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Resistance to epidermal growth factor receptor inhibition in non-small cell lung cancer

查看全文 作　　者：Nele Van Der [1,2,3]Steen;Elisa [1,4]Giovannetti;Daniela [1]Carbone;Alessandro [5]Leonetti;Christian [6]D.Rolfo;Godefridus [1]J.Peters 高影响力作者 机构地区：[1]Department of Medical Oncology,VU University Medical Center,Amsterdam 1081 HV,the Netherlands;[2]Department of Pathology,Antwerp University Hospital,Antwerp 2650,Belgium;[3]Center for Oncological Research,University of Antwerp,Antwerp 2610,Belgium;[4]Cancer Pharmacology Lab,AIRC Start-Up Unit,University of Pisa,Pisa 56124,Italy;[5]Medical Oncology Unit,University Hospital of Parma,Parma 43126,Italy;[6]University of Maryland Greenebaum Comprehensive Cancer Center,Baltimore,21220 MD,USA高影响力机构 出　　处：《Cancer Drug Resistance》索引2018年第1卷第4期,共20页高影响力期刊 摘　　要：Aberrant activation of the epidermal growth factor receptor(EGFR)is a driving force for cancer growth in a subgroup of non-small cell lung cancer patients.These patients can be identified by the presence of activating EGFR mutations.Currently three generations of EGFR-tyrosine kinase inhibitors(TKIs)have been approved by the Food and Drug Administration and European Medicine Agency.This paper reviews the structure of EGFR and the downstream signaling pathways of EGFR and describes the mechanisms of intrinsic and acquired resistance against EGFR-TKIs.These mechanisms include secondary or tertiary mutations in EGFR,the activation of bypassing signaling pathways or a histological transformation to small cell lung cancer.Moreover,drug efflux transporters will affect the cellular accumulation of EGFR-TKIs and penetration of the first generation of EGFR-TKI into the brain.Lysosomal sequestration of some EGFR-TKIs may also prevent the drugs to reach their target.In conclusion,resistance to EGFR-TKIs is multifactorial,including primary and acquired mutations in the EGFR gene,activation of bypassing pathways and limited uptake of drugs in the cells or target tissues.More pharmacological studies are needed in order to develop new specific compounds targeted to overcome new resistance mechanisms in order to enable a personalized treatment approach. 关 键 词：Epidermal growth factor receptor non-small cell lung cancer RESISTANCE EGFR-tyrosine kinase inhibitors ERLOTINIB GEFITINIB AFATINIB osimertinib rociletinib
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