Dipeptidyl peptidase 4 inhibitors in the treatment of type 2 diabetes mellitus
Publikation: Bidrag til tidsskrift › Review › Forskning › fagfællebedømt
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Dipeptidyl peptidase 4 inhibitors in the treatment of type 2 diabetes mellitus. / Deacon, Carolyn F.
I: Nature Reviews Endocrinology, Bind 16, Nr. 11, 2020, s. 642-653.Publikation: Bidrag til tidsskrift › Review › Forskning › fagfællebedømt
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TY - JOUR
T1 - Dipeptidyl peptidase 4 inhibitors in the treatment of type 2 diabetes mellitus
AU - Deacon, Carolyn F.
PY - 2020
Y1 - 2020
N2 - Dipeptidyl peptidase 4 inhibitors are now widely used in the treatment of patients with type 2 diabetes mellitus. This Review discusses the use of the five main dipeptidyl peptidase 4 inhibitors for this purpose, highlighting their benefits and risks.Dipeptidyl peptidase 4 inhibitors (DPP4i) have been available for treating type 2 diabetes mellitus since 2006. Although they are a diverse group, DPP4i are all small, orally available molecules that interact with the catalytic site of DPP4 without disturbing any of its other known functions, including its effects on the immune system. DPP4i have no intrinsic glucose-lowering activity, so their efficacy as anti-diabetic agents is related directly to their ability to inhibit DPP4 activity and is mediated through the effects of the substrates they protect. Of these, the incretin hormone, glucagon-like peptide 1, is probably the most important. As the effects of glucagon-like peptide 1 are glucose-dependent, the risk of hypoglycaemia with DPP4i is low. Class effects, which are directly related to the mechanism of action, are common to all DPP4i; these include their overall good safety profile and tolerability, as well as their efficacy in improving glycaemic control, but also, potentially, a small increased risk of acute pancreatitis. Compound-specific effects are those related to their differing chemistries and/or pharmacokinetic profiles. These compound-specific effects could affect the way in which individual DPP4i are used therapeutically and potentially explain off-target adverse effects, such as hospitalization for heart failure, which is seen only with one DPP4i. Overall, DPP4i have a favourable therapeutic profile and are safe and effective in the majority of patients with type 2 diabetes mellitus.
AB - Dipeptidyl peptidase 4 inhibitors are now widely used in the treatment of patients with type 2 diabetes mellitus. This Review discusses the use of the five main dipeptidyl peptidase 4 inhibitors for this purpose, highlighting their benefits and risks.Dipeptidyl peptidase 4 inhibitors (DPP4i) have been available for treating type 2 diabetes mellitus since 2006. Although they are a diverse group, DPP4i are all small, orally available molecules that interact with the catalytic site of DPP4 without disturbing any of its other known functions, including its effects on the immune system. DPP4i have no intrinsic glucose-lowering activity, so their efficacy as anti-diabetic agents is related directly to their ability to inhibit DPP4 activity and is mediated through the effects of the substrates they protect. Of these, the incretin hormone, glucagon-like peptide 1, is probably the most important. As the effects of glucagon-like peptide 1 are glucose-dependent, the risk of hypoglycaemia with DPP4i is low. Class effects, which are directly related to the mechanism of action, are common to all DPP4i; these include their overall good safety profile and tolerability, as well as their efficacy in improving glycaemic control, but also, potentially, a small increased risk of acute pancreatitis. Compound-specific effects are those related to their differing chemistries and/or pharmacokinetic profiles. These compound-specific effects could affect the way in which individual DPP4i are used therapeutically and potentially explain off-target adverse effects, such as hospitalization for heart failure, which is seen only with one DPP4i. Overall, DPP4i have a favourable therapeutic profile and are safe and effective in the majority of patients with type 2 diabetes mellitus.
KW - GLUCAGON-LIKE PEPTIDE-1
KW - DEPENDENT INSULINOTROPIC POLYPEPTIDE
KW - INCRETIN-BASED DRUGS
KW - BETA-CELL FUNCTION
KW - IV INHIBITOR
KW - DOUBLE-BLIND
KW - DPP-4 INHIBITOR
KW - POOLED ANALYSIS
KW - RENAL IMPAIRMENT
KW - ELDERLY-PATIENTS
U2 - 10.1038/s41574-020-0399-8
DO - 10.1038/s41574-020-0399-8
M3 - Review
C2 - 32929230
VL - 16
SP - 642
EP - 653
JO - Nature Reviews Endocrinology
JF - Nature Reviews Endocrinology
SN - 1759-5029
IS - 11
ER -
ID: 251794730