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OCT-1-mediated influx is a key determinant of the intracellular uptake of imatinib but not nilotinib (AMN107): reduced OCT-1 activity is the cause of low in vitro sensitivity to imatinib.
White DL, Saunders VA, Dang P, Engler J, Zannettino AC, Cambareri AC, Quinn SR, Manley PW, Hughes TP. White DL, et al. Among authors: saunders va. Blood. 2006 Jul 15;108(2):697-704. doi: 10.1182/blood-2005-11-4687. Epub 2006 Apr 4. Blood. 2006. PMID: 16597591 Free article.
Most CML patients who have a suboptimal response to imatinib have low OCT-1 activity: higher doses of imatinib may overcome the negative impact of low OCT-1 activity.
White DL, Saunders VA, Dang P, Engler J, Venables A, Zrim S, Zannettino A, Lynch K, Manley PW, Hughes T. White DL, et al. Among authors: saunders va. Blood. 2007 Dec 1;110(12):4064-72. doi: 10.1182/blood-2007-06-093617. Epub 2007 Aug 30. Blood. 2007. PMID: 17761829 Free article. Clinical Trial.
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