Brain and Testis Accumulation of Regorafenib is Restricted by Breast Cancer Resistance Protein (BCRP/ABCG2) and P-glycoprotein (P-GP/ABCB1)

Anita Kort; Selvi Durmus; Rolf W. Sparidans; Els Wagenaar; Jos H. Beijnen; Alfred H. Schinkel

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Brain and Testis Accumulation of Regorafenib is Restricted by Breast Cancer Resistance Protein (BCRP/ABCG2) and P-glycoprotein (P-GP/ABCB1)

机译：雷戈非尼在大脑和睾丸中的积累受到乳腺癌抵抗蛋白（BCRP / ABCG2）和P-糖蛋白（P-GP / ABCB1）的限制

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Purpose Regorafenib is a novel multikinase inhibitor, currently approved for the treatment of metastasized colorectal cancer and advanced gastrointestinal stromal tumors. We investigated whether regorafenib is a substrate for the multidrug efflux transporters ABCG2 and ABCB1 and whether oral availability, brain and testis accumulation of regorafenib and its active metabolites are influenced by these transporters.

机译：目的雷戈非尼是一种新型的多激酶抑制剂，目前被批准用于治疗转移性结直肠癌和晚期胃肠道间质瘤。我们调查了雷戈非尼是否是多药外排转运蛋白ABCG2和ABCB1的底物，以及雷戈非尼及其活性代谢产物的口服有效性，脑和睾丸的蓄积是否受这些转运蛋白的影响。

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来源
《Pharmaceutical Research》 |2015年第7期|2205-2216|共12页
作者
Anita Kort; Selvi Durmus; Rolf W. Sparidans; Els Wagenaar; Jos H. Beijnen; Alfred H. Schinkel;
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作者单位

Division of Molecular Oncology The Netherlands Cancer Institute">(1);

Department of Pharmacy Pharmacology The Netherlands Cancer Institute/ Slotervaart Hospital">(3);

Division of Molecular Oncology The Netherlands Cancer Institute">(1);

Division of Pharmacoepidemiology Clinical Pharmacology Department of Pharmaceutical Sciences Faculty of Science Utrecht University">(2);

Division of Molecular Oncology The Netherlands Cancer Institute">(1);

Division of Pharmacoepidemiology Clinical Pharmacology Department of Pharmaceutical Sciences Faculty of Science Utrecht University">(2);

Department of Pharmacy Pharmacology The Netherlands Cancer Institute/ Slotervaart Hospital">(3);

Department of Clinical Pharmacology The Netherlands Cancer Institute">(4);

Division of Molecular Oncology The Netherlands Cancer Institute">(1);

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1. Brain and Testis Accumulation of Regorafenib is Restricted by Breast Cancer Resistance Protein (BCRP/ABCG2) and P-glycoprotein (P-GP/ABCB1) [J] . Kort Anita, Durmus Selvi, Sparidans Rolf W., Pharmaceutical research . 2015,第7期

机译：雷戈非尼在大脑和睾丸中的积累受到乳腺癌抵抗蛋白（BCRP / ABCG2）和P-糖蛋白（P-GP / ABCB1）的限制
2. Brain accumulation of the EML4-ALK inhibitor ceritinib is restricted by P-glycoprotein (P-GP/ABCB1) and breast cancer resistance protein (BCRP/ABCG2) [J] . Kort Anita, Sparidans Rolf W., Wagenaar Els, Pharmacological research: The official journal of The Italian Pharmacological Society . 2015,第Null期

机译：EML4-ALK抑制剂ceritinib的大脑蓄积受到P-糖蛋白（P-GP / ABCB1）和乳腺癌抗性蛋白（BCRP / ABCG2）的限制
3. Kinetic Analysis of the Cooperation of P-Glycoprotein (P-gp/ Abcb1) and Breast Cancer Resistance Protein (Bcrp/Abcg2) in Limiting the Brain and Testis Penetration of Erlotinib, Flavopiridol, and Mitoxantrone [J] . Hiroshi Kodaira, Hiroyuki Kusuhara, Junko Ushiki, The Journal of Pharmacology and Experimental Therapeutics: Official Publication of the American Society for Pharmacology and Experimental Therapeutics . 2010,第3期

机译：P-糖蛋白（P-gp / Abcb1）和乳腺癌抗性蛋白（Bcrp / Abcg2）在限制厄洛替尼，黄酮吡啶酮和米托蒽醌限制脑部和睾丸渗透方面的动力学分析
4. Stilbene analogues as inhibitors of breast cancer Stem cells through P-glycoprotein efflux; A 3D quantitative structure-activity relationship study (Inhibitory activity of stilbenes analogues on breast cancer stem cells) [C] . Anushree Tripathi, Krishna Misra 2016 International Conference on Bioinformatics and Systems Biology . 2016

机译：Stilbene类似物通过P-糖蛋白外排作为乳腺癌干细胞的抑制剂； 3D定量结构-活性关系研究（Stilbenes类似物对乳腺癌干细胞的抑制活性）
5. Nilotinib (TasignaRTM) Modulates ABCB1/PGP- and ABCG2/BCRP-mediated multidrug resistance in cancer chemotherapy. [D] . Tiwari, Amit K. 2011

机译：尼洛替尼（TasignaRTM）在癌症化疗中调节ABCB1 / PGP和ABCG2 / BCRP介导的多药耐药性。
6. Co-administration strategy to enhance brain accumulation of vandetanib by modulating P-glycoprotein (P-gp/Abcb1) and breast cancer resistance protein (Bcrp1/Abcg2) mediated efflux with m-TOR inhibitors [O] . Mukul Minocha, Varun Khurana, Bin Qin, -1

机译：通过调节P-糖蛋白（P-GP / ABCB1）和乳腺癌抗性蛋白（BCRP1 / ABCG2）用M-TOR抑制剂的介导的介导的抗andetanib脑积累的共同施用策略
7. Brain and Testis Accumulation of Regorafenib is Restricted by Breast Cancer Resistance Protein (BCRP/ABCG2) and P-glycoprotein (P-GP/ABCB1) [O] . Anita Kort, Selvi Durmus, Rolf W. Sparidans, 2015

机译：RegoraFenib的脑和睾丸积聚受乳腺癌抗性蛋白（BCRP / ABCG2）和P-糖蛋白（P-GP / ABCB1）限制

Brain and Testis Accumulation of Regorafenib is Restricted by Breast Cancer Resistance Protein (BCRP/ABCG2) and P-glycoprotein (P-GP/ABCB1)

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