A GLP-1R agonist Exenatide approved by FDA.

This article comes from references available on internet. It is about a new drug called Glucagon-like Peptide-1 [GLP-1] Receptor Agonists.

So GLP-1R Agonists is analog of human glucagon-like peptide-1, and it acts as GLP-1 receptor agonist to increase insulin secretion in the presence of elevated blood glucose. Also it delays gastric emptying to decrease postprandial glucose and decreases glucagon secretion.

So what is Glucagon-like Peptide-1 [GLP-1]?

GLP-1 is one kind of native human hormones called Incretins, which is produced by the proglucagon gene in L-cells of the small intestine. GLP-1 decreases and control blood glucose by various mechanism including: [1].Liver: reduces hepatic glucose output by inhibiting glucagon release. [2]. Alpha cell: inhibits glucagon secretion. [3].CNS: promotes satiety. [4].Stomach: slows gastric emptying. [5].Beta cell: stimulates glucose-dependent insulin secretion and beta-cell differentiation and proliferation.

Thus, modulating GLP-1 levels and GLP-1 activity through administration of the native hormone, analogs, and mimetics or by inhibiting its degradation has become a major focus of investigation for treating type 2 diabetes over the past decade.

Another important thing, where can we find the receptor of GLP-1?

The receptor is found on pancreatic periductal cells and β-cells and in the kidney, heart, stomach, and brain. GLP-1 receptor (GLP-1R) knockout mice have fasting hyperglycemia and abnormal glucose tolerance but are not obese.


[1].Medscape: Guideline Discusses Oral Pharmacotherapy for Type 2 Diabetes. Full reference: http://www.medscape.org/viewarticle/758426?src=cmemp
[2].Glucagon-Like Peptide 1-Based Therapies for Type 2 Diabetes: A Focus on Exenatide. Full reference: http://clinical.diabetesjournals.org/content/23/2/56.full
[3].Glucagon-Like Peptide-1 Receptor Agonists Promote Weight Loss. Full reference: http://www.medscape.org/viewarticle/757036