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CORNINGHazieton MUTAGENICITY TEST ON T-6358 30 IN AN IN VIP'OMOUSE MICRONUCLEUS ASSAY FINAL R-EPORT AUTHOR Hemalatha Murli,Ph.D. PEP,FORMING LABORATORY Coming HazletonInc.(CHV) 9200 Leesburg Pike Vienna.Virginl'a'-"-182 LABORATORY PROJECT IDENTIFICATION CHV StudyNo.: 17388-0-455 SUBMITTED TO 3M 3M Center,Building220-2E-02 St.Paul,Minnesota 55144-1000 STUDY COMPLETION DATE May 14, 1996 CHV Study No.: 17388-0-455 1 of24 CORNING Hazleton QUALITY ASSURANCE STATEME-NT ProjeTcittteI@nUivoMouseMicronucieAusssay Pr01ectNo.: 20996 ProtocolNo.: 455 Assay No.: 17388 EditionNo.: 17 QuaiitNA,ssuranceinspectionosf thestudyand reviewof thefinalreportoftheabove referenced projecwtere conductedaccordingtothe StandardOperatingProceduresof theQualityAssurance Unitand accordingtothegeneralrequirementsof theappropriatGeood LaboratorNPractice regulationsF.indingsfrom theinspectionasnd finalreportreviewwere reportedtomanagement and tothestud-d,i,rectoorn thefollowingdates: Insl2ection/Date FindingsReRgrted Auditor TestArticleDilution/03/05/96 03/05/96 C. Smith Dosini!/03/05/96 03/05/96 C. Smith DraftReportReview/05/01,02,'1996 05/0211996 S. Ballenger FinalReportReview/05/14/1996 05/14/1996 S. Ballenger QualityAssurance Uni@J Date Released CHV Study No.: 17388-0-455 CORNING Hazleton STUD @'COMPLIANCE AND CERTIFICATION The describedstudn,was conductedincompliance withtheGood Laborator-P,r-acticerep-ulations assetforihintheFood and Drug Administratio(nFDA) Title21 oftheU.S.Code of Federal ReL,ulationPsart58.issuedDecember 22, 1978,(effectivJeune '-'01.979) withanN applicable amendments. There were no significandteviationsfrom theaforementionedregulationosr the signedprotocolthatwould affectheintesiriotfythestudyor theinterpretatioofnthetestresults. The raxkd,atahave been reviewedby theStudN,Directorw,ho certifitehsattheevaluationof the testarticlaespresentedhereinrepresentsan appropriateconclusionA@ithitnhecontextofthe stud,d.e,siizannd evaluationcriteria. Alltestand controlresultisnthisreportaresupportedbv an experimentaldatarecordand this recordhas been reviewedby theStud,@D,irector.All raw data.documentation.records,protocol and a copy of'thefinalreportgeneratedas a resultofthisstudvwillbe archivedinthestorage facilitioefsComing HazletonInc.foratleastone yearfollowingsubmissionof the finalreportto theSponsor.Aftertheone yearperiod,theSponsor may electtohave theaforementioned matenalsretainedinthestoragefacilitioefsComing HazletonInc.foran additionapleriodof time.orsenttoa storagefacilitdyesignatedby theSponsor. Submitted B@,,: Stud,,D,irector: Hemalatha Murli,Ph.D. ,\IammallanCvtogenetics DepartmentofGeneticand CellularToxicology Study'Completion Date CHV StudyNo.: 17388-0455 3 CORNING Hazleton TABLE OF CONTENTS PaL,eNO SLIN1.MARY .. ................. ...................... . . - -- 6 1.0 SPONSOR ..............................................-."........... -.0 MATERIAL (TestArticle)............................................7... 2.1 Client'Isdentification 2.2 Date Received 2.3 PhysicalDescription 2.4 GeneticsAssa,,.No. 3.0 TYPE OF ASSAY .............................................7 ......... 4.0 PROTOCOL NO ............................................7............. 5.0 STUDY DATES ...........................................7............. 5.1 Initiation Date 5.2 ExperimentalStartDate 5.3 ExperimentalTerminationDate 6,0 SUPERVISORY PERSONNEL ..................................7.......... 6.1 Study Director 6.2 LaboratorySupervisor 7.0 OBJECTIVE .............................................7.............. 8.0 MATERIALS .............................................8 ............. 9.0 SOLUBILITY AND STABILITY: .................................8 ......... 10.0 DOSE SELECTION STUDY ....................................9 .......... 10.1 Dose Selection 10.2 Dosing Information 10.3 Resultsand Interpretation 10.4 Conclusion 11.0 MICRONUCLEUS STUDY ....................................10.......... CHV Study No.: 17388-0-455 4 CORNING Hazleton 111. DoseSelection 11.-'NlicronucieusAssa,@D,osing Information 12.0 BONE MARROW'HARVEST. SLIDE PREPARATION AND ANALYSIS ......1.2 13.0EVALUATION CRITERIA.......................................... 13.1 General I Data Presentatioannd Interpretation 14.0 RESULTS AND INTERPRETATION ...................................... I-@.0 CONCLUSION .........................................1.4 ............ 16.0 REFERENCES ..........................................1..4..... 17.0 DEVIATION FROM THE SIGNED PROTOCOL .....................1.5...... 18.0EXPERIMENT DATA TABLES ................................16.... CHV StudyNo.: 17388-0-455 5 CORNING Hazleton SU@IVIMARY ivlutagenTiecsito-n,T-6358inanInlit-NoIous'evllcronucAisesuas-, . The objecti,.e of this in i,ii-o assav was to evaluate the abilit,,, of the test article. T-6-',-i8. to induce micronucieilnbone marrow polychromaticervthrocvteosf Crl:CD-I'(ICR)BR mice. Inthedose selectiosntudy.thetestaniclewas solubilizeidndeionizedwaterand dosed b,,oral @,avaL,aet200.400,600. 800.and 1000 m2/kg. Sixanimals(threemales and threefemales)" ere assignedtoeachdosegroup. Animals were observedforthreedavsafterdosingfortoxicsilns and/ormonalliNI. Based on theresultosf thedose selectiosntudy.themaximum toleratedose was estimatedas 800 mg/kg. Inthemicronucieusassay.thetestarticlweas solubilizeidndeionizedwaterand dosed b,,o,rali2avageat1-00,400.and 800 mg/kg. Ten animals(fivemales and fivefemales) were randomly assignedtoeach dose/harvestime group. Vehicleand positivecontrolgroups, euthanatizeadpproximately24 hoursafterdosing,were includedintheassav.The animals dosed with thetestarticlweere euthanatizeadpproximately24,48 and 72 hoursafterdosingfor extractioonf thebone marrow. The testmaterialT,-6358.did not inducea significanitncreaseinmicronucleiinbone marrow polychromaticerythrocyteusndertheconditionsofthisassayand isconsiderednegativeinthe mouse bone marrow micronucieustest. CHV StudyNo.: 17388-0455 6 CORNING Hazleton klutagenicTietsnt-onT-6')-i@n8aninv-i,M-oouseNlicronucieAusssa,, 1.0 SPONSOR:3M 2.0 jvlATERIAL (TestArticle) -,.I Client'IsdentificatioTn-:6358 @.2 Date Received:Januan,16,1996 2.3 PhysicalDescriptionW:hite powder 2.4 GeneticsAssa),No.-.17388 3.0 TYPE OF ASSAY: In T@ivoMouse Micronucieus Assay 4.0 PROTOCOL NO.: 455.Edition17 5.0 STUDY DATES 5.1 InitiatioDnate: January 18.1996 5.2 ExperimentalStartDate: February20, 1996 5.3 ExperimentalTerminationDate: April16,1996 6.0 SUPERVISORY PERSONNEL 6.1 Study Director:Hemalatha Muril,Ph.D. 6.2 LaboratorySupervisor:Monica Vegarra,B.S. 7.0 OBJECTIVE The objectiveofthisinvivoassaywas toevaluatetheabilitoyfthetestarticleT,-6358. to inducemicronucleiinbone marrow poivchromaticerythrocyteosf Crl:CD-I'(ICR) BR mice. This studywas conductedusingmodificationsof theproceduressuggestedby Heddle etal.(1983). CHV StudyNo.: 17388-0455 7 CORNING Hazleton 8.0 MATERIALS Adultmaleandfemalemice.straiCnri:CD]-'(ICR)BR. "-erpeurchasefdromCharles Ri@,-LearboratoriPeosr.tagMeI. Thishealthr\a-n.dombredstraiwnasselectetod maximize geneticheterogencitna.nd atthesame time assureaccesstoa common source. The protocolforthisstudywas approvedby theCHV-ACUC priortotheinitiatiootn- dosing. Animals were housed up toseven percage duringquarantinea,nd housed up tofi%-aet randomization.The temperatureand relativheumiditywere maintainedat726'F and -@-5=I respectively, except on Februan, 17. 18. 19, 24 and 25. 1996. for the dose selection stud@-, when the relative humidit@, was recorded as 39. 1'/"0,37.30/@. 34.59,b, 3'-.5"/'0,34.40/0. and 20.8%, respectively, and on March 2. 1996. for the micronucieus study. when the relative humiditv was recorded as 35.5%. A 12-hour light/ 12-hour dark c@,-ciewas maintained. A commercial diet (Purina' Certified Laboratory Pellets ' 0 5002) and waterwere availablaed libitumforthedurationofthestudy.The feedwas analyzed by themanufacturerforconcentrationosf specifiehdeavy metals,aflatoxinc.hlorinated hydrocarbons.organophosphatesa.nd specifiendutrientsT.he waterwas analyzedon a retrospectibvaesisforspecifiemdicroorganisms.pesticidesa,lkalinithye.avy metals.and halogens.Sanitizedcagingwas used forhousingtheanimals.Personnelhandlin2 animalsor workingwithintheanimal facilitiweesre requiredto wear suitablperotective garmentsand equipment. Animals were quarantinedforsevendays beforebeingplacedon study.Animals were randomlyassignedto studygroupsand were individuallwyeighed priortodosing,All animalswere dosed based upon theindividuablody weights.Animals were uniquely identifiebdy eartag. Dose or treatmentgroupswere identifiebdy cage card/label, At theterminatioonf thestudyallsurvivinganimalswere euthanatizebdv CO, followed by penetratioonf thethorax.Any extraanimalsnot used forthestudywere euthanatized by CO. followedby penetratioonf thethorax. 9.0 SOLUBILITY AND STABILITY: The testarticlTe-,6358,was suppliedasa whitepowder. The solubiliotfythetestarticle was evaluateidndeionizedwater.A clearc,olorlesssolutiownas obtainedata concentratioonfabout445.2mg/mi. The stabilitoyf thetestmaterialunderthedosing conditionsof thisassayistheresponsibiliotfythesponsor. CHV StudyNo.: 17388-0455 8 CORNING Hazleton 10.0 DOSE SELECTION STUDN' 10.1 Dose Selection Dose levelsof 200.400. 600. 800. and 1.000 miz/kg%%-eraedministeredb%-oral !,,avagfeorthedose selectiosntud,,. 10.2 Dosinp-Information The animalsused inthedoseselectionassaywere dosed on Februan,20. 1996. The weight rangeoftheanimalsused inthedose rangefindingassavwas 27.734.6and 21.6 -25.7grams.forthemalesand females,respectivelyD.osing solutionwsere preparedjustpriortodosingand were preparedby making a 100 mg/ml stockforthehighdose(1000 mg/kg).Thiswas preparedby adding 11.5ml of delonizedwater(Lot# 19,preparedatCHV) tol.20g of T-6358. resultinigna clearcolorlesssolutionD.ilutionosfthisstockwere preparedfor the200.400. 600,and 800 mg/kg dose levels. Dosing was achievedusinga 10 ml/kgdosingvolume. Allanimalswere eight weeks and one day oldatthetimeof dosing.An outlineofthedosingscheme is foundinthefollowingtable. A totalof 30 animalswas used inthisassay. DOSE GROUPS TREATMENT mF ----------------------------------------------------- T-6358 200 mg/kg 3 3 400 mg/kg 3 600 mg/kg 3 3 800 mg/kg 3 3 1000 mg/kg 3 3 -------- ---------------------------------------- Alldosesgivenwere on an acute(one-timeonly)basis. 10.3 Resultsand Interpretation Allanimalswere exarninedafterdosingand dailythroughoutthedurationof the study(threedays)fortoxiceffectasnd/ormortalitiesA.llanimalsappeared normal immediatelyafterdosing. CHV StudyNo.: 17388-0455 9 CORNING Hazleton Approximatelv one hour afterdosinv-.allanimals atthe 200 and 400 mg/k-g dose levelsappeared normal. All females and one male atthe 600 mg/kg dose level appeared hypoactive with themale alsoshowing lacrimationin both eyes. The remaininiamales appeared normal. The males at the 800 mg/kg dose level appeared normal. The females atthe 800 mg/k-g dose leveland allanimals at the 1000 mg/kg dose levelappeared hypoactive. Approximateiv 7-1h1ours afterdosing,allanimals atthe 200, 400. 600 and 800 ml,.ikgdose levelsappeared normal. At the 1000 mg/kg dose level.one male (;46485) and one female (46504) were found dead. The remaining males appeared hypoactive,with one male (# 6486) alsoshowing eyes glued shutwith chromodacrvorrhea. The remaining females appeared hypoacti-,,weith hunched postures. Approximately 45 hours afterdosing.one male (# 6486) at the 1000 mgfkg dose levelwas found dead. All remaining animals atalldose levelsappeared normal. The mortalitydata forthisassay are summarized in the following table: Summary of MortalitiesWithin 3 Days in Mice Dosed Acutely with T-6358 Treatment 200 mg/kg 400 mg/kg 600 mgikg 800 mg/kg 1000 mg/kg Male 0/3 0/3 0/3 0/3 -2/3 Female 0/3 0/3 0/3 0/1) 1/3 10.4 Conclusion Based on theseresults,the maximum tolerateddose was estimated to be 800 mg/kg. 11.0 MICRONUCLEUS STUDY 11.1 Dose Selection Based on resultsfrom the dose selectionstudy.dose levelsof 200, 400, and 800 mglkg were selectedfortestingin thisstudy. 11.2 M'icronucleusAssay Dosing Information The animals used in the micronucleus assay were dosed on March 5, 1996. Cyclophosphamide (CAS # 6055-19-2-,Sigma, Lot # 44H0486), the positive CHV Study No.: 17388-0-455 10 CORNING Hazleton control.was solubilizeidnsterildeelonizedwater(Lot:'IQ,preparedatCHV) and ",asadministeredbv oralv-a,.-aagte80.0mv/kv-.The vehiclecontrol. delonized %-.-at(eLrot # 19,prepared at CHV). %%,aasdministeredconcurrenti%,@ith the testarticleata volume of 10.0mi/kg. The A-eightranp-eof theanimals used in themicronucieusassaywas 28.) -35.2and 22.0 -29.1grams forthemales and females.respectively.The dosing solutionsforthe assa@-were prepared b@,' making a 80.0mg/ml stockforthehigh dose (800 mg/kg). This was preparedbN addinp thevehicleto2.1200 g of T-6358 up toa volume of26.5 mi. A clear colorlessolutionwas obtained.Dilutionsofthisstockw-ere preparedforthe remaining dose levels.A second group of animals (designatedSecondar--D,o-se Group) was alsoassignedtothestudvand was dosed withthehigh dose of'the testarticle.These animals were oni-,u,sed in the assav as replacementsforan%which died intheprimary dose group. Ten animals(fivemales and fivefemales)were randomly assignedtoeach dose,'harvesttime group. Vehicleand positivecontrolgroups,euthanatized approximately24 hoursafterdosing,were includedintheassay.The animals dosed with thetestarticlweere cuthanatizedapproximately24,48 and 72 hours afterdosing forextractionofthebone marrow. An outlineof thedosingscheme isfound inthefollowingtable: Dosing Scheme forMicronucieus Assay Number of Animals Assigned Treatment T-6358 200 mgikg Primary Dose Groups 24 Hr 48 Hr 72 Hr MFMFMF 55 55 55 Secondarv Dose GroupsA' Male Female 400 mg/kg 55 55 55 - - 800 mg/kg 55 55 55 5 5 Vehicle Control, deionized water, 10.0 ml/kg 55 -- -- - - PositiveControl,Cyclophosphamide, 80.0mg/kg 5 5 - A The animals assignedto the secondarydose groups were dosed and were only used to replaceanimalswhich died intheprimarydose group atthehigh dose level.Allextra animals not used as replacementswere euthanatizedatthe completionof the trial. The age of theanimals atthetimeof dosingwas eightweeks and one day. A totalof 120 animals was used in thisassay. Volumes dosed were 10.0ml/kg and were based upon individualanimal weights. CHV Study No.: 17388-0455 CORNING Hazleton 12.0 BONE lvIAPROW HARVEST. SLIDE PREPARATION AND ANALYSIS At theappropriateharvesttime.the animals were euthanatized%.%-iCtOh. folloa-edb, penetrationof thethorax. The adheringsofttissueand epiph@-sesof both femora were removed. The marrow was flushedfrom thebone and transferretdocentrifugetubes containing3 -5 ml bovine serum (one tubeforeach animal).Followingcentrifugatiotno pelletthetissue.thesupernatantwas removed by aspirationand portionsof the pellet %k,ersepreadon slidesand airdried.The slideswere fixedin methanol,and stainedin Nia,@--Grunwaisdolutiontollo"-edbv Glemsa (Schmid, 1975).The air-driesdlides-,%ere co%,erslippeudsing Depex' mounting medium. The slideswere coded foranalysisa.nd scoredformicronucieland thepolychromatic er-N,throcy(tPeCE) tonormochromatic erythrocyt(eNCE) cellratio.Standardforms Alere used to recordthesedata. One thousand PCEs per animal were scored. The frequencyof micronucieatedcellswas expressedas percentmicronucieatedcellsbased on the total PCEs presentinthescoredopticfield.The normal frequencyof micronucleiinthis Crl:CD-]'(ICR)BR strainisabout0.0-0.4%. The frequencyof PCEs versus NCEs was determined by scoringthe number of PCEs and NCEs observedintheopticfieldswhilescoringthefirst1000 erythrocytes. 13.0 EVALUATION CRITERIA-. 13.1 General The criterifaortheidentificatioofnmicronucleiwere thoseof Schmid (1976). Micronuclelwere darklystainedand generallyround,althoughalmond and ringshapedmicronucleioccasionallyoccurred.Micronuclelhad sharpborders and were generallybetween 1/20and 1/5thesizeofthe PCE. The unitof scoring was themicronucleatedcell,notthemicronucieus;thustheoccasionalcellwith more thanone micronucieuswas countedas one micronucieatedPCE, not two (or more) micronuciel.The stainingprocedurepermined thedifferentiatiboyncolor of PCEs and NCEs (bluish-greaynd red,respectively). 13.2 Data Presentationand Interpretation Data aresummarized by sex and dose groups forthe differentime points. Individualanimal data are alsopresented.The analysisof thesedatawas performed usingan analysisof variance(Winer, 1971) on eitheruntransformed (when variancesarehomogeneous) and ranktransformed(when variancesare heterogeneous)proportionsofcellswith micronucleiper animal. Iftheanalysis of variancewas significan(tp<0.05),a Dunnett'st-tes(tDunnett,1955; 1964) was used todeterminewhich dose groups,ifany,were significantdliyfferenftrom the CHV Study No.: 17388-0455 12 CORNING Hazleton neaatic%o,netroAln.alyseswere performedseparatelf,oreachharvesttimeand sexcombinatioTnh.ecritefroiradetermininga positivreesponseinvolveda statisticalsiiviznlficandtose-reiatedincreasein micronucleated PCES. or the detectionof a reproducibleand statisticalsliygnificanptositiveresponse torat leastone dose level.A testarticlethatinduced neithera statisticalsliygnificant dose response nor a statisticalsliygnificantand reproducibleincreaseatone dose levelwas considered negative. In eithercase.the finaldecisionwas based on scientifijcudgment. 14.0 RESULTS AND INTERPRETATION: All animals were observed immediately afterdosing and periodicallythroughout the durationofthe assay fortoxicsymptoms and/ormortalities.All animals in the vehicle and positivecontrolgroups appeared normal afterdosing and remained healthy untilthe appropriateharvesttimes. All testarticledosed groups appeared normal immediately and approximately 1.5hours afterdosing. Approximately 22 hours afterdosing.atthe 800 mg/kg dose level,one male (# 6748) and one female (#6764) from the24 hour harvestgroup and one male (# 6753) from the 48 hour harvestgroup were found dead. All remaining animals atalldose levelsappeared normal. Approximately 23.5 hours afterdosing,at the 800 mg/kg dose level,one female (# 6803) from the secondary group and one female (# 6766) from the 72 hour harvestgroup were found dead. One female (# 6790) from the secondary dose group appeared hypoactive. Approximately 46 hours afterdosing,atthe 800 mg/kg dose level,threefemales (O's6761, 48 hour harvestgroup; 6784, 72 hour harvestgroup, 6790, secondary dose group) were found dead. All remaining animals at alldose levelsappeared normal. Approximately 70 hours afterdosing,allremaining animals atalldose levelsappeared normal. The testarticleT,-6358, induced no significantincreasesin micronucleated polychromatic erythrocytesover the levelsobserved inthe vehiclecontrolsin eithersex or atany of the harvesttimes,except forthe females from the 48 hour harvestof the 800 mg/kg dose group. This isa statisticanlomaly, for the mean of thisgroup, 0.30%, is very closeto the historicaclontroldata (maximum of 0.24%) and withinthepublished historicadlata (Salamone and Mavoumin, 1994). The positivecontrol,CP, induced significantincreasesin micronucleated PCEs in both sexes as compared to the vehicle controls,with means and standarderrorsof 3.06% 0.50% and 4.24% 0.47% forthe CHV Study No.: 17388-0455 13 CORNING Hazleton males and females.respectivel-T,h.e datasummarized bv dose group arepresentedin Table I and individuaalnimaldataarefound inTables2 throuiz7h. Historicaclontrol dataarepresentedinTable 8. 1i.0 CONCLUSION: The testmaterialT.-6358.did notinducea significanitncreaseinmicronucielinbone marrow poivchromaticerythrocyteusndertheconditionsof thisassayand isconsidered negativeinthemouse micronucieusassay. 16.0 REFERENCES-. Dunnett.C.W.: A multiplecomparisonsprocedureforcomparing severaltreatmentwsith a control.J.Am. StatistA.ssoc..50:1096-1121.1955. Dunnett.C.W.: New tablesformultiplecomparisonswitha control.Biometrics2,D:482491, 1964. Heddle,J.A.,Hite.M., Kirkhart.B.,Larsen,K.,MacGregor, J.T.,Newell,G.@k'. and Salamone,M.F.: The inductionof micronucleias a measure of genotoxicity. MutationRes.,JZI:61-118,1983. Salamone.M.F..and Mavoumin, K.H. (1994),Bone marrow micronucieusassay:a reviewofthemouse stocksused and theirpublishedmean spontaneousmicronucieus frequenciesE.nv. and Mol. Mutagen..23,239-273. Schmid.W.: The micronucleustest.MutationRes.,li:9-15,1975. Schmid,W.-.The micronucieustestforcytogenetiacnalysis.Chemical Mutagens: Pn'ncipleasnd Methods forTheirDetectionV,ol.4 (A.Hollaender. ed.).Plenum,pp.31-53,1976. Winer,B.J.:StatisticParlincipleisnExperimentalDesign,McGraw-Hill,New York,Second Edition,1971. CHV StudyNo.: 17388-0455 14 CORNIIYG Hazleton 17.0 DEVIATIONS FROM THE SIGNED PROTOCOL Due to unknown reasons,on Februw-,,17. 18. 19.24 and 2-@.1996. forthedose selectionstudy.the relativehumidity was recorded as 39.1 @'o3.7.30/o3.4.50/,o, .59/o3,4.4%. and 20.8%, respectivel-o,n,,March 2. 1996.forthemicronucieus study,therelativheumiditywas recordedas 35.5%. This had no impacton the animalsor theintegritoyf thestudy. 2. Due toa technicalerror,thewater svstem was not checked on Februar-,24 and 2@. 1996. Although thesvstem was not checked.water was availableand hence there %vasno adverseeffctcson theanimals.and therewas no impact on the inte&,riotf,', the study. CHV Study No.: 17388-0-455 15 CORNING 14azieton 18.0 EXPERIMENT DATA TABLES CHV Study No.: 17388-0455 16 I I CORNINGHazicion TABLE I SPONSOR 3%1 MICRONUCLEUS DATA SUMMARY TABLE REST ARTICLE. T-63%8 ASSAY 17389 I*RE.,@'r,mF,NT DOSE C'ONTROLS HARVEST TIME iHR) 16,%41CRONL.'CLEATED PCE5 ',IEANOF 1000 PER ANIMAL = S@E MALES FEMALES ROTAL "FiilC'LL PoSITiVE W atcr 24 hr C'P80 0 mg/kg 24 hr 0,08. 004 306 = 0 50* 0 08 0.04 424 0 47' 0 08 0 02 3@65 0.38* RATIO PCE NCE MEAN = '-,,E '%IALES 0 (y4@ 0 11 063 . 010 0.60 00081 007 ri,.%ATRTICLE 200 mgjkg 400 mg/kg 800 mgikg 24 hr 48 hr 72 hr 24 ht 48 hr 72 hr 24 hr 48 hr 72 hr 0 14 . 0 O@ 016 = 004 0 10 . 0.05 016 005 0.08 :t0.0,4 010 . 003 0 12 . 006 0 16 z 005 008 = 002 004 002 0,08 O@04 002 002 006 004 010 0.04 026 0,21 004 002 030 0 04* 0 12 006 009 003 0 1.1 003 006 003 Oil 003 009 = 0.03 018 . Oil 008 t 003 022 004, 010 . 003 059 005 056 008 044 006 072 . 0,08 0.66 - 0,13 045 . 012 059 0 13 049 * 008 031 t 008 066 006 0 52 007 061 0 Ob 06' 0 i)Q 0 ;3 0 11 065 006 072 0 17 035 009 056 020 SipntFicantglryeaterthanthecorrespondingvehiclecontrolp.<0.05. CP = Cyciophosphamide CHV Study No.: 17388-0-455 17 CORNING Hazleton TABLEZ .1vilCRONUCLEUS TEST - INDIVIDUAL ANIMAL DATA SPONSOR..3M TEST ARTICLE. T-6358 ASSAY NO.@ 17388 f'REAT@,tENT 24 HOt R IIARN EST klALE ANINIAL PCES" RA FIC) NLI,\4BER 1000 PCEs PCE @NCE VEHICLE CONTROL POSITIVE CONTROL TEST ARTICLI-. \kater CP 80 0 mglkg 200 mgikg 400 mg/kg 800 mgikg 6697 0 01 6741 1 0 io 6744 1 ()4@ 6745 0 0 72 6752 2 1 02 6704 23 0 34 6716 16 066 6720 32 093 6724 42 0 i3 6730 40 0.66 6698 3 066 6701 0 0 75 6729 1 048 6737 2 058 6749 1 047 6699 3 6717 0 6721 1 6726 2 6728 2 0 75 1()0 069 061 O@56 6702 3 064 6703 0 0 38 6707 0 099 6722 1 0,70 6746 2 026 CP Cyclophospharnide .MN Micronucieus PCE Polychromaticcrythroc@-te 0 MN PCEs - MicronucleatedPCEs NCE = Normochromatic crythroc@t,e CHV Studv No.: 17388-0-455 18 CORNING TABLE3 -MICRONUCLEUS SPONSOR. 3Nl TEST -INDIVIDUAL ANINIAL DATA REST ARTICLE@ T-6358 ASSAY NO.: 17388 FREAT.%4ENT 24 NOt'R HARVEST FEMALE ANIMAI NUNIBER a MN PCEs,,' RATIO FCE NCE 1000 PcEs VEHICLE CONTROL POSITIVE CONTROL TEST ARTICLE %kater CP 80.0mgfkg 200 mg/kg 400 mg/kg 900 mglkg 6759 1 071 6762 0 063 6798 1 080 6810 2 045 6812 0 n 43 6757 61 095 6792 37 063 6787 41 091 6794 36 066 6909 37 1 ()0 6760 0 081 6765 1 061 6783 1 0.54 6796 0 080 6799 0 0 52 6767 2 062 6780 1 O@37 6807 0 0 75 6808 0 093 6813 0 0.@7 6758 0 067 6772 1 l@39 6786 1 038 6801 0 0.55 6906 0 061 CP Cyciophosphamide MN Micronucieus PCE Polychromaticcrythrgcvtc tiNfN PCEs = MicronucicaiedPCEs NCE = Normochromatic crythrocvte Hazleton CHV Study No.: 17388-0-455 19 CORNINGHazieton MICRONUCLEUS SPC)NSOR: 3M TEST ARTICLE: T-6358 ASSAY NO.: 17388 FREAT,@.IEN'T 48 HOTIR HARVEST TEST ARTICLE TABLE4 TEST - INDIVIDUAL ANIMAL DATA MALE 200 mg/kg 400 m?)kg 800 mg/kg ANIMAL RATIO NLJ.MBER PCES,, PCE NCE 1000 PCEs 6708 1 6709 2 6713 3 6742 1 6751 1 6719 1 6732 2 6739 0 6747 0 6754 1 6705 3 6711 0 6714 2 6740 2 6756 1 0 58 038 045 0 58 082 043 042 066 066 1 12 0 3() 030 0 54 043 077 ,MN Micronucicus PCE Polychromaticerythrocyte ItMN PCEs = MicronucleatedPCEs NCE = Normochromatic erythrocyte CHV StudyNo.: 17388-0455 20 CORNING Hazicton TABLE5 NIICRONUCLEUS TEST - INDIVIDUAL ANIMAL DATA SPONSOR. 3,M TEST ARTICLE: T-6358 ASSAY NO.: 17388 TREATMENT 48 HOt'R HAR.*EST FEKAALE ANIMAL NUNIBER :sMN RATIO PCES, PCE:NCE 1000 PCEs TFST ARTICLE 200 mpjkg 400 mgfkg 800 mg/kg 6763 1 062 6791 2 043 6795 1 0 36 6804 0 041 6805 0 0 75 6771 0 044 6776 2 093 6789 0 0.54 6797 1 049 6814 2 0,24 6774 2 0 5Q 6781 3 034 6795 3 0 14 6815 4 0 14 Animal found dead MN Macronucieus PCE Polychromaticerythrocyte # MN PCEs = MicronucleatedPCEs NCE = Nonnochromatic erythrocyte CHV StudyNo.: 17388-0455 CORNING TABLE6 .MICRONUCLEUS TEST -INDIVIDUAL ANIMAL DATA SPONSOR: 3%1 TEST ARTICLE- T-6358 ASSAY NO.: 17388 TREA-R.MFNT 72 HO[IR HARV'EST MALE ANIMAI. RATIO PCE&, NU\IBER 1000 PCEs PCE:NCE TEST ARTICLE 200 mg/kg 400 mgjkg 800 mg/kg 6715 3 0.5@ 6725 1 043 6727 1 O@28 6738 0 0 33 6755 0 061 6710 0 f)85 6718 1 0.50 6734 1 0.30 6735 1 048 6743 2 0 13 6700 0 007 6712 1 O@33 6731 1 0 57 6733 1 0 22 6736 1 036 MN Micronucieus PCE PoIN-chromatiecrvthrocvte MN PCEs = MicronucleatedPCEs NCE @ Normochromatic ervthroc%.tc Hazleton CHV Study No.: 17388-0-455 22 CORNING Hazleton TABLE'7 MICRONUCLEUS TEST - INDIVIDUAL ANIMAL DATA SPONSOR: 3.M TEST ARTICLE: T-6358 ASSAY NO.: 17388 TREATMENT 72 IfOI'R HAR%@EST FEMALE ANIMAL NU,MBER RATIO PCES,, FCE-NCE 1000 PCES TEST ARTICLE 200 mgikg 400 mg/kg 900 ma/kg 6768 0 062 6770 05i 6779 1 0 57 6800 0 085 6811 0 048 6769 0 069 6773 11 084 6775 0 0 6' 6792 0 047 6916 2 062 6777 3 1 31 6778 1 04-, 6788 2 0 25 6793 0 0 @7 6802 0 0 22 N4N %licronucieus PCE PoIN-chromaticcrythroc@-te b VN PCEs = MicronucleatedPCEs NCE = Normochromatic ervthrocyte CHV StudyNo.: 17388-0455 23 CORNING Hazleton TABLE8 ,MOUSE.MICRONUCLEUS HISTORICAL CONTROL DATA 7 9; THROUGH 12'95 liic-Fl,CO\FROLS %IIN %IAX Avci '..MICRO,NL:CI.EATED PCEs PER 1000 PCL MEAN OF 1000 PER ANI.MAL = S.E %1/',LES FEMALES TOTAL 0()0 0 22 0 097 @ 0 00' 47 ()()0 ()24 0 09 1@ 0 008 4- 001 0 17 0094.0004 47 RATIO PC[ NCI- %ILAN S F \I,-kLES Fi' 01) ()s; 0,55().0021 47 0 -14 I (I', ig-, .17 POSITIVF CO\TROL.; C @clopht)sphamide8.()0 rngikg .%11N @'@Al X AVG 200 5 69 692 0 240 1 ;o 6 36 3 170 = 0 245 19 2.41 5 38 3 426 10 lg.% IQ 041 0 72 0 577 t 0 020 iq ().40 ()IQ 0 ;98 @ 0 026 IQ Ilt)cin@romatic er-t%hrocyte NC'[' \@)r-mochromatiecn throcyte CHV StudyNo.: 17388-0-455 24 ClfV STUDY NO. PROTOCOL NO. 455, EDITION 17 CORNINGHazleton IN VIVO HOUSE MZCROMUCLEUS ASSAY Corning Hazleton Inc. (CHV) will conduct this study in compliance with Good Laboratory Practice (GLP) Regulations. This protocol, critical phase(s) of the work in progress and the final report will be subject to audit by Quality Assurance in accordance with SOPs at Corining Hazleton Inc. The study will be conducted by CHV at 9200 Leesburg Pike, Vienna, Virginia 22182. PART 1. SPONSOR INFORMATION AND APPROVALS I. SPONSOR IDENTIFICATION Company Name: 3tx Address: 51-. P,,O..i , /)tAJ II. TEST ARTICLE IDENTIFIR-ATION: & @5'9 III. TEST ARTICLE ANALYSIS Determination of the test article stability and the test article characteristics as defined in the GLP regulations is the responsibility of 6he Sponsor. IV. NOTIFICATION OF REGULATORY SUBM:ISSION In order to comply with the GLP regulations, consulting laboratories must be notified if all or part of a study is intended for regulatory submission. CHV maintains regulatory review. Please the results of this study: a master indicate schedule of studies which fall under which agency, if any. might receive rr"@ rr@ Und e termi n ed FDA EPA-TSCA 11------ @LAFF MOHW OECD OTHER EPA-FIFRA 4/95 1 of 10 PROTOCOL NO. 455, EDITIOV 17 V. STUDY DATES Proposed Experimental Start Date: Proposed Experimental Termination Date: VI. APPROVAL OF STUDY PROTOCOL Study Director: Hemalatha Murli. Ph.D. Sponsor's Authorized Representative: />1A/ CORNINGHazieton Date: Date: 4/95 2 of 10 PROTOCOL NO. 455, EDITION 17 CORNINGHazleton PART 2 STUDY PROTOCOL IN VTVO MOUSE M:ICRONUCLEUS ASSAY I. OBJECTIVE The objective of this study is to evaluate a test article for clastogenic activity and disruption of the mitotic apparatus in polychromatic erythrocyte stem cells in mouse bone marrow in vivo. ii. DEFIN'ITIONS Kicronucleus: a small chromatin body. consisting of entire chromosome(s) and/or of acentric chromosome fragment(s), which lags behind at mitotic anaphase. After telophase, these chromosome(s) and fragment(s) may not be included in the daughter nuclei, and my form single or multiple micronuclei in the cytoplasm. Ill. RATIONALE The micranucleus test can serve as a rapid screen for clastogenic agents and test articles which interfere with normal mitotic cell division (Schmid. 1975; Heddle et al., 1983). Kicronuclei are formed from chromosomes or chromosome fragments left behind during anaphase and can be scored during interphase because they persist (Schmid, 1975). In this assay, polychromatic erythrocytes (PCES) ;-n the bone uiarrow are scored for the presence of micranuclei. During maturation from erythroblast to erythrocyte the nucleus is extruded, while micronuclei, if present, remain in the cytoplasm. Detection of micronuclei in non-nucleated cellsis thus facilitated, and time involved in searching for metaphase spreads in treated cell populations is eliminated. Test articles affecting spindle-fiber function or formation as well as clastogenic agents can be detected through micronucleus induction (Schmid, 1975). IV. HATERIA.LS 'k Ar,4-mals Young adult male and female mice of the ICR strain, 810 weeks old at the time of dosing, will be purchased from Charles River Laboratories, Inc., or Harlan Sprague-Dawley, Inc. This strain has been selected to 4/95 3 of 10 PROTOCOL NO. 455, EDITION 17 CORNING maximize genetic heterogeneity and at the same time ensure access to a common source. B. Control Articles Cyclophosphamide (CP, 80 mg/kg; dosing volume of 10 ml/kg) will be used as the positive control article and will be administered by oral gavage. The vehicle control article will consist of the solvent or vehicle used for the test article and will be administered by the same route as. and concurrently with. the test article and in amounts equal to the maxim= volumes administered to the experimental animals. The dosing volume will not exceed 20 ml/kg for oral gavage and IP administrations. The vehicles generally used in the assay are water. 0.51 aqueous carboxymethylcellulose solution, or corn oil. Hazietori V. EXPERIMENTAL DESIGN A. Animal Husbandry All applicable CHV SOPs will be followed. Animals will be isolated by sex. Animals will be housed up to seven per cage during quarantine. and will be housed up to five prior to experiment initiation. Animals are housed under the following climatic conditions: temperature, 720F 6*F; huniidity, 551 151; light cycle, 12 hours light/dark. A commercial diet (Purinaa Certified Laboratory Chowa t5002) and tap water will be available ad lLiiboiirt-T=h.e feed is analyzed by the manufacturer for concentrations of specified heavy metals, aflatoxin, chlorinated hydrocarbons, organophosphates, and specified nutrients. The water is analyzed biannually on a retrospective basis for speci,.@'iemdicroorganisms, pesticides, heavy metals, alkalinity. and halogens. Animals will be quarantined for at least 7 days before being placed on study. Animals will be assigned to study groups at random according to Coning Hazleton Standard Operating Procedures. Animals will be weighed prior to dosing. They will be dosed based upon the individual animal weights. Animals will be uniquely identified by ear tag. Treatment groups will be identified by cage label/card. 4/95 4 of 10 PROTOCOL NO. 455, EDITION 17 CORNINGHazleton Sanitary cages will be used. Personnel handling animals or working within the animal facilities will be required to wear suitable protective garments and equipment. B. Dose Selection The high dose generally will be selected as 801 of the maximum tolerated dose. The high dose should produce some indication of toxicity (e.g., death, depression of ratio of PCEs to normochromatic erythrocytes (NCEs). One-half and one-quarter of this high dose will normally be used as the intermediate and low dose levels, respectively. Use of a high dose increases the likelihood that a weak clastogen willbe detected. and is therefore recommended. if no appropriate range finding finding study can be performed. rangefinding study will be 5000 will be issued as an amendment. data are available. a range The top dose tested in the dose mg/kg. The dose levels tested DOSE PANGEFINDING STUDY The dose rangefinding study will be conducted using five treatment groups. Each of the five groups will consist of 3 male and 3 female mice. Group Designation and Treatment Regimens Group No. 1 Number of Mice Male FemAle 3 3 Route PO Duration (Davs) 3 2 3 3 PO 3 3 3 3 PO 3 4 3 3 PO 3 5 3 3 PO 3 4/95 5 of 10 PROTOCOL NO. 455, EDITION 17 CORNINGHa2leton The route of administration will be oral gavage. In the event that test article characteristics preclude oral gavage. IP injection will be employed. These routes of administration have been selected because they are the most common routes of administration for this test procedure. The dosing volume will not exceed 20 ml/kg for oral gavage and IP administrations. Other routes of administration that may be used are intravenous. intramuscular, sub-cutaneous administrations or by feed. The test material will generally be solubilized in one of the following solvents: water, 0.9Z saline, 0.5Z aqueous carboxymethylcellulose solution, or corn oil. All animals will be dosed based upon individual body weights. Dose levels will be assigned by a protocol amendment. Body weights will be taken prior to dosing. Dosing formulation will be prepared just prior to dosing. Dosing solutions will be prepared and held at ambient temperatures until dosing (0-2 hours). All animals will be euthanized 3 days after receiving a single dose. The animals will be observed daily for toxic signs and mortality for the duration of the study. Animals will be euthanized by C02 inhalation followed by penetration of the thorax. The daily observations of toxic symptoms and/or mortalities data will be used to estimate the Maximum Tolerated Dose (MTD). Doses will then be assigned for the subsequent cytogenetics assay. MICROMUCLEUS STUDY C. Dosing Schedule and Route of Administration Normally an acute dosing regimen (single administration) will be used (see Table below). Harvest will be approximately 24, 48, 72 hours after administration of the test article, and at approximately 24 hours after administration of the control articles. A total of 110 animals will be used. Equal numbers of males and females will be used at each treatment group. An additional group of animals consisting of 3-10 males and 3-10 females may be dosed as a secondary dose group with the high dose of the test material. This group will be dosed if toxicity is expected at the high dose and the animals in this group will only be used as replacements for any which die prior to euthanasia. The use of the secondary dose group will be determined by the study director. Freshly prepared solutions will be 4/95 6 of 10 PROTOCOL NO. 455, EDITION 17 CORNINGHazieton employed. The animalswill be observeddaily for toxic signs and mortality. NUMBER OF ANIMALS USED FOR MICRONUCLEUS ASSAY GrouD No. Treatment Harvest Times After Treatment (Males and Females) 24 Hours 48 Hours 72 Hours i Positive Control 5 + 5 --- 2 Vehicle Control 5+5 --- --- 3 Low Dose 5 +5 5+5 5+ 5 4 Medium Dose 5 +5 5+ 5 5+ 5 5 High Dose 5+5 5+5 5+ 5 Total 5+ 5 5+ 5 15 + 15 15 + 15 15 + 15 TOTAL 25 + 25 15 + 15 is + 15 55 + 55 The route of administration will be oral gavage. In the event that test article characteristics preclude oral gavage, IP injection will be employed. The dosing volume will not exceed 20 mllkg. These routes of administration have been selected because they are the most common routes of administration for this test procedure. Other routes of administration that may be used are intravenous, intramuscular, sub-cutaneous administrations or by feed. D. Extraction of Bone Marrow Euthanasia will be with C02, followed by penetration of the thorax, and hind limb bones will be removed for marrow extraction. The marrow will be flushed from the bone and transferred to centrifuge tubes containing 3-5 ml bovine serum (one tube for each animal). E. Preparation of Slides Following centrifugation to pellet the tissue. the supernatant will be removed by aspiration and portions of the pellet will be spread on slides and air-dried. The slides will then be fixed in methanol. stained in May-Grunwald Solution and Giemsa, and protected by mounting with coverslips. For control of bias, all slides are coded for analysis. 4/95 7 of 10 PROTOCOL NO. 455, EDITION 17 CORNING F. Scoring the Slides An attempt will be made to score one-thousand PCEs per animal. The frequency of micronucleated cells will be expressed as percent micronucleated cells based an the number of PCEs analyzed. The normal background frequency of micronuclei in the ICR mouse strait is around 0.0-0.41. The frequency of PCEs versus mature erythrocytes (NCES) will be dete=ined by scoring the number of PCEs and NCEs observed in the optic fields while scoring the first 1000 erythrocytes on the slide. Hazleton vi. DATA The criteria for the identification of micranuclei are those of Schm.id (1976). Kicronuclei are darkly stained and generally round, although almond and ring-shaped micronuclei occasionally occur. Micronuclei have sharp borders and are generally between 1/20 and 1/5 the size of The PCE. The unit of scoring is the inicronucleated cell, not the micronucleus; thus the occasional cell with more than one micronucleus is counted as one micronucleated PCE. not two (or more) micronuclei. The staining procedure permits the differentiation by color of polychromatic and normochromatic erythrocytes (bluish-grey and red, respectively). Data Presentation The data reported will include the number of PCEs scored. the number of micronucleated PCES. the percentage of micronucleated PCES, and the ratio of polychromatic to normochromatic erythrocytes for each experimental animal. Evaluation Criteria The criteria for a positive response is a statistically significant dose-related increase in micronucleated PCES. or the detection of a reproducible and statistically significant positive response for at least one dose level. A test article that induces neither a statistically significant dose response nor a stat4-stically sign;ficant and reproducible increase at one dose level is considered negative. In either case, the final decision is based upon scientific judgement. 4/95 8 of 10 PROTOCOL NO. 455. EDITION 17 CORNINGHazleton VII. TEST INTERPRETATION The analysis of this data will be performed using an analysis of variance (Winer. 1971) on either untransformed (when variances are homogeneous) or rank transformed (when variances are heterogeneous) proportions of cells with micronuclei per animal. If the analysis of variance is significant (p<0.05), a Dunnett's t-test (Dunnett, 1955; 1964) will be used to determine which dose groups, if any, are significantly different from the negative control. Analyses will be performed separately for each harvest time and sex combination. VIII. REFERENCES Dunnett, C.W.: A multiple comparisons procedure for comparing several treatments with a control. J. Am. Statist. Assoc., 50:1096-1121. 1955. Dunnett, C.W.: New tables for multiple comparisons with a control. Biametrics, 20:482-491, 1964. Heddle, J.A., Hite, M., Kirkhart, B., Larsen, K., MacGregor, J.T., Newell, G.W. and Salamone, M.F.: The induction of micronuclei as a measure of genotoxicity. Mutation Res.. 123:61-118, 1983. Schmid, W.: The micronucleus test. Mutation Res., 3-1:9-15, 1975. Schmid. W.: The micranucleus test for cytogenetic analysis. In, Chemical Mutagens: Principles and Methods for Their Detection. .Vol-.4 (A. Hollaender. ed.). Plenum, pp. 31-53, 1976. Winer, B.J.: Statistical Principles in Experimental Design, McGraw-Hill, New York, Second Edition, 1971. IX. 4195 REPORT FORM&T CHV employs a standard report format for each assay design. The final report will provide the following information. Sponsor identification. Quality Assurance statement. Statement of GLP Compliance. Signature of study director. Test article identification and CHV Study Number. A physical description of the test article and date of receipt will be included in this section. Type of assay and protocol n=ber. Dates of study initiation and completion. Study director and senior technician. Methods. 9 of 10 PROTOCOL NO. 455, EDITION 17 CORNINGHazieton Evaluation criteria. Interpretation of results. Conclusions. References. 0 Test results presented in tabular form. X. CHANGES OR RE7ISIONS Any changes or revisions of this approved protocol will be doc=ented. signed by the Study Director. dated. and maintained with this protocol. xi. ANn4AL CARE AND USE STATEMENT In the opinion of the Study Director, no alternative testing methods are appropriate, the study does not duplicate any previous work with this material, and the number and species selected are appropriate. This protocol will be reviewed by the CHV-IACUC for compliance with regulatory guidelines concerning the care and use of animals. If not in compliance, a modification will be required. Any changes or revisions of this approved protocol will be sent to the CHV-IACUC for their review. XII. RECORDS TO BE MAINTAINED All raw data, documentation, records, protocols, and the final report generated as a result of this study will be archived in the storage facilities of Coning Hazleton Inc. for at least one year following submission of the final report to the sponsor. After the one year period, the sponsor may elect to have the aforementioned materials retained in the storage facilities of Corning Hazleton Inc. for an additional period of time or sent to a storage facility designated by the sponsor. 4/95 10 of 10 AMENDMENT TO THE STUDY PROTOCOL STUDY TITLE: IN VIVOMOUSE MICRONUCLEUS ASSAY PROTOCOL NO.: 455,Edition17 STUDY NO.: 17388-0-455 PageIofI Amendment 42 Section2.ParlV.C. Based on themortalitdyatainthedoseselectiosntudy,themouse micronucieusassaywillbe conductedtestinagqueouspreparationwsith dose groupsof 200,400,and 800 mg/kg. A secondarydosegroup willbe used. STUDY DIRECTOR alathaMuril,Ph.D. Mammalian Cytogenetics DepartmentofGeneticand CellulaTroxicology q Date AMENDMENT TO THE STUDY PROTOCOL STUD@'TITLE: ilvVIVO MOUSE MICRONUCLEUS ASSAY PROTOCOL NO.: 455,Edition17 STUDY NO.: 17388-0-455 Page Iof I Amendment #I Section2, PartV.B. The Sponsor has LD,, datain ratsof 440 mg/kg and inmice of 457 mg/kg solubilizeidnacetone/comoilmixture.Based on thisinformationt,he dose selectionstudywillbe conducted testingaqueous preparations(since thetestarticliessolubleinwater)withdose groupsof 200,400, 600,800, and 1000 mg/kg. STUDY DIRECTOR Hemalatha Murti,Ph.D. Date Mammalian Cytogenetics Departmentof Geneticand CellularToxicology