GLP-1R agonist, it stimulates cAMP production in pancreatic beta cells, leading to increased insulin secretion, reduced glucagon release, delayed gastric emptying, and enhanced satiety. Preclinical studies demonstrated that once-daily oral administration of GS-4571 improved glycemic control and promoted weight loss in obese diabetic cynomolgus monkeys. The drug is currently being evaluated in Phase 1 clinical trials to assess its pharmacokinetics, safety, and tolerability in healthy participants as well as those with obesity or type 2 diabetes.
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