Title : Variation in the Response of Clozapine Biotransformation Pathways in Human Hepatic Microsomes to CYP1A2- and CYP3A4-selective Inhibitors.

Pub. Date : 2018 Apr

PMID : 29155491






3 Functional Relationships(s)
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Protein Name
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1 The CYP3A4-selective inhibitor ketoconazole (2 muM) impaired CLZ N-oxide formation in all 14 of the livers used in inhibition studies (>=50% inhibition) while the CYP1A2-selective inhibitor fluvoxamine (10 muM) decreased norCLZ formation in nine. Ketoconazole cytochrome P450 family 3 subfamily A member 4 Homo sapiens
2 Ketoconazole effectively inhibited CLZ metabolism in five of seven livers that catalysed CYP3A4-dependent testosterone 6beta-hydroxylation at or above the median rate and in four other livers with lower intrinsic CYP3A4 activity. Ketoconazole cytochrome P450 family 3 subfamily A member 4 Homo sapiens
3 Ketoconazole effectively inhibited CLZ metabolism in five of seven livers that catalysed CYP3A4-dependent testosterone 6beta-hydroxylation at or above the median rate and in four other livers with lower intrinsic CYP3A4 activity. Ketoconazole cytochrome P450 family 3 subfamily A member 4 Homo sapiens