Description
Crizotinibisaninhibitorofanaplasticlymphomakinase(ALK),c-rosoncogene1(ROS1),andc-MET,bindingcompetitivelytotheATP-bindingpocketofkinases.Crizotinibexhibitsanticancerchemotherapeuticbenefitinthetreatmentofnon-smallcelllungcancer(NSCLC)andiscurrentlyinclinicaltrialsasapotentialtreatmentforneuroblastomaandotheradvancedsolidtumors.Incellularmodels,thiscompoundupregulatesexpressionofpro-apoptoticBIManddownregulatesexpressionofanti-apoptoticsurvivintoinduceapoptosisandinhibitcellproliferation.
References
TimmA,KolesarJM.Crizotinibforthetreatmentofnon-small-celllungcancer.AmJHealthSystPharm.2013Jun1;70(11):943-7.PMID:23686600.
OkamotoW,OkamotoI,AraoT,etal.AntitumoractionoftheMETtyrosinekinaseinhibitorcrizotinib(PF-02341066)ingastriccancerpositiveforMETamplification.MolCancerTher.2012Jul;11(7):1557-64.PMID:22729845.
TanizakiJ,OkamotoI,OkamotoK,etal.METtyrosinekinaseinhibitorcrizotinib(PF-02341066)showsdifferentialantitumoreffectsinnon-smallcelllungcanceraccordingtoMETalterations.JThoracOncol.2011Oct;6(10):1624-31.PMID:21716144.
