Journal
JAIDS-JOURNAL OF ACQUIRED IMMUNE DEFICIENCY SYNDROMES
Volume 66, Issue 5, Pages 484-486Publisher
LIPPINCOTT WILLIAMS & WILKINS
DOI: 10.1097/QAI.0000000000000222
Keywords
antiretroviral therapy; raltegravir; cerebrospinal fluid concentrations; blood-cerebrospinal fluid barrier; adenosine triphosphate-binding cassette transporter G2
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Funding
- Grant for National Center for Global Health and Medicine [H22-110]
- Japanese Ministry of Health, Labour and Welfare [H23-AIDS-001]
- MSD
- Janssen Pharmaceutical
- Abbott
- Roche Diagnostics
- Pfizer
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Adenosine triphosphate-binding cassette transporter G2 (ABCG2) is expressed on the cerebrospinal fluid (CSF) side of choroid plexus epithelial cells, which form the blood-CSF barrier. Raltegravir was recently identified as a substrate of ABCG2. In the present study, we analyzed the relationship between single-nucleotide polymorphisms of ABCB1 and ABCG2 genes and raltegravir concentrations in 31 plasma and 14 CSF samples of HIV-infected patients treated with raltegravir-containing regimens. The mean CSF raltegravir concentration was significantly lower in CA (25.5 ng/mL) and AA (<10 ng/mL) genotypes at position 421 in ABCG2 gene compared with CC (103.6 ng/mL) genotype holders (P = 0.016).
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