Comparative review of dipeptidyl peptidase‐4 inhibitors and sulphonylureas

Abstract

Type 2 diabetes (T2DM) is a progressive disease, and pharmacotherapy with a single agent does not generally provide durable glycaemic control over the long term. Sulphonylurea (SU) drugs have a history stretching back over 60 years, and have traditionally been the mainstay choice as second-line agents to be added to metformin once glycaemic control with metformin monotherapy deteriorates; however, they are associated with undesirable side effects, including increased hypoglycaemia risk and weight gain. Dipeptidyl peptidase (DPP)-4 inhibitors are, by comparison, more recent, with the first compound being launched in 2006, but the class now globally encompasses at least 11 different compounds. DPP-4 inhibitors improve glycaemic control with similar efficacy to SUs, but do not usually provoke hypoglycaemia or weight gain, are relatively free from adverse side effects, and have recently been shown not to increase cardiovascular risk in large prospective safety trials. Because of these factors, DPP-4 inhibitors have become an established therapy for T2DM and are increasingly being positioned earlier in treatment algorithms. The present article reviews these two classes of oral antidiabetic drugs (DPP-4 inhibitors and SUs), highlighting differences and similarities between members of the same class, as well as discussing the potential advantages and disadvantages of the two drug classes. While both classes have their merits, the choice of which to use depends on the characteristics of each individual patient; however, for the majority of patients, DPP-4 inhibitors are now the preferred choice.

Targeting endothelial metaflammation to counteract diabesity cardiovascular risk: Current and perspective therapeutic options

“…Currently approved DPP4 inhibitors include sitagliptin, saxagliptin, linagliptin and vildagliptin [157]. These small molecular-weight substances inhibit more than 90% of DPP4 activity and can be orally administered.…”

Parkinson';s Disease, Diabetes and Cognitive Impairment

“…DPP-4 inhibitors benefit from having an excellent safety profile, with very few adverse effects noted, in particular a low rate of hypoglycaemic episodes [75]. They are also available as oral preparations compared to GLP-1 agonists, making them more universally accessible to patients who cannot self-inject [75].…”

“…They are also available as oral preparations compared to GLP-1 agonists, making them more universally accessible to patients who cannot self-inject [75]. In addition, different DPP-4 inhibitors are hepatically or renally metabolised, which may broaden their use in patients with co-existent liver or renal disease.…”

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“…In type 2 diabetes, the incretin effect is markedly reduced (5), partly because the insulinotropic effect of GIP is essentially lost, whereas pharmacological doses of GLP-1 still stimulate insulin secretion substantially (6). GLP-1 also suppresses glucagon and slows gastric emptying (3,7).…”