Potential benefit of dolutegravir once daily: efficacy and safety

Alessandra Fantauzzi,1 Ombretta Turriziani,2 Ivano Mezzaroma11Department of Clinical Medicine, 2Department of Molecular Medicine, Sapienza, University of Rome, Rome, ItalyAbstract: The viral integrase enzyme has recently emerged as a primary alternative target to block HIV-1 replication, and integra...

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Autores principales:	Fantauzzi A, Turriziani O, Mezzaroma I
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2013
Materias:	Immunologic diseases. Allergy RC581-607
Acceso en línea:	https://doaj.org/article/c84ab631ed7c4efe96beff0bea26b856
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spelling	oai:doaj.org-article:c84ab631ed7c4efe96beff0bea26b8562021-12-02T01:29:51ZPotential benefit of dolutegravir once daily: efficacy and safety1179-1373https://doaj.org/article/c84ab631ed7c4efe96beff0bea26b8562013-02-01T00:00:00Zhttp://www.dovepress.com/potential-benefit-of-dolutegravir-once-daily-efficacy-and-safety-a12162https://doaj.org/toc/1179-1373Alessandra Fantauzzi,1 Ombretta Turriziani,2 Ivano Mezzaroma11Department of Clinical Medicine, 2Department of Molecular Medicine, Sapienza, University of Rome, Rome, ItalyAbstract: The viral integrase enzyme has recently emerged as a primary alternative target to block HIV-1 replication, and integrase inhibitors are considered a pivotal new class of antiretroviral drugs. Dolutegravir is an investigational next-generation integrase inhibitor showing some novel and intriguing characteristics, ie, it has a favorable pharmacokinetic profile with a prolonged intracellular half-life, rendering feasible once-daily dosing without the need for ritonavir boosting and without regard to meals. Moreover, dolutegravir is primarily metabolized via uridine diphosphate glucuronosyltranferase 1A1, with a minor component of the cytochrome P450 3A4 isoform, thereby limiting drug&ndash;drug interactions. Furthermore, its metabolic profile enables coadministration with most of the other available antiretroviral agents without dose adjustment. Recent findings also demonstrate that dolutegravir has significant activity against HIV-1 isolates with resistance mutations associated with raltegravir and/or elvitegravir. The attributes of once-daily administration and the potential to treat integrase inhibitor-resistant viruses make dolutegravir an interesting and promising investigational drug. In this review, the main concerns about the efficacy and safety of dolutegravir as well as its resistance profile are explored by analysis of currently available data from preclinical and clinical studies.Keywords: antiretroviral drugs, HIV-1 integrase, integrase inhibitors, dolutegravir, once dailyFantauzzi ATurriziani OMezzaroma IDove Medical PressarticleImmunologic diseases. AllergyRC581-607ENHIV/AIDS: Research and Palliative Care, Vol 2013, Iss default, Pp 29-40 (2013)
institution	DOAJ
collection	DOAJ
language	EN
topic	Immunologic diseases. Allergy RC581-607
spellingShingle	Immunologic diseases. Allergy RC581-607 Fantauzzi A Turriziani O Mezzaroma I Potential benefit of dolutegravir once daily: efficacy and safety
description	Alessandra Fantauzzi,1 Ombretta Turriziani,2 Ivano Mezzaroma11Department of Clinical Medicine, 2Department of Molecular Medicine, Sapienza, University of Rome, Rome, ItalyAbstract: The viral integrase enzyme has recently emerged as a primary alternative target to block HIV-1 replication, and integrase inhibitors are considered a pivotal new class of antiretroviral drugs. Dolutegravir is an investigational next-generation integrase inhibitor showing some novel and intriguing characteristics, ie, it has a favorable pharmacokinetic profile with a prolonged intracellular half-life, rendering feasible once-daily dosing without the need for ritonavir boosting and without regard to meals. Moreover, dolutegravir is primarily metabolized via uridine diphosphate glucuronosyltranferase 1A1, with a minor component of the cytochrome P450 3A4 isoform, thereby limiting drug&ndash;drug interactions. Furthermore, its metabolic profile enables coadministration with most of the other available antiretroviral agents without dose adjustment. Recent findings also demonstrate that dolutegravir has significant activity against HIV-1 isolates with resistance mutations associated with raltegravir and/or elvitegravir. The attributes of once-daily administration and the potential to treat integrase inhibitor-resistant viruses make dolutegravir an interesting and promising investigational drug. In this review, the main concerns about the efficacy and safety of dolutegravir as well as its resistance profile are explored by analysis of currently available data from preclinical and clinical studies.Keywords: antiretroviral drugs, HIV-1 integrase, integrase inhibitors, dolutegravir, once daily
format	article
author	Fantauzzi A Turriziani O Mezzaroma I
author_facet	Fantauzzi A Turriziani O Mezzaroma I
author_sort	Fantauzzi A
title	Potential benefit of dolutegravir once daily: efficacy and safety
title_short	Potential benefit of dolutegravir once daily: efficacy and safety
title_full	Potential benefit of dolutegravir once daily: efficacy and safety
title_fullStr	Potential benefit of dolutegravir once daily: efficacy and safety
title_full_unstemmed	Potential benefit of dolutegravir once daily: efficacy and safety
title_sort	potential benefit of dolutegravir once daily: efficacy and safety
publisher	Dove Medical Press
publishDate	2013
url	https://doaj.org/article/c84ab631ed7c4efe96beff0bea26b856
work_keys_str_mv	AT fantauzzia potentialbenefitofdolutegravironcedailyefficacyandsafety AT turrizianio potentialbenefitofdolutegravironcedailyefficacyandsafety AT mezzaromai potentialbenefitofdolutegravironcedailyefficacyandsafety
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Potential benefit of dolutegravir once daily: efficacy and safety

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