title: Imatinib activity on Schistosoma mansoni.
abstract: Imatinib, a drug used for treatment of human chronic myeloid leukaemia, due to its activity against protein kinases, has been also evaluated in vitro against Schistosoma mansoni showing high schistosomicidal activity. In the present experiments imatinib activity in vitro was confirmed at the doses of 25 µM, 50 µM and 100 µM. The first drug activity observed with the lower dose was interruption of egg-laying and with the higher dosages was the death of the worms. In mice infected with S. mansoni no activity was found even with 1,000 mg/kg/day, 500 mg/kg/day, single oral dose or when administered for three consecutive days. This is another example of the difference of results related to in vitro and in vivo trials using S. mansoni worms.
authors.affiliation: Fiocruz, Centro de Pesquisas René Rachou, Laboratório de Esquistossomose, Belo HorizonteMG, Brasil.
authors.forename: Naftale
authors.initials: N
authors.lastname: Katz
authors.forename: Flávia Fernanda Bubulo
authors.initials: FF
authors.lastname: Couto
authors.forename: Neusa
authors.initials: N
authors.lastname: Araújo
mesh_terms: D000818:Animals; D001549:Benzamides / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D000068877:Imatinib Mesylate; D051379:Mice; D059208:Parasite Load; D010879:Piperazines / Q000494:pharmacology*; D011743:Pyrimidines / Q000494:pharmacology*; D012550:Schistosoma mansoni / Q000187:drug effects*; D012555:Schistosomiasis mansoni / Q000188:drug therapy* / Q000469:parasitology; D012556:Schistosomicides / Q000494:pharmacology*; D013997:Time Factors
chemical_list: D001549:Benzamides; D010879:Piperazines; D011743:Pyrimidines; D012556:Schistosomicides; D000068877:Imatinib Mesylate
references.citation: Exp Parasitol. 2007 Nov;117(3):318-36
references.pmid: 17553494
references.citation: Inflammopharmacology. 2011 Dec;19(6):307-16
references.pmid: 21947519
references.citation: Int J Parasitol. 2001 Aug;31(10):1093-100
references.pmid: 11429173
references.citation: Curr Opin Cell Biol. 2009 Apr;21(2):317-24
references.pmid: 19217767
references.citation: Microbes Infect. 2005 Feb;7(2):204-12
references.pmid: 15725385
references.citation: Blood. 2008 Apr 15;111(8):4022-8
references.pmid: 18256322
references.citation: J Parasitol. 2000 Feb;86(1):146-9
references.pmid: 10701578
references.citation: N Engl J Med. 2002 Feb 28;346(9):683-93
references.pmid: 11870247
references.citation: PLoS Negl Trop Dis. 2009 Aug 18;3(8):e504
references.pmid: 19688043
references.citation: J Biol Chem. 2011 Dec 9;286(49):42325-42336
references.pmid: 22013071
references.citation: Biochim Biophys Acta. 2005 Dec 30;1754(1-2):151-9
references.pmid: 16198642
references.citation: Mem Inst Oswaldo Cruz. 2008 Dec;103(8):781-5
references.pmid: 19148417
references.citation: Am J Trop Med Hyg. 1962 Mar;11:201-15
references.pmid: 14484966
references.citation: Rev Bras Malariol Doencas Trop. 1956 Oct;8(4):589-97
references.pmid: 13494879
references.citation: Adv Parasitol. 1968;6:233-90
references.pmid: 4978052
references.citation: Mem Inst Oswaldo Cruz. 2002 Apr;97(3):381-5
references.pmid: 12048569
references.citation: Parasitology. 1965 Nov;55(4):695-700
references.pmid: 4957633
references.citation: Curr Opin Infect Dis. 2008 Dec;21(6):659-67
references.pmid: 18978535
references.citation: Int J Antimicrob Agents. 2012 Nov;40(5):458-62
references.pmid: 22947125
references.citation: BMC Genomics. 2004 Oct 12;5:79
references.pmid: 15479470
references.citation: Antimicrob Agents Chemother. 2013 Feb;57(2):990-5
references.pmid: 23229489
references.citation: Int J Parasitol. 2010 Apr;40(5):521-6
references.pmid: 20149792
references.citation: Bioessays. 2007 Dec;29(12):1281-8
references.pmid: 18022808
references.citation: Br J Clin Pharmacol. 2004 Aug;58(2):212-6
references.pmid: 15255805