Clinical Application of Glucagon-Like Peptide-1 Receptor Agonists

Se Hee Min; Young Min Cho

doi:10.4093/jkd.2015.16.4.252

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Min and Cho: Clinical Application of Glucagon-Like Peptide-1 Receptor Agonists

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J Korean Diabetes 2015;16(4):252-259.

Published online: 10 January 2015

DOI: https://doi.org/10.4093/jkd.2015.16.4.252

Clinical Application of Glucagon-Like Peptide-1 Receptor Agonists

Se Hee Min, Young Min Cho

Department of Internal Medicine, Seoul National University College of Medicine, Seoul, Korea

Corresponding author: Young Min Cho Department of Internal Medicine, Seoul National University College of Medicine, 101 Daehak-ro, Jongno-gu, Seoul 03080, Korea, E-mail: ymchomd@snu.ac.kr

Received 28 October 2015 Accepted 4 November 2015

This is an Open Access article distributed under the terms of the Creative Commons Attribution Non-Commercial License (http://creativecommons.org/licenses/by-nc/3.0) which permits unrestricted non-commercial use, distribution, and reproduction in any medium, provided the original work is properly cited.

Abstract

Glucagon-like peptide 1 (GLP-1) is an incretin hormone that is released from enteroendocrine L-cells upon nutrient absorption; it stimulates glucose-dependent insulin secretion from pancreatic beta-cells. GLP-1 has pleiotropic effects including deceleration of gastric emptying, decreased appetite, and increased satiety. Treatment with GLP-1 receptor agonists (GLP-1RAs) improves glycemic control in patients with type 2 diabetes without increasing the risk of hypoglycemia or weight gain. Current GLP-1RAs can be classified by their structure (exendin-4-based or human GLP-1-based), duration of action, and molecular size. Different GLP-1RAs exhibit different pharmacokinetics and pharmacodynamics. Herein we review the characteristics of available GLP-1RAs and discuss current issues such as insulin combination therapy and anti-obesity effects.

Keywords: Glucagon-like peptide 1, Obesity, Type 2 diabetes mellitus

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Table 1.

Half-life and recommended dosage of GLP-1 receptor agonists

Generic name (brand name)	Half-life	Initial dose	Maximum dose
Exenatide (Byetta)	3.3∼4.0 hours	5 μg BID	10 μg BID
Lixisenatide (Lyxumia)	2.7∼4.3 hours	10 μg QD	20 μg QD
Liraglutide (Victoza)	11∼15 hours	0.6 mg QD	1.8 mg QD
Exenatide once-weekly (Bydureon)	Roughly 2 weeks	2 mg QW
Albiglutide (Tanzeum)	6∼8 days	30 mg QW	50 mg QW
Dulaglutide (Trulicity)	Roughly 4 days	0.75 mg QW	1.5 mg QW

BID, twice a day; QD, once a day; QW, once a week.

Table 2.

Comparison of short-acting versus long-acting GLP-1 receptor agonists

Variable	Short-acting GLP-1 receptor agonist	Long-acting GLP-1 receptor agonist
Compounds	Exenatide	Liraglutide
	Lixisenatide	Exenatide once-weekly
		Albiglutide
		Dulaglutide
Half-life	2∼5 hours	12 hours to several days
Effects
Fasting plasma glucose	↓	↓↓
Postprandial hyperglycemia	↓↓	↓
Fasting insulin secretion	↑	↑↑
Postprandial insulin secretion	↓	↑
Gastric emptying rate	Deceleration	No effect
Body weight reduction	1∼5 kg	2∼5 kg
Nausea	20∼50%	20∼40%

GLP-1, glucagon-like peptide 1.

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