Linagliptin, a xanthine-based dipeptidyl peptidase-4 inhibitor with an unusual profile for the treatment of type 2 diabetes

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Linagliptin, a xanthine-based dipeptidyl peptidase-4 inhibitor with an unusual profile for the treatment of type 2 diabetes. / Deacon, Carolyn F; Holst, Jens Juul.

In: Expert Opinion on Investigational Drugs, Vol. 19, No. 1, 01.2010, p. 133-40.

Research output: Contribution to journalJournal articleResearchpeer-review

Harvard

Deacon, CF & Holst, JJ 2010, 'Linagliptin, a xanthine-based dipeptidyl peptidase-4 inhibitor with an unusual profile for the treatment of type 2 diabetes', Expert Opinion on Investigational Drugs, vol. 19, no. 1, pp. 133-40. https://doi.org/10.1517/13543780903463862

APA

Deacon, C. F., & Holst, J. J. (2010). Linagliptin, a xanthine-based dipeptidyl peptidase-4 inhibitor with an unusual profile for the treatment of type 2 diabetes. Expert Opinion on Investigational Drugs, 19(1), 133-40. https://doi.org/10.1517/13543780903463862

Vancouver

Deacon CF, Holst JJ. Linagliptin, a xanthine-based dipeptidyl peptidase-4 inhibitor with an unusual profile for the treatment of type 2 diabetes. Expert Opinion on Investigational Drugs. 2010 Jan;19(1):133-40. https://doi.org/10.1517/13543780903463862

Author

Deacon, Carolyn F ; Holst, Jens Juul. / Linagliptin, a xanthine-based dipeptidyl peptidase-4 inhibitor with an unusual profile for the treatment of type 2 diabetes. In: Expert Opinion on Investigational Drugs. 2010 ; Vol. 19, No. 1. pp. 133-40.

Bibtex

@article{f5053f48031a4d9d8f265c61e48d30be,
title = "Linagliptin, a xanthine-based dipeptidyl peptidase-4 inhibitor with an unusual profile for the treatment of type 2 diabetes",
abstract = "IMPORTANCE OF THE FIELD: Type 2 diabetes is a progressive disease for which current treatments are often unsatisfactory with respect to achieving therapeutic goals and unwanted side effects.AREAS COVERED: Preclinical and clinical studies of linagliptin, a new oral antidiabetic agent, including data presented at Scientific Meetings and peer-reviewed studies published since 2007.WHAT THE READER WILL GAIN: This article reviews pharmacokinetic and pharmacodynamic characteristics of linagliptin. Linagliptin belongs to a new chemical class of dipeptidyl pepidase-4 (DPP-4) inhibitors, which comprise xanthine-based compounds. It is a potent, long-acting inhibitor with high selectivity for DPP-4 versus the related enzymes DPP-8 and DPP-9. The drug has modest oral availability in humans, but is absorbed rapidly to inhibit plasma DPP-4 activity by > 80{\%} over 24 h. It is not metabolized appreciably in vivo, but binds extensively to plasma proteins, with elimination occurring primarily in the liver. Linagliptin reduces degradation of the incretin hormone glucagon-like peptide-1 and is associated with reduced fasting and postprandial glucose in preclinical and clinical studies. Limited data from longer duration clinical trials show it improves glycemic control in patients with type 2 diabetes.TAKE HOME MESSAGE: Linagliptin is a new oral antidiabetic agent associated with minimal risk of hypoglycemia, which holds promise for treatment of type 2 diabetes.",
keywords = "Animals, Clinical Trials as Topic, Diabetes Mellitus, Type 2, Dipeptidyl-Peptidase IV Inhibitors, Drug Evaluation, Preclinical, Humans, Hypoglycemic Agents, Molecular Structure, Purines, Quinazolines, Xanthine",
author = "Deacon, {Carolyn F} and Holst, {Jens Juul}",
year = "2010",
month = "1",
doi = "10.1517/13543780903463862",
language = "English",
volume = "19",
pages = "133--40",
journal = "Expert Opinion on Investigational Drugs",
issn = "1354-3784",
publisher = "Taylor & Francis",
number = "1",

}

RIS

TY - JOUR

T1 - Linagliptin, a xanthine-based dipeptidyl peptidase-4 inhibitor with an unusual profile for the treatment of type 2 diabetes

AU - Deacon, Carolyn F

AU - Holst, Jens Juul

PY - 2010/1

Y1 - 2010/1

N2 - IMPORTANCE OF THE FIELD: Type 2 diabetes is a progressive disease for which current treatments are often unsatisfactory with respect to achieving therapeutic goals and unwanted side effects.AREAS COVERED: Preclinical and clinical studies of linagliptin, a new oral antidiabetic agent, including data presented at Scientific Meetings and peer-reviewed studies published since 2007.WHAT THE READER WILL GAIN: This article reviews pharmacokinetic and pharmacodynamic characteristics of linagliptin. Linagliptin belongs to a new chemical class of dipeptidyl pepidase-4 (DPP-4) inhibitors, which comprise xanthine-based compounds. It is a potent, long-acting inhibitor with high selectivity for DPP-4 versus the related enzymes DPP-8 and DPP-9. The drug has modest oral availability in humans, but is absorbed rapidly to inhibit plasma DPP-4 activity by > 80% over 24 h. It is not metabolized appreciably in vivo, but binds extensively to plasma proteins, with elimination occurring primarily in the liver. Linagliptin reduces degradation of the incretin hormone glucagon-like peptide-1 and is associated with reduced fasting and postprandial glucose in preclinical and clinical studies. Limited data from longer duration clinical trials show it improves glycemic control in patients with type 2 diabetes.TAKE HOME MESSAGE: Linagliptin is a new oral antidiabetic agent associated with minimal risk of hypoglycemia, which holds promise for treatment of type 2 diabetes.

AB - IMPORTANCE OF THE FIELD: Type 2 diabetes is a progressive disease for which current treatments are often unsatisfactory with respect to achieving therapeutic goals and unwanted side effects.AREAS COVERED: Preclinical and clinical studies of linagliptin, a new oral antidiabetic agent, including data presented at Scientific Meetings and peer-reviewed studies published since 2007.WHAT THE READER WILL GAIN: This article reviews pharmacokinetic and pharmacodynamic characteristics of linagliptin. Linagliptin belongs to a new chemical class of dipeptidyl pepidase-4 (DPP-4) inhibitors, which comprise xanthine-based compounds. It is a potent, long-acting inhibitor with high selectivity for DPP-4 versus the related enzymes DPP-8 and DPP-9. The drug has modest oral availability in humans, but is absorbed rapidly to inhibit plasma DPP-4 activity by > 80% over 24 h. It is not metabolized appreciably in vivo, but binds extensively to plasma proteins, with elimination occurring primarily in the liver. Linagliptin reduces degradation of the incretin hormone glucagon-like peptide-1 and is associated with reduced fasting and postprandial glucose in preclinical and clinical studies. Limited data from longer duration clinical trials show it improves glycemic control in patients with type 2 diabetes.TAKE HOME MESSAGE: Linagliptin is a new oral antidiabetic agent associated with minimal risk of hypoglycemia, which holds promise for treatment of type 2 diabetes.

KW - Animals

KW - Clinical Trials as Topic

KW - Diabetes Mellitus, Type 2

KW - Dipeptidyl-Peptidase IV Inhibitors

KW - Drug Evaluation, Preclinical

KW - Humans

KW - Hypoglycemic Agents

KW - Molecular Structure

KW - Purines

KW - Quinazolines

KW - Xanthine

U2 - 10.1517/13543780903463862

DO - 10.1517/13543780903463862

M3 - Journal article

C2 - 19947894

VL - 19

SP - 133

EP - 140

JO - Expert Opinion on Investigational Drugs

JF - Expert Opinion on Investigational Drugs

SN - 1354-3784

IS - 1

ER -

ID: 132048040