Abstract

ObjectsImigliptin is a novel dipeptidyl peptidase-4 inhibitor. In the present study, we aimed to evaluate the effects of imigliptin and alogliptin on insulin resistance and beta-cell function in Chinese patients with type-2 diabetes mellitus (T2DM).MethodsA total of 37 Chinese T2DM patients were randomized to receive 25 mg imigliptin, 50 mg imigliptin, placebo, and 25 mg alogliptin (positive drug) for 13 days. Oral glucose tolerance tests were conducted at baseline and on day 13, followed by the oral minimal model (OMM).ResultsImigliptin or alogliptin treatment, compared with their baseline or placebo, was associated with higher beta-cell function parameters (φ s and φ tot) and lower glucose area under the curve (AUC) and postprandial glucose levels. The changes in the AUC for the glucose appearance rate between 0 and 120 min also showed a decrease in imigliptin or alogliptin groups. However, the insulin resistance parameter, fasting glucose, was not changed. For the homeostatic model assessment (HOMA-β and HOMA-IR) parameters or secretory units of islets in transplantation index (SUIT), no statistically significant changes were found both within treatments and between treatments.ConclusionsAfter 13 days of treatment, imigliptin and alogliptin could decrease glycemic levels by improving beta-cell function. By comparing OMM with HOMA or SUIT results, glucose stimulation might be more sensitive for detecting changes in beta-cell function.

Highlights

  • Diabetes is a serious and global health concern

  • Chinese subjects with naïve type 2 diabetes mellitus (T2DM) were recruited if they met the criteria as follows: newly diagnosed with T2DM, age between 18 and 65 years, body mass index of between 20 and 30 kg/m2 and body weight ≥50 kg, HbA1c between 6.5 and 11%, serum creatine less than the upper limit of normal, and hepatic transaminase level less than two times the upper limit of normal

  • No statistically significant changes were observed between imigliptin and alogliptin at △GAUC and △PPG

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Summary

Introduction

There are 463 million patients with diabetes all over the world, and the number of patients with diabetes may increase up to 700 million by 2045 [1] Most of these patients are type 2 diabetes mellitus (T2DM). As a new class of anti-diabetic drugs, dipeptidyl peptidase-4 (DPP-4) inhibitors exhibit many favorable features, such as a low risk of hypoglycemia, weight neutrality, and a lower glycemic variability [3] with comparable glucose control capability [4]. The National Medical Products Administration has approved imigliptin for clinical trials, and it has finished single- and multiple-dose studies (unpublished data). Alogliptin has been used as the positive drug in the multiple-dose study for imigliptin

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