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Role of Cytochrome P450 Enzymes in the Metabolic Activation of Tyrosine Kinase Inhibitors

College of Pharmacy and Health Sciences, Lipscomb University, Nashville, TN 37204, USA
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Int. J. Mol. Sci. 2018, 19(8), 2367; https://doi.org/10.3390/ijms19082367
Received: 8 May 2018 / Revised: 7 August 2018 / Accepted: 8 August 2018 / Published: 11 August 2018
(This article belongs to the Special Issue Cytochromes P450: Drug Metabolism and Bioactivation)
Tyrosine kinase inhibitors are a rapidly expanding class of molecular targeted therapies for the treatment of various types of cancer and other diseases. An increasing number of clinically important small molecule tyrosine kinase inhibitors have been shown to undergo cytochrome P450-mediated bioactivation to form chemically reactive, potentially toxic products. Metabolic activation of tyrosine kinase inhibitors is proposed to contribute to the development of serious adverse reactions, including idiosyncratic hepatotoxicity. This article will review recent findings and ongoing studies to elucidate the link between drug metabolism and tyrosine kinase inhibitor-associated hepatotoxicity. View Full-Text
Keywords: tyrosine kinase inhibitor; bioactivation; cytochrome P450; hepatotoxicity tyrosine kinase inhibitor; bioactivation; cytochrome P450; hepatotoxicity
MDPI and ACS Style

Jackson, K.D.; Durandis, R.; Vergne, M.J. Role of Cytochrome P450 Enzymes in the Metabolic Activation of Tyrosine Kinase Inhibitors. Int. J. Mol. Sci. 2018, 19, 2367.

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