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The incretin system: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes

Glucagon-like peptide 1 (GLP-1) is a gut-derived incretin hormone that stimulates insulin and suppresses glucagon secretion, inhibits gastric emptying, and reduces appetite and food intake. Therapeutic approaches for enhancing incretin action include degradation-resistant GLP-1 receptor agonists (in... Full description

Journal Title: The Lancet (British edition) 2006, Vol.368 (9548), p.1696-1705
Main Author: Drucker, Daniel J
Other Authors: Nauck, Michael A
Format: Electronic Article Electronic Article
Language: English
Subjects:
Quelle: Alma/SFX Local Collection
Publisher: London: Elsevier Ltd
ID: ISSN: 0140-6736
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recordid: cdi_proquest_journals_199067766
title: The incretin system: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes
format: Article
creator:
  • Drucker, Daniel J
  • Nauck, Michael A
subjects:
  • Adamantane - administration & dosage
  • Adamantane - adverse effects
  • Adamantane - analogs & derivatives
  • Adamantane - therapeutic use
  • Adenosine Deaminase Inhibitors
  • Analysis
  • Biological and medical sciences
  • Care and treatment
  • Clinical Trials as Topic
  • Diabetes
  • Diabetes Mellitus, Type 2 - drug therapy
  • Diabetes. Impaired glucose tolerance
  • Diagnosis
  • Dipeptidyl Peptidase 4
  • Dipeptidyl-Peptidase IV Inhibitors
  • Dosage and administration
  • Drug Administration Schedule
  • Drug therapy
  • Endocrine pancreas. Apud cells (diseases)
  • Endocrinopathies
  • Etiopathogenesis. Screening. Investigations. Target tissue resistance
  • General aspects
  • Glucagon
  • Glucagon-Like Peptide 1 - administration & dosage
  • Glucagon-Like Peptide 1 - adverse effects
  • Glucagon-Like Peptide 1 - analogs & derivatives
  • Glucagon-Like Peptide 1 - biosynthesis
  • Glucagon-Like Peptide 1 - classification
  • Glucagon-Like Peptide 1 - physiology
  • Glucagon-Like Peptide 1 - therapeutic use
  • Glucagon-Like Peptide-1 Receptor
  • Glycoproteins - antagonists & inhibitors
  • Humans
  • Hypoglycemic Agents - administration & dosage
  • Hypoglycemic Agents - adverse effects
  • Hypoglycemic Agents - therapeutic use
  • Insulin
  • Kinases
  • Liraglutide
  • Medical sciences
  • Nitriles
  • Peptides - administration & dosage
  • Peptides - adverse effects
  • Peptides - therapeutic use
  • Protease inhibitors
  • Proteins
  • Pyrazines - administration & dosage
  • Pyrazines - adverse effects
  • Pyrazines - therapeutic use
  • Pyrrolidines
  • Receptors, Glucagon - agonists
  • Rodents
  • Sitagliptin Phosphate
  • Triazoles - administration & dosage
  • Triazoles - adverse effects
  • Triazoles - therapeutic use
  • Type 2 diabetes
  • Venoms - administration & dosage
  • Venoms - adverse effects
  • Venoms - therapeutic use
ispartof: The Lancet (British edition), 2006, Vol.368 (9548), p.1696-1705
description: Glucagon-like peptide 1 (GLP-1) is a gut-derived incretin hormone that stimulates insulin and suppresses glucagon secretion, inhibits gastric emptying, and reduces appetite and food intake. Therapeutic approaches for enhancing incretin action include degradation-resistant GLP-1 receptor agonists (incretin mimetics), and inhibitors of dipeptidyl peptidase-4 (DPP-4) activity (incretin enhancers). Clinical trials with the incretin mimetic exenatide (two injections per day or long-acting release form once weekly) and liraglutide (one injection per day) show reductions in fasting and postprandial glucose concentrations, and haemoglobin A 1c (HbA 1c) (1–2%), associated with weight loss (2–5 kg). The most common adverse event associated with GLP-1 receptor agonists is mild nausea, which lessens over time. Orally administered DPP-4 inhibitors, such as sitagliptin and vildagliptin, reduce HbA 1c by 0·5–1·0%, with few adverse events and no weight gain. These new classes of antidiabetic agents, and incretin mimetics and enhancers, also expand β-cell mass in preclinical studies. However, long-term clinical studies are needed to determine the benefits of targeting the incretin axis for the treatment of type 2 diabetes.
language: eng
source: Alma/SFX Local Collection
identifier: ISSN: 0140-6736
fulltext: fulltext
issn:
  • 0140-6736
  • 1474-547X
url: Link


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descriptionGlucagon-like peptide 1 (GLP-1) is a gut-derived incretin hormone that stimulates insulin and suppresses glucagon secretion, inhibits gastric emptying, and reduces appetite and food intake. Therapeutic approaches for enhancing incretin action include degradation-resistant GLP-1 receptor agonists (incretin mimetics), and inhibitors of dipeptidyl peptidase-4 (DPP-4) activity (incretin enhancers). Clinical trials with the incretin mimetic exenatide (two injections per day or long-acting release form once weekly) and liraglutide (one injection per day) show reductions in fasting and postprandial glucose concentrations, and haemoglobin A 1c (HbA 1c) (1–2%), associated with weight loss (2–5 kg). The most common adverse event associated with GLP-1 receptor agonists is mild nausea, which lessens over time. Orally administered DPP-4 inhibitors, such as sitagliptin and vildagliptin, reduce HbA 1c by 0·5–1·0%, with few adverse events and no weight gain. These new classes of antidiabetic agents, and incretin mimetics and enhancers, also expand β-cell mass in preclinical studies. However, long-term clinical studies are needed to determine the benefits of targeting the incretin axis for the treatment of type 2 diabetes.
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descriptionGlucagon-like peptide 1 (GLP-1) is a gut-derived incretin hormone that stimulates insulin and suppresses glucagon secretion, inhibits gastric emptying, and reduces appetite and food intake. Therapeutic approaches for enhancing incretin action include degradation-resistant GLP-1 receptor agonists (incretin mimetics), and inhibitors of dipeptidyl peptidase-4 (DPP-4) activity (incretin enhancers). Clinical trials with the incretin mimetic exenatide (two injections per day or long-acting release form once weekly) and liraglutide (one injection per day) show reductions in fasting and postprandial glucose concentrations, and haemoglobin A 1c (HbA 1c) (1–2%), associated with weight loss (2–5 kg). The most common adverse event associated with GLP-1 receptor agonists is mild nausea, which lessens over time. Orally administered DPP-4 inhibitors, such as sitagliptin and vildagliptin, reduce HbA 1c by 0·5–1·0%, with few adverse events and no weight gain. These new classes of antidiabetic agents, and incretin mimetics and enhancers, also expand β-cell mass in preclinical studies. However, long-term clinical studies are needed to determine the benefits of targeting the incretin axis for the treatment of type 2 diabetes.
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1Adamantane - adverse effects
2Adamantane - analogs & derivatives
3Adamantane - therapeutic use
4Adenosine Deaminase Inhibitors
5Analysis
6Biological and medical sciences
7Care and treatment
8Clinical Trials as Topic
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10Diabetes Mellitus, Type 2 - drug therapy
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13Dipeptidyl Peptidase 4
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16Drug Administration Schedule
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20Etiopathogenesis. Screening. Investigations. Target tissue resistance
21General aspects
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23Glucagon-Like Peptide 1 - administration & dosage
24Glucagon-Like Peptide 1 - adverse effects
25Glucagon-Like Peptide 1 - analogs & derivatives
26Glucagon-Like Peptide 1 - biosynthesis
27Glucagon-Like Peptide 1 - classification
28Glucagon-Like Peptide 1 - physiology
29Glucagon-Like Peptide 1 - therapeutic use
30Glucagon-Like Peptide-1 Receptor
31Glycoproteins - antagonists & inhibitors
32Humans
33Hypoglycemic Agents - administration & dosage
34Hypoglycemic Agents - adverse effects
35Hypoglycemic Agents - therapeutic use
36Insulin
37Kinases
38Liraglutide
39Medical sciences
40Nitriles
41Peptides - administration & dosage
42Peptides - adverse effects
43Peptides - therapeutic use
44Protease inhibitors
45Proteins
46Pyrazines - administration & dosage
47Pyrazines - adverse effects
48Pyrazines - therapeutic use
49Pyrrolidines
50Receptors, Glucagon - agonists
51Rodents
52Sitagliptin Phosphate
53Triazoles - administration & dosage
54Triazoles - adverse effects
55Triazoles - therapeutic use
56Type 2 diabetes
57Venoms - administration & dosage
58Venoms - adverse effects
59Venoms - therapeutic use
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16Drug Administration Schedule
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19Endocrinopathies
20Etiopathogenesis. Screening. Investigations. Target tissue resistance
21General aspects
22Glucagon
23Glucagon-Like Peptide 1 - administration & dosage
24Glucagon-Like Peptide 1 - adverse effects
25Glucagon-Like Peptide 1 - analogs & derivatives
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31Glycoproteins - antagonists & inhibitors
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39Medical sciences
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44Protease inhibitors
45Proteins
46Pyrazines - administration & dosage
47Pyrazines - adverse effects
48Pyrazines - therapeutic use
49Pyrrolidines
50Receptors, Glucagon - agonists
51Rodents
52Sitagliptin Phosphate
53Triazoles - administration & dosage
54Triazoles - adverse effects
55Triazoles - therapeutic use
56Type 2 diabetes
57Venoms - administration & dosage
58Venoms - adverse effects
59Venoms - therapeutic use
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abstractGlucagon-like peptide 1 (GLP-1) is a gut-derived incretin hormone that stimulates insulin and suppresses glucagon secretion, inhibits gastric emptying, and reduces appetite and food intake. Therapeutic approaches for enhancing incretin action include degradation-resistant GLP-1 receptor agonists (incretin mimetics), and inhibitors of dipeptidyl peptidase-4 (DPP-4) activity (incretin enhancers). Clinical trials with the incretin mimetic exenatide (two injections per day or long-acting release form once weekly) and liraglutide (one injection per day) show reductions in fasting and postprandial glucose concentrations, and haemoglobin A 1c (HbA 1c) (1–2%), associated with weight loss (2–5 kg). The most common adverse event associated with GLP-1 receptor agonists is mild nausea, which lessens over time. Orally administered DPP-4 inhibitors, such as sitagliptin and vildagliptin, reduce HbA 1c by 0·5–1·0%, with few adverse events and no weight gain. These new classes of antidiabetic agents, and incretin mimetics and enhancers, also expand β-cell mass in preclinical studies. However, long-term clinical studies are needed to determine the benefits of targeting the incretin axis for the treatment of type 2 diabetes.
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