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Maraviroc

A Review of its Use in the Management of CCR5-Tropic HIV-1 Infection

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Abstract

Maraviroc (Celsentri®; Selzentry®) is a CCR5 coreceptor antagonist used in the treatment of CCR5-tropic HIV-1 infection. Administered orally twice daily, maraviroc, in combination with optimized background therapy regimens, showed good virological and immunological efficacy over 48 weeks in antiretroviral treatment-experienced patients aged ≥16 years with CCR5-tropic HIV-1 infection, in the randomized, double-blind, placebo-controlled, multicentre, MOTIVATE 1 and MOTIVATE 2 studies. Initial data indicate that the efficacy of maraviroc in this patient population is sustained for up to 96 weeks.

In the MERIT study in antiretroviral therapy-naive patients aged ≥16 years with CCR5-tropic HIV-1 infection, maraviroc was noninferior to efavirenz (each in combination with zidovudine/lamivudine) for one primary virological endpoint (HIV-1-RNA levels <400 copies/mL), but not for the other primary endpoint (HIV-1 RNA levels <50 copies/mL) in the primary analysis at 48 weeks. However, in a subsequent analysis, which used a more sensitive tropism testing assay than the one originally used and retrospectively excluded patients with non CCR5-tropic HIV-1 infection who were ineligible for inclusion in the study, maraviroc demonstrated noninferiority to efavirenz on both primary virological endpoints. Maraviroc showed sustained virological efficacy in this patient population and improved immunological markers for up to 96 weeks.

Maraviroc was generally well tolerated by both treatment-experienced and treatment-naive patients with CCR5-tropic HIV-1 infection.

Thus, maraviroc, as a component of antiretroviral combination therapy regimens, is an important option for use in treatment-experienced adults with CCR5-tropic HIV-1 infection. Available data indicate that maraviroc may also have a role in treatment-naive adults with CCR5-tropic HIV-1 infection, a population in whom CCR5-tropic HIV-1 is often the major quasispecies.

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    Caroline M. Perry

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Correspondence to Caroline M. Perry.

Additional information

Various sections of the manuscript reviewed by: A. Castagna, Clinica di Malattie Infettive, Vita-Salute San Raffaele University, Milan, Italy; F. Gutiérrez, Internal Medicine Department, Hospital General Universitario de Elche, Elche, Spain; K. Marx, College of Pharmacy, Western University of Health Sciences, Pomona, California, USA; M. Nelson, Department of HIV Medicine, Chelsea and Westminster Hospital, London, England; S. Ngo, College of Pharmacy, Western University of Health Sciences, Pomona, California, USA; D. Podzamczer, Infectious Disease Service, Hospital Universitario de Bellvitge, Barcelona, Spain; J.D. Scott, College of Pharmacy, Western University of Health Sciences, Pomona, California, USA.

Data Selection

Sources: Medical literature published in any language since 1980 on ‘maraviroc’, identified using MEDLINE and EMBASE, supplemented by AdisBase (a proprietary database). Additional references were identified from the reference lists of published articles. Bibliographical information, including contributory unpublished data, was also requested from the company developing the drug.

Search strategy: MEDLINE, EMBASE and AdisBase search terms were ‘maraviroc’ and HIV-1 infection. Searches were last updated 23 May 2010.

Selection: Studies in patients with HIV-1 infection who received maraviroc. Inclusion of studies was based mainly on the methods section of the trials. When available, large, well controlled trials with appropriate statistical methodology were preferred. Relevant pharmacodynamic and pharmacokinetic data are also included.

Index terms: Maraviroc, CCR5 coreceptor antagonist, HIV-1 infection, antiretroviral therapy, pharmacodynamics, pharmacokinetics, therapeutic use, tolerability.

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Perry, C.M. Maraviroc. Drugs 70, 1189–1213 (2010). https://doi.org/10.2165/11203940-000000000-00000

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