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Int. J. Mol. Sci. 2018, 19(8), 2367;

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
Author to whom correspondence should be addressed.
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)
Full-Text   |   PDF [259 KB, uploaded 11 August 2018]


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
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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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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