Low raltegravir concentration in cerebrospinal fluid in patients with ABCG2 genetic variants

Kiyoto Tsuchiya; Tsunefusa Hayashida; Akinobu Hamada; Shingo Kato; Shinichi Oka; Hiroyuki Gatanaga

doi:10.1097/QAI.0000000000000222

Low raltegravir concentration in cerebrospinal fluid in patients with ABCG2 genetic variants

Kiyoto Tsuchiya, Tsunefusa Hayashida, Akinobu Hamada, Shingo Kato, Shinichi Oka, Hiroyuki Gatanaga

Department of Microbiology and Immunology

Research output: Contribution to journal › Article

13 Citations (Scopus)

Abstract

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).

Original language	English
Pages (from-to)	484-486
Number of pages	3
Journal	Journal of Acquired Immune Deficiency Syndromes
Volume	66
Issue number	5
DOIs	https://doi.org/10.1097/QAI.0000000000000222
Publication status	Published - 2014 Aug 15

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Keywords

Adenosine triphosphate-binding cassette transporter G2
Antiretroviral therapy
Blood-cerebrospinal fluid barrier
Cerebrospinal fluid concentrations
Raltegravir

ASJC Scopus subject areas

Infectious Diseases
Pharmacology (medical)

Cite this

Tsuchiya, K., Hayashida, T., Hamada, A., Kato, S., Oka, S., & Gatanaga, H. (2014). Low raltegravir concentration in cerebrospinal fluid in patients with ABCG2 genetic variants. Journal of Acquired Immune Deficiency Syndromes, 66(5), 484-486. https://doi.org/10.1097/QAI.0000000000000222

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abstract = "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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AU - Oka, Shinichi

AU - Gatanaga, Hiroyuki

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Access to Document

10.1097/QAI.0000000000000222