Title : Studies on the role of metabolic activation in tyrosine kinase inhibitor-dependent hepatotoxicity: induction of CYP3A4 enhances the cytotoxicity of lapatinib in HepaRG cells.

Pub. Date : 2014 Jan

PMID : 24191259






2 Functional Relationships(s)
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1 A recent clinical study reported that concomitant use of lapatinib with dexamethasone increased the incidence of hepatotoxicity in metastatic breast cancer patients treated with lapatinib, and so we hypothesized that induction of CYP3A enhances the bioactivation of lapatinib to reactive intermediates that contribute to hepatotoxicity. Dexamethasone cytochrome P450 family 3 subfamily A member 4 Homo sapiens
2 Induction of CYP3A4 by dexamethasone or rifampicin enhanced lapatinib-induced cytotoxicity, compared with treatment with lapatinib alone. Dexamethasone cytochrome P450 family 3 subfamily A member 4 Homo sapiens