Abstract
Introduction: Recently, incretin-based therapy was introduced for the treatment of type 2 diabetes (T2D). In particular, dipeptidyl peptidase-4 inhibitors (DPP-4i) (sitagliptin, vildagliptin, saxagliptin, linagliptin and alogliptin) play an increasing role in the management of T2D.Areas covered: An extensive literature search was performed to analyze the pharmacological characteristics of DPP-4i and their clinical implications.Expert opinion: DPP-4i present significant pharmacokinetic differences. They also differ in chemical structure, in the interaction with distinct subsites of the enzyme and in different levels of selectivity and potency of enzyme inhibition. Moreover, disparities in the effects on glycated hemoglobin, glucagon-like peptide-1 and glucagon levels and on glucose variability have been observed. However, indirect comparisons indicate that all DPP-4i have a similar safety and efficacy profiles. DPP-4i are preferred in overweight/obese and elderly patients because of the advantages of minimal or no influence on weight gain and low risk of hypoglycemia. For the same reasons, DPP-4i can be safely combined with insulin. However, currently cardiovascular outcomes related to DPP-4i are widely debated and the available evidence is controversial. Today, long-term studies are still in progress and upcoming results will allow us to better define the strengths and limits of this therapeutic class.
| Original language | English |
|---|---|
| Journal | Expert Opinion on Drug Safety |
| Volume | 13 |
| Issue number | SUPPL. 1 |
| DOIs | |
| Publication status | Published - 2014 |
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Keywords
- Dipeptidyl peptidase-4 inhibitors
- Glucose variability
- Pharmacodynamics
- Pharmacokinetics
- Pharmacology
- Type 2 diabetes
ASJC Scopus subject areas
- Pharmacology (medical)
- Medicine(all)
Cite this
DPP-4 inhibitors : Pharmacological differences and their clinical implications. / Ceriello, Antonio; Sportiello, Liberata; Rafaniello, Concetta; Rossi, Francesco.
In: Expert Opinion on Drug Safety, Vol. 13, No. SUPPL. 1, 2014.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - DPP-4 inhibitors
T2 - Pharmacological differences and their clinical implications
AU - Ceriello, Antonio
AU - Sportiello, Liberata
AU - Rafaniello, Concetta
AU - Rossi, Francesco
PY - 2014
Y1 - 2014
N2 - Introduction: Recently, incretin-based therapy was introduced for the treatment of type 2 diabetes (T2D). In particular, dipeptidyl peptidase-4 inhibitors (DPP-4i) (sitagliptin, vildagliptin, saxagliptin, linagliptin and alogliptin) play an increasing role in the management of T2D.Areas covered: An extensive literature search was performed to analyze the pharmacological characteristics of DPP-4i and their clinical implications.Expert opinion: DPP-4i present significant pharmacokinetic differences. They also differ in chemical structure, in the interaction with distinct subsites of the enzyme and in different levels of selectivity and potency of enzyme inhibition. Moreover, disparities in the effects on glycated hemoglobin, glucagon-like peptide-1 and glucagon levels and on glucose variability have been observed. However, indirect comparisons indicate that all DPP-4i have a similar safety and efficacy profiles. DPP-4i are preferred in overweight/obese and elderly patients because of the advantages of minimal or no influence on weight gain and low risk of hypoglycemia. For the same reasons, DPP-4i can be safely combined with insulin. However, currently cardiovascular outcomes related to DPP-4i are widely debated and the available evidence is controversial. Today, long-term studies are still in progress and upcoming results will allow us to better define the strengths and limits of this therapeutic class.
AB - Introduction: Recently, incretin-based therapy was introduced for the treatment of type 2 diabetes (T2D). In particular, dipeptidyl peptidase-4 inhibitors (DPP-4i) (sitagliptin, vildagliptin, saxagliptin, linagliptin and alogliptin) play an increasing role in the management of T2D.Areas covered: An extensive literature search was performed to analyze the pharmacological characteristics of DPP-4i and their clinical implications.Expert opinion: DPP-4i present significant pharmacokinetic differences. They also differ in chemical structure, in the interaction with distinct subsites of the enzyme and in different levels of selectivity and potency of enzyme inhibition. Moreover, disparities in the effects on glycated hemoglobin, glucagon-like peptide-1 and glucagon levels and on glucose variability have been observed. However, indirect comparisons indicate that all DPP-4i have a similar safety and efficacy profiles. DPP-4i are preferred in overweight/obese and elderly patients because of the advantages of minimal or no influence on weight gain and low risk of hypoglycemia. For the same reasons, DPP-4i can be safely combined with insulin. However, currently cardiovascular outcomes related to DPP-4i are widely debated and the available evidence is controversial. Today, long-term studies are still in progress and upcoming results will allow us to better define the strengths and limits of this therapeutic class.
KW - Dipeptidyl peptidase-4 inhibitors
KW - Glucose variability
KW - Pharmacodynamics
KW - Pharmacokinetics
KW - Pharmacology
KW - Type 2 diabetes
UR - http://www.scopus.com/inward/record.url?scp=84907030397&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84907030397&partnerID=8YFLogxK
U2 - 10.1517/14740338.2014.944862
DO - 10.1517/14740338.2014.944862
M3 - Article
C2 - 25171159
AN - SCOPUS:84907030397
VL - 13
JO - Expert Opinion on Drug Safety
JF - Expert Opinion on Drug Safety
SN - 1474-0338
IS - SUPPL. 1
ER -