Physiology, pharmacology and prospects for dipeptidilpeptidase-4 inhibitors use

Modern requirements for the treatment of type 2 diabetes mellitus (DM2) include not only achieving a glycemic control, but also reducing the risk of developing cardiovascular complications. Dipeptidyl peptidase 4 (DPP-4) inhibitors are inferior in the effectiveness to some other actively developing...

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Main Authors: D. V. Kurkin, D. A. Bakulin, E. I. Morkovin, A. V. Strygin, Yu. V. Gorbunova, E. V. Volotova, I. E. Makarenko, V. B. Saparova, R. V. Drai, V. I. Petrov
Format: Article
Language:Russian
Published: Volgograd State Medical University, Pyatigorsk Medical and Pharmaceutical Institute 2023-05-01
Series:Фармация и фармакология (Пятигорск)
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Online Access:https://www.pharmpharm.ru/jour/article/view/1257
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author D. V. Kurkin
D. A. Bakulin
E. I. Morkovin
A. V. Strygin
Yu. V. Gorbunova
E. V. Volotova
I. E. Makarenko
V. B. Saparova
R. V. Drai
V. I. Petrov
author_facet D. V. Kurkin
D. A. Bakulin
E. I. Morkovin
A. V. Strygin
Yu. V. Gorbunova
E. V. Volotova
I. E. Makarenko
V. B. Saparova
R. V. Drai
V. I. Petrov
author_sort D. V. Kurkin
collection DOAJ
description Modern requirements for the treatment of type 2 diabetes mellitus (DM2) include not only achieving a glycemic control, but also reducing the risk of developing cardiovascular complications. Dipeptidyl peptidase 4 (DPP-4) inhibitors are inferior in the effectiveness to some other actively developing groups of hypoglycemic drugs (SGLT2 inhibitors and GLP-1 receptor agonists); however, they seem relevant at the present time.The aim of the study is to analyze the literature data on the therapeutic potential and results of the of DPP-4 inhibitors research.Materials and methods. When searching for the review article materials, the abstracting databases of PubMed, Google Scholar and e-Library were used. The search was carried out on the publications for the period from 2006 to 2022, using the following keywords: DPP-4 inhibitors; glucagonlike peptide-1 (GLP-1); glucose-dependent insulinotropic peptide (GIP); sitagliptin, and other drugs.Results. DPP-4 belongs to the serine proteases family and is involved in the degradation of various chemokines and peptide hormones, including incretins secreted by intestinal L- and K-cells – GLP-1 and GIP. They regulate a postprandial insulin secretion and a β-cell function, modulate a fasting and postprandial glucagon secretion, regulate the eating behavior and have many pleiotropic (immunomodulatory, anti-inflammatory, antifibrotic, etc.) effects. DPP-4 inhibitors reduce an enzyme activity by 70–90%, increasing plasma incretin levels by 2–4 times and have been used to treat DM2 since 2006. Now there are 13 DPP-4 inhibitors on the market in different countries, differing primarily in pharmacokinetic parameters. They are actively used in the combination therapy for type 2 diabetes, increasing the glycemic control effectiveness without increasing the risk of hypoglycemia. The evidence is emerging about the therapeutic potential of DPP-4 inhibitors in COVID-19.Conclusion. A peroral form, an ability to create effective combinations with other hypoglycemic drugs without increasing the risk of hypoglycemia, the pleiotropic effects of DPP-4 inhibitors, make this group relevant at the present time.
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spelling doaj-art-f0fe50a3b67f4dd0bc0505b700df99352025-08-20T02:55:58ZrusVolgograd State Medical University, Pyatigorsk Medical and Pharmaceutical InstituteФармация и фармакология (Пятигорск)2307-92662413-22412023-05-01111194710.19163/2307-9266-2023-11-1-19-47469Physiology, pharmacology and prospects for dipeptidilpeptidase-4 inhibitors useD. V. Kurkin0D. A. Bakulin1E. I. Morkovin2A. V. Strygin3Yu. V. Gorbunova4E. V. Volotova5I. E. Makarenko6V. B. Saparova7R. V. Drai8V. I. Petrov9Volgograd State Medical UniversityVolgograd State Medical UniversityVolgograd State Medical UniversityVolgograd State Medical UniversityVolgograd State Medical UniversityVolgograd State Medical University1. Moscow State Medical and Dental University named after A.I. Evdokimov 2. Farm-Holding,1. Moscow State Medical and Dental University named after A.I. Evdokimov 2. Farm-Holding,Farm-HoldingVolgograd State Medical UniversityModern requirements for the treatment of type 2 diabetes mellitus (DM2) include not only achieving a glycemic control, but also reducing the risk of developing cardiovascular complications. Dipeptidyl peptidase 4 (DPP-4) inhibitors are inferior in the effectiveness to some other actively developing groups of hypoglycemic drugs (SGLT2 inhibitors and GLP-1 receptor agonists); however, they seem relevant at the present time.The aim of the study is to analyze the literature data on the therapeutic potential and results of the of DPP-4 inhibitors research.Materials and methods. When searching for the review article materials, the abstracting databases of PubMed, Google Scholar and e-Library were used. The search was carried out on the publications for the period from 2006 to 2022, using the following keywords: DPP-4 inhibitors; glucagonlike peptide-1 (GLP-1); glucose-dependent insulinotropic peptide (GIP); sitagliptin, and other drugs.Results. DPP-4 belongs to the serine proteases family and is involved in the degradation of various chemokines and peptide hormones, including incretins secreted by intestinal L- and K-cells – GLP-1 and GIP. They regulate a postprandial insulin secretion and a β-cell function, modulate a fasting and postprandial glucagon secretion, regulate the eating behavior and have many pleiotropic (immunomodulatory, anti-inflammatory, antifibrotic, etc.) effects. DPP-4 inhibitors reduce an enzyme activity by 70–90%, increasing plasma incretin levels by 2–4 times and have been used to treat DM2 since 2006. Now there are 13 DPP-4 inhibitors on the market in different countries, differing primarily in pharmacokinetic parameters. They are actively used in the combination therapy for type 2 diabetes, increasing the glycemic control effectiveness without increasing the risk of hypoglycemia. The evidence is emerging about the therapeutic potential of DPP-4 inhibitors in COVID-19.Conclusion. A peroral form, an ability to create effective combinations with other hypoglycemic drugs without increasing the risk of hypoglycemia, the pleiotropic effects of DPP-4 inhibitors, make this group relevant at the present time.https://www.pharmpharm.ru/jour/article/view/1257diabetes mellitusdipeptidyl peptidase 4glucagonlike peptide-1glucose-dependent insulinotropic peptidesitagliptincovid-19
spellingShingle D. V. Kurkin
D. A. Bakulin
E. I. Morkovin
A. V. Strygin
Yu. V. Gorbunova
E. V. Volotova
I. E. Makarenko
V. B. Saparova
R. V. Drai
V. I. Petrov
Physiology, pharmacology and prospects for dipeptidilpeptidase-4 inhibitors use
Фармация и фармакология (Пятигорск)
diabetes mellitus
dipeptidyl peptidase 4
glucagonlike peptide-1
glucose-dependent insulinotropic peptide
sitagliptin
covid-19
title Physiology, pharmacology and prospects for dipeptidilpeptidase-4 inhibitors use
title_full Physiology, pharmacology and prospects for dipeptidilpeptidase-4 inhibitors use
title_fullStr Physiology, pharmacology and prospects for dipeptidilpeptidase-4 inhibitors use
title_full_unstemmed Physiology, pharmacology and prospects for dipeptidilpeptidase-4 inhibitors use
title_short Physiology, pharmacology and prospects for dipeptidilpeptidase-4 inhibitors use
title_sort physiology pharmacology and prospects for dipeptidilpeptidase 4 inhibitors use
topic diabetes mellitus
dipeptidyl peptidase 4
glucagonlike peptide-1
glucose-dependent insulinotropic peptide
sitagliptin
covid-19
url https://www.pharmpharm.ru/jour/article/view/1257
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