DPP-4 inhibitors.
(2007) In Baillière's Best Practice & Research in Clinical Endocrinology & Metabolism 21(4). p.517-533- Abstract
- Inhibition of dipeptidyl peptidase 4 (DPP-4) is a novel treatment for type-2 diabetes. DPP-4 inhibition prevents the inactivation of glucagon-like peptide 1 (GLP-1), which increases levels of active GLP-1. This increases insulin secretion and reduces glucagon secretion, thereby lowering glucose levels. Several DPP-4 inhibitors are in clinical development. Most experience so far has been with sitagliptin (Merck; approved by the FDA) and vildagliptin (Novartis; filed). These are orally active compounds with a long duration, allowing once-daily administration. Both sitagliptin and vildagliptin improve metabolic control in type-2 diabetes, both in monotherapy and in combination with metformin and thiazolidinediones. A reduction in HbA(1c) of... (More)
- Inhibition of dipeptidyl peptidase 4 (DPP-4) is a novel treatment for type-2 diabetes. DPP-4 inhibition prevents the inactivation of glucagon-like peptide 1 (GLP-1), which increases levels of active GLP-1. This increases insulin secretion and reduces glucagon secretion, thereby lowering glucose levels. Several DPP-4 inhibitors are in clinical development. Most experience so far has been with sitagliptin (Merck; approved by the FDA) and vildagliptin (Novartis; filed). These are orally active compounds with a long duration, allowing once-daily administration. Both sitagliptin and vildagliptin improve metabolic control in type-2 diabetes, both in monotherapy and in combination with metformin and thiazolidinediones. A reduction in HbA(1c) of approximately 1% is seen in studies of DPP-4 inhibition of up to 52 weeks' duration. DPP-4 inhibition is safe and well tolerated, the risk of hypoglycaemia is minimal, and DPP-4 inhibition is body-weight neutral. DPP-4 inhibition is suggested to be a first-line treatment of type-2 diabetes, particularly in its early stages in combination with metformin. However, the durability and long-term safety of DPP-4 inhibition remain to be established. (Less)
Please use this url to cite or link to this publication:
https://lup.lub.lu.se/record/1035713
- author
- Ahrén, Bo LU
- organization
- publishing date
- 2007
- type
- Contribution to journal
- publication status
- published
- subject
- keywords
- Adamantane/adverse effects Adamantane/analogs & derivatives Adamantane/therapeutic use Animals Antigens, CD26/antagonists & inhibitors* Body Weight/drug effects Diabetes Mellitus, Type 2/drug therapy* Drug Therapy, Combination Glucagon/secretion Glucagon-Like Peptide 1/antagonists & inhibitors* Glucagon-Like Peptide 1/physiology Humans Hypoglycemia/chemically induced Hypoglycemic Agents/therapeutic use* Insulin/secretion Insulin/therapeutic use Lipid Metabolism/drug effects Metformin/therapeutic use Nitriles/adverse effects Nitriles/therapeutic use Protease Inhibitors/therapeutic use* Pyrazines/adverse effects Pyrazines/therapeutic use Pyrrolidines/adverse effects Pyrrolidines/therapeutic use Substrate Specificity Thiazolidinediones/therapeutic use Triazoles/adverse effects Triazoles/therapeutic use
- in
- Baillière's Best Practice & Research in Clinical Endocrinology & Metabolism
- volume
- 21
- issue
- 4
- pages
- 517 - 533
- publisher
- Bailliere Tindall Ltd
- external identifiers
-
- pmid:18054733
- wos:000252142600003
- scopus:36549009003
- pmid:18054733
- ISSN
- 1521-690X
- DOI
- 10.1016/j.beem.2007.07.005
- language
- English
- LU publication?
- yes
- id
- 8a223fcc-0adf-46d9-bdc6-4d6fe7110e5e (old id 1035713)
- alternative location
- http://www.ncbi.nlm.nih.gov/pubmed/18054733?dopt=Abstract
- date added to LUP
- 2016-04-04 09:37:54
- date last changed
- 2024-02-11 14:48:09
@article{8a223fcc-0adf-46d9-bdc6-4d6fe7110e5e,
abstract = {{Inhibition of dipeptidyl peptidase 4 (DPP-4) is a novel treatment for type-2 diabetes. DPP-4 inhibition prevents the inactivation of glucagon-like peptide 1 (GLP-1), which increases levels of active GLP-1. This increases insulin secretion and reduces glucagon secretion, thereby lowering glucose levels. Several DPP-4 inhibitors are in clinical development. Most experience so far has been with sitagliptin (Merck; approved by the FDA) and vildagliptin (Novartis; filed). These are orally active compounds with a long duration, allowing once-daily administration. Both sitagliptin and vildagliptin improve metabolic control in type-2 diabetes, both in monotherapy and in combination with metformin and thiazolidinediones. A reduction in HbA(1c) of approximately 1% is seen in studies of DPP-4 inhibition of up to 52 weeks' duration. DPP-4 inhibition is safe and well tolerated, the risk of hypoglycaemia is minimal, and DPP-4 inhibition is body-weight neutral. DPP-4 inhibition is suggested to be a first-line treatment of type-2 diabetes, particularly in its early stages in combination with metformin. However, the durability and long-term safety of DPP-4 inhibition remain to be established.}},
author = {{Ahrén, Bo}},
issn = {{1521-690X}},
keywords = {{Adamantane/adverse effects
Adamantane/analogs & derivatives
Adamantane/therapeutic use
Animals
Antigens; CD26/antagonists & inhibitors*
Body Weight/drug effects
Diabetes Mellitus; Type 2/drug therapy*
Drug Therapy; Combination
Glucagon/secretion
Glucagon-Like Peptide 1/antagonists & inhibitors*
Glucagon-Like Peptide 1/physiology
Humans
Hypoglycemia/chemically induced
Hypoglycemic Agents/therapeutic use*
Insulin/secretion
Insulin/therapeutic use
Lipid Metabolism/drug effects
Metformin/therapeutic use
Nitriles/adverse effects
Nitriles/therapeutic use
Protease Inhibitors/therapeutic use*
Pyrazines/adverse effects
Pyrazines/therapeutic use
Pyrrolidines/adverse effects
Pyrrolidines/therapeutic use
Substrate Specificity
Thiazolidinediones/therapeutic use
Triazoles/adverse effects
Triazoles/therapeutic use}},
language = {{eng}},
number = {{4}},
pages = {{517--533}},
publisher = {{Bailliere Tindall Ltd}},
series = {{Baillière's Best Practice & Research in Clinical Endocrinology & Metabolism}},
title = {{DPP-4 inhibitors.}},
url = {{http://dx.doi.org/10.1016/j.beem.2007.07.005}},
doi = {{10.1016/j.beem.2007.07.005}},
volume = {{21}},
year = {{2007}},
}