GEFTINAT吉非替尼片剂说明书全文(中英对照翻译).pdf

《GEFTINAT吉非替尼片剂说明书全文(中英对照翻译).pdf》由会员上传分享，免费在线阅读，更多相关内容在教育资源-天天文库。

1、FortheuseonlyofaCancerSpecialistoraHospitaloranInstitutionGEFTINAT*(GefitinibTabletsIP)CompositionEachfilmcoatedtabletcontains:GefitinibIP250mgDESCRIPTIONGEFTINAT(gefitinibtabletsIP)contain250mgofgefitinibIPandareavailableasreddishbrownfilm-coatedtabl

2、etsengravedwithGEFTINATononesideand250onanothersidetordailyoraladministration.Gefitinibisananilinoquinazolinewiththechemicalname4-Quinazolinamine,N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-4-morpholin]propoxy].IthasthemolecularformulaC22H24C1F4O3,arel

3、ativemolecularmassof446.9andisawhite-coloredpowder.Gefitinibisafreebase.CLINICALPHARMACOLOGYMechanismofAction:Themechanismoftheclinicalantitumoractionofgefitinibisnotfullycharacterized.Gefitinibinhibitstheintracellularphosphorylationofnumeroustyrosine

4、kinasesassociatedwithtransmembranecellsurfacereceptors,includingthetyrosinekinasesassociatedwiththeepidermalgrowthfactorreceptor(EGFRTK).EGFRisexpressedonthecellsurfaceofmanynormalcellsandcancercells.Noclinicalstudieshavebeenperformedthatdemonstrateac

5、orrelationbetweenEGFRreceptorexpressionandresponsetogefitinib.Pharmacokinetics:Gefitinibisabsorbedslowlyafteroraladministrationwithmeanbioavailabilityof60%.Eliminationisbymetabolism(primarilyCYP3A4)andexcretioninfeces.Theeliminationhalt-lifeisabout48h

6、ours.Dailyoraladministrationofgefitinibtocancerpatientsresultedina2-foldaccumulationcomparedtosingledoseadministration.Steadystateplasmaconcentrationsareachievedwithin10days.AbsorptionandDistribution:Gefitinibisslowlyabsorbed,withpeakplasmalevelsoccur

7、ring3-7hoursafterdosingandmeanoralbioavailabilityof60%.Bioavailabilityisnotsignificantlyalteredbyfood.Gefitinibisextensivelydistributedthroughoutthebodywithameansteadystatevolumeofdistributionof1400Lfollowingintravenousadministration.Invitrobindingofg

8、efitinibtohumanplasmaproteins(serumalbuminandal-acidglycoprotein)is90%andisindependentofdrugconcentrations.MetabolismandElimination:Gefitinibundergoesextensivehepaticmetabolisminhumans,predominantlybyCYP3A4.Threesitesofbiotransformationhavebee