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Maraviroc (Selzentry)

Table of Contents

Maraviroc Selzentry Summary Drug Summary Key Clinical Trials Manufacturer for United States Key Drug Interactions Citations Figures

Drug Summary

Maraviroc is a unique antiretroviral medication—it is an HIV entry inhibitor that selectively binds to human C- C chemokine receptor 5 (CCR5). Maraviroc is currently the only FDA-approved agent in the CCR5 antagonist class and the only antiretroviral medication that acts by blocking or inhibiting a host protein or receptor, rather than a viral target. The entry of HIV into host cells requires HIV initially binding to the CD4 receptor followed by binding to either the CCR5 receptor or the C-X-C chemokine receptor type 4 (CXCR4). The HIV type that utilizes the CCR5 coreceptor pathway is referred to as R5-tropic HIV whereas virus that enters via the CXCR4 receptor is considered X4-tropic HIV. Because maraviroc does not block X4-tropic strains from entering host cells, it is useful only in patients who exclusively have R5-tropic HIV. Accordingly, prior to prescribing maraviroc, it is necessary to evaluate the patient’s viral tropism and maraviroc should only be prescribed in patients who solely harbor R5-tropic HIV. Maraviroc is generally well tolerated and causes few long-term adverse effects or drug interactions with non-antiretroviral medications (though dose adjustment is required with some medications that are strong hepatic enzyme inducers or inhibitors). The main limitations of maraviroc are the need for twice-daily dosing, the requirement to perform an HIV tropism assay prior to use, and the lack of efficacy in patients who do not have pure R5-tropic HIV. In addition, maraviroc is generally reserved for salvage therapy, since the likelihood of X4-tropic HIV increases as patients develop more advanced immunosuppression. Thus, maraviroc is not an option for many treatment-experienced patients with advanced disease.

Key Clinical Trials

MOTIVATE 1 and MOTIVATE 2: Maraviroc was assessed in two phase III, double-blind, randomized controlled studies, in which treatment-experienced adults (with 3-class drug resistance, an HIV RNA level above 5,000 copies/mL, and exclusive R5-tropic HIV) were randomized to maraviroc once daily, maraviroc twice daily, or placebo, each with an optimized background regimen.[1] In a combined analysis of these two studies, individuals in the maraviroc arms had significantly greater rates of HIV RNA suppression and greater increases in CD4 count than those who received placebo.[2]

Page 1/3 MERIT: In this trial, investigators enrolled treatment-naïve adults with R5-tropic HIV and compared maraviroc (once-daily or twice-daily) to efavirenz, each given with zidovudine-lamivudine.[3] After the week 48 analysis, the once-daily maraviroc arm was discontinued due to inferior virologic suppression.[3] The twice-daily maraviroc arm was initially found to have lower rates of HIV suppression than the efavirenz arm, but a later reanalysis found that the response rates were similar (in this reevaluation, viral tropism was retested using a more sensitive assay and a number of subjects whose virus was not truly R5-tropic at baseline were retrospectively excluded from the analysis).[4] ROCnRAL: Maraviroc has also been studied as part of several 2-drug combinations for simplification of therapy and overall has not shown favorable efficacy.[5]

Manufacturer for United States

Maraviroc (Selzentry [sell-ZEN-tree]) is available as a 300 mg tablet (Figure 1), 150 mg tablet (Figure 2), and a 20 ml/mg oral solution. Maraviroc (Selzentry) is manufactured by ViiV Healthcare.

Key Drug Interactions

For complete information on maraviroc-related drug interactions, see the Drug Interactions section in the Maraviroc (Selzentry) Prescribing Information.

Citations

1. 1.Gulick RM, Fatkenheuer G, Burnside R, et al. Five-year safety evaluation of maraviroc in HIV-1-infected treatment-experienced patients. J Acquir Immune Defic Syndr. 2014;65:78-81. [PubMed Abstract] -

2. 2.Gulick RM, Lalezari J, Goodrich J, et al. Maraviroc for previously treated patients with R5 HIV-1 infection. N Engl J Med. 2008;359:1429-41. [PubMed Abstract] -

3. 3.Cooper DA, Heera J, Goodrich J, et al. Maraviroc versus efavirenz, both in combination with zidovudine-lamivudine, for the treatment of antiretroviral-naive subjects with CCR5-tropic HIV-1 infection. J Infect Dis. 2010;201:803-13. [PubMed Abstract] -

4. 4.McGovern RA, Thielen A, Portsmouth S, et al. Population-based sequencing of the V3-loop can predict the virological response to maraviroc in treatment-naive patients of the MERIT trial. J Acquir Immune Defic Syndr. 2012;61:279-86. [PubMed Abstract] -

5. 5.Katlama C, Assoumou L, Valantin MA, et al. Maraviroc plus raltegravir failed to maintain virological suppression in HIV-infected patients with lipohypertrophy: results from the ROCnRAL ANRS 157 study.

Page 2/3 J Antimicrob Chemother. 2014;69:1648-52. [PubMed Abstract] -

Figures

Figure 1. Maraviroc 300 mg tablet

Figure 2. Maraviroc 150 mg tablet

The most up to date version of this content may be obtained from: https://www.hiv.uw.edu/page/treatment/drugs/maraviroc

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