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
SN - 1525-4135
VL - 66
SP - 484
EP - 486
JO - Journal of Acquired Immune Deficiency Syndromes
JF - Journal of Acquired Immune Deficiency Syndromes
IS - 5
ER -
