Article
Deactivation of anti-cancer drug letrozole to a carbinol metabolite by polymorphic cytochrome P450 2A6 in human liver microsomes.
Xenobiotica; the fate of foreign compounds in biological systems - 1 Nov 2009
Murai K, Yamazaki H, Nakagawa K, Kawai R, Kamataki T
Abstract excerpt
Cytochromes P450 (P450) involved in letrozole metabolism were investigated. Among 13 recombinant P450 forms examined, only P450 2A6 and 3A4 showed activities in transforming letrozole to its carbinol metabolite with small K(m) and high Vmax values yielding apparent Vmax/K(m) values of 0.48 and 0.24 nl min(-1) nmol(-1) P450, respectively. The metabolic activities of individual human liver microsomes showed a...
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