Clinical Analysis and <i>in Vitro</i> Correlation of BCRP-Mediated Drug–Drug Interaction in the Gastrointestinal Tract

DOI Web Site PubMed 参考文献26件
  • Perera Liyanage Manosika Buddhini
    Laboratory of Biopharmaceutics, Department of Pharmacology, Faculty of Pharmacy, Takasaki University of Health and Welfare
  • Okazaki Kenzo
    Laboratory of Biopharmaceutics, Department of Pharmacology, Faculty of Pharmacy, Takasaki University of Health and Welfare
  • Woo Yunje
    Laboratory of Biopharmaceutics, Department of Pharmacology, Faculty of Pharmacy, Takasaki University of Health and Welfare
  • Takahashi Saori
    Laboratory of Biopharmaceutics, Department of Pharmacology, Faculty of Pharmacy, Takasaki University of Health and Welfare
  • Zhang Xieyi
    Research Institute for Science and Technology, Tokyo University of Science
  • Mizoi Kenta
    Department of Pharmaceutical Sciences, School of Pharmacy, International University of Health and Welfare
  • Takahashi Toshinari
    Medical Affairs Department, Mochida Pharmaceutical Co., Ltd.
  • Ogihara Takuo
    Laboratory of Biopharmaceutics, Department of Pharmacology, Faculty of Pharmacy, Takasaki University of Health and Welfare Graduate School of Pharmaceutical Sciences, Takasaki University of Health and Welfare

抄録

<p>Breast cancer resistance protein (BCRP) is a drug efflux transporter expressed on the epithelial cells of the small intestine and on the lateral membrane of the bile duct in the liver; and is involved in the efflux of substrate drugs into the gastrointestinal lumen and secretion into bile. Recently, the area under the plasma concentration–time curve (AUC) of rosuvastatin (ROS), a BCRP substrate drug, has been reported to be increased by BCRP inhibitors, and BCRP-mediated drug–drug interaction (DDI) has attracted attention. In this study, we performed a ROS uptake study using human colon cancer-derived Caco-2 cells and confirmed that BCRP inhibitors significantly increased the intracellular accumulation of ROS. The correlation between the cell to medium (C/M) ratio of ROS obtained by the in vitro study and the absorption rate constant (ka) ratio obtained by clinical analysis was examined, and a significant positive correlation was observed. Therefore, it is suggested that the in vitro study using Caco-2 cells could be used to quantitatively estimate BCRP-mediated DDI with ROS in the gastrointestinal tract.</p>

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