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View the Table of Contents for the May 15 issue of Clinical Cancer Research.
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The activity of imatinib in leukemia has recently been linked to the organic cation transporter 1 (OCT1) gene SLC22A1. To further understand mechanisms involved in the drug’s cellular entry, Hu and colleagues characterized the interaction of imatinib with 15 transporters in amphibian and mammalian models. They found that imatinib could be transported by various ABC transporters and by OATP1A2, but not by OCT1. An expression microarray, however, showed that SLC22A1 provides a composite surrogate for the expression of multiple transporters relevant to imatinib. Given that it is highly expressed in the intestine, gliomas, and leukemia cells, these findings suggest that OATP1A2 may play a key role in imatinib pharmacokinetics and pharmacodynamics.