Clinical use of cobicistat as a pharmacoenhancer of human immunodeficiency virus therapy

Nils von Hentig HIV Center, Medical Department II, Hospital of the JW Goethe-University, Frankfurt, BAG Darab-Kaboly/von Hentig, General Medicine and HIV Care, Frankfurt am Main, Germany Abstract: The pharmacoenhancement of plasma concentrations of protease inhibitors by coadministration of so-calle...

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Autor principal:	von Hentig N
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2015
Materias:	Keywords: HIV fixed dose combinations pharmacoenhancers drug safety Immunologic diseases. Allergy RC581-607
Acceso en línea:	https://doaj.org/article/954ef647f6c445ce81d4960adf07588a
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spelling	oai:doaj.org-article:954ef647f6c445ce81d4960adf07588a2021-12-02T05:09:37ZClinical use of cobicistat as a pharmacoenhancer of human immunodeficiency virus therapy1179-1373https://doaj.org/article/954ef647f6c445ce81d4960adf07588a2015-12-01T00:00:00Zhttps://www.dovepress.com/clinical-use-of-cobicistat-as-a-pharmacoenhancer-of-human-immunodefici-peer-reviewed-article-HIVhttps://doaj.org/toc/1179-1373Nils von Hentig HIV Center, Medical Department II, Hospital of the JW Goethe-University, Frankfurt, BAG Darab-Kaboly/von Hentig, General Medicine and HIV Care, Frankfurt am Main, Germany Abstract: The pharmacoenhancement of plasma concentrations of protease inhibitors by coadministration of so-called boosters has been an integral part of antiretroviral therapy for human immunodeficiency virus (HIV) for 1.5 decades. Nearly all HIV protease inhibitors are combined with low-dose ritonavir or cobicistat, which are able to effectively inhibit the cytochrome-mediated metabolism of HIV protease inhibitors in the liver and thus enhance the plasma concentration and prolong the dosing interval of the antiretrovirally active combination partners. Therapies created in this way are clinically effective regimens, being convenient for patients and showing a high genetic barrier to viral resistance. In addition to ritonavir, which has been in use since 1996, cobicistat, a new pharmacoenhancer, has been approved and is widely used now. The outstanding property of cobicistat is its cytochrome P450 3A-selective inhibition of hepatic metabolism of antiretroviral drugs, in contrast with ritonavir, which not only inhibits but also induces a number of cytochrome P450 enzymes, UDP-glucuronosyltransferase, P-glycoprotein, and other cellular transporters. This article reviews the current literature, and compares the pharmacokinetics, pharmacodynamics, and safety of both pharmacoenhancers and discusses the clinical utility of cobicistat in up-to-date and future HIV therapy. Keywords: human immunodeficiency virus, fixed-dose combinations, pharmacoenhancers, drug safetyvon Hentig NDove Medical PressarticleKeywords: HIVfixed dose combinationspharmacoenhancersdrug safetyImmunologic diseases. AllergyRC581-607ENHIV/AIDS: Research and Palliative Care, Vol 2016, Iss Issue 1, Pp 1-16 (2015)
institution	DOAJ
collection	DOAJ
language	EN
topic	Keywords: HIV fixed dose combinations pharmacoenhancers drug safety Immunologic diseases. Allergy RC581-607
spellingShingle	Keywords: HIV fixed dose combinations pharmacoenhancers drug safety Immunologic diseases. Allergy RC581-607 von Hentig N Clinical use of cobicistat as a pharmacoenhancer of human immunodeficiency virus therapy
description	Nils von Hentig HIV Center, Medical Department II, Hospital of the JW Goethe-University, Frankfurt, BAG Darab-Kaboly/von Hentig, General Medicine and HIV Care, Frankfurt am Main, Germany Abstract: The pharmacoenhancement of plasma concentrations of protease inhibitors by coadministration of so-called boosters has been an integral part of antiretroviral therapy for human immunodeficiency virus (HIV) for 1.5 decades. Nearly all HIV protease inhibitors are combined with low-dose ritonavir or cobicistat, which are able to effectively inhibit the cytochrome-mediated metabolism of HIV protease inhibitors in the liver and thus enhance the plasma concentration and prolong the dosing interval of the antiretrovirally active combination partners. Therapies created in this way are clinically effective regimens, being convenient for patients and showing a high genetic barrier to viral resistance. In addition to ritonavir, which has been in use since 1996, cobicistat, a new pharmacoenhancer, has been approved and is widely used now. The outstanding property of cobicistat is its cytochrome P450 3A-selective inhibition of hepatic metabolism of antiretroviral drugs, in contrast with ritonavir, which not only inhibits but also induces a number of cytochrome P450 enzymes, UDP-glucuronosyltransferase, P-glycoprotein, and other cellular transporters. This article reviews the current literature, and compares the pharmacokinetics, pharmacodynamics, and safety of both pharmacoenhancers and discusses the clinical utility of cobicistat in up-to-date and future HIV therapy. Keywords: human immunodeficiency virus, fixed-dose combinations, pharmacoenhancers, drug safety
format	article
author	von Hentig N
author_facet	von Hentig N
author_sort	von Hentig N
title	Clinical use of cobicistat as a pharmacoenhancer of human immunodeficiency virus therapy
title_short	Clinical use of cobicistat as a pharmacoenhancer of human immunodeficiency virus therapy
title_full	Clinical use of cobicistat as a pharmacoenhancer of human immunodeficiency virus therapy
title_fullStr	Clinical use of cobicistat as a pharmacoenhancer of human immunodeficiency virus therapy
title_full_unstemmed	Clinical use of cobicistat as a pharmacoenhancer of human immunodeficiency virus therapy
title_sort	clinical use of cobicistat as a pharmacoenhancer of human immunodeficiency virus therapy
publisher	Dove Medical Press
publishDate	2015
url	https://doaj.org/article/954ef647f6c445ce81d4960adf07588a
work_keys_str_mv	AT vonhentign clinicaluseofcobicistatasapharmacoenhancerofhumanimmunodeficiencyvirustherapy
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Clinical use of cobicistat as a pharmacoenhancer of human immunodeficiency virus therapy

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