Regular ArticleImpact of Genetic Variation in Breast Cancer Resistance Protein (BCRP/ABCG2) on Sunitinib Pharmacokinetics
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2020, Pharmacological ResearchCitation Excerpt :As this transporter was first identified in the context of chemotherapy, the irinotecan metabolite SN-38, topotecan, and doxorubicin are examples for BCRP substrates [53]. Also newer drugs like the tyrosine-kinase inhibitor sunitinib are both substrates and inhibitors of BCRP, as it has been shown in humans [54], in rat experiments using pantoprazole as an inhibitor of BCRP [55] and in cells overexpressing BCRP [56]. However, it has to be acknowledged that the impact of hepatic BCRP on the overall pharmacokinetics of BCRP substrates cannot readily be estimated, because BCRP is also present in the intestines and the kidneys, where the effect of BCRP on the pharmacokinetics of drugs is probably much larger than at the canalicular side of liver cells.
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This work was supported in part by a Grant-in-Aid for Scientific Research from the Ministry of Education, Culture, Sports, Science and Technology of Japan. T. Mizuno is a Research Assistant in the Global COE Program “Center for Frontier Medicine.”
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Present address: Department of Pharmacy, Shiga University Medical Science of Hospital, Seta Tsukinowa-cho, Otsu 520–2192, Japan.
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Present address: Kyoto Pharmaceutical University, Misasagi-Nakauchicho 5, Yamashina-ku, Kyoto 607–8414, Japan.