Description
AEE-788isaninhibitorofEGFR,HER2,VEGFR2,andFLT3thatexhibitsanticancerchemotherapeuticactivity.Inanimalmodelswithependymomaxenografts,AEE-788increasessurvivalrates.Inacutemyelogenousleukemia(AML)cells,AEE-788inhibitscellproliferationandinducesapoptosis.Thiscompounddisplaysmixedresultsinaclinicalsettingduetohightoxicity.
References
BaselgaJ,MitaAC,SchöffskiP,etal.Usingpharmacokineticandpharmacodynamicdatainearlydecisionmakingregardingdrugdevelopment:aphaseIclinicaltrialevaluatingtyrosinekinaseinhibitor,AEE788.ClinCancerRes.2012Nov15;18(22):6364-72.PMID:23014528.
ServideiT,MecoD,TrivieriN,etal.Effectsofepidermalgrowthfactorreceptorblockadeonependymomastemcellsinvitroandinorthotopicmousemodels.IntJCancer.2012Sep1;131(5):E791-803.PMID:22120695.
ReardonDA,ConradCA,CloughesyT,etal.PhaseIstudyofAEE788,anovelmultitargetinhibitorofErbB-andVEGF-receptor-familytyrosinekinases,inrecurrentglioblastomapatients.CancerChemotherPharmacol.2012Jun;69(6):1507-18.PMID:22392572.
BarbarrojaN,TorresLA,Rodriguez-ArizaA,etal.AEE788isavascularendothelialgrowthfactorreceptortyrosinekinaseinhibitorwithantiproliferativeandproapoptoticeffectsinacutemyeloidleukemia.ExpHematol.2010Aug;38(8):641-52.PMID:20380868.