Introduction: The dipeptidyl peptidase-4 inhibitors (DPP-4is), which belong to the class of incretin-based medications, are recommended as second or third-line therapies in guidelines for the management of type 2 diabetes mellitus. They have a favorable drug tolerability and safety profile compared to other glucose-lowering agents.
Objective: This review discusses data concerning the use of DPP-4is and their cardiovascular profile, and gives an updated comparison with the other oral glucose-lowering medications with regards to safety and efficacy. Currently available original studies, abstracts, reviews articles, systematic reviews and meta-analyses were included in the review.
Discussion: DPP4is are moderately efficient in decreasing the HbA1c by an average of 0.5% as monotherapy, and 1.0% in combination therapy with other drugs. They have a good tolerability and safety profile compared to other glucose-lowering drugs. However, there are possible risks pertaining to acute pancreatitis and pancreatic cancer.
Conclusion: Cardiovascular outcome trials thus far have proven the cardiovascular safety for ischemic events in patients treated with sitagliptin, saxagliptin, alogliptin, linagliptin and vildagliptin. Data showing increased rate of hospitalisation in the case of saxagliptin did not seem to be a class effect.
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http://dx.doi.org/10.1016/j.metabol.2020.154295 | DOI Listing |
EClinicalMedicine
December 2024
Nottingham Digestive Diseases Centre (NDDC), Translational Medical Sciences, School of Medicine, University of Nottingham, NG7 2UH, UK.
Background: Despite the availability of various pharmacological and behavioural interventions, alcohol-related mortality is rising. This systematic review aimed to critically evaluate the existing literature on the association between glucagon-like peptide-1 receptor agonists use (GLP-1 RAs) and alcohol consumption.
Methods: Electronic searches were conducted on Ovid Medline, EMBASE, PsycINFO, clintrials.
Dipeptidyl peptidase 4 (DPP4) is a transmembrane serine exopeptidase abundantly expressed in the kidneys, predominantly in the proximal tubule (PT); however, its non-enzymatic functions in this nephron segment remain poorly understood. While DPP4 physically associates with the Na /H exchanger isoform 3 (NHE3) and its inhibitors exert natriuretic effects, the DPP4 role in blood pressure (BP) regulation remains controversial. This study investigated the effects of PT-specific deletion ( ) and global deletion ( ) on systolic blood pressure (SBP), natriuresis, and NHE3 regulation under baseline and angiotensin II (Ang II)-stimulated conditions in both male and female mice.
View Article and Find Full Text PDFChem Biodivers
December 2024
University of Nis Faculty of Medicine, Department of Chemistry, Bulevar Dr Zorana Đinđića 81, 18000 Niš, Serbia, Niš, SERBIA.
The thieno[2,3-d]pyrimidine fragment is in the structure of many drug-like candidate derivatives with a wide range of biological activities. However, very few dipeptidyl peptidase-4 (DPP-4) inhibitors with this building block are currently known. Here, the selection of a novel DPP-4 inhibitor based on the thienopyrimidine scaffold is reported.
View Article and Find Full Text PDFClin J Am Soc Nephrol
October 2024
OptumLabs, Eden Prairie, Minnesota.
Diabetes Obes Metab
December 2024
Department of Rheumatology, Endocrinology and Nephrology, Faculty of Medicine and Graduate School of Medicine, Hokkaido University, Sapporo, Japan.
Aims: To compare the efficacy of adding imeglimin versus that of metformin dose escalation on glycemic control in subjects with type 2 diabetes treated with a dipeptidyl peptidase-4 inhibitor plus low-dose metformin (500-1000 mg/day).
Materials And Methods: In this multicentre, open-labelled, prospective, randomized, parallel-group comparison study, the addition of imeglimin (2000 mg/day) or metformin escalation was applied for 24 weeks in eligible subjects. The primary endpoint was the mean change in glycated haemoglobin (HbA1c) over 24 weeks.
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