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DPP-4 inhibitors.

Ahrén, Bo LU (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)
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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
2020-12-29 04:13:08
@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},
  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},
}