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DPP-4 inhibitors and GLP-1. Inhibitors of dipeptidyl peptidase 4 (DPP-4 inhibitors or gliptins) are a class of oral hypoglycemics that block the enzyme dipeptidyl peptidase-4 (DPP-4). They can be used to treat diabetes mellitus type 2. The first agent of the class – sitagliptin – was approved by the FDA in 2006. [1]
With nearly half of Americans saying weight loss is a goal for them, it’s no wonder that interest in GLP-1 medications has been on the rise. GLP-1 (short for glucagon-like peptide-1) medications ...
Another class of anti-diabetes drugs, DPP-4 inhibitors, work by reducing the breakdown of endogenous GLP-1, and are generally considered less potent than GLP-1 agonists. [3] Some of the metabolic effects of GLP-1 agonists in rodents are mediated via increased synthesis of fibroblast growth factor 21 . Pharmaceutical companies have developed ...
Serious side effects may include angioedema, pancreatitis, joint pain. [10] [8] Use in pregnancy and breastfeeding is not recommended. [10] Linagliptin is a dipeptidyl peptidase-4 inhibitor [8] that works by increasing the production of insulin and decreasing the production of glucagon by the pancreas. [8]
To overcome this, GLP-1 receptor agonists and DPP-4 inhibitors have been developed to increase GLP-1 activity. As opposed to common treatment agents such as insulin and sulphonylureas, GLP-1-based treatment has been associated with weight loss and a lower risk of hypoglycemia, two important considerations for patients with type 2 diabetes.
GLP-1 analogs resulted in weight loss and had more gastrointestinal side-effects, while in general dipeptidyl peptidase-4 (DPP-4) inhibitors were weight-neutral and are associated with increased risk for infection and headache. Both classes appear to present an alternative to other antidiabetic drugs.
A 2018 review found that SGLT2 inhibitors and GLP-1 agonists, but not DPP-4 inhibitors, were associated with lower mortality than placebo or no treatment. [129] Rosiglitazone , a thiazolidinedione, has not been found to improve long-term outcomes even though it improves blood sugar levels. [ 130 ]
Most patients taking GLP-1 drugs for weight management didn’t stay on their prescribed treatment for the minimum 12 weeks, meaning they were unlikely to attain clinically meaningful weight loss.