Biological and Pharmaceutical Bulletin
Online ISSN : 1347-5215
Print ISSN : 0918-6158
ISSN-L : 0918-6158
Notes
Multidrug Resistance Protein 2 Implicates Anticancer Drug-Resistance to Sorafenib
Yoshihiko ShibayamaKou NakanoHiroshi MaedaMiyuki TaguchiRyuji IkedaMitsuru SugawaraKen IsekiYasuo TakedaKatsushi Yamada
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2011 Volume 34 Issue 3 Pages 433-435

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Abstract

Sorafenib and sunitinib is a small molecule inhibitor of certain receptor tyrosine kinases, and have improved outcomes for patients with advanced renal cell carcinoma. Inhibitory concentration of 50% cell growth of sorafenib significantly rose to 6.4-fold in a multidrug resistance protein 2 (MRP2) transfected cell line versus control cell line. The concentration of sorafenib was significantly decreased to 74% of control cells after 3 h treatment. In contrast, a tyrosine kinase inhibitor sunitinib did not show alteration of inhibitory concentration of 50% cell growth and accumulation into the cells of MRP2 transfected cells. The present study suggest that sorafenib is a substrate for MRP2, suggesting that MRP2 may implicate drug resistance to sorafenib.

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© 2011 The Pharmaceutical Society of Japan
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