Takeda San Diego, Inc., 10410 Science Center Drive, San Diego, CA 92121, USA.
Expert Rev Clin Pharmacol. 2009 Nov;2(6):589-600. doi: 10.1586/ecp.09.45.
Alogliptin is a new, potent, highly selective, orally available inhibitor of the dipeptidyl peptidase-4 (DPP-4) enzyme developed for the treatment of Type 2 diabetes mellitus (T2DM). Inhibition of the DPP-4 enzyme, prevents the inactivation of the incretin hormones, glucagon-like peptide (GLP-1) and glucose-dependent insulinotropic peptide (GIP), both of which have very short half-lives. GLP-1 and GIP are released in response to food ingestion; they enhance nutrient-induced insulin secretion and inhibit postprandial glucagon secretion. The pharmacokinetics and pharmacodynamics of alogliptin are suitable for once-daily dosing. In two Phase I clinical trials, one in healthy subjects and one in early-diagnosed patients with T2DM, alogliptin has been shown to be safe and well tolerated. In a Phase II clinical trial, alogliptin was shown to be safe and demonstrated efficacy in patients with T2DM with a dose-response profile suitable for Phase III dose selection.
阿格列汀是一种新型、强效、高度选择性的二肽基肽酶-4（DPP-4）抑制剂，开发用于治疗 2 型糖尿病（T2DM）。DPP-4 酶的抑制作用可防止肠促胰岛素激素胰高血糖素样肽-1（GLP-1）和葡萄糖依赖性胰岛素释放肽（GIP）失活，这两种激素的半衰期都非常短。GLP-1 和 GIP 是响应食物摄入而释放的；它们增强了营养物质诱导的胰岛素分泌，并抑制了餐后胰高血糖素的分泌。阿格列汀的药代动力学和药效学适合每日一次给药。在两项 I 期临床试验中，一项在健康受试者中进行，另一项在早期诊断的 T2DM 患者中进行，阿格列汀已被证明是安全且耐受良好的。在一项 II 期临床试验中，阿格列汀被证明是安全的，并在 T2DM 患者中显示出疗效，其剂量反应曲线适合 III 期剂量选择。
