Description
ErlotinibisaninhibitorofEGFRthatexhibitsanticancerchemotherapeuticbenefit;itiscurrentlyinclinicaltrialsforthetreatmentofcolorectalcancer,non-smallcelllungcancers(NSCLCs),andotheradvancedcancers.InNSCLCcells,erlotinibincreasesactivationofp53andAMPKandinhibitsactivityofmTOR,inducingautophagy.InotherinvitromodelsofNSCLC,thiscompoundupregulatesexpressionofp27anddownregulatesexpressionofskp2,inducingG1/Sphasecellcyclearrestandinhibitingcellulargrowth.Inanimalmodelsofpancreaticductaladenocarcinoma,erlotinibinhibitsMAPKsignalingandincreasesoverallsurvivalrates.Additionally,inmalemousemodelsoflungadenocarcinoma,erlotinibdecreasestumorburden.
References
LiYY,LamSK,MakJC,etal.Erlotinib-inducedautophagyinepidermalgrowthfactorreceptormutatednon-smallcelllungcancer.LungCancer.2013Sep;81(3):354-61.PMID:23769318.
MiyabayashiK,IjichiH,MohriD,etal.ErlotinibprolongssurvivalinpancreaticcancerbyblockinggemcitABIne-inducedMAPKsignals.CancerRes.2013Apr1;73(7):2221-34.PMID:23378339.
WeickhardtAJ,PriceTJ,ChongG,etal.Dualtargetingoftheepidermalgrowthfactorreceptorusingthecombinationofcetuximabanderlotinib:preclinicalevaluationandresultsofthephaseIIDUXstudyinchemotherapy-refractory,advancedcolorectalcancer.JClinOncol.2012May1;30(13):1505-12.PMID:22412142.
ZerbeLK,Dwyer-NieldLD,FritzJM,etal.Inhibitionbyerlotinibofprimarylungadenocarcinomaatanearlystageinmalemice.CancerChemotherPharmacol.2008Sep;62(4):605-20.PMID:18030469.
LingYH,LiT,YuanZ,etal.Erlotinib,aneffectiveepidermalgrowthfactorreceptortyrosinekinaseinhibitor,inducesp27KIP1up-regulationandnucleartranslocationinassociationwithcellgrowthinhibitionandG1/Sphasearrestinhumannon-small-celllungcancercelllines.MolPharmacol.2007Aug;72(2):248-58.PMID:17456787.