Linagliptin: a thorough characterization beyond its clinical efficacy

Linagliptin, one of the five dipeptidyl peptidase-4 inhibitors available, has recently entered the market both in US and in most European countries for the treatment of type 2 diabetes mellitus. It presents a xanthine-based structure, and is characterized by unique pharmacokinetics, with non-linear...

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Main Authors: Maria Angela eSortino, Tiziana eSinagra, Pier Luigi eCanonico
Format: Article
Language:English
Published: Frontiers Media S.A. 2013-02-01
Series:Frontiers in Endocrinology
Subjects:
Online Access:http://journal.frontiersin.org/Journal/10.3389/fendo.2013.00016/full
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author Maria Angela eSortino
Tiziana eSinagra
Pier Luigi eCanonico
author_facet Maria Angela eSortino
Tiziana eSinagra
Pier Luigi eCanonico
author_sort Maria Angela eSortino
collection DOAJ
description Linagliptin, one of the five dipeptidyl peptidase-4 inhibitors available, has recently entered the market both in US and in most European countries for the treatment of type 2 diabetes mellitus. It presents a xanthine-based structure, and is characterized by unique pharmacokinetics, with non-linear profile, long terminal half-life allowing prolonged exposure to the drug. It is eliminated predominately through the intestinal tract and only minimally into urine, so that it can be administered, without any dose adjustment, in conditions of renal impairment. Linagliptin is effective in modifying all parameters of hyperglycemia either in monotherapy, or as add-on therapy, together with metformin or a sulphonylurea. It exhibits also a good tolerability profile with the appearance of few side effects, absence (when used in monotherapy) or low risk (when in combination with a sulphonylurea) of hypoglycemia. More importantly it has a neutral weight gain effect. A comprehensive report of the literature on linagliptin is provided, paying attention in particular to pre-clinical studies, interactions with other drugs, safety and tolerability and results obtained in animal models that highlight properties of linagliptin suggestive of potential additional uses. Particularly promising appear in fact data demonstrating a positive effect of linagliptin on metabolic dysfunction and renal and/or cardiovascular damage together with the more recently reported effects of linagliptin on tissue repair and neuroprotection.
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spelling doaj.art-0922908b52f143b796c396032ffdaec72022-12-22T00:58:07ZengFrontiers Media S.A.Frontiers in Endocrinology1664-23922013-02-01410.3389/fendo.2013.0001643063Linagliptin: a thorough characterization beyond its clinical efficacyMaria Angela eSortino0Tiziana eSinagra1Pier Luigi eCanonico2University of CataniaUniversity of CataniaUniversity of Piemonte OrientaleLinagliptin, one of the five dipeptidyl peptidase-4 inhibitors available, has recently entered the market both in US and in most European countries for the treatment of type 2 diabetes mellitus. It presents a xanthine-based structure, and is characterized by unique pharmacokinetics, with non-linear profile, long terminal half-life allowing prolonged exposure to the drug. It is eliminated predominately through the intestinal tract and only minimally into urine, so that it can be administered, without any dose adjustment, in conditions of renal impairment. Linagliptin is effective in modifying all parameters of hyperglycemia either in monotherapy, or as add-on therapy, together with metformin or a sulphonylurea. It exhibits also a good tolerability profile with the appearance of few side effects, absence (when used in monotherapy) or low risk (when in combination with a sulphonylurea) of hypoglycemia. More importantly it has a neutral weight gain effect. A comprehensive report of the literature on linagliptin is provided, paying attention in particular to pre-clinical studies, interactions with other drugs, safety and tolerability and results obtained in animal models that highlight properties of linagliptin suggestive of potential additional uses. Particularly promising appear in fact data demonstrating a positive effect of linagliptin on metabolic dysfunction and renal and/or cardiovascular damage together with the more recently reported effects of linagliptin on tissue repair and neuroprotection.http://journal.frontiersin.org/Journal/10.3389/fendo.2013.00016/fullDiabetes MellitusGLP-1IncretinDPP-4 inhibitorsanti-diabetic drugs
spellingShingle Maria Angela eSortino
Tiziana eSinagra
Pier Luigi eCanonico
Linagliptin: a thorough characterization beyond its clinical efficacy
Frontiers in Endocrinology
Diabetes Mellitus
GLP-1
Incretin
DPP-4 inhibitors
anti-diabetic drugs
title Linagliptin: a thorough characterization beyond its clinical efficacy
title_full Linagliptin: a thorough characterization beyond its clinical efficacy
title_fullStr Linagliptin: a thorough characterization beyond its clinical efficacy
title_full_unstemmed Linagliptin: a thorough characterization beyond its clinical efficacy
title_short Linagliptin: a thorough characterization beyond its clinical efficacy
title_sort linagliptin a thorough characterization beyond its clinical efficacy
topic Diabetes Mellitus
GLP-1
Incretin
DPP-4 inhibitors
anti-diabetic drugs
url http://journal.frontiersin.org/Journal/10.3389/fendo.2013.00016/full
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