Characterization of human cytochrome P450 mediated bioactivation of amodiaquine and its major metabolite N‐desethylamodiaquine

Abstract

The major metabolite DEAQ is likely to be quantitatively more important than AQ with respect to hepatic exposure to reactive metabolites in vivo. High expression of CYP3A4, CYP2C8, CYP2C9, and CYP2D6 may be risk factors for hepatotoxicity caused by AQ-therapy.