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- SRPT T-766( AR RR G -- 1260 MIN 314/022208 'PERFLUOROOCTANESULFONYL FLUORIDEEOD Tb. BACTERIAL REVERSE MUTATION TEST Sponsor 33BuMMilCCioenrnptgoe2rra0t2e5T.o0xi2cology SMivav Ssizsaz0 Usa Research Laboratory HWuonotlilnegyRdoonaLdife Sciences Ld. AHucnotninigaiyon CPaEmRbSriHdgSeshire ENGLAND Report sued23 October 2002 Pace 10129 001570 MIN3141022208 CONTENTS Page COMPLIANCEWITHGOODLABORATORYPRACTICE STANDARDS ccc 3 QUALITY ASSURANCE STATEMENT ..c.c.cvnsssssssnnns 4 INTROBUCTION sommes sms 7 EXPERIMENTAL PROCEDURE... sm 10 ASSESSOFMREESUNLTTS ccs: 14 DEVIFAROTMPRIOTOOCNOLS cc sms MAINTENANCE OFRECORDS. sm----------15 TABLES 1. Resultsobtainedwith S.typhimurTiA9uBm: test | (ange-inging) coven 18 2. Resultsobtainedwith 5.hphimurium TADS:test2, With pre-Iubation ce 19 3. ResultsobtainedwithS.pphimurium TAL0D:test 1 (a0ge-fnding) cree 20 4. Resultsobtainedwith 5.pphimoium TA100: test 2, with re-incubation eves 21 5. Resultsobtainedwith. yphimuzism TAIS3S:test 1 (ange-Anding) .crvvcvoncen 22 6. Resultsoblainedwith 5 nphimarium TALS3S: tet 2, With pre-ncubation vcs 23 7. ResultsobtainedwithS. yphTAIi S37:m test|z (rngi e-HGim 0g) vores 8. Resultsobtainedwith S. yphimurium TA1S37: test2, withpreincubation 2245 9. 10. RReessuullttssoobbttaaiinneeddwwiitthh E.ccoollii WWPP22uurrAA/IppKKMM1I0OI1 ((CCMMS8911))::tteste2|,s(wriattnhgep-rfei-nidnicnugb)ation...227 APPENDICES 1 Sictaoslmoab delamsasmmsgamsispmsmmon 39 2. EyeResearch CeatreGLP ComplianceStatement2001 -.. senator 39 001571 `20 * : MIN 314/022208 COMPLUANGEWITH GOODLABORATORYPRACTICESTANDARDS eyderived nisreports contd inol ithelingGrd Libris iy lA oSCOvEitConA DrPmo goseefGiod LStIt n-- PSrttssiFetAes G997,TErNVM--CKAH--TEIM--ORT--. Practice Stanwidtha therexd ceps tio, nsstatedbelow,and I conths edai tagdenee ratr edtobe valid. CNoumitt35chm.ayior, Sr Study Director, coms 2u3e..0ckbex. 262 001572 a . MN 31402208 `QUALITY ASSURANCE STATEMENT The following inspections sad audits havebeen cae aut in elation to thi dy: Study Phase Protocol Audit $PF5roPcoreespsmaBrautsoenndadITntsepaeocmteinnonts PieScoring Report Autit DateofInspection 16 October 2001 3115Oectmoabreyr22000012 24Osobe 2001 4 Febrary 2002 Date of Reporting 16October 2001 3115OJcatnoubaerry22000021 24October2001 5 February 2002 PrDoirteocctoorlaAdudCiotm:pAannyaMudainoafgtehmeeprnoatsociondlicfaotretdhsihsosvaedywas conducted ndreported 1 theStudy PnraocreespseBtiatsiveedpIrnoscpeedcutrieosnesm:plAtoyoerdshonothtihsetyipmeeotfisstsudtyuwdeyrweascairniperdoogrue.s Tihnesspeectwieornescoofndrouucttineed nd reported appCamrpanyoMapnagiemeen1s indictedsbove CRoempotrteAuadidtrTehpsoireepo0rtthheaSstbueyenDaiudsiotendabnydthCeomQpuaanliytMyaAnsasgueramnecnetD1epianrdmicaatt.edsTbhoivseauditwas eThse ametohfotdhsi,sprtoceddrurfeslandthoebsrearwvadtaito.ns were found to be accrtely described and the reported AGnrgoeulaManMaogtelrn,nings, B.Sc, MSE, PhD, MRQA. Due HDuenptairnmgednotnoLfifQeuaSlcietnycAesssLustn.ce, 001573 co RESPONSIBLE PERSONNEL Kenneth May, B.Sc., C.Biol,, M1Biol. Study Director Elizabeth Farral, B.Sc. Scientist MIN 3141022208 001574 5 : MIN3141022208 SUMMARY hIinsttihdiisneindevpietrnodeanstseasusxmoetnrtopohficthmeutmaunttaogefnSiaclmpoonteenltliaalpopfhiPmerzfiluumor,ooscttaainnessuTlAfIonSy3lS,flTuoArIiSd3e7(,POTSAES)S, (CaMnBd9T1A)I,0w0e,reaenxdpoasetdrtyopttohpehtaenstsduebpsetnadnecnet. mutant of Escherichia coli, stain WP2iorA/GKMI0L ATrwoocilnodre1pe2n5de4ntimnutdartuaitcosn(et5ed9ssmiwxe)r.eBpoetrhfotersmtes diinnvtohlveepdraepsrenecea-nid anbscesuncabegoeafintliaviierrtopirgnehtpavreastseilosn.sfrom Comnutcaetnitornatteisotnss.TohfisPeirsftuhoreosotcatnadnaersdullifmointyc]onfcleunotrriadtei(onPrOeScFo)mumpetnodedSi00n0pthge/rpelgaultaetwoerryegutiedsetleidnienstthhate thisassyfollows. Nosignsoftoxicitywereobserved towardsthetesterstrainsin ethermutationtes. Noevidenceof mutagenicactivity wasseenatanyconcentrationofPerfluorooctanesulfonyl fivoride (POSF)ineither mutatiteosnt. "Theconcurrentpositivecontrols demonstratedthesensitivityoftheassay andthe metabolisingactivity ofthe liverpreparations. shItoiwsecdonnocleuvdieddentcheaor,fumnudteargetnhiecatcetsitvictoynidinttihoinssbaecmtpelroiyaesdy,stPeemr.fluorooctanesulfonyl fluoride (POS) 00157s 16: MIN 3141022208 INTRODUCTION "Tfhluiosrriedpeo(rPtOdSesFc)riibnesa a studydesigned bacterial system. toThaesssetsusdtyhweamsutcaogneduncitcpeodteinntciaolmoplfiPaenrcfeluwoirtohoctthaencfsolullofwoinnyg|. guidelines: R`eOvEeCrDseGMuuitdealtiinoensTesfotr, tGhueidTeelsitnien4g71o.f Chemical. (1997) Genetic Toxicology: Bacterial E`mCutaCtoiomnmitessstiionnbaDciterreicat.ivNeo.20L0013362//57E.C Annex 4D-B.13/14. Mutagenicity - Reverse US EPA (199) Health Effects Test Guidelines. OPPTS 870.5100 Bacteriel reverse `mutation test. EPA 712-C-98-247. GJeanpearnalM,inAigsrtircuylotufraAlgrPircoudltuucrtei,onFoBruersetaruy.aNnodhSFiasnheNroie.s.42(0109.85) Notification of Director EiJosienitNDoi.rec1t2i7vaesndoKfiEkPyA,oNkJouM.E2(W31aOcntJdobMeIrT1L99(7)3.1 October 1997) Kanpoan No. 287, IMHW Genotoxicity Testing Guideline, PAB Notification No. 1604 (1 November 1999) Official Notice ofJMOL. (8 February 1999). TrheecommmeetnhdoadtidoenscsorifbtehdewUansitaeldsoKidnegsidgonmedEntvoircoonmmpelnytawliMthutIaCgeHn(S1o9c9i5et&y (G1a9t97e)h,ouasnedeffaolll1o9w90e)d. the TMhaeroinn avintdroAtmeecshni1q9u8e3)deesncarbliebsedthbeymAutmaegsenaincdehfifseccoof-waotreksetrssub(sAtmaensc,etMocbCeadnentearnmdinYeadmabsyakeixpo1s9i7n5g, CspaepcaiballelyosfseylnetctheedsisstianigntsohfeSeaslsmeontniealllaamtiynpohiacmiudr,iuhimsttioditnhee, tbeustt stuhbestmauntcea.nt NsotrramianlsluyseS.d pipnhtihimsarteisut marei:s oriiginnachiaosftiptdhiinaesifnbudneclpteinoend.enWtfhoermnttahkeessepsltaacienisnarapereopxoprotsieodn1o0fthaempuotpaugleanti,roenv.erTse mhuatraeteiroenfestrroetedtheo `asmerdeiveurmt(asntu,ppalnedmeanrteerdeawdiitlhydbeitoeticnt,esdinbcyetthheeisreabsiltiatiynstoargeraolwsainndcafpoabmlecooflboinoitesinosnynathhiesstiisd)i.ne deficient AmutteacnhtnisqruaeibnaosfeEdsocnhesriimcihliaaprcionlcitphlaetsahraesailnscaobpaebelendoefsscyrnitbheedsbisyinGgrteheena(m1i9n84o).acTihditsrsyypsttoepmhaenm,pwlhoiycsh is required for growth. .Thephsitmrauirnsiuumsesdtraciansryhaavdediatidoenfaelctmivuetacteiloncsoatt,hawthriecnhdearllotwhsemgremaotrere pseernmseiatbiivleittyoofmueasgtesnusb.stanTchees inpotsostehssecellp.laAslmidth(epsKtMaIi0n1s)a,rewdheicfh iinctironidnueocernsmatalnDeNroAr-rperpoanierprreopcaeisrsperso.ceIsnsa, rdesudltiingtthirneieionofcrnteahs,eemd sensitivity to some mutageas. 001576 7 Co MIN314022208 Manontaysuvbsataniicnetshdleobaancotteberxiaellrtceea mlu.tTahgereenfiocreef,fetchte ubnatcitletrhieayahnadvteebsteesunbsmteatnacbeoalrieseidbncyuebantzeydimnesbyostthtemhse awbistehncaseuabnstdapnrceese(nAcroeoclfor1s2u5p4p)lkenmoewntntedoilinvdeurcfaecathioinghl(e5v9emlioxf)epnrzeypmaeraecdtfirvoiym.raspreviously treated "oTnh3e1pJrulyo20tw01aoasnacpdpbroyotvlheedSbtyudHyDiurecntoLrnitf1e5SiOcciteonnbceers2Mg0a0n1ad.gemoentnon 18July2001,bythe Sponsor 17`T2h3e 7stPuXd,yEwnaglsacnodn.ducted at Huntingdon Life Sciences Li, Eye Research Centre, Eye, Suffolk, EExpexrimpentealcsoramrplidetteimo:n2d1eaNto:nve31mtbJearna2ua0r0ly12.002. 001577 :: Identiy: Appearance: Storage conditions: Lotoumber: Expiry date: Pui Specific gravity: Date received: MIN 314/022208 TEST SUBSTANCE Perfluorooctanesufonyl fluoride (POSF) Clear liquid Room temperature oa0227 dSuproantsioornosfresstpuodnsyibility; assumed sable for 595.5% cals 14 June 2001 001578 : MIN 314022208 EXPERIMENTAL PROCEDURE BACTERIAL STRAINS "The following strains were used: . typhimurium TALS3S:DcNonAtarienpsaaihrissytsidtienme m(is7sBe)nsaenmduhtaatsioande(fHeicstGi4v6e) bluitpiospaollsoysdeafcicciheanrtcioindseta obanset-hpeaicrelsluwbasltlat(ifoanm,ubtuattiiosnn)o.t sItenissrieivevtroetefdrabmyesmhiafntymuatgaegnetnss.causing S phimurium TAIOD: icsonftehrerisnagmeampaiscilTliAnISr3eSsisbtauntcecoanntadinisncraeasriensgi.stasnecnseittirvaintsyfefro fsaoctmoer mutagens (plasmid pKMI01). In addition to base-pair substitutions, it is: alo able todetect certain frameshift mutagen. S pphimuriumTAI537: bdeefaercstiavehisitnidainDeNfAr.amreesphaiifrt smyusttaetmioannd(hlsiCp3o0p7o6l)y.saccLhiakreidTeAIcoSt3.S, Iitt iiss sensitive to agents causing frameshift mutations involving insertion or deletion ofa single basepai. S. typhimurium TASB: caondteafiencstiavneotDheNrAhisrteipdaiinre sfyrsatmeemshiafntdmultiaptoipoonly(siacscDh3a0r5i2d)e.coAsgtaibnutit halasso ocofnttawionsatdhjeacpenKtMbIaOseppaliarsmsid(.douIbtlie rfervaemretsehdifbtymaugteanttisoncsa)u,sibnugtdenloettiboyn simple alkylating agents causing base-pais substitutions. EWPc2oilinrA/GKMIOL: (M89) cbaosnet-apianisransuobcshtrietumtuitoantsiona.t tItheis r0epveErteldobcyusmaonry baygenGts-Ccausbiasneg-pAa-iTr saulbssotidteuftiicoinesntinintraansDfeNrARNrAepaliorciseylssteewmhe(ruevriAn),theancdhriosmomsoormee.reaIdtiliys trheeveprKteMdIbOyIceprltaasimnidm.utagensthan its paren strain WP. It also contains The sinsofS. ophimirim were obtained from the National Collection of Type Caltures, London, England. The sin of E. cal was obiained from the National Collections of Industrial and Marine Bacteria, Aberdeen, Scotand. Baatlicqhueotssoofftnuhtersirenatnbsrwoethrceuolbtluraeisneadnfdrwoemrmeasttoerrsetaotck-s80heCl.diDnimleitquhiydlnisturlopgheonx.idTeh(eDtMesStOba)tcwhaessawdedreed taoptplhiecabcluel,tufroersacetll8m%emvbirvaan5e paecmrmyeoapbrielsietryva(tiavem.utEataicohn)b,atsecnhsiotifviftiyutzoenUsVtraliignhwt aasndtetshteedp,RwMhIeOrLe pmluatsamgiedn,swwheircehaclosnofaesrssesrseesdi.stance to ampicillin. The responses ofthe strains 0 a seriesofdiagnostic Foshrakuisneg,inatte3s7ts,Cafnoral1i0quhooutorsf.frTohzeesnecuclutltuurreewsawseardedientdetnode2d5tmoiproofvinudteraipepnrtobxriomtahtaenldy 1i0ncucbealtsepde,wrimtl,h `swuhrifcahcewoefrpelamteeassoufrendutbryiesnptraegaadrinagnadlicqouuonttsin(g0.th1emr)esoulfatan1t0coldoinluitcisonofte overnight cultures on the 001579 10 MIN 3141022208 POSITIVE CONTROLS In the absence o$f9 mix CSuAppSliNero:: PuLortinu:mber: ASpoplevaernta:nce: Concentation: Identity: SuCpApSliNeor.: LPuortitnyu:mber: SAoplpveeanrta:nce: Concentration: CIdAenStiNtyo:: SuLpoptliuemrb:er Purity: SAoplpveeanrta:nce: Concentration ICdAenStitNyo:. Supplier PLuortintuy:mber: SAapipveeanrta:nce: Concentration: In the presenceof$9 mix CeAntSitNyo:: SLuoptplniuemrb:er: APpupseiatrya:nce: Solvent: Concentration: 2Si6g6m2a82C0h2e8mical mTin.H9O5% D`WMhiSteOp(oAwldderirch, A.C:S.spectrophotometri grade) 0.5ugplat forstains TALS3S and TAI00 9-Amincacridine 9Si0g4m5a9Chemical >10o6mF%-06681 YDeMllSoOwp(oAwlddreicrh, ACS. spectrophotometric grade) 30ugporlsaianTtAISe37 02N7i-o5f7l8uorene `8A0l5d0ri1c-h2C0h2e2m7ical Company 98% Beige powder '1DMgSO/(Alpfdorrislcha,aiAnCtTSA.e9s%pectrophotometrc grade) 236828-5-37F34uSnritwyo-2l-fr)y) acrylamide (AF-2) WakoPure ChemicalIndustriesLd. 9P8A-E10121S%] RDeMdSpOow(dAeldrrich, A.C, specrophotometric grade) 005ug/pat forsainWP2orA/pKMI01 (M81) 62-1A3m-i1n3o8antiracene A5l2d2r3i4ch02C4hemical Company 9Gr6e%en powder DMSO (Aldrich,A.C. spectophotometrc grade) 210gkigpplltaetfofrosrtsraaiinnTWAIPS23uS0rA/pKMIOL (CME91) n: 001580 MIN 3141022208 ICdeAntSitNyo:: SLuoptplniuemrb:er: Appuprietayrance: SCaolncveenntr:ation: 5Be0a.z3o2f8alpyrene Al7d7r7i8c-h10Ch5eancalCompany 9Ye8l%low powder DSuM/SpOlt(eAfkorriscthr,aAi.nCs:TS.AIsSp3e7c,trToApShoBtaonmdetTrAcIg0ra0de) PREPARATION OF $9 FRACTION SSepexc:ies: SStoauricne: Weight: RMaatle S`pCrhaasgiuees-RDiavwerleUyKdeLrtidv.ed <00g 5M9cfCraacntnioannwdaYsapmraespaakried(1f9r7o5m).a gMrioxuepdoffcunacti1o0nanoiximdaalsseacscyosrtdeimnsg in0tthheeramtetlihvoerdsdewsecrreibsetdibmuylaAtmedesb,y Absoodcylowrei1gh2t5.4,aOndthme fiifth8ndaaiysiansfgtleetiinnjereac-tirpoen,retfoonldellowiingnjoveecmiitngichtomnfastoilnga,t tahedratos wosefreSa0k0ilmgleidkebey cervialdislocation an thirliversaseptically removed. `0Th1e5foMllKowCiIngGstemplswKeCrIec:ar1rigedloiuvetr)atbe0f4oreCubenidnegratrsaenpstfiercrceodndtiotiaonPso.tTteh-eEllvievhejsemwerheompogleanicseeird.n frFaocltlioownin(g59pfrreapcatriaotni)onw,atshdeihsopmeongseendaitnetowaalisqucoetntsrainfudgesdtoarte9d0a0t0 -g80foCro1r0bmeilnouwte.sE. scThhebastucpheomafta5n9t fractionwastestedfo sterilityand efficacy. Dateofpreparation: 17Jly2001 (est 1); 15 Jan20u02atre 2y) PREPARATION OF $9 MIX `PTHhe7.$49m(i1x00comntMa)i,nedg:luc$o9fsrea-c6t-ipohnos(p1h0at%e v(A5),mMM)g,ClNA(8DmPMH),(4KCmIM()33amnMd)N,AsDodHiu(m4phmoMs)p.hateAlbluftfheer cofactors were fler-trilsed before use. FORMULATION OFTEST SUBSTANCE h"Tehxeanseo.lubiIltiwtyaosftihnesotluebtlesuibnstDaMncSeOw,asetahsaensolseadnidn daciemteotnhey,lasnudlpwhaoxsidke n(DoMtSwoOb)n,eetihnasnoollu,blaeceitnonweataenr.d a`Alhtihsocuognhcseonlturbalteioinn hweaxsanfeouatnd50tombge/tmo,othtoxvioctloumweaorfdhstehxeatneestresqyusitreedmt.adImtwians,itshterteehfroertee,sdtescuibdsetadntcoe administheer test substance by direct addition without the seof solvent. A(lPlOScoFn)cesnatmrpalteioanssrceicteeidviend.this report aerxpressed in termsofthe Perfluorooctanesalfony] fluoride 001581 2: MIN 314022208 MUTATESTTPRIOCOEDUNRE Firsttest (range-finding) cTohnecteentsrtastuibosntoafntceewstassuabdstdaendcteotceusltteurdwesaosf5th0e0f0ipvgeptelsaetrest(roabitnasianetdsbevyeandcdiotnicoenntorfati2o.8nsu.lTohfethhiegtheesstt substance). Thi assay follows. Tihsethoethsetrandcaorndcenlitmriatticoonnscewnterraetio2n50r0ecpoglmpmleanteded(1i4n tyhl)e, re1g7u5l0atoprgyipgluaitdeel(in1e0s twhli)s, 1250 pg/pate (0.7), 700 gfplate controls andtheappropriatepositive c(o0:n4frwoll,sw3e5r0eapllsaoitnecl(u0de2d.i)and 175 pple (0.1 i). Untreated Fsoollultoiwoinn)gtothaeiratdidghittigolnasosfvtehsseelasb,ov0e.5amlliquSo9tsmoifxtohre 0t.e5stmsiub0s.t1anMcep(hoorsp0h.1atmelbuofffepros(iptHive7.c4o)ntwraosl `maidnduetde,sfwiotlh lsohbawykien0gd.1bemfloorfeaa1dd0ithioounrobfa2cmtloefrcauiglataurlrceo.nTthaeinmiinxgtuhriesstiwdeinreei(0.n5 mcM)uaabntd3a7trCtypfteooprh3dan0 (c0o.n5tamiMni)n.g T2h5 emmlixtmuirneismawleragatrh.oroEuagchhlysPheatkedniashndwaosverilnadiidvoindutaolplryevliaboeulslleydprweitphareadPuentiqrudeischoedse ccoornrceenstproantdiionn.g 1Pl0aatesshweetr,eidaelnstoipfryeinpgartehdewcointtheonutttsohefatdhdeidtiisonh.oTfbharceteerPieatirnidoirsdehrestowaesrseesusstehdefsoterreilaictyh ohfotuhresteAsfttseurbtshtiasnpceer,i5o9dmthiexaapnpdesaordainucmeopfhtoshpehbaatcekbgurfofuern.dAbalclteprliaatleswaewrnewiansceubxaatmeidnaetd3a7ndCfroevrecratan72t coloniescountedusing aDominoautomatedcolonycounter cAonuyntosxoircbeyfftehctesaobfstehnceetoesftsaucbosmtpalnecteewboauclkdgbreoduentdebcatcetedrbiyal alsauwbns.tanItnitahleraebdsucetnicoenoifnarneyveorxainctceoflfeocntys ttohxitcopefcfoencctesnwterarteioobnsneorrvmaeldlyaluosweedricnotnhceenstercaotnidontmeistgwhotubledbcheotsehne,seanmseuraisntghtahtautsseidginsntohfebfaicrtsetr.iaIlf insibhidbooenaoubrtealpirneedsde.ntIafptrtehciep1i9tpactoenwceernteroatbisoenr.vedIdoeanlltyhae pmliaantttihoemefntsuhdromefetnohne-tinocxuibcactoinocnenpterriaotdi,onast Dleiarsetctfoorur non-precipitting dose levels should be obiained, unless otherwise justified by the Srudy Second test `5T0h0es0cucgpolnadttevstawsaagsaainnecxhaocsterneapetaht otfotphcoencfiernsttrtaetsito,ne.xceptthatonlyfiveconcentrationswereused. STABANIDFOLRMIULATTIYON ANALYSIS s"yTshtesemuwearebonifottlhdetetteyesrtmsiunbesdtaanscepaantdothfetshtiabssiltiotdyya.ndAnhaolmyosgiesnoeiftsyochfitchvetdecstosnubcsteanncterinawtathesinotoenstt perafspoartroftmhisesuddy. 001582 B MIN 314022208 ASSESSMENT OF RESULTS Acceptance `Faocrhasttersati1n0sbheouclodnlsiiedweirtehdivnatlhiedt9h9e%mcoenfoaifdetnnhecelsimoitslofvtheecnucrortnetnrvtohliersetvoherriticaanltcccoolnltooenly rnaunmgbeeorfsthfoer alsabaorrosltloirnygunrleecsosrodtoherwviasmeaejxuistmirfuimedboyfftihvee ySetaurdsy. ADilrseoc,totrh.e Tpohseithiivsetocroinctarlorlacnogmepwoiullndbse mmuaisnttacaiunseed. atleast a doublingof mean revertant colony numbersoverthe negative control. Analysis `fTohrethmeeasonlvneunmt/bveerhoifclreevceornttraonltcgorloounpise.s for alltreatmentgroups willbecompared with those obiained Evaluation I`cfoenxcpuorsreunrte1s0olavteenstt/vseuhbisctlaenccoenptrrooldsu,cewisathnsionmcereaesveidiennrceevoefrtaanpcoosiltoinvye ndosue-mrelobatfieaonrlsheiasptt(winiccreeatsheed trwevoesretpanatractoeleoxnpyerciomuennttssa,twictonhcaennytrbaatcitoenrisablesltroawintehiatthaetrwinhtihceh ptrheesmeaacxeiomraalbsinecnrceeaosefis$9ombtiaxi,neidt)w,ililn be considered to show evidofemutnagceniec activity in thistes system. No statistical analysis will be performed. Ifexposure10 a testsubstancedoes notproduceanincreaseinrevertan colony numbers in two separate experiments,withanybacterial staineitherinthepresenceorabsenceof S9mix,itwillbe: considered to show no evidenceof mutagenic activity in tis test system. No statistical analysis will be performed. afItthrethreeasduldtistioobntaalitneesdtifaniglouotlsiantiesdfiyntthheecrmiuttearitaiofnotreastlpearr"poosicttivhee"toedrst"dunaetgraamtiaevye"b,reesspounbsje,ecetveteodn satnaatliysstiicsaltoprdoecteedrumrienseutsheedswtililtbiealthossiegndiefsiccraincbeeodfbaynMyahinocnreeafseasl (i1n9r8e9v)eratnadntwiclollounsuyalnluymbbeerasn.alyTsihse: woiftvharsitaanticsetifcaolllsoiwgendifibcyanDcue.nnetIt'sshtoesutl.d Bbieolnoogitceadltshiagtniifticisancaeccsehpotualbdlealtwoaycsonbcelucdoensaindeerqeudivaloocnagl. responseifno clear results can be obtained. DEVIATIONS FROM PROTOCOL Although the protocol indicated that a solvento vehicle would be employed, it was not possible to obiain a solution or suspensionofthetetsubstance that would be compatible withth test system. "The test substance was, therefore, added directly othetest system. Since this procedure complies with the test guidelines that this study follows, tis deviation does not impact on the integrityofthe study. 001583 1 MIN 3141022208. MAINTENANCE OF RECORDS rAellmarianwtdhaetap,rospaemrptlyoesftahned sSppeocnsiomre.ns(Tiyfpeapsproofpsraimaptel)eaarnisdinsgpefcriommetnhewhpiecrhfoarrmeanuncseuoiftatbhlies, sbtyudryeawsiolnl oHfuinntstianbgidliotny,LfifoerlScoinegncteersmStraentdeanrtdioOnpaernadtairncghPirvoicnegdmuraeys.bedisposedofafterthe periodsstatedin arAclhlitvheefrosramappleersiaonddosfpfeicviemyeeanrssafnrdoalmltrhaewddaatteaownilwlhbiecrhetthaeinSetdubdyyDHiurnetcitnogrdsoingLnisftehSecfiicnaaclerseipnoritt,s Areftteenrtisounchotfimteh,etmhaeSteproianlsso.rwiIlflrbeequceosntteadc,teHduanntdinhgidsoandvLiicfeesoSucgihetncoenstwhielrletcuornn,tidniusepotsoalroertafiunrtthheer materials subject to. reasonable fee being agreed with the Sponsor. Huntingdon Life Sciences will `ofthe final report n is archive retain the Quality indefinitely. Assurance records relevant to this study and a copy 001584 150 MIN 3141022208 RESULTS aTrheeprreessuelnttseodbtianiTnaebdlewsith1 tPoer1l0u.crTohoectmaeneasnulvfaolnuyels fqluuootrieddeh(aPvOeSbFe)enancdorproescitteidvetocotnhteronleacroemstpowuhnodles number. `The absenceofcolonies on sterility check plates confirmed the absenceofmicrobial contamination. dTehnesittoytaolftchoelocnuy lcotunuotrfsteohsne niuntdriiveindtuaalgaorrgpalnaitsemss.(see Tables) confirmed the viability and high cell `tThheecmureraenntrheivsetrotriacnalcocloonntyrocloruanntgseofofrtthhee sloalbvoeranttocroyn.troAlpspwreoprreiawtiethpionstihtiev9e9c%ontrcoolnfcihdeemnicceallismi(twsitohf c9onmfiirxmiwnhgerseensrietqiuviirtyedo)ftihneduccueldtusruebssatnandtiaacltiviintcyreoafstehsei9n remvixe.rtant colony numbers with all stains, FIRST TEST (RANGE-FINDING) NthoetseusbtsertasnitriaailnsinfcorlelaosweisingnerxepvoerstuarnetctoolPoernfylonruomobcetrasneosvuelrfocnoynltoflluocroiudnets(PwOeSrFe)aobtaainnyecdownictenhtarnaytoiofn in therthe preorasbseencenof$c9meix. tNooPveirsfilbulreotohcitnanniensgoulfftonhyel bfalcukorgirdoeu(nPdOSlFa)w.nofAnomraexviemruamnetxpceolslusrweacsonocbetnatirnaetdiofnoloofwSi0n0g0euxgp/opsluartee. was,therefore,selectedforuseinthesecond test. SECOND TEST Nthoe tseusbtsetransttiaailnsifnoclrleaosweisngienxrpeovesrutraenttcooPleornfylonruomobcetrasneosvuelrfocnoynltrfolluocroiudnet(swPeOrSFe)obattaainnyedconwcietnhtarantyioonf in cther the presence or absenceof 9 mix. NtooPveirsfilbuloertohcicntnainncgsouflftohney bfalucokrgirdoeu(nPdOSlEa)w.nofnon-revertant cells was oblained following exposure CONCLUSION sTthoiswecdonncoleuvdieddentchaet,ofumnudteargetahicatcetsitvictoyndiinttihoinssbaecmtperlioayledsy,stPeemr.lvoroostanesulfonyl fluoride (POSF) 001585 6: | MIN 314022208 REFERENCES mAuMtEaSg,enBNw.it,htMhceCSAalNmNo,neJl.laanmdamYmAalMiAaSnAmKiIc,roEs.om(e19m7u5t)ageMniectihtoydtsestf.orMdiedtaecrtoinngRecsa.rc3i1n,o5g4e7n.s36a4n.d MB`auGcaAtgeTreEinaHilOcUmiSuytEa,TteisDot.niGnga,.ssRaORyesWpLoirnAt:.NKDIP,RaKrLtRL.A,INWrDeIv,LisCeDdO..JX.,(BPEa4,s)iC.cAMLiUaLKaAgENeMnDiSEciRSt,uybR-TDceo.smsm:aintdUieKFeEORMoSnSGTuREieRdc,eolmRi.mnee(ns1df9e9od0r). Procedioes, pp.13-61.CambridgeUniversity Press, Cambridge. L`GERGEAETNO,RM,HML,. N(I1C9H8O)LMSu,tWa.gaenndteRstAiMngEuLs,ingC.tr(Epd"s)r.eveHrsioan inn EodscfhMeburtiacogheinaoiccoikltiyinTeKstILPrBoEcYe,dirBeJs., Second dion, pp.161-187, Elsevier Science Publishes BY, Amsterdam. ICH (1995) Genotoricity: Guidance on Specific AspectsofRegulatory Genotoxicty Tests. ICH (1997) Genotoricity: A Standard BatyofGenotosicity TestingofPharmaceuticals. TMWAEHAOTNS,,GDAJ.T,(19G8R9E)EANn,alyMsHisLo,fdaMaI.DfDrLomETmiOcNro,biaB, lMIcTolCoHnEyLaLs,sayLseinG:.,KIRROBKILNASNODN,,DWJ..D.(Eadn)d. o'fUKMuEtMaSgSenicuitybTes-t Dactoa,noGpupi-md2e6l-6im5n.e CiafmobtrMruitdtaggeeeUnniicveersiTteystPirnegs,s,ReCpaomrbt.riPdagret. Ll, Sistical Evaluation MuMtAaRrOoNn,ReDs.M.13a,nd17A3-M2E15S., BN. (1983) Revised methods for the Salmonella mutagenicity test. 001586 1 TALE Rests cianswith ypimariam TAS: test 1 (angeTodin) MN314022208 rNaoe] sin r-on| 4 ene 3m o-r roeses.ble sity ck oop) : rcotse ret Go = rroossee saopse ++ a drroossr oosuu ++ " dsroosste Csopop + 25 Cioows es Eo TawE [si [e ol] afloosst arsao aala|u| w[wae foosse sooon 5" ||ew [|u| ws ljoossee a aso $a5 l|au f[uwlsn [[eeod Bemspr [[wwene [ Jse sw s-- e[ [G 555w ]] [NT oter s pole) [mw Jr[am [ae|e| ners stc Sombatbiois.n1,224p 21 icloncon) 001587 os TanLE2 Results ctanedwith. ophimariem TAS:tet 2 MN 31422208 Jo on,STtes sock locsei,n vce froosre rroossee Fos [ofwoess rroossee rroossee [[Ameetsme (e|mNoinei;g1n0e% dngitu,tionaofcs sonic rr Johonn c 3[ cone GEoon + 55 aarea ++ 5; osu + s == 5Ja5[1oo] aasnm - x5 | |= sooonn aFE | Gromer Tw [5s%o[[5s[e5a|+er]] 7 ES EC CCE TI ET : wn Sanctpiboe.n1, 2.30 17 od olny on) 001588 0 Tames Results obtained with S. typhimurium TA100: test 1 (range-finding) MN 314022208 Astin ssoonri | A orm --: Foeses.strseyck com : ofsyces rT = wr ppoosset sropnmo ++ s-o o= roossee Cooonp ++ wwot u4s ppoosset Gwoasn ++ i5 0- [Tilrows Ta [a[a[ova] | poposste rpovee || u1ss isppooswr oconean | |wB roosse [ree rn | [[CffopmetibreGw__[Tomn [ [o wr as a] r [finns swan [0 [on [en]a [N(oenem;i10%cdoirlueti,onoufes . w| [<1] 4J Sandotr a -- 001559 0 TABL4E Resultsabsinedwith.phimariarm TAIOO:et MN 3141022208 sion pSomne | A orem i ot e$2r feny: tr sy eck opp : rJosy ctu ET wT rroosses awonn ++ || 1 w|| 1os6 drroosse w os e ++ || 1us w|w |0 [orwoses om 5To[iw [oEBr[wel5] laloosset raosum 0= sproossee sooosgupupn 2nse [IAmE ma ar Tw[0 w3 w[wa] I cE ET EE ET o[emrecurr, pt . 0 wo | 4[SiSa vUt 001590 a TABLsE Reso cso with. phimariam TASS: et ragefio) Ma 3141022208 sion B= eetSl iycock reorsie hock Froosse rroossee lorossee rose [oTwFess isfrroosst srpoossee rroossee [[oleasmi IC Rare 1T 0%gona erm =SE.a [Jec I=] comp : ell G saano + |m | m |e e |u| os wwooue ++ || ||x 0|n ||wu]|| Gcoowunns ++ | 2|v ||B ||%w ||u| aspen + |u| | wl o=T 5[& [ow] aaspseusr o[0s w[a |6 u||| wcooeer | 5 | [6 aa |[| ws aasnpeesn - | | ||i | lw | |w]||2 Ggi +=mo onT[aaa[lw]] 0 ES ET 0EI EE PEreeoveoes.n1,23n42 Co lncnc 001591 2 Tames Results obianedwitS. pharm TAISSS:ts2 NaN 3141022208 sion ocrmee emresreiyahecek crotse, vce rrooswe droossee ose [owFoers rroossee rroossee [[oolwAemsine: [CofiRcia1m0%tansin:oF veomgetectauger ps fSromset BN c e:r : opus Go opT i0s wTsT sJeorsuopn + 2i w5e fren w wl --+ I= [w 0 o[=CRE] aameo nw vl| 7 soonp w 2 wl Jo[aw[=a]| | swim[ww] | A PEracvtdssa. 1,230 17 od slony cous) 001592 =n: TABLE? Results cbtwitih.opnhinearidam TAISS: est 1(ranging) MIN 314022208 tion i 1 eebrstyce rJoceshe.ock rroossee dsfrroossre dlrroosser sfrosr [Oiwoses iasroosse roosset elpoosstt [[[ieeAtsmamsrie o0nGi:nof a Sonic | 4 Ji > oman : S feoomio en aSI) =2 [opiuesee+ | 2 2u ooppee ++ || %2 25 ws | 1 = Gow 1ToCE [%[5133] e ro n wvo | fw 5: Qossu ww | |e 5: sWsoirnnsg 5RElw 5: Grashme +s [T5w[[oe ol|o a]] [w aw |e e] |fme ee ta | 4Sc ani dep vin1,220p 42onl o. lnysr) | v [+] 001593 as TALES Results binedwih. pphimarlam TAISS 2 MN 3141022208 Jo nbSt sityduck rosie,y heck rroossee drroosse rose [lfoowse rroossee rroossee [[fmeessts [CiAm-- oneri-- ve oemvi icuse, es some | 4 Jl i coop : o apT+ srs u ++ pose ow Se To[ov [%[aCR l] asoounp "5 wwss scooopuuripes "5 o|l: Grom vw [ 9% [Wm w Jse [ale s]| Gogh J[we[| a | | . 4BSxunt ederxt1,240 17 ooo coun) 001594 as MIN 314022208 Tames Renu ahaa withEcllWrAKMI0E (CHI: st 1 (rung din) roue] ction fmroxnt) jlo) IA c ToNor ter rlityycc 3: Jroise. heck com Froosee rose oswmen + [ mo o|e |r | oTw] E mses + |e | me | om| os rroossee rose scopeer ++ | wwm s|e w|me |||| a Goer + |m os |e |e |e rose [OTimoe arsmws + |w lm wo [us| a GoTr m w o o[mw] ] isaffroossre wespmaee m - |iwus w|es | |oe|| ow sppoosset sopeer - | [5m0 f[mwsw |||e| oonw rflroosstt a[oerse | w EN mEN I| B|Vwl|w [P[[hmlo eearsmsen Owr e J [5T[ [w5o w[owo[wmwoi|a|]| NaTovGrerrr |p[eee ne | =[=] " BE 4*ESuxmitpdrtoise.1r, 202 elcolony cen) 20 Fah ei 001595 0 TABL1E0 Resets cane with EcolWor AlGKMIOL CMI): tt MN 31422208 sien rsomte Te j7l 1 roesee.trsey ce on : FJoyr cot ST Es wT rroossee G aeos ++ == wwoi|| = rroossee Gooop ++ wwso wwow|| =an [oosee Em waa [we [wwi rroossee aa ma - Iwn ` rroossee Consg w0t 55 C[meaemsi Gov +T[m[ omr w[e [wmeas ]|a7]| [eer0edos nor ose ion[oo oe [| [oer Pcrpelss.e12.00 1 olleyon) 260Fe sr facie [= =| 001596 n MIN3141022208 APPENDIX1 Historicalcontrol data Presentedbelowarethehistoricalcontroldatafromtheperiod 1 April 1997to 30September2001. Untreated controls swin TAI00 TAISIS WeaeApOMOL TASS TAISST (cman) S9mix See Te Minimum wow on Maximum M9 16s 3 Mean 09 ue 18 No.ofvalues 39 33 307 Sunduwdde16vi2 si3 on Upper9%limit ISI 168 33 Lowerso%limit 76 78 12 0% 10 12 31 24 31 29 10 10 6 Wm 20 a5 se 16 38 4 28 3 35 B 4 5 2m 49 ss 6 2 28 77 BH 21 38 32 3s 23 35 76 Positive contro Swain Somix MMaixniimmuom MeNoaonfviies Sundwddevigion a0 TAISIS See W@o@W MWm) HGG2 6 480s 1set BseSl 2T0Ms M409;AMS M1260 M17I5 810889 M119 a1946 7194 WRArARKMIOL TASS T(cmT an) H w(0) GI DBMB) 2I2M I6SH 0649 923 1S03u1 41828 41135 290 71S B16O5 TASS @HEh) 1093 s24e6 359 8800 W(E)NENNSGNpp3Ggg.. (ENG 24g @(SAodFiu2m0si04d5ge 0.535. ((8)-2ANmiiwnoofaucorri1ed3npig0e.nuge 0)2BeAnmaisnloaslnptyhrSreauncg2ee.unge. 02Aminosnthra1c0e5n. 001597 8 Inm--et" ` MIN 314/022208 SiSer a8,MRTH, & "0 ET `THEDEPOA FHER ALTHT OFM THEE GOVEN RNMT ENT pI EFer-- Lm.etai -- EEreREr-- BEreJ eE= sEEeanlmTRreae,s Eye Ecosystems. soto Sa e roTh I t Te N mae 29January2001 Be fier eeseer fA. VULSYS