gliptin

Dipeptidyl peptidase 4 (DPP4) is a serine protease known to cleave incretin hormones, which stimulate insulin secretion after food intake, a fact that supported the development of its inhibitors (DPP4i or gliptins) for the treatment of type 2 diabetes mellitus. In addition to their glucose-lowering effects, DPP4i show benefits for the cardiovascular system that could be related, at least in part, to their protective action on vascular endothelium. DPP4i have been associated with the reversal of endothelial dysfunction, an important predictor of cardiovascular events and a hallmark of diseases such as atherosclerosis, diabetes mellitus, hypertension, and heart failure...

The drug metabolism and drug degradation pathways may overlap, resulting in the formation of similar constituents. Therefore, the metabolism data can be helpful for deriving safe levels of degradation impurities and improving the quality of respective pharmaceutical products. The present article contains considerations on possible links between metabolic and degradation pathways for new antidiabetic drugs such as glutides, gliflozins, and gliptins. Special attention was paid to their reported metabolites and identified degradation products...

Metabolic-Associated Fatty Liver Disease (MAFLD) is a prevalent metabolic complication among patients with obesity and type 2 diabetes, associated with bad prognosis. Classical antidiabetics have little effects on this complication, except pioglitazone that exerts a positive impact but with uncertain safety. Gliptins are almost neutral, whereas glucagon-like peptide-1 receptor agonists showed benefits, the most potent ones being those associated with a greater weight loss such as liraglutide or semaglutide...

Traumatic brain injury (TBI) often leads to long-term neurocognitive dysfunctions. Adult neurogenesis in the hippocampal dentate gyrus (DG) serves critical functions in cognition but can be disrupted by brain injury and insult in serval forms. In the present study, we explore the cellular and molecular targets of DPP-4 inhibitors (or gliptins) as related to hippocampal function and TBI cognitive sequelae. Two structurally different gliptins, sitagliptin and vildagliptin, were examined using a controlled cortical impact (CCI) model of moderate TBI in mice...

This paper is part II of the review on metabolism and chemical degradation of new antidiabetic drugs from glutides, gliflozins and gliptins. It is well known that metabolism data can be helpful for deriving safe levels of degradation impurities and their qualifying as far as toxicological aspects are concerned. As a result, it could link the quality of respective pharmaceutical products to clinical practice and patients. Some overlapping pathways of transformations of these important drugs of different chemical structures and different mechanisms of action were discussed...

Herein, we report on the development of disposable screen printed carbon, nanostructure thin film Au/Pt and Pt/Pt all-solid state potentiometric sensors for some antidiabetic compounds called glibtins. The electrodes showed excellent calibration curves (1 × 10-5 -1 × 10-2  M) for alogliptin, saxagliptin and vildagliptin. The electrodes were fully characterized with respect to potential stability, dynamic response time, detection limit, effect of pH and interference according to the IUPAC recommendation...

Highly mutated SARS-CoV-2 is known aetiological factor for COVID-19. Here, we have demonstrated that the receptor binding domain (RBD) of the spike protein can interact with human dipeptidyl peptidase 4 (DPP4) to facilitate virus entry, in addition to the usual route of ACE2-RBD binding. Significant number of residues of RBD makes hydrogen bonds and hydrophobic interactions with α/β-hydrolase domain of DPP4. With this observation, we created a strategy to combat COVID-19 by circumventing the catalytic activity of DPP4 using its inhibitors...

UNLABELLED: Cystic fibrosis-related diabetes (CFRD) is a complication associated with a negative prognosis in patients with cystic fibrosis (CF). Although the oral glucose tolerance test (OGTT) is the widely recommended screening test for CFRD diagnosis, continuous glucose monitoring (CGM) is increasingly considered a useful and easy-to-perform test for diagnosis and follow-up in clinical practice. Regarding CFRD treatment, although insulin is the classic approved pharmacological option, incretins could also be a helpful alternative in early stages...

Dipeptidyl peptidase-4 inhibitors (DPP-4i), or gliptins, are a widely used glucose-lowering agents. A growing amount of evidence pointed to a possible role of DPP-4i in the induction of bullous pemphigoid (BP), which is an auto-immune skin blistering disease that mainly affects the elderly. In this article we discuss a case of DPP-4i associated BP and we provide an updated review of the current knowledge regarding this emerging entity. Use of DPP-4i, particularly vildagliptin, was found to significantly increase the risk of BP...

Dipeptidyl peptidase-4 (DPP4) inhibitors are a potent therapeutic treatment for type 2 diabetes mellitus (T2DM). There is a family of compounds used as DPP4 inhibitors (DPP4Is) called gliptins. They bind tightly to DPP4 to form an inactive protein-ligand complex. However, there remains a need to identify novel DPP4Is that are more efficacious and safer due to the increasing prevalence of T2DM and the undesirable side effects of gliptins. To identify potential DPP4Is, we screened over 1800 novel compounds in a comparative study with gliptins...

Public safety (prevention of accidents) is the primary objective in assessing fitness to drive a motor vehicle. However, general access to mobility should not be restricted if there is no particular risk to public safety. For people with diabetes mellitus, the Führerscheingesetz (Driving Licence Legislation) and the Führerscheingesetz-Gesundheitsverordnung (Driving Licence Legislation Health enactment) regulate important aspects of driving safety in connection with acute and chronic complications of the disease...

Diabetic patients are at particular risk of severe COVID-19. Human dipeptidyl peptidase-4 (DPP-4) is a membrane-bound aminopeptidase that regulates insulin release by inactivating incretin. DPP-4 inhibitors (DPP-4is) are therefore used as oral anti-diabetic drugs to restore normal insulin levels. These molecules also have anti-inflammatory and anti-hypertension effects. Recent studies on the interactions of SARS-CoV-2 spike glycoprotein and DPP-4 predict a possible entry route for SARS-CoV-2. Therefore, DPP-4is could be effective at reducing the virus-induced 'cytokine storm', thereby ceasing inflammatory injury to vital organs...

Dry eye disease encompasses a broad range of etiologies and disease subtypes which have similar clinical manifestations. Medications can cause dry eye disease or symptoms of dryness as a side effect by either interfering with the lacrimal gland or meibomian gland function, or both, and by other mechanisms that affect the ocular surface homeostasis. This is important to know and recognize as eliminating the offending medication can reverse the symptoms and, in many cases, prevent further deterioration of the ocular surface inflammation...

AIMS: Vascular dysfunction and elevated circulating dipeptidyl peptidase 4 (DPP4) activity are both reported to be involved in the progression of heart failure (HF). While the cardiac benefits of DPP4 inhibitors (DPP4i) have been extensively studied, little is known about the effects of DPP4i on vascular dysfunction in nondiabetic HF. This study tested the hypothesis that vildagliptin (DPP4i) mitigates aortic hyperreactivity in male HF rats. MATERIALS AND METHODS: Male Wistar rats were subjected to left ventricle (LV) radiofrequency ablation to HF induction or sham operation (SO)...

BACKGROUND: Gliflozins and gliptins are two distinct groups of pharmacological drugs that reduce blood glucose levels in individuals with type II diabetes in various ways that may perform their functions harmoniously. Trijardy® tablet, which contains empagliflozin, linagliptin, and metformin, was recently approved. The scientific database does not yet have a method that is sensitive enough to quantify the aforementioned medications in the presence of metformin official toxic impurities melamine and cyanoguanidine...

No abstract text is available yet for this article.

The pharmacotherapy of type 2 diabetes mellitus (T2DM) has markedly evolved in the last two decades. Classical antidiabetic agents (sulphonylureas, metformin, insulin) are now in competition with new glucose-lowering medications. Alpha-glucosidase inhibitors and thiazolidinediones (glitazones) were not able to replace older agents, because of insufficient efficacy and/or poor tolerability/safety. In contrast, incretin-based therapies, both dipeptidyl peptidase-4 inhibitors (DPP-4is or gliptins, oral agents) and glucagon-like peptide-1 receptor agonists (GLP-1RAs, subcutaneous injections) are a major breakthrough in the management of T2DM...

Bullous pemphigoid is the most common acquired bullous disease with an autoimmune basis and a tendency to involve mostly old people. By rising incidence of diabetes all over the world, consumption of antidiabetes medications has also increased. One of the most used antidiabetes drugs is gliptin family (dipeptidyl-peptidase 4 inhibitor). Recently, this class of oral antidiabetic agents showed a correlation with the occurrence of bullous pemphigoid and its subtypes, including mucous membrane pemphigoid and pemphigoid nodularis...

Background: Poor control of diabetes mellitus (DM) is partly attributed to doctors' poor adherence to guidelines. Objective: To evaluate doctors' adherence to pharmacotherapeutic recommendations of DM management guidelines and factors associated with guidelines adherence and glycaemic control. Methods: This prospective observational study included 30 doctors who were treating DM patients in their private clinics in Quetta, Pakistan. On visit 1, a total of 600 prescriptions written by 30 enrolled doctors (20 patients per doctor) were noted along with patients' sociodemographic and clinical characteristics...

Sodium-glucose cotransporter type 2 inhibitors (SGLT2i or gliflozins) improve the prognosis of patients with heart failure, independently of the presence of diabetes. They are now recommended for the treatment of heart failure in international guidelines. The addition of a gliflozin driven by such a cardiological indication may require some adjustment of the antidiabetic therapy. The aim of this concise article is to discuss the potential risk of hypoglycaemia, highly deleterious in fragile patients at risk, following the prescription of a gliflozin in patients with heart failure...