Gemigliptin: An Update of Its Clinical Use in the Management of Type 2 Diabetes Mellitus

Abstract

Dipeptidyl peptidase-4 (DPP-4) inhibitors are a new class of oral antidiabetic agent for the treatment of type 2 diabetes mellitus. They increase endogenous levels of incretin hormones, which stimulate glucose-dependent insulin secretion, decrease glucagon secretion, and contribute to reducing postprandial hyperglycemia. Although DPP-4 inhibitors have similar benefits, they can be differentiated in terms of their chemical structure, pharmacology, efficacy and safety profiles, and clinical considerations. Gemigliptin (brand name: Zemiglo), developed by LG Life Sciences, is a potent, selective, competitive, and long acting DPP-4 inhibitor. Various studies have shown that gemigliptin is an optimized DPP-4 inhibitor in terms of efficacy, safety, and patient compliance for treatment of type 2 diabetes mellitus. In this review, we summarize the characteristics of gemigliptin and discuss its potential benefits in clinical practice.

Efficacy and safety of gemigliptin, a dipeptidyl peptidase‐4 inhibitor, in patients with type 2 diabetes mellitus inadequately controlled with combination treatment of metformin and sulphonylurea: a 24‐week, multicentre, randomized, double‐blind, placebo‐controlled study (TROICA study)

“…Gemigliptin is a potent DPP‐4 inhibitor showing >80% inhibition of DPP‐4 in the usual dose range, and selective for DPP‐4 with >23 000‐fold selectivity over other proteases, which is similar to other DPP‐4 inhibitors such as sitagliptin or vildagliptin . It has a long half‐life (17‐21 hours) and can be used in once‐daily regimen . The elimination of gemigliptin is balanced between urinary or faecal excretion and hepatic metabolism, and no dose adjustment is needed for renal impairment .…”

“…13 It has a long half-life (17-21 hours) and can be used in once-daily regimen. 13 The elimination of gemigliptin is balanced between urinary or faecal excretion and hepatic metabolism, and no dose adjustment is needed for renal impairment. 14 Furthermore, gemigliptin has demonstrated efficacy as monotherapy and dual therapy with metformin.…”

Effects of gemigliptin, a dipeptidyl peptidase‐4 inhibitor, on lipid metabolism and endotoxemia after a high‐fat meal in patients with type 2 diabetes

“…Indeed, several DPP-4 inhibitors have been shown to reduce postprandial lipaemia 7-10 ; however, their effects on endotoxemia and associated inflammatory responses have not been investigated. The aim of the present study, therefore, was to evaluate the effect of gemigliptin, a highly selective DPP-4 inhibitor, 11 on postprandial metabolic abnormalities, endotoxemia and inflammatory responses. was obtained and immediately frozen with liquid nitrogen.…”

Lung ischemia reperfusion injury: the therapeutic role of dipeptidyl peptidase 4 inhibition

“…GLP-1 suppresses the secretion of glucagon, is important for basal β cell function and is involved on many levels in the control of glucose in the intestinal tract and peripheral tissues (2). Because of the GLP-1 enhancing actions, DPP4 inhibitors are used in the treatment of diabetes mellitus type 2 (3). DPP4 functions beyond glycemic control include potential roles in cancer, HIV, autoimmunity and immunology (4,5).…”