The development of imatinib as a therapeutic agent for chronic myeloid leukemia

M Deininger, E Buchdunger, BJ Druker - Blood, 2005 - ashpublications.org
Imatinib has revolutionized drug therapy of chronic myeloid leukemia (CML). Preclinical
studies were promising but the results of clinical trials by far exceeded expectations …

Polymorphisms in Human MDR1 (P‐glycoprotein): Recent Advances and Clinical Relevance

C Marzolini, E Paus, T Buclin… - Clinical Pharmacology & …, 2004 - Wiley Online Library
Drug transporters are increasingly recognized to be important to drug disposition and
response. P‐glycoprotein, the encoded product of the human MDR1 (ABCB1) gene, is of …

Active transport of imatinib into and out of cells: implications for drug resistance

J Thomas, L Wang, RE Clark, M Pirmohamed - Blood, 2004 - ashpublications.org
Imatinib is a tyrosine kinase inhibitor that is effective in the treatment of chronic myeloid
leukemia (CML). Not all patients achieve cytogenetic response. Some patients even lose the …

Imatinib mesylate (STI571) is a substrate for the breast cancer resistance protein (BCRP)/ABCG2 drug pump

H Burger, H van Tol, AWM Boersma, M Brok… - Blood, 2004 - ashpublications.org
Abstract Imatinib mesylate (STI571), a potent tyrosine kinase inhibitor, is successfully used
in the treatment of chronic myelogenous leukemia and gastrointestinal stromal tumors …

Sprycel for chronic myeloid leukemia and Philadelphia chromosome–positive acute lymphoblastic leukemia resistant to or intolerant of imatinib mesylate

M Brave, V Goodman, E Kaminskas, A Farrell… - Clinical Cancer …, 2008 - AACR
Abstract Purpose: On June 28, 2006, the US Food and Drug Administration approved
dasatinib (Sprycel; Bristol-Myers Squibb), a new small-molecule inhibitor of multiple tyrosine …

Expression of the uptake drug transporter hOCT1 is an important clinical determinant of the response to imatinib in chronic myeloid leukemia

L Wang, A Giannoudis, S Lane… - Clinical …, 2008 - Wiley Online Library
Some chronic myeloid leukemia (CML) patients do not respond to imatinib, whereas others
lose an initial response. To identify potential imatinib failures, we investigated the …

Drug transporters and imatinib treatment: implications for clinical practice

K Eechoute, A Sparreboom, H Burger, RM Franke… - Clinical Cancer …, 2011 - AACR
Imatinib mesylate is approved for the treatment of chronic myeloid leukemia (CML) and
advanced gastrointestinal stromal tumors (GIST). Unfortunately, in the course of treatment …

Chronic imatinib mesylate exposure leads to reduced intracellular drug accumulation by induction of the ABCG2 (BCRP) and ABCB1 (MDR1) drug transport pumps

H Burger, H Van Tol, M Brok, EAC Wiemer… - Cancer biology & …, 2005 - Taylor & Francis
Imatinib mesylate is a selective tyrosine kinase inhibitor that is successfully used in the
treatment of Philadelphia-positive chronic and acute leukaemia's, and gastrointestinal …

ABC multidrug transporters: target for modulation of drug pharmacokinetics and drug-drug interactions

B Marquez, F Van Bambeke - Current drug targets, 2011 - ingentaconnect.com
Nine proteins of the ABC superfamily (P-glycoprotein, 7 MRPs and BCRP) are involved in
multidrug transport. Being localised at the surface of endothelial or epithelial cells, they …

Dasatinib cellular uptake and efflux in chronic myeloid leukemia cells: therapeutic implications

DK Hiwase, V Saunders, D Hewett, A Frede, S Zrim… - Clinical Cancer …, 2008 - AACR
Purpose: The organic cation transporter OCT-1 mediates active transport of imatinib. We
recently showed that low OCT-1 activity is a major contributor to suboptimal response in …