Dipeptidyl peptidase-4 inhibitor: Difference between revisions

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{{Short description|Enzyme blocker and diabetes treatment drug}}
{{Short description|Enzyme blocker and diabetes treatment drug}}
[[Image:Incretins and DPP 4 inhibitors.svg|thumb|300px|right|DPP-4 inhibitors and GLP-1]]
[[Image:Incretins and DPP 4 inhibitors.svg|thumb|300px|right|DPP-4 inhibitors and GLP-1]]


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'''Inhibitors of dipeptidyl peptidase 4''' ('''DPP-4 inhibitors''' or '''gliptins''') are a class of [[oral hypoglycemic]]s that [[Enzyme inhibitors|block]] the [[enzyme]] [[dipeptidyl peptidase-4]] (DPP-4). They can be used to treat [[diabetes mellitus type 2]].
'''Inhibitors of dipeptidyl peptidase 4''' ('''DPP-4 inhibitors''' or '''gliptins''') are a class of [[oral hypoglycemic]]s that [[Enzyme inhibitors|block]] the [[enzyme]] [[dipeptidyl peptidase-4]] (DPP-4). They can be used to treat [[diabetes mellitus type 2]].


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The first agent of the class – [[sitagliptin]] – was approved by the [[U.S. Food and Drug Administration|FDA]] in 2006.
The first agent of the class – [[sitagliptin]] – was approved by the [[U.S. Food and Drug Administration|FDA]] in 2006.


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[[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 ([[GLP-1]] and [[gastric inhibitory polypeptide|GIP]]), which inhibit [[glucagon]] release, which in turn increases [[insulin]] secretion, decreases gastric emptying, and decreases [[blood glucose]] levels.
[[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 ([[GLP-1]] and [[gastric inhibitory polypeptide|GIP]]), which inhibit [[glucagon]] release, which in turn increases [[insulin]] secretion, decreases gastric emptying, and decreases [[blood glucose]] levels.


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A 2018 [[meta-analysis]] found no favorable effect of DPP-4 inhibitors on all-cause mortality, cardiovascular mortality, [[myocardial infarction]] or [[stroke]] in patients with type 2 diabetes.
A 2018 [[meta-analysis]] found no favorable effect of DPP-4 inhibitors on all-cause mortality, cardiovascular mortality, [[myocardial infarction]] or [[stroke]] in patients with type 2 diabetes.


==Examples==
==Examples== <!--T:6-->
Drugs belonging to this class are:
Drugs belonging to this class are:
* [[Sitagliptin]] (FDA approved 2006, marketed by [[Merck & Co.]] as [[Januvia]])
* [[Sitagliptin]] (FDA approved 2006, marketed by [[Merck & Co.]] as [[Januvia]])
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* [[Prusogliptin]]
* [[Prusogliptin]]


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Other chemicals which may inhibit DPP-4 include:
Other chemicals which may inhibit DPP-4 include:
* [[Berberine]], an [[alkaloid]] found in plants of the genus ''[[Berberis]]'', inhibits dipeptidyl peptidase-4 which may at least partly explains its antihyperglycemic activity.
* [[Berberine]], an [[alkaloid]] found in plants of the genus ''[[Berberis]]'', inhibits dipeptidyl peptidase-4 which may at least partly explains its antihyperglycemic activity.


==Adverse effects==
==Adverse effects== <!--T:8-->
In those already taking [[sulphonylurea]]s, there is an increased risk of [[hypoglycemia|low blood sugar]] when taking a medicine in the DPP-4 drug class.
In those already taking [[sulphonylurea]]s, there is an increased risk of [[hypoglycemia|low blood sugar]] when taking a medicine in the DPP-4 drug class.


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Adverse effects include nasopharyngitis, [[headache]], [[nausea]], [[heart failure]], hypersensitivity and skin reactions.
Adverse effects include nasopharyngitis, [[headache]], [[nausea]], [[heart failure]], hypersensitivity and skin reactions.


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The U.S. Food and Drug Administration (FDA) is warning that the type 2 diabetes medicines like [[sitagliptin]], [[saxagliptin]], [[linagliptin]], and [[alogliptin]] may cause joint pain that can be severe and disabling. FDA has added a new Warning and Precaution about this risk to the labels of all medicines in this drug class, called dipeptidyl peptidase-4 (DPP-4) inhibitors. However, studies assessing risk of rheumatoid arthritis among DPP-4 inhibitor users have been inconclusive.
The U.S. Food and Drug Administration (FDA) is warning that the type 2 diabetes medicines like [[sitagliptin]], [[saxagliptin]], [[linagliptin]], and [[alogliptin]] may cause joint pain that can be severe and disabling. FDA has added a new Warning and Precaution about this risk to the labels of all medicines in this drug class, called dipeptidyl peptidase-4 (DPP-4) inhibitors. However, studies assessing risk of rheumatoid arthritis among DPP-4 inhibitor users have been inconclusive.


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A 2014 review found increased risk of [[heart failure]] with saxagliptin and alogliptin, prompting the FDA in 2016 to add warnings to the relevant drug labels.
A 2014 review found increased risk of [[heart failure]] with saxagliptin and alogliptin, prompting the FDA in 2016 to add warnings to the relevant drug labels.


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A 2018 meta analysis showed that use of DPP-4 inhibitors was associated with a 58% increased risk of developing acute pancreatitis compared with placebo or no treatment.
A 2018 meta analysis showed that use of DPP-4 inhibitors was associated with a 58% increased risk of developing acute pancreatitis compared with placebo or no treatment.


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A 2018 observational study suggested an elevated risk of developing inflammatory bowel disease (specifically, ulcerative colitis), reaching a peak after three to four years of use and decreasing after more than four years of use.
A 2018 observational study suggested an elevated risk of developing inflammatory bowel disease (specifically, ulcerative colitis), reaching a peak after three to four years of use and decreasing after more than four years of use.


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A 2020 Cochrane systematic review did not find enough evidence of reduction of all-cause mortality, serious adverse events, cardiovascular mortality, non-fatal [[myocardial infarction]], non-fatal [[stroke]] or [[Chronic kidney disease|end-stage renal disease]] when comparing [[metformin]] monotherapy to dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.
A 2020 Cochrane systematic review did not find enough evidence of reduction of all-cause mortality, serious adverse events, cardiovascular mortality, non-fatal [[myocardial infarction]], non-fatal [[stroke]] or [[Chronic kidney disease|end-stage renal disease]] when comparing [[metformin]] monotherapy to dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.


===Cancer===
===Cancer=== <!--T:15-->
In response to a report of precancerous changes in the pancreases of rats and organ donors treated with the DPP-4 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-4 inhibitors with pancreatic cancer. In a joint letter to the New England Journal of Medicine, the agencies stated that they had not yet reached a final conclusion regarding a possible causative relationship.
In response to a report of precancerous changes in the pancreases of rats and organ donors treated with the DPP-4 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-4 inhibitors with pancreatic cancer. In a joint letter to the New England Journal of Medicine, the agencies stated that they had not yet reached a final conclusion regarding a possible causative relationship.


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A 2014 meta-analysis found no evidence for increased [[pancreatic cancer]] risk in people treated with DPP-4 inhibitors, but owing to the modest amount of data available, was not able to completely exclude possible risk.
A 2014 meta-analysis found no evidence for increased [[pancreatic cancer]] risk in people treated with DPP-4 inhibitors, but owing to the modest amount of data available, was not able to completely exclude possible risk.


==Combination drugs==
==Combination drugs== <!--T:17-->
Some DPP-4 inhibitor drugs have received approval from the FDA to be used with [[metformin]] concomitantly with additive effect to increase the level of glucagon-like peptide 1 (GLP-1) which also decreases [[hepatic]] [[gluconeogenesis|glucose production]].
Some DPP-4 inhibitor drugs have received approval from the FDA to be used with [[metformin]] concomitantly with additive effect to increase the level of glucagon-like peptide 1 (GLP-1) which also decreases [[hepatic]] [[gluconeogenesis|glucose production]].


== See also ==
== See also == <!--T:18-->
* [[Development of dipeptidyl peptidase-4 inhibitors]]
* [[Development of dipeptidyl peptidase-4 inhibitors]]




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{{Oral hypoglycemics}}
{{Oral hypoglycemics}}
{{Enzyme inhibition}}
{{Enzyme inhibition}}


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{{二次利用|date=1 February 2024}}
{{二次利用|date=1 February 2024}}
{{DEFAULTSORT:Dipeptidyl Peptidase-4 Inhibitor}}
{{DEFAULTSORT:Dipeptidyl Peptidase-4 Inhibitor}}
[[Category:Dipeptidyl peptidase-4 inhibitors| ]]
[[Category:Dipeptidyl peptidase-4 inhibitors| ]]
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Latest revision as of 17:34, 12 March 2024

Other languages:
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.

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 (GLP-1 and GIP), which inhibit glucagon release, which in turn increases insulin secretion, decreases gastric emptying, and decreases blood glucose levels.

A 2018 meta-analysis found no favorable effect of DPP-4 inhibitors on all-cause mortality, cardiovascular mortality, myocardial infarction or stroke in patients with type 2 diabetes.

Examples

Drugs belonging to this class are:

Other chemicals which may inhibit DPP-4 include:

  • Berberine, an alkaloid found in plants of the genus Berberis, inhibits dipeptidyl peptidase-4 which may at least partly explains its antihyperglycemic activity.

Adverse effects

In those already taking sulphonylureas, there is an increased risk of low blood sugar when taking a medicine in the DPP-4 drug class.

Adverse effects include nasopharyngitis, headache, nausea, heart failure, hypersensitivity and skin reactions.

The U.S. Food and Drug Administration (FDA) is warning that the type 2 diabetes medicines like sitagliptin, saxagliptin, linagliptin, and alogliptin may cause joint pain that can be severe and disabling. FDA has added a new Warning and Precaution about this risk to the labels of all medicines in this drug class, called dipeptidyl peptidase-4 (DPP-4) inhibitors. However, studies assessing risk of rheumatoid arthritis among DPP-4 inhibitor users have been inconclusive.

A 2014 review found increased risk of heart failure with saxagliptin and alogliptin, prompting the FDA in 2016 to add warnings to the relevant drug labels.

A 2018 meta analysis showed that use of DPP-4 inhibitors was associated with a 58% increased risk of developing acute pancreatitis compared with placebo or no treatment.

A 2018 observational study suggested an elevated risk of developing inflammatory bowel disease (specifically, ulcerative colitis), reaching a peak after three to four years of use and decreasing after more than four years of use.

A 2020 Cochrane systematic review did not find enough evidence of reduction of all-cause mortality, serious adverse events, cardiovascular mortality, non-fatal myocardial infarction, non-fatal stroke or end-stage renal disease when comparing metformin monotherapy to dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.

Cancer

In response to a report of precancerous changes in the pancreases of rats and organ donors treated with the DPP-4 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-4 inhibitors with pancreatic cancer. In a joint letter to the New England Journal of Medicine, 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-4 inhibitors, but owing to the modest amount of data available, was not able to completely exclude possible risk.

Combination drugs

Some DPP-4 inhibitor drugs have received approval from the FDA to be used with metformin concomitantly with additive effect to increase the level of glucagon-like peptide 1 (GLP-1) which also decreases hepatic glucose production.

See also


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