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ADVANCES IN THERAPY FOR TYPE 2 DIABETES: GLP–1 RECEPTOR AGONISTS AND DPP–4 INHIBITORS. Amandeep Kaur, Kamaldeep Kaur, Dinesh Kumar, Pooja Sharma, Harwinder Singh Rao

ADVANCES IN THERAPY FOR TYPE 2 DIABETES: GLP–1 RECEPTOR AGONISTS AND DPP–4 INHIBITORS.

Amandeep Kaur, Kamaldeep Kaur, Dinesh Kumar, Pooja Sharma, Harwinder Singh Rao

International Journal of Natural Product Science 2012: Spl Issue 1:195.

Abstract(RBIP-195)

Type 2 Diabetes Mellitus is characterized by progressive decline in pancreatic insulin secretion and insulin resistance in muscle and adipose tissue, unrestrained hepatic glucose production, and other hormonal deficiencies. Recent research has led to the development of incretin based therapies, such as: glucagon-like peptide–1 (GLP-1) receptor agonists and dipeptidyl peptidase–4(DPP-4) inhibitors. Incretins are a group of gastrointestinal hormones that cause an increase in the amount of insulin released from the pancreatic beta cells after eating. They also reduce gastric emptying and inhibit glucagon release. The two incretins are glucagon-like peptide-1 (GLP-1) and gastric inhibitory peptide (GIP). Both are rapidly inactivated by the enzyme dipeptidyl peptidase-4 (DPP-4). Several long-lasting analogs of GLP 1 having insulinotropic activity have been developed: exenatide (Byetta) and liraglutide (Victoza). Exenatide binds to the GLP-1 receptor, resists DPP-IV degradation, and has produced effects similar to those of endogenous GLP-1. Three double-blind, placebo-controlled studies evaluated the effect of exenatide on glycemic control in T2DM patients. The main disadvantage of these GLP-1 analogs is these must be administered by subcutaneous injection. Another approach is to inhibit the enzyme DPP-4, that inactivates GLP-1 and GIP. Several DPP-4 inhibitors that can be taken orally as a tablet have been developed. One of them, Januvia (Sitagliptin) was approved by the FDA on October 18, 2006.

Keywords: glucagon-like peptide–1 (GLP-1), receptor, agonists, dipeptidyl peptidase–4 (DPP-4) inhibitors.
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