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Suppression of carboxylesterases by imatinib mediated by the down‐regulation of pregnane X receptor

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Imatinib mesylate (IM) is a first‐line treatment for chronic myeloid leukaemia (CML) as a specific inhibitor of BCR‐ABL tyrosine kinase. As IM is widely used in CML, in combination with… Click to show full abstract

Imatinib mesylate (IM) is a first‐line treatment for chronic myeloid leukaemia (CML) as a specific inhibitor of BCR‐ABL tyrosine kinase. As IM is widely used in CML, in combination with other drugs, the effects of IM on drug‐metabolizing enzymes (DMEs) are crucial to the design of rational drug administration. Carboxylesterases (CESs) are enzymes catalysing the hydrolytic biotransformation of several clinically useful drugs. Although IM is known to inhibit cytochromes P450 (CYPs), its effects on DMEs, and CESs in particular, are still largely undefined.

Keywords: regulation pregnane; mediated regulation; carboxylesterases imatinib; imatinib mediated; suppression carboxylesterases; pregnane receptor

Journal Title: British Journal of Pharmacology
Year Published: 2017

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