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To measure maraviroc total cerebrospinal fluid (CSF) concentrations and compare them with total and unbound plasma concentrations. Total maraviroc was measured by reverse-phase high-performance liquid chromatography with tandem mass spectrometry, whereas ultrafiltration was used for unbound maraviroc. Maraviroc was detected in all nine CSF/plasma pairs with a median CSF total concentration of 2.4 ng/ml. CSF concentrations exceeded the 50% inhibitory concentration of wild-type CC chemokine receptor 5-tropic HIV-1 in all specimens. CSF concentrations are lower than expected based on plasma concentrations and physicochemical characteristics. Unbound maraviroc plasma concentrations may be informative in estimating concentrations in CSF.

In order to assess the penetration of maraviroc to the central nervous system, we measured maraviroc concentrations in cerebrospinal fluid (CSF) and plasma. Concentrations were determined by liquid chromatography tandem mass spectrometry (lower limit of quantitation 1.25 ng/ml) in seven paired CSF and plasma samples. The median plasma maraviroc concentration was 94.9 ng/ml (range 21.4-478.0) and the median CSF concentration was 3.63 ng/ml (range 1.83-12.2). CSF samples exceeded the median EC90 for maraviroc (0.57 ng/ml) by at least three-fold. The CSF levels of maraviroc found in this study likely contribute to viral suppression in the CSF.