Does Crizotinib Auto-Inhibit CYP3A in vivo?
Keyword(s):
Crizotinib is a tyrosine kinase inhibitor used to treat anaplastic lymphoma kinase-positive lung cancer. There is in vitro evidence that crizotinib may auto-inhibit cytochrome P450 3A (CYP3A) activity, with important implications for crizotinib pharmacokinetics. In order to test whether crizotinib treatment alters CYP3A activity in vivo, mice were treated with 5 and 25 mg/kg crizotinib (p.o.) daily for 14 days. Results showed that crizotinib treatment did not alter CYP3A activity as determined by erythromycin <i>N</i>-demethylation. In addition, CYP3A polypeptide expression as measured by Western blot was unchanged. Therefore, our results do not support CYP3A inhibition by crizotinib in vivo.
2018 ◽
Vol 33
(2)
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pp. 65-73
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Keyword(s):
2016 ◽
Vol 23
(8)
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pp. 602-614
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2020 ◽
Vol Publish Ahead of Print
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2017 ◽
Vol 10
(6)
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pp. 576-581
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