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Long-term efficacy and safety of raltegravir in the management of HIV infection

Authors Liedtke MD, Tomlin CR, Lockhart SM, Miller MM, Rathbun RC

Received 19 November 2013

Accepted for publication 8 January 2014

Published 18 March 2014 Volume 2014:7 Pages 73—84

DOI https://doi.org/10.2147/IDR.S40168

Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 3

Michelle D Liedtke, C Ryan Tomlin, Staci M Lockhart, Misty M Miller, R Chris Rathbun

Department of Clinical and Administrative Sciences, College of Pharmacy, University of Oklahoma Health Sciences Center, Oklahoma City, OK, USA

Abstract: Raltegravir is an integrase strand-transfer inhibitor approved for the treatment of HIV infection. It was the first medication in a novel class of antiretroviral agents to be approved for use in the United States in 2007. Raltegravir exhibits potent activity against wild-type HIV-1, but resistance development has been noted through three different pathways. It is metabolized primarily through uridine diphosphate glucuronosyltransferase 1A1 and has a single inactive glucuronide metabolite. Raltegravir is not a substrate, inhibitor, or inducer of cytochrome P450 enzymes and exhibits low potential for drug–drug interactions; however, strong uridine diphosphate glucuronosyltransferase 1A1 inhibitors or inducers can alter the pharmacokinetics of raltegravir. It is well tolerated, and the most commonly reported adverse effects include headache, nausea, and diarrhea. Serious adverse effects with raltegravir are rare but include rhabdomyolysis and severe skin and hypersensitivity reactions. It has been approved for use in both treatment-naïve and treatment-experienced patients and is a preferred first-line agent in both United States and European HIV treatment guidelines. Although initial approval was granted on 48-week data, 5-year clinical data have recently been published. This article reviews the data supporting long-term efficacy and safety of raltegravir in the treatment of HIV infection.

Keywords: antiretroviral, integrase inhibitor, INSTI, Isentress®

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