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Clinical Analysis and in Vitro Correlation of BCRP-Mediated Drug-Drug Interaction in the Gastrointestinal Tract
https://tus.repo.nii.ac.jp/records/2000340
https://tus.repo.nii.ac.jp/records/200034046e1a57a-c19d-455a-865d-a4ab3dcbd908
| 名前 / ファイル | ライセンス | アクション |
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(6)Clinical Analysis and in Vitro Correlation of BCRP-Mediated.pdf (784.2 KB)
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| アイテムタイプ | 学術雑誌論文 / Journal Article(1) | |||||||||
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| 公開日 | 2025-07-01 | |||||||||
| タイトル | ||||||||||
| タイトル | Clinical Analysis and in Vitro Correlation of BCRP-Mediated Drug-Drug Interaction in the Gastrointestinal Tract | |||||||||
| 言語 | ||||||||||
| 言語 | eng | |||||||||
| キーワード | ||||||||||
| 主題 | Caco-2, absorption rate constant (ka), breast cancer resistance protein, cell to medium ratio, drug–drug interaction, rosuvastatin | |||||||||
| 資源タイプ | ||||||||||
| 資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||||||
| 資源タイプ | journal article | |||||||||
| 著者 |
荻原 琢男
× 荻原 琢男
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| 抄録 | ||||||||||
| 内容記述タイプ | Abstract | |||||||||
| 内容記述 | 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. | |||||||||
| 書誌情報 |
BIOLOGICAL & PHARMACEUTICAL BULLETIN 巻 47, 号 4, p. 750-757 |
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| 収録物識別子タイプ | PISSN | |||||||||
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| 関連タイプ | isVersionOf | |||||||||
| 識別子タイプ | DOI | |||||||||
| 関連識別子 | DOI: 10.1248/bpb.b23-00786 | |||||||||
