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

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

Research output: Contribution to journalArticle

13 Citations (Scopus)


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 languageEnglish
Pages (from-to)484-486
Number of pages3
JournalJournal of Acquired Immune Deficiency Syndromes
Issue number5
Publication statusPublished - 2014 Aug 15



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

ASJC Scopus subject areas

  • Infectious Diseases
  • Pharmacology (medical)

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