Garber Alan J, Sharma Morali D
Professor of Medicine, Biochemistry & Molecular Biology, and Molecular & Cellular Biology, Baylor College of Medicine, Division of Diabetes, Endocrinology & Metabolism, 1709 Dryden, Suite 1000, Houston, TX 77030, USA.
Expert Opin Investig Drugs. 2008 Jan;17(1):105-13. doi: 10.1517/13543784.17.1.105.
Vildagliptin is a selective inhibitor of dipeptidyl peptidase-4, and prevents the rapid degradation of the incretin hormones glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide. Vildagliptin has been evaluated in > 4800 patients in nine Phase III studies in the range of 24 - 52 weeks in duration: four placebo- or active-controlled monotherapy trials that enrolled drug-naive patients; four add-on studies in which vildagliptin was added to a stable regimen of either metformin, a sulfonylurea, a thiazolidinedione or insulin; and a study in which an initial combination of vildagliptin plus pioglitazone in drug-naive patients was evaluated. Across studies, vildagliptin was effective in reducing HbA(1c), had a low risk of hypoglycemia and was weight-neutral and well tolerated.
维格列汀是二肽基肽酶-4的选择性抑制剂，可防止肠促胰岛素激素胰高血糖素样肽-1和葡萄糖依赖性促胰岛素多肽的快速降解。在9项为期24至52周的III期研究中，超过4800名患者接受了维格列汀的评估：4项安慰剂或活性对照单药治疗试验，纳入了未接受过药物治疗的患者；4项附加研究，将维格列汀添加到二甲双胍、磺脲类、噻唑烷二酮类或胰岛素的稳定治疗方案中；以及1项对未接受过药物治疗的患者评估维格列汀加吡格列酮初始联合治疗的研究。在各项研究中，维格列汀在降低糖化血红蛋白方面有效，低血糖风险低，对体重无影响且耐受性良好。
