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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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@misc{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},
  keyword      = {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    = {ARRAY(0xb869820)},
  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},
  volume       = {21},
  year         = {2007},
}