title: A clinical drug library screen identifies astemizole as an antimalarial agent.
abstract: 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.
authors.affiliation: Department of Pharmacology and Molecular Sciences. The Johns Hopkins University School of Medicine, Baltimore, Maryland 21205, USA.
authors.forename: Curtis R
authors.initials: CR
authors.lastname: Chong
authors.forename: Xiaochun
authors.initials: X
authors.lastname: Chen
authors.forename: Lirong
authors.initials: L
authors.lastname: Shi
authors.forename: Jun O
authors.initials: JO
authors.lastname: Liu
authors.forename: David J
authors.initials: DJ
authors.lastname: Sullivan
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000009:adverse effects / Q000378:metabolism / Q000494:pharmacology*; D016589:Astemizole / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology*; D002738:Chloroquine / Q000494:pharmacology; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D004351:Drug Resistance; D018432:Drug Resistance, Multiple; D006801:Humans; D051379:Mice; D010963:Plasmodium falciparum / Q000187:drug effects*; D010967:Plasmodium yoelii / Q000187:drug effects
chemical_list: D000962:Antimalarials; D016589:Astemizole; D002738:Chloroquine; C040463:desmethylastemizole