Incretins

Focus on incretin-based therapies: targeting the core defects of type 2 diabetes

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Jellinger PS. Focus on incretin-based therapies: targeting the core defects of type 2 diabetes. Postgrad Med. 2011 Jan;123(1):53-65. Glucose homeostasis is regulated by a complex interaction of hormones, principally including insulin, glucagon, amylin, and the incretins. Glucagon, cortisol, catecholamines, and growth hormone serve as the classic glucose counterregulatory hormones.

Clinical efficacy of GLP-1 agonists and their place in the diabetes treatment algorithm

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Unger J. Clinical efficacy of GLP 1 agonists and their place in the diabetes treatment algorithm. J Am Osteopath Assoc. 2011;111(2 Suppl 1):eS2-9. Incretin-based therapies (subcutaneously administered glucagon-like peptide-1 [GLP-1] agonists and oral dipeptidyl peptidase-4 inhibitors) represent a new mechanism of action with which to target the adverse effects of type 2 diabetes mellitus.

Saxagliptin: a new DPP-4 inhibitor for the treatment of type 2 diabetes mellitus

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Tahrani AA, Piya MK, Barnett AH. Saxagliptin: a new DPP-4 inhibitor for the treatment of type 2 diabetes mellitus. Adv Ther. 2009;26(3):249-262. Type 2 diabetes mellitus (T2DM) is a global epidemic with increasing impact on individuals and healthcare providers. Available treatments (such as metformin, sulfonylureas, glitazones, and insulin) have proven unsatisfactory in producing a long-lasting impact on glycemic control.

Treatment with the dipeptidyl peptidase-4 inhibitor vildagliptin improves fasting islet-cell function in subjects with type 2 diabetes

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D'Alessio DA, Denney AM, Hermiller LM, et al. Treatment with the dipeptidyl peptidase-4 inhibitor vildagliptin improves fasting islet-cell function in subjects with type 2 diabetes.J Clin Endocrinol Metab. 2009;94(1):81-88. Dipeptidyl peptidase 4 (DPP-4) inhibitors are proposed to lower blood glucose in type 2 diabetes mellitus (T2DM) by prolonging the activity of the circulating incretins, glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide 1 (GLP-1).

The role of incretins in glucose homeostasis and diabetes treatment

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Kim W, Egan JM. The role of incretins in glucose homeostasis and diabetes treatment. Pharmacol Rev. Pharmacol Rev. 2008;60(4):470-512. Incretins are gut hormones that are secreted from enteroendocrine cells into the blood within minutes after eating. One of their many physiological roles is to regulate the amount of insulin that is secreted after eating. In this manner, as well as others to be described in this review, their final common raison d'être is to aid in disposal of the products of digestion.

The dipeptidyl peptidase-4 inhibitor alogliptin w/ pioglitazone improves glycemic control, lipid profiles, & increases pancreatic insulin content in mice

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Moritoh Y, Takeuchi K, Asakawa T, Kataoka O, Odaka H. The dipeptidyl peptidase-4 inhibitor alogliptin in combination with pioglitazone improves glycemic control, lipid profiles, and increases pancreatic insulin content in ob/ob mice. Eur J Pharmacol. 2009;602(2-3):448-454. The combination of two agents with different but complementary mechanisms of action is a logical approach for treating patients with type 2 diabetes.

The incretins: From the concept to their use in the treatment of type 2 diabetes. Part A: Incretins: Concept and physiologic functions

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Girard J. The incretins: From the concept to their use in the treatment of type 2 diabetes. Part A: Incretins: Concept and physiologic functions. Diabetes Metab. 2008;34(6):550-559. This paper briefly reviews the concept of incretins and describes the biological effects of the two incretins identified so far: the glucose-dependent insulinotropic polypeptide (GIP); and the glucagon-like peptide-1 (GLP-1). GIP is released by the Kcells of the duodenum, while GLP-1 is released by the Lcells of the distal ileum, in response to nutrient absorption.

The role of incretins in cardiovascular control

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Mafong DD, Henry RR. The role of incretins in cardiovascular control. Curr Hypertens Rep. 2009;11(1):18-22. Glucagon-like peptide-1 (GLP-1) is an incretin secreted in response to nutrient ingestion. Understanding the incretin effect on diabetes pathophysiology has led to development of a new class of agents termed incretin mimetics. Exenatide is the first GLP-1 agonist approved to treat type 2 diabetes mellitus (T2DM).

Targeting Incretins in Type 2 Diabetes: Role of GLP-1 Receptor Agonists and DPP-4 Inhibitors

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Pratley RE, Gilbert M. Targeting Incretins in Type 2 Diabetes: Role of GLP-1 Receptor Agonists and DPP-4 Inhibitors. Rev Diabet Stud. 2008;5(2):73-94. Until recently, the pathogenesis of type 2 diabetes mellitus (T2DM) has been conceptualized in terms of the predominant defects in insulin secretion and insulin action. It is now recognized that abnormalities in other hormones also contribute to the development of hyperglycemia.

Incretin-based therapies in type 2 diabetes: A review of clinical results

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Bosi E. Lucotti P, Setola E, Monti L, Piatti PM. Incretin-based therapies in type 2 diabetes: A review of clinical results. Diabetes Res Clin Pract. 2008;82(suppl 2):s102-S107. GLP-1 analogues (incretin mimetics) and DPP-4 inhibitors (incretin enhancers) represent new classes of anti-diabetic agents for the treatment of type 2 diabetes. The efficacy and safety of the incretin mimetic exenatide and of the DPP-4 inhibitors, sitagliptin and vildagliptin, have been clearly demonstrated by a very large number of clinical trials. 

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