Research paperMefloquine metabolism by human liver microsomes: Effect of other antimalarial drugs
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2009, Acta TropicaCitation Excerpt :However, it is not known whether or to what extent the increased mefloquine efflux is associated with increased susceptibility to the drug, or whether other mechanisms are also involved. Mefloquine has been shown both in vitro and in vivo to be biotransformed by the liver enzyme cytochrome P450 (CYP) to an inactive product, carboxymefloquine (Na-Bangchang et al., 1992; Na-Bangchang et al., 2007). Although there is no direct evidence to support the existence of CYP in P. falciparum, we have previously provided indirect evidence for the possibility of the involvement of CYP-mediated metabolism of mefloquine in P. falciparum clones by the ability of the parasite to biotransform mefloquine to carboxymefloquine and an unidentified metabolite (Na-Bangchang et al., 2007).
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