Article
Differential cytochrome P450 2D metabolism alters tafenoquine pharmacokinetics.
Antimicrobial agents and chemotherapy - 1 Jul 2015
Vuong Chau, Xie Lisa H, Potter Brittney M J, Zhang Jing, Zhang Ping, Duan Dehui, Nolan Christina K, Sciotti Richard J, Zottig Victor E, Nanayakkara N P Dhammika, Tekwani Babu L, Walker Larry A, Smith Philip L, Paris Robert M, Read Lisa T, Li Qigui, Pybus Brandon S, Sousa Jason C, Reichard Gregory A, Smith Bryan, Marcsisin Sean R
Abstract excerpt
Cytochrome P450 (CYP) 2D metabolism is required for the liver-stage antimalarial efficacy of the 8-aminoquinoline molecule tafenoquine in mice. This could be problematic for Plasmodium vivax radical cure, as the human CYP 2D ortholog (2D6) is highly polymorphic. Diminished CYP 2D6 enzyme activity, as in the poor-metabolizer phenotype, could compromise radical curative efficacy in humans. Despite the importance of...
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