bcrp - publications

Predict more bcrp - ligand interactions now!


1. J Cardiovasc Pharmacol. 2012 Apr 10. [Epub ahead of print]

Influence of ABCC2, SLCO1B1, and ABCG2 polymorphisms on the pharmacokinetics of
olmesartan.

Kim CO, Cho SK, Oh ES, Park MS, Chung JY.

1Department of Clinical Pharmacology, Severance Hospital, Yonsei University
Health System, Seoul, Korea 2Department of Clinical Pharmacology and
Therapeutics, Seoul National University College of Medicine and Bundang Hospital,
Seongnam, Korea.

ABSTRACT: This study was designed to determine whether genetic polymorphisms of
multidrug resistant protein 2 (ABCC2), organic anion transporting polypeptide 1B1
(SLCO1B1), and breast cancer resistance protein (ABCG2) have an effect on
olmesartan pharmacokinetics in Korean subjects. Sixty-eight healthy male
volunteers who participated in previous pharmacokinetics studies of olmesartan
medoxomil (single dose, 20 mg or 40 mg) were enrolled. All subjects were analyzed
and grouped according to the genotypes of ABCC2, SLCO1B1, and ABCG2. The
dose-normalized peak plasma concentration (Cmax) and area under the plasma
concentration-time curve (AUCt) values were analyzed. The dose-normalized mean
Cmax and AUCt in the ABCC2 -24CT genotype group were higher than those in the
-24CC genotype group (Cmax,dn: CT 26.1±6.5 [ng/ml]/mg vs. CC 22.1±6.7 [ng/ml]/mg,
p=0.010, AUCt,dn: CT 178.7±45.6 [h*ng/ml]/mg vs. CC 149.9±39.8 [h*ng/ml]/mg,
p=0.010). The difference in AUCt,dn between the ABCC2 -1549GG and -1549GA
genotype groups was statistically significant (GG 149.0±41.0 [h*ng/ml]/mg vs. GA
174.1±43.3 [h*ng/ml]/mg, p=0.019). No significant differences were observed for
any other single nucleotide polymorphism in ABCC2, SLCO1B1, or ABCG2. The ABCC2
-24CC genotype group exhibited lower systemic exposure of olmesartan than the
-24CT genotype group, whereas no significant differences were observed in the
other transporter genotype groups.

PMID: 22494992 [PubMed - as supplied by publisher]