Kutoh Eiji, Hirate Mitsuru, Ikeno Yu
Biomedical Center, Tokyo, Japan ; Division of Diabetes and Endocrinology, Department of Internal Medicine, Gyoda General Hospital, Saitama, Japan.
Biomedical Center, Tokyo, Japan.
J Clin Med Res. 2014 Aug;6(4):287-94. doi: 10.14740/jocmr1841e. Epub 2014 May 22.
Teneligliptin is a novel, highly selective dipeptidyl peptidase-4 (DPP-4) inhibitor. The aim of this study is to explore the glycemic and non-glycemic efficacies of teneligliptin as an initial therapy.
Newly diagnosed, drug naive Japanese subjects with type 2 diabetes (T2DM) were assigned to 20 mg/day teneligliptin monotherapy (n = 31). At 3 months, levels of glycemic and other parameters were compared with those at baseline.
Significant reductions of HbA1c (from 10.34 ± 2.06 to 8.38 ± 2.23%) and fasting blood glucose (FGB, from 211.3 ± 68.4 to 167.3 ± 70.2 mg/dL) levels were observed without any clinically significant adverse events. However, significant increases of uric acids (UA) levels were observed and two subjects reported mild hypoglycemic events. Homeostasis model assessment-B (HOMA-B) levels significantly increased, while high HOMA-R levels significantly decreased. Significant correlations were observed between the changes (Δ) of HbA1c and those of HOMA-B, and between ΔFBG and ΔHOMA-R. No changes in lipid and body weight were noted.
Teneligliptin might be effectively and safely used as an initial therapy for newly diagnosed T2DM. Glycemic efficacy of teneligliptin is obtained through activating beta-cell function as well as decreasing insulin resistance.
替奈利汀是一种新型、高选择性二肽基肽酶-4（DPP-4）抑制剂。本研究的目的是探讨替奈利汀作为初始治疗的血糖和非血糖疗效。
将新诊断的、未接受过药物治疗的日本2型糖尿病（T2DM）患者分配至20mg/天替奈利汀单药治疗组（n = 31）。3个月时，将血糖及其他参数水平与基线时进行比较。
观察到糖化血红蛋白（HbA1c）水平显著降低（从10.34±2.06%降至8.38±2.23%），空腹血糖（FGB）水平显著降低（从211.3±68.4mg/dL降至167.3±70.2mg/dL），且无任何具有临床意义的不良事件。然而，观察到尿酸（UA）水平显著升高，两名受试者报告有轻度低血糖事件。稳态模型评估-B（HOMA-B）水平显著升高，而高HOMA-R水平显著降低。观察到HbA1c的变化（Δ）与HOMA-B的变化之间、ΔFBG与ΔHOMA-R之间存在显著相关性。未观察到血脂和体重的变化。
替奈利汀可有效且安全地用作新诊断T2DM的初始治疗。替奈利汀的血糖疗效是通过激活β细胞功能以及降低胰岛素抵抗获得的。
