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SLCO1B1 (OATP1B1, an Uptake Transporter) and ABCG2 (BCRP, an Efflux Transporter) Variant Alleles and Pharmacokinetics of Pitavastatin in Healthy Volunteers
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 (AUC(0-24)) 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, AUC(0-24) 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.
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Thompson, P. D., Clarkson, P., & Karas, R. H. (2003) · JAMA · doi:10.1001/jama.289.13.1681 · Cited by 1,463
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Knauer, M. J., Urquhart, B. L., Meyer zu Schwabedissen, H. E., Schwarz, U. I., Lemke, C. J., Leake, B. F., Kim, R. B., & Tirona, R. G. (2010) · Circulation Research · doi:10.1161/circresaha.109.203596 · Cited by 222
Metadata
- 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.
- Venue
- Clinical Pharmacology & Therapeutics
- Publisher
- Wiley
- Published
- 2007-04-25
- Volume
- 82
- Issue
- 5
- Pages
- 541-547
- ISSN
- 0009-9236 (ISSN-L)
- 1532-6535
- OpenAlex
- W2039299577
- Cited by
- 164
- References
- 1
- FWCI
- 12.56
- Type
- journal article
- Language
- en
- Open access
- closed
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- CoChat. (2026). Citation check: SLCO1B1 (OATP1B1, an Uptake Transporter) and ABCG2 (BCRP, an Efflux Transporter) Variant Alleles and Pharmacokinetics of Pitavastatin in Healthy Volunteers. https://app.cochat.ai/papers/10.1038/sj.clpt.6100190
- The paper
- 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 & Therapeutics. https://doi.org/10.1038/sj.clpt.6100190
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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