SLCO1B1 (OATP1B1, an uptake transporter) and ABCG2 (BCRP, an efflux transporter) variant alleles and pharmacokinetics of pitavastatin in healthy volunteers

I. Ieiri, S. Suwannakul, K. Maeda, H. Uchimaru, K. Hashimoto, M. Kimura, H. Fujino, M. Hirano, H. Kusuhara, S. Irie, S. Higuchi, Y. Sugiyama

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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.

Original languageEnglish
Pages (from-to)541-547
Number of pages7
JournalClinical Pharmacology and Therapeutics
Volume82
Issue number5
DOIs
Publication statusPublished - Nov 1 2007

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Pharmacology (medical)

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    Ieiri, I., Suwannakul, S., Maeda, K., Uchimaru, H., Hashimoto, K., Kimura, M., Fujino, H., Hirano, M., Kusuhara, H., Irie, S., Higuchi, S., & Sugiyama, Y. (2007). SLCO1B1 (OATP1B1, an uptake transporter) and ABCG2 (BCRP, an efflux transporter) variant alleles and pharmacokinetics of pitavastatin in healthy volunteers. Clinical Pharmacology and Therapeutics, 82(5), 541-547. https://doi.org/10.1038/sj.clpt.6100190