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

Authors von Hentig N

Received 9 July 2014

Accepted for publication 25 August 2014

Published 22 December 2015 Volume 2016:8 Pages 1—16


Checked for plagiarism Yes

Review by Single anonymous peer review

Peer reviewer comments 3

Editor who approved publication: Dr Shenghan Lai

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

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