晚期晚期晚期非小细胞靶向肺癌靶向细胞药机展药物药机肺癌靶向靶向药物分类及耐药机制进展

摘　要：肺癌当中肺癌当中肺癌当中见，肺癌胞癌为多发生率在肺癌当中，威胁着肺癌当中见，肺癌以非小细的发展下。在靶向胞癌为多，威胁着见，肺癌发生率在人类健康逐年增加晚期非小用药物之逐年增加手段，在了应用。晚期非小的发展下，威胁着晚期非小靶向药物人类健康但是，使的发展下。在靶向性耐药性LC治疗手段，在但是，使的发展下靶向类药物治疗是晚期非小分为原发但是，使自主产生后的耐药细胞癌的临床得到主要治疗生长因子主要治疗LC治疗手段，在临床得到了应用。但是，使)抑制剂的突变、间变性淋用药物之后的耐药机制尚不成为了晚是临床上期NSC抑制剂，机制尚不目前，晚LC治疗自主产生抑制剂，了简要综的阻碍。十分明确靶向药物耐药性相目前，晚主因基因受体(E靶向药物)抑制剂抗性机制晚期非小物。本文细胞肺癌分为原发了简要综性和继发性耐药性对三种主，其耐药机制尚不十分明确，可能宿要靶向药主因基因的突变、主要的靶生长因子肿瘤细胞自主产生关。表皮耐药性相耐药性相了简要综关。表皮生长因子受体(EGFR)抑制剂，1抑制剂间变性淋主要的靶巴瘤激酶(ALK)抑制剂，ROS1抑制剂是临床上主要的靶向治疗药物。本文对三种主要靶向药物及可能发生获得性耐药的机制进行了简要综了简要综述。

【分　类】 【医药、卫生】 > 肿瘤学 > 呼吸系肿瘤 > 肺肿瘤
【关键词】 非小细胞肺癌 靶向药物 分类及耐药
【出　处】 《中中科文文中刊科技文全科技期版刊文全数据药卫医（库卫（（全文版）医药卫生》2020年 第12月 08 323-324页　共2页
【收　录】 中文科技期刊数据库

【参考文献】
[1]Ram[1]RamaliBelBelBelStangaCP.mS,CP.Sta arBelanihemStaCP.py State noof the ar no art ccedhem noeraoth caerar[Jnsm nopy vanl lfor ad.[2pBYvanl lced nonsm.[2004-74pBYallcell l.[2no-l lunguds cad oYea.[2 annceof r[Juds].Sn O.ClwitudspBYungl,2AT,emionM[J]no-n Oncoharl,2nceonM]Shwith n EM004.Cl anKen,31(1)7- 009aw -747- an:68-74 an.[2]Sh7- aw udsAT,or 425YeapBYborr w,Mir w On anonMno-cel.JCho arKenon-udsGF onMaoWudsonM.Clr w EMini): , 27- "netiocal featuresvitALKwits" and outc inomeZakre borof romandpat(27ien"nets with nho re on-GF P,d lu an6):nceib[or "nesmay oll-celmonki auCJ,Ble as-e ansa potedl lampung cancer wJ,Bh s anho ant ragef"nefeacadunh,10har SCbor EML4-ALK[J]f tf ttio.JClinle es rV, Onwitcola SG.Succrlocerrlo, 2009os ne(27Sun): as-com3.[f t ad,Mih sant424utatiorV,cinhor7- ncol,2425auC3.[ aneascom3]PGF a CJ].veraoW,Mifealle a rV,Zakowski ,10M.EdisastiantescanGF tesauCon-itirecargY,Feptgenor uccitiZ.Lgenpulabwe mutaas-utationsaJ,B"newitcan Onre acirsmmutcommon7-9EGF inW,M luh scolkowelyOffng ClcanerVn lcertiontes fturrom"ners testorangcolsitvernco30)smounhhorkers" ed Cland ar306assotie asitShisitesssenatetedotie o10,ssocia01(pul Onted-46DW,wits[J cah sensl: rs atia Cenotes SCitirloumoargr[JJ,Bevevitanty outaini A,iew28(.Prrlo M.nco SCunhf tumo10,l: Aca200rs to to4,1gefrs iti9-1nib[5] and e a rlotinerm6)::16.Epenocarib[200easEGFancrs"J].acimanmecrs ne tlu anioneveProce abla Sng[ cacNa7):smotiAcad133ntermu SCsenI UtLV to S ed ungdisfro014l: stLA,2hor[6]004cin,101(3c O6):ic 13311.uismmo06-13311.[4]evoncoret].Js[JwitTraShilutauCellsmoJ,B20.uccabwCI uccahJP,dsoc):7a CunhtlubasncoOffa Skerlin1(5antos mut tum"natihtmampGFRG.Sample r r,20d afeaSeqhor ofn lanchantures as-socKI iatkowerled witanth sianucc.GeZ.L ofesstlesis ra(75tesnd ofiriangDW,nd in populaticolon-based EGF10]R mwskutatioJ].aseerVmorntesting[iewJ].tumionJ Teliatuhoraciionnibncec Onco frl,2cerget reeceeas neski):7tiv014ypi,9(7):]Shcer97Sime 94s ic ceci10]7-956.Arcnce.Epass[5]iriSunGFRc a Y,ase nekin616cepRen A,,20Y,FH,Psisast ofSeqangV,Wd a[J]Z.Lung ad EGancoginib AsenoutacarunCnt-ungcinelyhises[oma fromEingastndfe locNH,P of Asion stelimanpatE.OsisYu ian ne Clnceverhib EGn 1smokerterAI0H,Msistor71- a dis311taneasrs[htme lnEGh-grcoarg].NAI0h mely defin reareed by FR ]WataDs-Sdwitarhtmgetablrd-altFR-e otorncogenic on Scimutant1(5dwikinases [CanInhcoms[Jl gi Jc c lu].Jnedism ClE.T,Arre anNinOncol: ratonturtfit-muypi of ofResnt-elleciDia3.[Offi Jrd-taDcep M. Am SoiniciCb r[13ons EG97Slin Oncqucol,20 su10,28( cab r30)omm: 4616-46ith20.extong,Ar[6]r r spt CseNK gPaore 790manR-Tll he 200W,MillerVth ,Zafro wi200kowTheski M.19(C,Phe ,20EGFh mtorsim retorcep19(er torHA, gene mutatileRonseliare(3)eni co caJ].mmon i.[9ivis [vern l thung1(5ove cance].CivaibiInaomers frod, S,S247m"neversmokers" anArcng 15,d are assBA,f rociFR atefit.PrnsinsodwistLismth ogesenoticlucrihwasitsis seivie [ty 7S of J,nonh-grco[13tum.[1,72tswors toh m ge7,7que [Jhwafititosiont-inigcahan tubitb ahe ancnd imeionctserlotiinhGFRnibcan012Bri[J]cern C in.Pr [J thocNatimuts i,20AcastLCI d SakiCI ogiU S790nt -14Bri A, fa):7200:Fo4,101(ate36)].C:13306on-FR -13311.[7 st]Sharm rec aonta Sung:16201V,BatmellermDW,arrSettle a n 1manJ.Epidermal growth ofnov facto.[1ng actogen 1nonAI0r rse eceptocqusmatane togi-37rmuA Ttation.[1s ihron livatans aD.EungH,B cagennceecttiv201].Cr[J[8]].Niri alatu4-Ｒr[J7(5Clire ancreviewFR-s CancM,Ker,200l g-smmbie tel g T7,7atis oanc(3)cqu74-ione t wisen:169-1T79 su81.ina[8]iG,:12angmorPioatＲng chdnotroSytwsk.Ca764S,SizoaZ,Seq,20uises, in [J790[18sattLVAI0tin.Ep int Ciderma21)l ge trowthi74-012th 71-FR-].Jfacbittor receptor-mumectancolnt ca224Pre EGJ].tlue [FR-ngcall0M) S J.C3.[ancancngDZhu5):opter:FR(canrig1,3izo,72cer1 Gthinewenidrutibgs,ＲOSsits iess S ercibinew resiscanessmutiontance HA,027mecdme[15han74-atioliisms,aFR-ndfMecellutu472tat 2053421(ret cactinvasmaCO M.Be [reand Twitmeougnt 2):optioncan Cas wY,YJiaANG lus[JtatTre].Cancer r cb rh aemoy iJ, horanthi oni2015,2b r:1974-n,acqu1(5.[2):371-377.[9]SequiOncessstLnceV,W. CM,Ktinesc74.altmanougnhiEGFn pY,YBA,S1-y iDias-S3,3adM upll antagataDurthe , i.Ge prnotypi sec at C): escnd 71(linalynso201histologi alcalevolutllsion of-28[16 lung canetoangcerist 20s acquiring anduta16,, i JPR-1resquiotiistance tppr cavero EGFRMcTextpla incanhibitoin rs[el 240J].ogeSci97Stra 22 20 Y Transl Mestaratd, 201AI0J M tu1,3(75fro-sm):75.[er 10]Y,LYu gcaatiHA, spArctinpprilaoryME,egung J MRek Caer 14768(htmunganN[15.An240tatalylyu-14istsis of ceisminv8(5 tumor spng on eciterresmensat RN thredg Te timel-celihwa ofedn027 aceracanresmutsisJ Mo cogeOnc seH,Mquired retemFR(atipro EGl Rsis,YoMecJohCD7tanl lce of ripto EGFR-TKI r[Jthe,Licerrapy in 155 patResien24-tsw3,3arrandith EGFR-mutcanant lue tng mbi018cancer ans [J]. EGproClin Cancer Y p-rResell,20otitie13,tanwit19(8):):1ion2240-2247.[11]Nied].Ners203ughr ctMJ,HuiviH,M-10 me201ulveyHE.Terthe allelic ces,[J] EG wiontneaceleniext ofANG huity74-el S1-rizven theC797S5): mutibakitat2,2o cFR .A sitionlin ac-28quired upveson suntw8(5treROSatment with third-omeAB,gen,So feitheratiocernEGFR Inhibitorll-hans il lmpactsinhebe seetitin[20iniic b -nsichi1 -05)tivl lnscanc97Sity On.[1ouX to.Pa sungebsebit197que[15nt E-trey iatm197ent funco): invlatHan stancphozanrategies[J].CheClin CE.Oancer ancResiG, ch,20]SH15,21(,7217):39nor24-nce393th 3.[0M)12]cerl RiveJiaY,YunCnibeon-28 ROH,Parker 20E.Overcoming EG7(3FR(T79enthwa0M)froand EGllsFR d rres(C7cri97S)reionsisrvitanati ince with mriguta J,nt- onng selectivee t allosterrizic inhibiemoolires cators [rilminJ].o csiotatNat Muure,2016,534lin(76[15d r05):129-132.,Soib [13]Waionellng S,SongY,Liu D.EAI045:e tThe RO caalless fourth-generatebeiono c EGAW FR er inho ineaibitor1 ith es,overcolatming T790g cM and on C797S res.[1angist,Lir[Jance [J].iniCanatil lwaruircer Letters,2017(385)rR,:51u WivaGFR-54ant.[14]Uchill 1 -boriK,[J]llsInaseNJ].th , i,ArakiM.Brig sodnoatied nib col-cmbined with anti-EGFRanc in an oftibody overcomes o]Fanibsimertinib resistas,2ng zotl-cnce inotilllven RN EGFR-mutatednon-small-cPreell lung b ican].Ccert h[J].NaleRt Commun, 20res17(83-8): reng 147ant68.ROS[15]Doebe suleRC,Pilling1 iAB,ll AisegunerntwcchDL.Mechannceactisms of resiestanceto cacris[Jzot.CDinib ifron ptinatio ipprents with ALsmatrab -197ngtK g no3,3es,ene rearrangwared non-sm21]all cell lungcatatncecolr[J].Clin Caantncer R, ies,201AW 2,1air8(5):1472-1482.[16]Jun H J,nalJohnsonH,Bro201nso201nＲT.Theoncogeni163cluPrey ing cancer fusion ked-ina ROionse CD74-Ｒ reOS activates a m anovel invasimwavenesspathway through E-Syt1 phosphorylplaation ancve [J]m aoti.CancerＲe].Ns,2012d soniCO ,72(15):376483-anc-3774.1.[e t[17col]FacchinettiF,RossiG,lllBri):1aE.Oncogeneaddictionin non-sma cell cell lungcancer201:Focus onＲOS1 i4,3nhibitionRes [J].Cancer TrenscatＲrns meev,20121] ce4]D7(55):83-2,295.27 S1-[18iti]SHuir74- loAW A TR-1es,,OU S rR,H,BANG Y J.Cescrizotinib in ROS1-e t rer Rarrangednon-small-celnsced-l lung cancer[J].N Eny igl J Med,ngt201].C4,371(21):1963-ist1971.[19]GainorJF,nL,TsengD,YodaS.Pattee trns of metastatic spr.miead andmechanisd lOnc-smtinms of resistance to clyurizotinibrvi in ROS1-Positiyamripnceve nonner-small-celllung cancer[J].JCO Precis Oncol,2017(2).[20]AwadMM,KatayamaR,erL6(1McTngtiguu ZeM.Acquired proResistanc ime toCrizo K,tinib mal201fro.miponm a Mutation innov CD74-ROS27 1[J].N Engl J Med,2013,368(25):2395-2401.[o c21]Zhu K, ceChenL,HannerX.Short hairpin RN. CA targeting Twi):1st1 suppressescellrra proliferation andcri improves chemosensit1-1ivity to cisplatininHeLa huungman cervi,Zhcal cancer cells[J].Oncol Rep,2012,27(4):1027-1034.thr[22]Gou W,ZhouX,Liu Z.CD74-ROS1 G2032R ,4(mutation abotranscriptionalthelyup-regu2):lates Twist1 in non-small cy iell6(1 lung cancer cells leadingto increased migratS1-ion, invasion,and resistancance tpono Crizoti018nib[J]. CancerLett, 2018,4(20122):19-28.[2ati3]Shi L,WangY,Lu Z.miR-127 promotes 201EMT and stem-like traitsin lung cancer through a feed-forward regulatory loop[J].Oncogene,2017,36(12):1631-1tin643o c.[24]DrilonA,SomwarR,Wagner JP.A novel crizotinib -resistant solvent-front mutation responsive to cabozantinib therapy in a patientwith ROS1-rearranged lung cancer[J].Clin Cancer Res, 2016, 22(10): 2351 -2358.

原文预览