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Description: Artemisone (also known as BAY-44-9585, BAY-449585, and Artemifone) is a novel, potent and semi-synthetic antimalarial agent that inhibits P. falciparum strains, with a mean IC50 of 0.83 nM. Artemisone was 10 times more potent than artesunate in vitro against a panel of 12 P. falciparum strains, independent of their susceptibility profile to antimalarial drugs, and consistently 4 to 10 times more potent than artesunate in rodent models against drug-susceptible and primaquine- or sulfadoxine/pyrimethamine-resistant Plasmodium berghei lines and chloroquine- or artemisinin-resistant lines of Plasmodium yoelii. Slight antagonistic trends were found between artemisone and chloroquine, amodiaquine, tafenoquine, atovaquone or pyrimethamine and additive to slight synergistic trends with artemisone and mefloquine, lumefantrine or quinine. Various degrees of synergy were observed in vivo between artemisone and mefloquine, chloroquine or clindamycin.
References: J Antimicrob Chemother. 2007 Apr; 59(4):658-65.
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