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Recent reports of increased tolerance to artemisinin derivatives--the most recently adopted class of antimalarials--have prompted a need for new treatments. The spirotetrahydro-beta-carbolines, or spiroindolones, are potent drugs that kill the blood stages of Plasmodium falciparum and Plasmodium vivax clinical isolates at low nanomolar concentration. Spiroindolones rapidly inhibit protein synthesis in P. falciparum, an effect that is ablated in parasites bearing nonsynonymous mutations in the gene encoding the P-type cation-transporter ATPase4 (PfATP4). The optimized spiroindolone NITD609 shows pharmacokinetic properties compatible with once-daily oral dosing and has single-dose efficacy in a rodent malaria model.

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A group in Novartis led by Thierry Diagana and a group in Scripps led by Elizabeth Winzeler had a joint collaboration and have reported in Science on some spiroindolone compounds that had anti-malarial activity.Science paper...
PHARMACEUTICALPfizer drops Celldex brain cancer drugPharma giant Pfizer has pulled out of its 2008 deal with Celldex to develop and commercialise the brain cancer vaccine rindopepimut.According to the US biotech, Pfizer has decided the project is no longer...