Comparing hypoglycemic activity of novel GPR119 agonist and DPP-4 inhibitor sitagliptin

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Clinical review of sitagliptin: a DPP-4 inhibitor.

Type 2 Diabetes Mellitus is most common form of diabetes. Oral agents are the main stay of pharmacological treatment for type 2 diabetes mellitus. Dipeptidyl peptidase-4 (DPP-4) inhibitors represent a new therapeutic approach for type 2 diabetes. Sitagliptin is highly selective DPP-4 inhibitor that has been approved for type 2 diabetes therapy. It acts by increasing the levels of incretins by i...

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Stimulating β-Cell Regeneration by Combining a GPR119 Agonist with a DPP-IV Inhibitor

BACKGROUND Activating G-protein coupled receptor 119 (GPR119) by its agonists can stimulate glucagon like peptide-1 (GLP-1) release. GLP-1 is rapidly degraded and inactivated by dipeptidylpeptidase-IV (DPP-IV). We studied the efficiency of combining PSN632408, a GPR119 agonist, with sitagliptin, a DPP-IV inhibitor, on β-cell regeneration in diabetic mice. MATERIALS & METHODS Diabetes in C57BL...

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Physiological and pharmacological mechanisms through which the DPP-4 inhibitor sitagliptin regulates glycemia in mice.

Inhibition of dipeptidyl peptidase-4 (DPP-4) activity improves glucose homeostasis through a mode of action related to the stabilization of the active forms of DPP-4-sensitive hormones such as the incretins that enhance glucose-induced insulin secretion. However, the DPP-4 enzyme is highly expressed on the surface of intestinal epithelial cells; hence, the role of intestinal vs. systemic DPP-4 ...

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Randomized clinical trial comparing the efficacy and safety of treatment with the once‐weekly dipeptidyl peptidase‐4 (DPP‐4) inhibitor omarigliptin or the once‐daily DPP‐4 inhibitor sitagliptin in patients with type 2 diabetes inadequately controlled on metformin monotherapy

AIM To compare the efficacy and safety of the once-weekly oral dipeptidyl peptidase-4 (DPP-4) inhibitor omarigliptin or once-daily DPP-4 inhibitor sitagliptin in patients with type 2 diabetes (T2DM) and inadequate glycaemic control on metformin. MATERIALS AND METHODS Patients with T2DM with a glycated haemoglobin (HbA1c) concentration ≥6.5% to ≤9.0% while on a stable dose of metformin (≥1500 ...

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Sitagliptin, a DPP-4 Inhibitor, Acutely Inhibits Intestinal Lipoprotein Particle Secretion in Healthy Humans

The dipeptidyl peptidase-4 inhibitor sitagliptin, an antidiabetic agent, which lowers blood glucose levels, also reduces postprandial lipid excursion after a mixed meal. The underlying mechanism of this effect, however, is not clear. This study examined the production and clearance of triglyceride-rich lipoprotein particles from the liver and intestine in healthy volunteers in response to a sin...

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ژورنال

عنوان ژورنال: Problems of Endocrinology

سال: 2016

ISSN: 2308-1430,0375-9660

DOI: 10.14341/probl201662138-43