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Dipeptidyl peptidase-4 inhibitor

October 11, 2019


Inhibitors of dipeptidyl peptidase 4,
also DPP-4 inhibitors or gliptins, are a class of oral hypoglycemics that block
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. Glucagon increases blood glucose levels,
and DPP-4 inhibitors reduce glucagon and blood glucose levels. The mechanism of
DPP-4 inhibitors is to increase incretin levels, which inhibit glucagon release,
which in turn increases insulin secretion, decreases gastric emptying,
and decreases blood glucose levels. A recent meta analysis found no
favorable or harmful effect of DPPIV inhibitors on all-cause mortality,
cardiovascular mortality, or stroke, but a marginally statistically significant
increase in heart failure. Examples
Drugs belonging to this class are : Sitagliptin,
Vildagliptin, Saxagliptin,
Linagliptin, Anagliptin
Teneligliptin Alogliptin
Trelagliptin, approved for use in Japan in 2015
Gemigliptin Dutogliptin, Phase III
Omarigliptin Other chemicals which inhibit DPP4
include: Berberine, the common herbal dietary
supplement, too inhibits dipeptidyl peptidase-4, which at least partly
explains its antihyperglycemic activity. Lupeol, found in mango, red alder, and
dandelion coffee. Adverse effects
Adverse effects, including nasopharyngitis, headache, nausea, heart
failure, hypersensitivity and skin reactions, have been observed in
clinical studies. They may cause severe joint pain.
In response to a report of precancerous changes in the pancreases of rats and
organ donors treated with the DPP IV inhibitor sitagliptin, the United States
FDA and the European Medicines Agency each undertook independent reviews of
all clinical and preclinical data related to the possible association of
DPP-IV inhibitors with pancreatic cancer. In a joint letter to the New
England Journal of Medicines, the agencies stated that they had not yet
reached a final conclusion regarding a possible causative relationship.
A 2014 meta analysis found no evidence for increased pancreatic cancer risk in
people treated with DPP IV inhibitors, but owing to the modest amount of data
available, was not able to completely exclude possible risk.
See also Development of dipeptidyl peptidase-4
inhibitors References

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