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,LHRH,(LH)(FSH),,;;;NewprogressofanticancercetrorelixdrugCAIJia2li,CHENZhao2hui,GENGRong2xia,etal.SchoolofChemistryandChemicalEngineering,SouthwestUniversity,Chongqing400715,ChinaAbstractAnticancerCetrorelixisadenovosyntheticantagonistofgonadotrophinreleasinghormone(GRH),whichregulatesthesecretionofluteinizinghormone(LH)andfolliclestimulatinghormone(FSH)throughcompetingthemembranereceptoronthepituicytewithendogenousLHRH.Agreatquantityofresear2chesindicatethatcetrorelixnotonlyhasabettertherapeuticeffectforovariancancer,prostaticcarcinoma,metrofioma,endometriosisandsoon,butalsopreventsandimprovesthebenignprostatichypertrophy(BPH)andthesyndromeofovaries2excessedstimulation.Thearticlereviewedthenewdevelopmentofcetrorelixapplicaton.KeywordsCetrorelix;Ovariancancer;Benignprostatichypertrophy(BPH);Prostaticcarcinoma1111AstaMedicaLHRH,,,Ares2Serono19998200045:dNal(1)2dCpa(2)2dPal(3)2Ser(4)2Tyr(5)2dCit(6)2Leu(7)2Arg(8)2Pro(9)2dAla(10)(1)1112,22,,LHRH,,1121122,LHRH,(LH)(FSH),:(:SWUB2006018);(:CSCT,2006BB4341):400715();()()(),,11212Grundker,LHRH[1]:(Phosphotyrosinephosphatase,PTP),(epidermalgrowthfactor,EGF)EGF,,c2fos,[2][3],,LHRH,PADondi2(DU145PC3)12008133ChinaPracMed,Jan2008,Vol.3,No.3,,(urokinase2typePA,uPA),(PAinhibi2tors,PAI21),[4]1121370%80%LHRH,LHRH(pertussistoxin)Gi/(ser2ine/threonineproteinphosphate2A,PP2A)GiLHRH,Gi/,[5]TrkAP75,TrkA,P75SanchezLHRHLHRH,P75,TrkA[6]P75,TrkALHRHP75,TrkAP75,,221121111,2,LHRH,LHRH,2,LH,LHRH,[7],LHRH,HCG,HCG,,15mm,10%[8]21112Felberbaum[9],10,14d3mg,44dLHRH,17,LHRH3,;1;616d,31%,,21113,LHRH,,,,,Kupker[10]15,3mg/,8,50mg/ml,15(100%)(),,60%21114Steger[11],,21115Al2pha252alpha2Comaru,,[12]21116,,LHRH53,,,PSA,[13]11BPH6,,[14]29,(5060mg,60120mg,34),2[15]21296120h,0125mg,1/d,,7,3mg,5d,0125mg/d,0125mg,24h;3mg,LH4d,,85%,30h3,,:22,,,,,1GrundkerC,SchlotawaL,ViereckV,etal.AntiproliferativeeffectsoftheGnRHantagonistcetrorelixandofGnRH2IIonhumanendometrialandovariancancercellsarenotmediatedthroughtheGnRHtypeIre2ceptor.EurJEndocrinol,2004,151(1):1412149.2GrundkerC,VolkerP,EmonsG.Antiproliferativesignalingofluteinz2inghormonereleasinghormoneinhumanendometrialandovariancanercellsthroughGproteinalpha(1)mediatedactivationofphosphotyrosinephosphatase.Endocrinolgy,2001,142(6):236922380.3CastellonE,ClementiM,HitschfeldC,etal.Effectofleuprolideandcetrorelixoncellgrowth,apoptosis,andGnRHreceptorexpressioninprimarycellculturesfromhumanprostatecarcinoma.CancerInvest,22008133ChinaPracMed,Jan2008,Vol.3,No.32006,24(3):2612268.4DondiD,FestucciaC,PiccolellaM,etal.GnRHagonistsandantago2nistsdecreasethemetastaticprogressionofhumanprostatecancercelllinesbyinhibitingtheplasminogenactivatorsystem.OncolRep,2006,15(2):3932400.5ImaiA,SugiyamaM,FuruiT,etal.Giprotein2mediatedtranslocationofserine/threoninephosphatasetotheplasmamembraneandapoptosisofovariancancercellinresponsetogonadotropin2releasinghormonean2tagonistcetrorelix.ObstetGynaecol,2006,26(1):37241.6SanchezC,ClementiM,BenitezD,etal.EffectofGnRHanalogsontheexpressionofTrkAandp75neurotrophinreceptorsinprimarycellcul2turesfromhumanprostateadenocarcinoma.Prostate,2005,65(3):1952202.7KoichiK,YukikoN,ShimaK,etal.Efficacyoflow2dosehumanchori2onicgonadotropin(HCG)inaGnRHantagonistprotocol.JAssistRe2prodGenet,2006,23(5):2232228.8MarciR,CasertaD,DoloV,etal.GnRHantagonistinIVFpoor2re2sponderpatients:resultsofarandomizedtrial.ReprodBiomedOnline,2005,11(2):1892193.9FelberbaumRE,KupkerW,KrappM,etal.Preoperativereductionofuterinefibroidsinonly16daysbyadministrationofagonadotrophin2re2leasinghormoneantagonist(Cetrotide).ReprodBiomedOnline,2001,3(1):14218.10KupkerW,FelberbaumRE,KrappM,etal.UseofGnRHantagonistsinthetreatmentofendometriosis.ReprodBiomedOnline,2002,5(1):12216.11VerschraegenCF,WestphalenS,HuW,etal.PhaseIIstudyofcetro2relix,aluteinizinghormone2releasinghormoneantagonistinpatientswithplatinum2resistantovariancancer.GynecolOncol,2003,90(3):5522559.12Comaru2SchallyM.GnRHantagonistsandbenignprostatichyperplasi2a.AnnUrol(Paris),2005,39(3):73277.13Cetrorelix.DrugsFuture,1996,21(3):3072308.14GonzalezBarcenaD,VadilloBuenfilM,GomezOrtaF,etal.Re22sponsestotheantagonisticanalogofLHRH(SB275,cetrorelix)inpa2tientswithbenignprostatichyperplasiaandprostaticcancer.Prostate,1994,24(2):84.15TunnUW,MelamedRJ,SchnaarsY,etal.Tolerabilityandhor2monalsuppressionoftheLHRH2antagonistcetrorelixinpatientswithpros2tatecancer.JUrol,1997,157(Suppl4):S551.;;,2176,,1111176,142,34,1455,3415,68,108,126,7116%,10,517%,30min3h[1]112,,,,,,20ml+5%250ml,,018112mg+10%250ml,018mg+10%20ml112210mg+10%250ml2,,,30min1h,12h,34h,3,[1],:650011,,,,,,,,,[2],,[3],2,,,2,,,[4],,,2,,,,,,1..,2005:9832985.2,.,2001,8(4):2542255.3...4..,1994,14(1):1.32008133ChinaPracMed,Jan2008,Vol.3,No.3