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Nat Chem Biol. 2006 Aug;2(8):415-6. Epub 2006 Jul 2.

A clinical drug library screen identifies astemizole as an antimalarial agent.

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  • 1Department of Pharmacology and Molecular Sciences. The Johns Hopkins University School of Medicine, Baltimore, Maryland 21205, USA.


The high cost and protracted time line of new drug discovery are major roadblocks to creating therapies for neglected diseases. To accelerate drug discovery we created a library of 2,687 existing drugs and screened for inhibitors of the human malaria parasite Plasmodium falciparum. The antihistamine astemizole and its principal human metabolite are promising new inhibitors of chloroquine-sensitive and multidrug-resistant parasites, and they show efficacy in two mouse models of malaria.

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