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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]
However, compared to participants taking dipeptidyl peptidase-4 inhibitors (DPP4is), GLP-1RAs were associated with a slight decrease in depression risk. ... In both comparison groups, the average ...
One of the first reported DPP-4 inhibitor was P32/98 from Merck. It used thiazolidide as the P1-substitute and was the first DPP-4 inhibitor that showed effects in both animals and humans but it was not developed to a market drug due to side effects. Another old inhibitor is DPP-728 from Novartis, where 2-cyanopyrrolidine is used as the P1 ...
However, weight gain and/or hypoglycemia have been observed when dipeptidyl peptidase-4 inhibitors were used with sulfonylureas; effects on long-term health and morbidity rates are still unknown. [42] DPP-4 inhibitors increase blood concentration of the incretin GLP-1 by inhibiting its degradation by DPP-4. Examples are:
Alogliptin, sold under the brand names Nesina and Vipidia, [2] [3] is an oral anti-diabetic drug in the DPP-4 inhibitor (gliptin) class. [4] Like other members of the gliptin class, it causes little or no weight gain, exhibits relatively little risk of hypoglycemia, and has relatively modest glucose-lowering activity. [1]
Gemigliptin is a competitive, reversible DPP-4 inhibitor (Ki = 7.25 ± 0.67 nM) with excellent selectivity over other critical human proteases such as DPP-2, DPP-8, DPP-9, elastase, trypsin, urokinase and cathepsin G. The kinetics of DPP-4 inhibition by gemigliptin was characterized by a fast association and a slow dissociation rate compared to ...
Being resistant to dipeptidyl peptidase-4 (DPP-4), [5] the enzyme that breaks down GLP-1, albiglutide has a biological half-life of five (four to seven) days, which is considerably longer than the older GLP-1 analogs exenatide and liraglutide.
A class of oral hypoglycemics called dipeptidyl peptidase-4 inhibitors works by inhibiting the action of this enzyme, thereby prolonging incretin effect in vivo. [18] Middle East respiratory syndrome coronavirus has been found to bind to DPP4. It is found on the surface of cells in the airways (such as the lungs) and kidneys.