Literature DB >> 20371753

Raltegravir plasma concentrations in treatment-experienced patients receiving salvage regimens based on raltegravir with and without maraviroc coadministration.

Silvia Baroncelli1, Paola Villani, Liliana E Weimer, Nicoletta Ladisa, Daniela Francisci, Chiara Tommasi, Vincenzo Vullo, Roberta Preziosi, Stefania Cicalini, Maria Cusato, Clementina Galluzzo, Marco Floridia, Mario Regazzi.   

Abstract

BACKGROUND: Raltegravir and maraviroc represent new, important resources for HIV-infected patients with intolerance or resistance to other antiretroviral agents. The safety and efficacy of both drugs have been investigated, but there is no information on possible pharmacokinetic interactions between these 2 drugs in clinical practice.
OBJECTIVE: To evaluate raltegravir plasma concentrations in heavily treatment-experienced patients receiving salvage regimens and explore, in a preliminary assessment, the potential influence of maraviroc coadministration and other cofactors on raltegravir trough concentrations (C(trough)).
METHODS: Fifty-four HIV-infected patients with triple class (nucleoside reverse transcriptase inhibitor, nonnucleoside reverse transcriptase inhibitor, protease inhibitor) treatment experience starting raltegravir 400 mg twice daily, with (n = 11) or without (n = 43) concomitant maraviroc 300 mg twice daily, were evaluated. All regimens included at least 3 drugs of at least 2 different classes. Raltegravir plasma Ctrough, after at least 1 month of treatment, were analyzed to compare groups of patients taking raltegravir only and raltegravir plus maraviroc. Immunovirological (CD4, HIV-RNA) and clinical data after 6 months of treatment were also collected and described.
RESULTS: Raltegravir plasma Ctrough showed a large variability (range <0.020-2.47 microg/mL). Median levels were similar in the 2 groups (raltegravir + maraviroc 0.104 microg/mL, range 0.025-0.826; raltegravir 0.090 microg/mL, range <0.020-2.47, p = 0.400). Detectable (>0.02 microg/mL) raltegravir concentrations were observed in all patients receiving raltegravir + maraviroc and in 74% of patients receiving raltegravir alone (p = 0.060). After 6 months of treatment, the 2 groups had similar clinical, virologic, and immunologic conditions.
CONCLUSIONS: Coadministration of maraviroc does not seem to have any relevant effects on raltegravir plasma Ctrough in heavily treatment-experienced patients receiving salvage regimens. Further studies should evaluate the potential additional benefits of maraviroc coadministration in terms of virologic and immunologic response.

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Year:  2010        PMID: 20371753     DOI: 10.1345/aph.1M688

Source DB:  PubMed          Journal:  Ann Pharmacother        ISSN: 1060-0280            Impact factor:   3.154


  7 in total

1.  Transmitted raltegravir resistance in an HIV-1 CRF_AG-infected patient.

Authors:  Sarita D Boyd; Frank Maldarelli; Irini Sereti; G Laissa Ouedraogo; Catherine A Rehm; Valerie Boltz; Diana Shoemaker; Alice K Pau
Journal:  Antivir Ther       Date:  2011

2.  Impaired maraviroc and raltegravir clearance in a human immunodeficiency virus-infected patient with end-stage liver disease and renal impairment: a management dilemma.

Authors:  Alice K Pau; Scott R Penzak; Sarita D Boyd; Mary McLaughlin; Caryn G Morse
Journal:  Pharmacotherapy       Date:  2012-01       Impact factor: 4.705

3.  Pharmacokinetic interaction of rifapentine and raltegravir in healthy volunteers.

Authors:  Marc Weiner; Eric F Egelund; Melissa Engle; Melissa Kiser; Thomas J Prihoda; Jonathan A L Gelfond; William Mac Kenzie; Charles A Peloquin
Journal:  J Antimicrob Chemother       Date:  2013-12-15       Impact factor: 5.790

4.  A long-acting formulation of the integrase inhibitor raltegravir protects humanized BLT mice from repeated high-dose vaginal HIV challenges.

Authors:  Martina Kovarova; Michael D Swanson; Rosa I Sanchez; Caroline E Baker; Justin Steve; Rae Ann Spagnuolo; Bonnie J Howell; Daria J Hazuda; J Victor Garcia
Journal:  J Antimicrob Chemother       Date:  2016-03-21       Impact factor: 5.790

5.  Population pharmacokinetic analysis and pharmacogenetics of raltegravir in HIV-positive and healthy individuals.

Authors:  Mona Arab-Alameddine; Aurélie Fayet-Mello; Rubin Lubomirov; Michael Neely; Julia di Iulio; Andrew Owen; Marta Boffito; Matthias Cavassini; Huldrych F Günthard; Katharina Rentsch; Thierry Buclin; Manel Aouri; Amalio Telenti; Laurent Arthur Decosterd; Margalida Rotger; Chantal Csajka
Journal:  Antimicrob Agents Chemother       Date:  2012-02-27       Impact factor: 5.191

Review 6.  Maraviroc: a review of its use in HIV infection and beyond.

Authors:  Shawna M Woollard; Georgette D Kanmogne
Journal:  Drug Des Devel Ther       Date:  2015-10-01       Impact factor: 4.162

7.  HIV Increases the Inhibitory Impact of Morphine and Antiretrovirals on Autophagy in Primary Human Macrophages: Contributions to Neuropathogenesis.

Authors:  John M Barbaro; Ana Maria Cuervo; Joan W Berman
Journal:  Cells       Date:  2021-08-24       Impact factor: 6.600

  7 in total

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