Exenatide: a GLP-1 receptor agonist as novel therapy for Type 2 diabetes mellitus

@article{Briones2006ExenatideAG,
  title={Exenatide: a GLP-1 receptor agonist as novel therapy for Type 2 diabetes mellitus},
  author={Ma Briones and Mandeep Bajaj},
  journal={Expert Opinion on Pharmacotherapy},
  year={2006},
  volume={7},
  pages={1055 - 1064}
}
  • Ma Briones, M. Bajaj
  • Published 24 May 2006
  • Medicine, Biology
  • Expert Opinion on Pharmacotherapy
Exenatide is a glucagon-like peptide 1 receptor agonist, which has recently received FDA approval in the US for the treatment of Type 2 diabetes. Exenatide is an incretin mimetic that improves glycaemic control in patients with diabetes through acute mechanisms, such as glucose-dependent stimulation of insulin secretion, suppression of inappropriate glucagon secretion and slowing of gastric emptying, as well as chronic mechanisms that include enhancement of β-cell mass in rodent studies and… 
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References

SHOWING 1-10 OF 89 REFERENCES
Pharmacology of exenatide (synthetic exendin-4): a potential therapeutic for improved glycemic control of type 2 diabetes
Enhancing incretin action for the treatment of type 2 diabetes.
TLDR
The need for daily injections of potentially immunogenic GLP-1-derived peptides and the potential for unanticipated side effects with chronic use of DPP-IV inhibitors will require ongoing scrutiny of the risk-benefit ratio for these new therapies as they are evaluated in the clinic.
Effects of 1-mo bolus subcutaneous administration of exendin-4 in type 2 diabetes.
TLDR
The data suggest that, even with this short duration of therapy, exendin-4 treatment had a significant effect on glucose homeostasis.
The insulinotropic effect of acute exendin-4 administered to humans: comparison of nondiabetic state to type 2 diabetes.
TLDR
It is concluded that exendin-4 is a potent and long-lasting insulinotropic agent in nondiabetic and diabetic subjects.
Synthetic exendin-4 (exenatide) significantly reduces postprandial and fasting plasma glucose in subjects with type 2 diabetes.
TLDR
In conclusion, AC2993 acutely and markedly reduces fasting and postprandial glucose concentrations in patients with type 2 diabetes.
Effect on glycemic control of exenatide (synthetic exendin-4) additive to existing metformin and/or sulfonylurea treatment in patients with type 2 diabetes.
TLDR
AC2993 had significant effects on HbA(1c) levels in patients not currently achieving optimal glucose control with diet and/or OAAs, confirming AC2993 effects on fasting and postprandial glycemia.
Therapy of type 2 diabetes mellitus based on the actions of glucagon‐like peptide‐1
  • J. Holst
  • Medicine, Biology
    Diabetes/metabolism research and reviews
  • 2002
TLDR
Continuous subcutaneous administration of the GLP‐1‐based therapy of type 2 diabetes mellitus for six weeks in patients with rather advanced disease greatly improved glucose profiles and lowered body weight, haemoglobin A1C, and free fatty acids.
Glucagon-like peptide-1 promotes satiety and reduces food intake in patients with diabetes mellitus type 2.
TLDR
A marked effect of GLP-1 on appetite is demonstrated by showing enhanced satiety and reduced energy intake in patients with diabetes type 2.
Antidiabetogenic effect of glucagon-like peptide-1 (7-36)amide in normal subjects and patients with diabetes mellitus.
TLDR
GLIP has an antidiabetogenic effect, and it may therefore be useful in the treatment of patients with NIDDM, indicating that GLIP had an insulinotropic effect.
Exendin-4 reduces fasting and postprandial glucose and decreases energy intake in healthy volunteers.
TLDR
The results are in accord with the possibility that exendin-4 may be a potential treatment for type 2 diabetes, particularly for obese patients, because it acts to reduce plasma glucose at least partly by a delay in gastric emptying, as well as by reducing calorie intake.
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