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- Title
SLCO1B1 (OATP1B1, an Uptake Transporter) and ABCG2 (BCRP, an Efflux Transporter) Variant Alleles and Pharmacokinetics of Pitavastatin in Healthy Volunteers.
- Authors
Ieiri, I.; Suwannakul, S.; Maeda, K.; Uchimaru, H.; Hashimoto, K.; Kimura, M.; Fujino, H.; Hirano, M.; Kusuhara, H.; Irie, S.; Higuchi, S.; Sugiyama, Y.
- Abstract
To investigate the contribution of genetic polymorphisms of SLCO1B1 and ABCG2 to the pharmacokinetics of a dual substrate, pitavastatin, 2 mg of pitavastatin was administered to 38 healthy volunteers and pharmacokinetic parameters were compared among the following groups: 421C/C*1b/*1b (group 1), 421C/C*1b/*15 (group 2), 421C/C*15/*15 and 421C/A*15/*15 (group 3), 421C/A*1b/*1b (group 4), 421A/A*1b/*1b (group 5), and 421C/A*1b/*15 (group 6). In SLCO1B1, pitavastatin area under plasma concentration–time curve from 0 to 24 h (AUC0–24) for groups 1, 2, and 3 was 81.1±18.1, 144±32, and 250±57 ng h/ml, respectively, with significant differences among all three groups. In contrast to SLCO1B1, AUC0–24 in groups 1, 4, and 5 was 81.1±18.1, 96.7±35.4, and 78.2±8.2 ng h/ml, respectively. Although the SLCO1B1 polymorphism was found to have a significant effect on the pharmacokinetics of pitavastatin, a nonsynonymous ABCG2 variant, 421C>A, did not appear to be associated with the altered pharmacokinetics of pitavastatin.Clinical Pharmacology & Therapeutics (2007) 82, 541–547. doi:10.1038/sj.clpt.6100190; published online 25 April 2007
- Subjects
GENETIC polymorphisms; PHARMACOKINETICS; CLINICAL medicine; POPULATION genetics; CLINICAL pharmacology
- Publication
Clinical Pharmacology & Therapeutics, 2007, Vol 82, Issue 5, p541
- ISSN
0009-9236
- Publication type
Article
- DOI
10.1038/sj.clpt.6100190