Role of human cytochrome P450 3A4 and 3A5 in the metabolism of taxotere and its derivatives: enzyme specificity, interindividual distribution and metabolic …

M Shou, M Martinet, KR Korzekwa… - Pharmacogenetics …, 1998 - journals.lww.com
Taxotere, a promising anticancer agent, is metabolized almost exclusively in liver and
excreted from bile in all species. To determine which cytochrome P450 is involved in
taxotere biotransformation, 11 cDNA-expressed human cytochrome P450s were examined
for their activity in the metabolism of taxotere and its derivatives. Of all P450s, cytochrome
P450 3A4 and 3A5 were the most active for the oxidation of taxotere to the primary
metabolite RPR 1049 5 2 and for subsequent oxidation of RPR104952 to RPR111059 and …