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 | |
| 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
Low raltegravir concentration in cerebrospinal fluid in patients with ABCG2 genetic variants. / Tsuchiya, Kiyoto; Hayashida, Tsunefusa; Hamada, Akinobu; Kato, Shingo; Oka, Shinichi; Gatanaga, Hiroyuki.
In: Journal of Acquired Immune Deficiency Syndromes, Vol. 66, No. 5, 15.08.2014, p. 484-486.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Low raltegravir concentration in cerebrospinal fluid in patients with ABCG2 genetic variants
AU - Tsuchiya, Kiyoto
AU - Hayashida, Tsunefusa
AU - Hamada, Akinobu
AU - Kato, Shingo
AU - Oka, Shinichi
AU - Gatanaga, Hiroyuki
PY - 2014/8/15
Y1 - 2014/8/15
N2 - 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).
AB - 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).
KW - Adenosine triphosphate-binding cassette transporter G2
KW - Antiretroviral therapy
KW - Blood-cerebrospinal fluid barrier
KW - Cerebrospinal fluid concentrations
KW - Raltegravir
UR - http://www.scopus.com/inward/record.url?scp=84904465734&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84904465734&partnerID=8YFLogxK
U2 - 10.1097/QAI.0000000000000222
DO - 10.1097/QAI.0000000000000222
M3 - Article
C2 - 24872134
AN - SCOPUS:84904465734
VL - 66
SP - 484
EP - 486
JO - Journal of Acquired Immune Deficiency Syndromes
JF - Journal of Acquired Immune Deficiency Syndromes
SN - 1525-4135
IS - 5
ER -