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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]
Serious side effects may include angioedema, low blood sugar, kidney problems, pancreatitis, and joint pain. [8] Whether use in pregnancy or breastfeeding is safe is unclear. [10] It is in the dipeptidyl peptidase-4 (DPP-4) inhibitor class and works by increasing the production of insulin and decreasing the production of glucagon by the ...
Dipeptidyl peptidase-4 (DPP4 or DPPIV), also known as adenosine deaminase complexing protein 2 or CD26 (cluster of differentiation 26) is a protein that, in humans, is encoded by the DPP4 gene. [5] DPP4 is related to FAP , DPP8 , and DPP9 .
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.
Gemigliptin , sold under the brand name Zemiglo, is an oral anti-hyperglycemic agent (anti-diabetic drug) of the dipeptidyl peptidase-4 inhibitor (DPP-4 inhibitor) class of drugs. [1] Glucose lowering effects of DPP-4 inhibitors are mainly mediated by GLP-1 and gastric inhibitory polypeptide (GIP) incretin hormones which are inactivated by DPP-4.
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.
Once secreted, GLP-1 is extremely susceptible to the catalytic activity of the proteolytic enzyme dipeptidyl peptidase-4 (DPP-4). Specifically, DPP-4 cleaves the peptide bond between Ala 8-Glu 9 resulting in the abundant GLP-1 (9–36) amide constituting 60–80% of total GLP-1 in circulation. DPP-4 is widely expressed in multiple tissues and ...
Native GLP-1 is a peptide hormone with a half-life of two minutes because it is rapidly cleared by the enzyme dipeptidyl peptidase-4. [29] As a result, different GLP-1 agonist drugs are modified in various ways to extend the half-life, resulting in drugs that can be dosed multiple times per day, daily, weekly, or less often. [29]