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Desethylchloroquine is a major active metabolite of chloroquine (Item No. 14194).1 Desethylchloroquine is formed when chloroquine undergoes dealkylation, primarily by the cytochrome P450 (CYP) isoforms CYP2C8 and CYP3A4 and to a lesser extent by CYP2D6. It inhibits the growth of the P. falciparum strain LA136 in vitro (IC50 = 9.9 ng/ml).2
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1. In vitro metabolism of chloroquine: Identification of CYP2C8, CYP3A4, and CYP2D6 as the main isoforms catalyzing N-
2. In vitro assessment of the antimalarial activity of chloroquine and its major metabolites. Ann. Trop. Med. Parasitol. 78(6), 581-585 (1984).