Title : Sorafenib and sunitinib, two anticancer drugs, inhibit CYP3A4-mediated and activate CY3A5-mediated midazolam 1'-hydroxylation.

Pub. Date : 2011 May

PMID : 21266595






3 Functional Relationships(s)
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1 In contrast, midazolam 1"-hydroxylation catalyzed by recombinant CYP3A5 was enhanced by the coexistence of sorafenib or sunitinib in a concentration-dependent manner, with saturation occurring at approximately 10 muM. Sorafenib cytochrome P450 family 3 subfamily A member 5 Homo sapiens
2 Our results thus showed that sorafenib and sunitinib activated midazolam 1"-hydroxylation by CYP3A5 but inhibited that by CYP3A4. Sorafenib cytochrome P450 family 3 subfamily A member 5 Homo sapiens
3 Unexpected drug interactions involving sorafenib and sunitinib might occur via heterotropic cooperativity of CYP3A5. Sorafenib cytochrome P450 family 3 subfamily A member 5 Homo sapiens