期刊
DIABETES METABOLIC SYNDROME AND OBESITY-TARGETS AND THERAPY
卷 3, 期 -, 页码 325-335出版社
DOVE MEDICAL PRESS LTD
DOI: 10.2147/DMSOTT.S12241
关键词
saxagliptin; dipeptidyl peptidase-4 (DPP-4) inhibitor; type 2 diabetes
资金
- Eli Lilly
- MSD
- Novartis
- Novo Nordisk
- Bristol-Myers Squibb
- AstraZeneca
- sanofi-aventis
Saxagliptin (Onglyza (TM)) is a potent, selective, once-daily dipeptidyl peptidase-4 (DPP-4) inhibitor indicated for improving glycemic control in patients with type 2 diabetes (T2D). By blocking DPP-4, saxagliptin increases and prolongs the effects of incretins, a group of peptide hormones released by intestinal cells after meals, which stimulate glucose-dependent insulin secretion to lower blood glucose. In controlled clinical trials, saxagliptin administered as monotherapy or in combination with metformin, glyburide, or a thiazolidinedione improved glycemic control in a clinically significant manner, reflected by significant decreases in glycated hemoglobin (monotherapy, -0.5%; add-on to metformin, thiazolidinedione, or sulfonylurea, -0.6% to 0.9%; initial combination with metformin, -2.5%), fasting plasma glucose, and postprandial glucose compared with controls. Additionally, saxagliptin improved beta-cell function, reflected as increases in homeostasis model assessment (HOMA)-2 beta. Saxagliptin was generally well tolerated; it did not increase hypoglycemia compared with controls, and was weight neutral. A meta-analysis of Phase II and III trials showed that saxagliptin did not increase the risk of major cardiovascular events. Professional organizations have updated their guidelines for T2D to include a DPP-4 inhibitor as an early treatment option-either as initial therapy in combination with metformin, or as add-on therapy for patients whose glycemia is inadequately controlled by a single oral antidiabetic drug.
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