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lInnlteerrnnaatliioonnaall RReesseeaarrcchh aanndd DDecvreell(oqp~mmeenntl CCoorrppovrra~ttiioonn oT" 8 AX sores SPONSOR: smazer: coCOuMzPoOrUDND:: SUBJECT: p-- 3M Company pSriunneiteyt-ibayeiSuybacute hares okey FFlluuoorraadd? FFlluuoorraocchheesmiiccaal! SSeurrffaaccets~anrt FFCo--9355 Ninety-Day Subacu~e Rhesus Monkey Toxicity Study. --Sa 0-20 Director of Reseerch sifu Collaborators: 5e_0. Tessa, Phe, Associate D. C. Jessup, Ph.D., Associate ile Eimet Direc=or of Research ee pression: R. G. Gei!, D.V.M., Vice President ooand Director of Patho!ogy LT oe ot J. S. Mehring, Ph.D., Director of ffs anton Large Animal Toxicology sates sucsrses 13. 197 Date: December 18, 1978 113377--009922 EExxhhiibbiitt 11119911 State of Minnesota v. 3M Co., Court File No. 27-CV-10-28862 11119911..00000011 33MMAA1100006655000044 | f | nierntional RRosecapreohn rantd D DeL veloC CpormR poerantiton _ | Page TABLE OF CONTENTS Page FY Synopsis .......................... i IL Compound ieee II. Compound .......................... 33 IIL Clinical Stufes +s vv svn eau nana llI. Clinical Studies ...................... b4 he eT + teenie &4 A. 1M.etGheodner.a.l .P. roc.ed.ur.e.... .+..s.i....u.u.. e.a......... .c4h 2i.. GCeonmeproaunldPArdomciendiusrter.at.io.n.... .os ..e..e..s..s.. e... 4 32. OCbovmeprovunadtloAndsmin+istrsattioen .v.e..r.r.a.n.e.e.e.r.r. e. e. s 8 43.. COlbisneircvaaltioLnasbor.at.or.y .Te.st.s..+.+..o.. o. ov.v.s.e..nS5 4. 8aCb.liniBHi cEeaBmlAaTto OoLLlaOobRgoyYrcat. o+r. h yL.tTLre.e sLit.se....m..a.a ...i ..i.l.a . .s .i..i..tia . .i. .ir. .i. . .iy . .i. .l S3 3obc&l..0 StUBUarirtioiincnahsaletlymiysicsisaistslr.y.mm. . Lsil. .y.s. .tis. ... .Li. .Li. ..e.. .e.. .i.. .i.. .i.. .i.. .i.. .i.. .i.. .i.. .l.. . 6656 Be Besuld.th Steatvisetincasl Antalaysriser.r.r.r.a.e.e.e.r.e.n.n.n.e. 86 B. R1.esulGtesne.ra.l.Be.ha.vi.or.,.A.pp.ea.ra.nc.e .an.d .S.u.r.v.i.+v.+a.+l.+,. + 66 I. General Behavior, Appearance and Survival ...... a5Vo.. oC0T .o5wntmrego3 /lk.lg/.a dsa.y . .g . . e..e. a f .a..i..a a..a..i. f .i..i.i a .i..i.. i. m. i.. l.. . i.. l. 767 A USmfaMer. sais c. 1.5 mg/kg/day ................. 4.5 mg/kg/day .................. 87 8 2 Bdo.dy HANES eee nina ana 88 32.. LaBbodoyraWteoirgyhtsTS.S .+..+ .e.e..e...a.u.a.e..e..a... 88 3. aLa5..0aboOrTOnhanereteoMerMoyonnMtotThnhetshtoossff ott.fhhee.thSS.ettuu.ddSy. ytu. d. y. ....LL..L..Lo...... ........ L.L. .oi. . .l. ... 988 19. Pathologi5.calThSrteuedieMsont+hs+ +of sthenStuady .. n.a.a.n.n..a.s.a.s. i1009 IV. APeathMoelhoogidcSael + vee e eae. Studies .................... 1i00 A. M1e.thGordoss.s .Pa.Ch.ol.og.ys.. . .. vv..s.sn..n.u. e .e.n..n.a... 1I00 2I.. HGroEss PSathotlogyo+.. +pv.e.an.t.ts.n.ha ..o.n.l.a.o.e.g.s . y. 1I00 2. Histopathology ................... B. R1.esulGtrsos.s .Pa.th.ol.og.y.a.nd.O.rg.an.W..e.. i..g...-h.-. t...s....... IIii ii 2i. BGrosEs PaStholtogyoan+dpOsrgA nanetWseiaghhatsaO .e.el .e.eo .e.. ga.s. ye. 1ii 2. Histopathology ................... 113377--009922 11119911..00000022 33MMAA1100006655000055 || Interntional esearch and Developrent Corporation | taste or cowienis I Teonctmued) TABLE OF CONTENTS (Continued) PPaaggee Table No. Table1 No.Individual Body Helghts ee uuta ea... 1 2. MIenadnisvidaunadlSBiogdnyifiWceaingchetsof.E.ea.ta.l. og. ic.al.V.al.ue.s.......... 131-I5 14-15 3-52.. MIenadnisvidaunadlSHiegmnaitfoilcoagniccealofVHaelumetsalo.gl+ca+l +Voalusess.o..o.o . 16-18 16-18 6. 3-5. SIunmdmiavriyduaolf MHeeamnatoBlloogcihceanlicaVlaluVeaslue.s,..+ .+ .+ .+ .+ ..b..+. 1920 19-20 7-96.. SIunmdmiavridyuaolf MBeiaoncheBsitoecahlemiVcaalluesValues.+ .+ +. ses. s ns 223 21-23 7- 9. Individual Biochemical Values ..... PP 24-25 11-1I30.. ISnumdmiavriyduaolf MUerainnalUyrsiinsalyVsailsuesV.alues+ o u s esos oo 2628 26-28 Li. 11-13. NIencdriovpisdyualObsUerrivnaatliyosniss + + Values ...u ...s eesat 29 29 1145.. NAebcsorlouptsey OanbdseRrevlataitoinvse O.rg.an..He.ig.ht.s..+ + + oo + 30 30 1165.. Meroscopic Observations. + + tue e ease Absolute and Relative Organ Weights . . Microscopic Observations ........ 303 31-35 16. 137-092 137-092 11119911..00000033 33MMAA1100006655000066 1 | ficial src and Descloptions Corpor ion: b | PPaaggee 1| 1. sworsis SYNOPFSlIuSorad Pluorochenical Surfactant 70-35 vas administered by gave a5 age to thesus monkeys ac dosage levels Fluorad Fluorochemical Surfactant to rhesus monkeys at dosage levels of 0, FC-95 of 0, (distilled water was administered (distilled water only) by gay- only) 0.5, 0.5, 1.5 1.5 and and 4.5 4.5 amgg//kkga//ddaayy ffoorr 090 ddaayyss.. TTeweo smaallee aanndd ttwwoo ffeemmaallee mSoonnkkeeyyss wweerree iinniitciiaatteedd aact eeaacchh ddoossaaggee lleevveell aanndd aallssoo iinn tthhee ccoonnctrrooll Soup. The sonkeys vere observed tuice daily for general physical sgpropuepa.sancTeh,e mboenhkaevyisorwaerned pobhsaerrsvaecdotetxwiicce sidganisl.y foSrodygewneeirgahltsphwyesriecal arpepceoarrdaendcev,eekbleyh.avioHremaatnodlopghiacramlacaontdoxibclocshiegnast.calBosdtyudiweesighatnsd wuerrienaly- 5r8e5corwdeerde wceoenkdluyc.tedHeamncaetoliongitchaelcoanndcrobliocphereimoidcalandstuatdietshe anedndurofinatlhey- fsiisrstweraend cotnhidrudctesdontohnceof inthethestucdoyn.trol period and at the end of the firstTheandmontiheiyrsd mtornetahtedofatthethest4ud.y5.-ag/kg/day dosage level died or wereThseacmroinfkiecyesd itnresaxtterdeaatts thbeet4w.ee5n-mgw/eekkg/d3ayanddo7sagoef tlheevelstuddiye.d or These were These sonkeys exhibited signs of toxiciy sacrificed i._9.n extremis between week monkeys exhibited signs of toxicity 5 tn the and 7 in the gascroincescinal of the study. gastrointestinal trace tract (smorexts, (anorexia, emesis, emesis, bbllaacckk ssttooooll aanndd ddeehhyyddrraattiioonn)) fFrroomm tthhee Ffiirrsset of second day of study. or second day of study. AAlLlL tthhee hhiigghh--ddoossee amoonnkkeeyyss hbaadd ddeeccrreeaasseedd aaccttiivv-- Sty and before death shoved marked to severe ripidicy, convulsions, sietyneraanldizbeedforbeodydeattrhembslhionwge,d mparroksecdrattioonseavnedrelorsisgidoiftyb,odyconeviuglhsti.ons,The scan body weight generalized body mean body weight decreased from 3.44 k trembling, prostration decreased from 3.44 kg at the begianing and !oss of body at the beginning of the weight. of the studyThe study 0 2.70 kg a5 week 3 of study. to 2.70 kg at week 5 of study. AAtt I1 msoonncthh ooff ssttuuddyy aallll mmoonnkkeeyyss aatt tthhee 4.5-38/kg/dsy dosage level had decreased serus cholesterol values and 4c.e5r-unmg/aklgka/ldianye dopshaogsephalteavseel haacdtivdietcyr.eased serum cholesterol values and serum alkaline phosphatase activity. AAllll mmoonnkkeeyyss aatt tthhee 11..55--umgg//kkgg//ddaayy ddoossaaggee lleevveell ssuurrvviivveedd ttoo tthhee eenndd of the study. The sonkeys exbibred sitghely decressed activity fron of the study. The monkeys exhibi=ed slightly decreased activity from the fires week of the study vhich occasionally becase soderate to the first week of the study which occasionally became moderate to mmaarrkkeedd.. MMoonnkkeeyyss aatt tthhee 11..55--mmgg//kkgg//ddaayy ddoossaaggee lleevveell ooccccaassiioonnaallllyy hhaadd black stools, diarches, sucous in the stool and bloody scood and exhib black stools, diarrhea, mucous in the stool and bloody stool and exhibited dahydration or general body trembling at the end of study. The ited dehydration or general body trembling at the end of study. The sonkeys fron this group had a slight decrease in sean body weight. monkeys from this group had a slight decrease in mean body weight. 137-052 137-092 11119911..00000044 33MMAA1100006655000077 huersitioial Kescarelr wid Developimeni Corporation. PPaaggee 22 In the laboratory tests, there was a decrease in the alkaline phospha- In the laboratory tests, there was a decrease in the alkaline phospha- tase activity and the concentration of inorganic phosphate in the tase activity and the concentration of inorganic phosphate in the sseerruusm aatt 33 mmoonntthhss ooff ssttuuddyy.. AALlLl mmoonnkkeeyyss aatt tthhee 00..55--magg//kkgg//ddaayy cdoossaaggee lleevveell ssuurrvviivveedd ttoo tthhee eenndd ooff tthhee ssttuuddyy.. MMoonnkkeeyyss aatt tthhiiss ddoossaaggee lleevveell eexxhhiibbiitteedd aann ooccccaassiioonnaall soft scool, diarrhea, anorexia and emesis. Slightly decreased activ- istofytwasstoonlo,teddiairnrhtehar,ee amnoonrkeexyisa aatnd tehimsesidso.sageSlilgevhetll.y dAetcre3asmeodnthasctiofv- ity was noted in three monkeys at this dosage level. At 3 months of study a slight decrease in the serus alkaline phosphatase activity wsatsudynotaeds.light decrease in the serum alkaline phosphatase activity was noted. NNoo ggrroossss oorr mmiiccrroossccooppiicc ppaatthhoollooggiiccaall lleessiioonnss wwhhiicchh, wweerree ccoonnssiiddeerreedd ccoommppoouunndd--rreellaatteedd wveerree sseeeenn iinn ttiissssuueess ootthheerr tthhaann tthhee aaddrreennaallss,, pancreas, and subbandibular salivary glands of male and female thesus pancreas, monkeys a t and th e s4u.b5m-aangd/ibkugl/adray salivary dosage glands level. Moifcrmoaslceopaincdalfleym,aletherheasdurse- monkeys at the 4.5-mg/kg/day dosage level. Microscopica!ly, the adre- nneallss ffrroomm msaallee aanndd ffeemmaallee mmoonnkkeeyyss aact tthhee 44..55--mugg//kkgg//ddaayy ddoossaaggee lleevveell hhaadd ccoommppoouunndd--rreellaatteedd mmaarrkkeedd ddiiffffuussee lliippiidd ddeepplleettiioonn;; tthhee ppaannccrreeaass ffrroomm mmaallee aanndd ffeemaaallee mmoonnkkeeyyss aatt tthhee ~4..55--magg//kkgg//ddaayy ddoossaaggee lleevveell hhaadd ccoommppoouunndd- rreellaatteedd mmooddeerraattee ddiiffffuussee aattrroopphhyy ooff eexxooccrriinnee cceellllss;; tthhee ssuubbsmaannddiibbuullaarr salivary glands from male and female monkeys had cospound-related salivary glands from male and female monkeys had compound-related mmooddeerraattee ddiiffffuussee aattrroopphhyy ooff tthhee sseerroouuss aallvveeoollaarr cceellllss.. No statistically significant variations in sex group sean weights No statistically significant variations in sex group mean weights ooff oorrggaannss ooccccuurrrreedd bbeettwweeeenn tthhee ccoonnttrrooll aanndd eexxppeerriimmeennttaal! ggrroouuppss.. 113377--009922 11119911..00000055 33MMAA1100006655000088 hIn~tteerrmna.t,tiioonnaall RReesseeaarrcchh aanndd DDeevveellooppmmeenntt CCoorrppoorraattiioonn PPaaggee 33 1. comonn II. COMPTOhUeNDcompound vas received from IM Company, Saint Paul, Hinsesocs on OcThteobecrom2p4o,und197w7asasrecsehiowvnedbeflroowm: 3M Company, Saint Paul, Minnesota on October 24, 197L7avea:s shown below: Descripston TFFlluu5oorr5aadd5s FFllSuutooarLrcaookbccehholeernmiicc3aa8ll-02SS0uu7rr-ff0aa1cc0tt3aa.nn7tt white powder Description white powder TFoCr-958403-MetStowec.k 5 ine: 22 kor No. 98-0207-0103-7 Lot 640 Net w~. 5 ibs. 2,2 kg. 137-02 137-092 11119911..00000066 33MMAA1100006655000099 International Research and Development Corporation res mn cme stems a vem: CLINICAL STUD!IS vI=.~HncDemsrat rrocature: i. GTeineenralmaiPsrocCeedeutraen:ins rom 2.35 5 353 kp) and eta fesade CuetgningEigfhrtomma2l.e75 (t~oeig3h.i75ngkaf)romth2e.s5e5s s=oom3e.r5s5 wkge)reanfdafseiigahc~ed fedmnalSehi s(uwaetiyg.hin~Toefrokma2y.7e:$ twoeve3.7p5urkcgh)aserdhesfursommoPnrkiemyasteweTraeporitnsi,tlaF=oertJ in this Ssatsuadyi.ngioTnh,e mSoernkeYyosrk.wereToepumrotshkaeserJs sferroem Pnroismsaetde nidmtpvoirdtusc,tiPsortfn hansina WLaisrheinmgetsohn,"aNqeewcsYeonrtku.pe"Thecompeosnkeaynsd wsearfeniahionuesded fnindaivSiadeuraalltyariens,hanhguimnigc wLiorme amnedsh g"hseqmuceoenzet-rtoylplee"d cae~vevsizoannsdanmta.intauirniedneinMoankteeympeSrhaotxu?res-a, fodhumidciitty-esanadns!ifzahyt-zanodntrFor!elsehd apepnlveisronwmeernat.fadPu3ritnian.eDsMoankweeyek.ChoFrdacewarssafsed at~viactetaelaecha2dayMoatnndumf.resh apples were fed 3 times a ~eek. Wa~er ~as availablebeardinglibtihteumc.ondiziontag serial, the senkers see taseseed 03 the tunerDursiunrgfacteheofcontdheiticohniignhganpderifoads,raptehelpemdonrkaelyssu~b-=e-=r~.s- uittaattotoeesdts on the inner ~urface of the thigh and intrapalpebral tuberculin tests wCerraeeinceonnsducpteerdi.od. TubCeormcplueltien sthe~rtssiesallsosw~a:seirneatcioonndsuctveedrs tc~iocneducdtuerding4 thhee straeia?tmevne~sev;eirnieordi.en pCroimoprletteo pihnyfstiicaaslionexaofmincaotmipoonusndweardeuiactosnidruacLtieodn.by d~e Ss.t=y~ sovnecteerrsinafrniagneodprihoeraictho vienristiasteiloenciaodf. compound administration. Only Tats monkeTs sineugsoodwasheaflntihtie~ceerde osneleFcetberdu.ary 15, 1973. Terminal sacrificeIsbiswersetudcyond"~uacsteidnitoniatYeady o17n, 1573. February 16, 1978. Yermina! sacri3.ficeGsepwoerset caonddsuncitsecdraocnioMna:y 17, i978. 2. iCo=pSoheundadAdmoifnitshteractoinodni:sioning period the Somers sere diviisd toto fouAr~ gr~hoeups~ndon &of ~rhaendocmonddies$iiso,nins~o ptehratiodthetheLamfoclnekleysavweerraege dbiovdiy!ed sienttgohefsourser~erouspisattoans:a random basis, so that the ininial average body ,;eights ';era similar: So[ sazs A teva: Dosage Level wfv-uirsobbeer- ooff v~'on-i'i"ery"s~ 3H0 (Ym((gGC.ao:nnkctger/oodtla))y) >:ale 232 Female ::2 fi0h!.e.5d5 3:2 2 ::22 ~.5 2 o 137-392 11119911..00000077 33MMAA1100006655001100 Intersil Research and Development Corporation Page Page 5 i The monkeys in the control group were previously esployed as the The control monkeys in the control group fn an aborted 90 group were day study i npremvonikoeuyssly o nempFlCo-y95ed as t(hsetudcyont1r3o7l-08g7r)o.up Tihne antesatborctoeadpou9n0ddasyuspsetnuddyed ininmodniksetyislleodn uFaCt-e9r5, vas (study 137-087). The administered 7 days a test week cbyompgoauvnagde.susApLeLndeddoseisn wdeirsetilglievdenwaitnert,hewas administered 7 same voluse of days a water. weTehiks byvolguavmaegeo.f dAilsltildloesdeswawteerre vgaisvengivienn thteo the csoamnetrovlolugmreoupo.f waItnedri.viduTahlisdaviollyumedosoefsdwiesrteillbeadsedwatuepronwatshegibvoedny to the wceoingthrtosl ogrbotuapi.nedIwnedeikvliyd.ual daily doses were based upon the body 3. weights Oobbstearivnaetdiownese:kly. 3. TOhbesermvoantkieoynss:vere observed twice daily for general physical The appearance, monkeys were behavior and observed twice daily pharmacotoxic signs. foIrndigveindeuraall pbhoydysical wapepiegahrtasncwee,reberheacvoirodredanwdeekplhya.rmaGceonteorxaicl psihgynssi.cal Ienxdaimviinduaatlionbsodywere con- weights ducted were in th e reccoonrtdreodl wpeeerkiloyd. andGenmeornatlhlyphydsuircianlg etxheamisntautdyi.ons Fwooedre ccoonn- dsuucmtpetdioninwatsheesctoinmtartoe!d.period and monthly during the study. Food con- sump~4.ionCwlaisniceasltimLaatbeodr.atory Tests: 4. BCBlllooioonddicaaalnnddLauubrroiirnneeatossraayzmppllTeeessstsww:eerree oobbttaaiinneedd ffoorr aannaallyyssiiss ffrroomm aallll monkeys once during the control period and ac 1 and 3 monchs of monkeys study. once during The monkeys vtehere cofnatsrtoeld poevreirondighatnd partiori atnod t3hemocnotlhlsectofion of study. The monkeys were fasted overnight prior to the collection of bblloooodd aanndd uurriinnee ssaammpplleess.. a. Hematology: a. HHHeeemmmaaatttooolllooogggyii:ccaall ssttuuddiieess iinncclluuddeedd:: hheemmoogglloobbiinnIl,, hheemmaattooccrrittc2?,, eerryytthhrrooccyyttee ccoouunntt3d,, ttoottaall3) aanndd ddiiffffeerreennttiiaall lleeuuccooccyyttee ccoouunnttss,, rreettiiccuullooccyyttee ccoouunntt4,, ppllaatteelleett ccoouunntc5d,, pprrootthhrroomsbbiinn ttiimmee6d aanndd aaccttiivvaatteedd ppaarrttiiaall tthhrroommbbooppllaassttilnn ttiimmee7' ((AAPTTTT)).. MMeeaann ccoorrppuussccuullaarr hemoglobin, mean corpuscular volume and mean corpuscular hesoglobin hceomnocgelnotbriant,iomneawnerecocraplucsuclualtaerd.volume and mean corpuscular hemoglobin concentrabt.ionBlwoecrheeatcsatlrcyu:lated. b. BBiioocchheemaiisctarly:studies included: the deteratnations of fasting Biochemical blood glucosed, bsltouoddiesureianclnuidterdo:gendt,he tdheetearcmtiinvaittiioenssofof fasting blood glucose8, blood urea nitrogen8, the activities of sseerruumm aallkkaalliinnee pphhoosspphhaattaassee8,, sseerruumm gglluuttaammiicc ooxxaallaacceettiicc . 113377--009922 11119911..00000088 33MMAA1100006655001111 International Research and Development Corporation Page 6 ttrraannssaamnitnnaasseegd~, aanndd sseerruumn gglluuttaammiicc ppyyrruuvviicc cransasinased, transaminaseg, and and the the ccoonncceennttrraattiioonnss ooff cchhoolleesstteerrooll9?, ttoottaall pprrootteeiinn'9,, aailbbuuamitna8,, sso0ddiuuamlI0,, ppoottaassssiivuamlI0,, cchhlloorriiddee?9,, iinnoorrggaanniicc pphhoosspphhaattee'9,, aass wweellll aass cthhee aaccttiivviittiieess ooff v~--gglluuttaamsyyll ttrraannssppeeppctiiddaassee!IlI and and creati- creati- nniinnee pphhoosspphhookkiinnaasseel1Z2,. c. Urinalysis: c. Urinalysis: UUrriinnaallyyssiiss iinncclluuddeedd:: mmeeaassuurreemmeenntt ooff vvoolluummee,, ppH!1d3 aanndd ssppeecciiffiicc ggrraavviittyy;; ddeessccrriippttiioonn of of color color and and appearance; appearance; qualitative qualitative tteessttss ffoorr pprrootteeiinn1l3?,, gglluuccoossee1l33,, kkeettoonneess1!33,, ooccccuulltt bblloooodd1l33 aanndd sicroscopic examination of the sediment. 4. microscopic eSxtaatmiisntaitciaoln Aonfaltyhsetss:ediment. d. ASLtLatissttaitciasltiAcnaallyasniasl:yses compared the treataent groups with the conAtlrlol sgtraotuips,ticbayl saexn.alyses compared the treatment groups with the contBroodly wgeroiugph~tsby(ueseexk. 13), percent change in body weights bet= ween controlBopdeyriowdeigahntds 1,(we2eaknd13)3,mopnetrhcsent(secxheasngecomibninbeodd)y, wehiegmhatcsolobgeit-- wcaele,n cbolnotcrhoelntcpaelrioadndanudrini,aly2siasndp3armaosnetthesrs ((seaxoensthscom1biannedd)3,) andhematologi- acabls,olubtieochaenmdicraellatanidveuroirngaalnyswiesighptasram(etteerrmsina(lmonstahcsrif1icaen)d w3e)reandcompared abbbyysoaalnnuaatlleyysstiassnd ooffrevlvaaartriiivaaenncceeorg((aoonnneew--evwiaagyyhtccsllaass(sstiieffriimcciaanttaiiloonns))a,,criBBfaairrcttell)eetttwt'e'ssre tteecssottmpaffrooerrd hosogenetzy of vartances and the appropriate t-test (for equal or une- hqoumalogevnaeriiatnyceosf) vaasriadnecsecsribaendd btyheStaepeplroparnidatTeorrti-etlest us(ifnogr equal or une- Duqnuanletvta!raialn5ceusl)ttapsledesccormipbaerdisobny Sttaebelles antdo Tjourdrgiee1s4igunsiifnigcance of dif Dunnett's15 multiple comparison tables to judge significance of dif- f5.erenRceess.ts: B. RIE.SULGTeSn:era) Behavior, Appearance and Survival: I. TGheenreeral#asBehnaovimoorr,caAlpipteyarianncteheancdontSruorlv,iva0l.:5- an 1.5-ag/kg/day dosage lTehveelrse. wasThrneoemowrontkaelyistyatin thtehe&.cSo-ntargo/lk,g/d0a.y5-doansdsge1.5le-vmegl/kgd/iedday dboestawgeeenlueeveelks.5 anTdhre6e ofmontkheeysstuadty.theTh4e.5-fmogu/rktgh/dmaoynkedyosafgreomletvheils dgireodup vbaestweseancriwfeiecked5 ianndex6troefattshe instuwdeye.k 7 Thoef fthoeurtshtudmyo.nkey from this group was sacrai.ficeCdontirnolesxtremis in week 7 of the study. a. TChoentrsooln:keys from this group shoved an occasional soft stool or diaTrhreheamon(kseLyisghtfrotmo tsheivsereg)r.oup Fosrhowoende adnayoMcocnakseiyona7l358sohftad stool or diarrhea (slight to severe). For one day Monkey 7358 had 113377--009822 11119911..00000099 33MMAA1100006655001122 Interasional Research and Developmen Corporation rage 7 Page 7 bBllooooddyy ddtiaacrtrhheesa,, sannoorreexxitas sanndd sslliigghhtt aattaaxxiiaa aanndd ffoorr 33 ddaayyss MHoonnkkeeyy 7368 had snorexts. Eeests vas noted rarely. 7368 hadbeano0r.ex5iam.aligE/maeasyl:s was noted rarely. b. Y0o.5rkem~y/skg7/4d6a6y:and 7504 exhibited occasional diarrhea oc Soft stools. MonFkoerysMon7k4e6y6san7d463750a4nde7x4h8i3bittehde soocfctasisotnoaollsdianadrrhdeiaareohres wsaorfet fsrtoeoqluse.nt wFiorthMoonckceayssion7a4l63 aapnpdear74a8n3ce=hoef msuofctus sftnooltshe ansdtoodlisa.rrheOan waenereocfcraesquieonntbwliotohdyomcuccaussion1anl thaeppesatroacnlceandof fmnuctuhse r~nefutshee psatnoolssa.s On oonbeserovcecdasifoorn Nbolnokoedyy m74u8c3u.s inOcctahesiosntaololananodrexiinathaendreenfeussies pavnerewasnoted foobrserMvoendkeyfsor7M4o63n,key74674683a.nd 7O5c0c4a.sionSatlatlaanrolrye,xiaa asnldighetmestiasterweariettennotted dfoercreMaosnekeytsa 7a4c6t3i,vit7y466vasandnot75e0d4.forSMiomnikleayrsly,746a3,sl7ig4h8t3 ainndte7r5m0i4t.tent decrease in activity was noted for Monkeys 7463, 7483 and 7504. c. A1L.5L mmgo/rkige/ydsaya:t this dosage level exhibited a slight decrease tn Aalclcivmiocnykeydsuriatngthtihse fdiorssatgeweleekvelof esxthuidbyi.tedFoarsNliogahktey 7501 dtheecredaesceteaisnedactaicvtiitvyitydurfirnegquetnhetlyfirussst wneoetked ofthsrtouudgyh.outFotrheMosntkuedyy 7a5n0d1 btyhewedeekcre13asehdad abcetciovmietymofdreerqauteen.tlyAlwatshoungohtednotehareosuigsh,outsofthe sstotouldsy aanndd bdytarwecehkes13verhead mbeetceodmeformodtehriastem.onkeAyl,thosuigthghtnogeenmeersaisl, bosdoyft trsteomobllsingandand mduicaursrhe1an wteherestnoootledusfsorobthsiesrvemdonkieny,vesskilg1h2,t gaseneerlall absodyslitgrhetmbling and mduechuysdraitniotnhe instowoelekswas12 oabnsderv1e3.d iFnorweeHkonk1e2,y 7a5s01weallndas750s0liaghntorexia bdeechaymderatpieornsisitnenwteekdsuri12ngawndeek1s3. 12Foarnd 13.MonkeyF7or501Monakndey75705000andoiraerrxhieaa and bsoefctamestopoelrsisspteeanrtedduralionnggweweiktsh s12ucuasnd fn13.theFosrtooMlonkateywe7e5k002,dabrlrahceka and sstofotol sattoolveeakpp8earaendd aslloingghtwidtehhymdurcautsioninintheveesktoo1l2. atThwiesekso2,nkebylacekxhisiscteodol "abtruwieseikng"8 aanrdounsdligthhet drieghhytdraetyeionfolinlowweedekby12.bruTihsiisngm"onkaeryounedxhibbiottehd e"ybersulsatingv"eskaro1u2.nd the right eye followed by "bruising" around both eyes atFowreekYon12k.ey 7486 occasional soft stool and diarrhea were observed alonFgorwiMtohnkeaynor7e4x8i6aowchciacshionbaelcanseoftpersstioosltenatndindivaererkhea10.were Doubrsiernvgedweeaklsong10wistnhd a11norselxiigahtwhdiechhydrbaetciaomen vpaesrsiasltseontnotiend.weeMkonik0.ey 7462 Dhuadrinogccwaeseikosns]i0 saonfdt sIItoosll,ighetmesdieshydfroarti1ondaywaseacahlsoianowteeedk.s 1 Moannkdey3 a7n4d62 htahde doecccraesaisoendalacstofitvitsytoowla,s oebmseselrsvedforfn1 wedeaky e1 acohnlyi.n weeks i and 3 and the decreased activity was observed in week I only. 11-002 137-092 11119911..00001100 33MMAA1100006655001133 . International Research and Development Corporation a 3 mginateas: d. S"e. a 6m .3=l m.<3Z./. kcga/yd: ay the onkers showed apparent sigms of _-'_t /'.5 m.~/k~/dav the monkeys showed ag~aren: si~.ns a"orxizoif:ythein sstuhedy ~aCsetnro~rienxtieasteinrd.a!per:trlaacl~ afnroormex:ihae, fiermsetsist,~ b:lheackse:s~sra.dcl daany./oorf d~hsehpis~zuadcvi.on(anforroen~:isaliganh~t' ptoartsieadlaraatneo)r.exiaA,l1 had Zecressad emesis.. "~-~"~.~=~ anti wanii.t"orfro/mehysiiriz~hteionto frsoevmersa~-.h*~_~3,_eftooremoddeersacthe)t.hey='si~howhe~dd miaercireedasaIio severe vsiitsvtiifsryo,m csolnigvhutlsi~oonss,evseroed.eratBeefogreenerdaelaithzedtheSyodyshocwreadsb~l2irngkedasdto fsieavaelrley ri~idiny, convulsions, moderate ~eneralized body ~re~bilng drostratfon. Vonkey 7485 tad petachial hemorrhages on The asnkdin offinally ptrhoescfrnagtuifonns.l a~r'e[so,nkeyth7o4r8a5x haandd vfeacteechsinadlYohnekmaoyrrh7a4g3%esnaodn pthaele skgiunns ofafter the inguinal area, thorax and face and ~o~kev 7484 had pale =~ _ after week ....~_~'" 33 ooff tthhee ssttuuddyy.. 2. 3odr eights (Zable 1: 2. CBhosdyzze~-s[eiignhtsths(Tbaobdlye wi)ai:ghes were sinlla: for serieys fn the contral Chan~as in ead ot the 0t.he3-abgo/dyX a/%-deaiy~hZdsos were ege si~i!ar level. fBr The m~nkevs ala mor t in ars the fn tchoentr1o.l3-asn3d/kaat/datyhe d0o.sa5g-emg/lkegviedlayhaddosaagdeecrlaeuvsele. fnYhtehemiralefomdonkweeysitin the 1.5-mg/k~/day dosage leve! had a decrease in ~heir body rom 3.13 kz 2t the beginalag of the study fo 2.93 k3 at the ead of from 3.!5 the suey kz at the beginning mf fro 3.22 kg to 2of.75thke3 s[fuordy thteo 2f.e9m3alekgmoannketyhse. endTheof . c~ ..h.a.ngsezuifvn. =-B.a-.d;~r frwoemigh3t._~_for'~.=o to _9.75 kg for the female This group of menkers was fme:onksenyastisiieally chan~e signif iciannth.ofdyronweitghhet for this group control group. of monkeys was not 3t~tiszica!!y The significant fwroonmketrhse actonttrhoel&.g3r-Bump3./k3/dey dosage laval snowed 2 iss The monkeys at ~he A.5-mg!kg/day dosage level sho~ed of the bady seizht after 2 weeks of the study. Their svarazs bdr oufatg~hhee bdoedcyreawseeid~h:froamfte3r.2%2 kwegeka~t otfhe :bheegi~n:nuidyn.g oTfhetihre asvieii=ya~e22 bo1d2y3 kz weight deoreased from 3.44 kg (sash 2) = 3.13 kg (soak 3) = at the beginning of 2.97 kg (weak 2) = the 2.70 skt'z;!y(week 3 Zor (week 2) - 3.!B Soth sexes. A: kg (~-eek 3) - 2.97 week and 7 of the kg (week &) - 2.70 k~ (week stuiy thay dad, There vis 5) 20 for bsottahtissteixcesa.l eAv:alwueaet~i'on6 oafnd t7he ofBodtyhewesitguhdtys for .._.~.e.2 di=d.~ Yhere ~a~ no conkers at the fu3- Ssatfaetpii~dtiacya!isseavzae!ual~eivoeln, ofbectahuesebodtyheyweivgehrtss noftor almiovnekeyasc awtestthe13,4.w5h-en mg/kgidav,. /o~aSe level, because they. were not a!i~-e a: w=~::__ 13, when the siatissizs were done. the statiszi.zs were done. 33.. LL~a-.v~:s..c.aa_z.oo.rr.}y Tests Tests ((TTaabblleess 22--1133]):: 3. ne Month of the Study: a. One 3c 1 Month month of of thsetud~ytudtyh:ese sere no pazhologizal changes in 7alues far oAk~evI smonftrhomofthestcudoyntr~ohleresad<-;eDr.a5n-omg/9iatshiodlsoygifzaa!s.uze:halne.=v==e_sl_. in values for monkeys from the control and 0.5-mg/kg/day dosa~e lave!. 1[3377--009822 11119911..00001111 33MMAA1100006655001144 | Internztional Resear i snd DevelopmentCorporation Page 9 Page AAtt tthhee 11..55--amgg//kkgg//ddaayy ddoossaaggee lleevveell oonnllyy MMoonnkkeeyy 77550011 hhaadd aa sslliigghhtt ddeeccrreeaassee tinn tthhee erythrocytes erythrocytes vwhhiicchh vwaass rreeccoovveerreedd iinn tthhee tthhiirrdd mmoonntthh ooff ssteuuddyy.. BBootthh tthhee mmaallee aanndd ffeemmaallee mmoonnkkeeyyss aatt tthhee 44..55--m2gg//kkgg//ddaayy ddoossaaggee lleevveell hhaadd llooww vvaalluueess ffoorr sseerruusm cchhoolleesstteerrooll wwhhiicchh wweerree ssttaatt~issttli- cally significance. cally Monkey significance. 7484 had a decreased alkaline phosphatase activity (312 untt/1),Monskeeryum74p8o4tahsasdiuma d(e3.c6remaesqe/dliatlekra)linaend pchholsoprhiad~ease activity c(o3n12cenutnirta/tli)o,n s(e10r2ummepao/t1aistseiru)m a(n3d.6Mmoenqk/elyit7e5r0)3 aalndsochhaldorildoew serus ccholnocreindteratcioonncen(t10r2atmieoqn/l(l1t0e2r)meqa/nlditMeorn)k.ey 7503 also had low serum chloride conAcletnhtoruagthionthe(1502.6.m0e.q7/.lltaecrt)i.vity of male Monkeys 7484 and 7485 was in AtlhtehohuigghhesttheexSp.Ge.cOt.eTd. noarcstailvitryangoef m(a1l15e Muonnitkse)ys t7he484diafnd 7f4e8r5enwcaess binetwteheenhitghheessetvaelxupeescteadnd notrhamtalofrantghee c(o11n5troulnitvse)re thmeot disft-a- , tfiesrteinecaelslybetswiegennifitchaenste. values and that of the control were not sta- tistically sTihgenifoinclayntu.nusual changes fa the urinalysis vere the The only unusual changes in the urinalysis were the aappppeeaarraannccee ooff gglluuccoossee ffrroomm MMoonnkkeeyy 77550000 ((11..55 mmgg//kkgg//ddaayy)) aanndd ffrroomm MMoonnkkeeyyss 77448855 aanndd 77550033 ((44..55 mmgg//kkgg//ddaayy)).. HHoowweevveerr,, tthheessee mmoonnkkeeyyss hhaadd nmoo ppaatthhoollooggiiccaall iinnccrreeaassee ooff tthhee bblloooodd gglluuccoossee.. bb.. TThhrreeee MMoonntthhss ooff ethhee SSttuuddyy:: There was a staciscically sigatficant decrease fn the serum alkalinTeherpehowsapshataassetataicsctiivcicayllyforsicghneifmiaclaentsodnekceryesaseat intheth0e.5- serum alkaline phosphatase activity for the male monkeys at the 0.5- mmgg//kkgg//ddaayy ddoossaaggee lleevveell aanndd ffoorr ttwwoo MMoonnkkeeyyss,, 77550000 aanndd 77550011,, aatt tthhee 11..55-- mmgg//kkgg//ddaayy values of ddsooessraauggaee pollteeavveeslls..iua TThhceeossneecenlltaarttattteeirronmmsoo.nnkkeeyyMssorkaaellyssoo75hh0aa1dd at 1.5 aa ddeeccrreeaasseedd avagl/ukegs/daoyf bsaedrumverpyotalsowsiusmerucnonccehnotlreasttieornosl. anMdonMkoenykey75071500atat1.51-.5 mag8//kkgg//ddaayy bhaadd vaersyliglhotw dseecrruemasceholfensttehreolfaoarndgenMtocnkepyho7s5p0h0ateat (41..25-38/100 ma1g)/kgc/odnacyenthraadtiaons.light decrease in the inorganic phosphate (4.2 mg/100 ml) concentration. 119377--009922 11119911..00001122 33MMAA1100006655001155 e re | Imerniationad Research ae nd Developrizeri Corporationsome PPaaggee I100 IIVv.. PPAATTHHOOLLOOGGIICCAALL SSTTUUDDIIEESS AA.. MmEoTHpOsDS:; 1i.. GGrroossss PPaatthhoollooggyy:: AAfftteerr ccoommpplleettiioonn ooff tthhee ccoommppoouunndd aaddmmiinniissttrraattiioonn ppeerriioodd aallll ssuurrvviivviinngg mmoonnkkeeyyss vweerree aanneesstthheettiizzeedd wwiitthh SSeerrnnyyllaann**,, eexxssaanngguuiinnaatteedd aanndd nneeccrrooppssiieedd.. AAtt nneeccrrooppssyy tthhee hheeaarrtt,, lliivveerr,, aaddrreennaallss,, sspplleeeenn,, ppiittuuiittaarryy,, kkiiddnneeyyss,, tteesstteess//oovvaarriieess aanndd bbrraaiinn wveerree wweeiigghheedd aanndd rreepprreesseennttaattiivvee ttiissssuueess vweerree ccoolllleecctteedd iinn bbuuffffeerreedd nneeuuttrraall 1100%7 ffoorrmmaalliinn.. EEyyeess wveerree ffiixxeedd iinn RRuusssseellll''ss ffiixxaattiivvee.. TThhee tthhyyrrooiidd//ppaarraatthhyyrrooiidd wwaass wweeiigghheedd aafftteerr ffiixxaattiioonn.. MMoonnkkeeyyss wwhhiicchh ddiieedd dduurriinngg tthhee ssttuuddyy wweerree nneeccrrooppssiieedd aass aabboovvee.. 22.. HBiissttooDpaatthhoollooggyy:: MMiiccrroossccooppiicc eexxaammiinnaattiioonn ooff ffoorrmmaalliinn ffiixxeedd hheemmaattooxxyylliinn aanndd eeoossiinn ssttaaiinneedd ppaarraaffffiinn sseeccttiioonnss wwaass ppeerrffoorrmmeedd ffoorr aallll aanniimmaallss iinn tthhee ccoonnttrrooll aanndd ttrreeaantmmeenntt ggrroouuppss.. TThhee ffoolllloowwiinngg ttiissssuueess wweerree eexxaammiinneedd;: adadrreennaallss baarooarrittnaa ebserosaopiphhnaagguuss egyeaeylselsbladder hhgeeaaalrrlttbla((dwwdiiettrhh duovvdeeesssaseuellnss)) dliuleoeduwemnum jjeejjuunnuumm ccoceleccouunmm crroeelccotununm ccoorroonnaarryy aanndd aannyy kkiiddnneeyyss ssaalliivvaarryy ggllaanndd Llliuivnvegerr plliuutsmubbiaatrrarssyppiinnaall ccoorrdd sslkkuiningn pssitttooummiaatccahhry mmreeessteernnottpeehrraiirccynglleyyaomlpphhlnnyoomddpeeh tttehesystrteoesisd//oovvaerriieess rcneantcoormddoaeeprhyargylnangdeal lymph ppttaahhrryyaamrttuohshiyydrrooiidd mnear~vaery(wgiltahndmuscle) nseprlveeen (with muscle) ttthrryaamccuhhseeaa tonsil papsanpnlccerreeenaass tctooonnnggsuuieel prporsotstaattee//uutteerruuss bone/bone marrow (rib uvurarigininanararyy bbllaaddddeerr boJnjueun/ncbctotinioeonn))marrow (rib vttaaagttittnooaoo ootthheerr ttiissssuuee((ss)) wwiitthh lleessiioonnss 113377--009922 p*SPhehe.enncJcyoycsclelipihdd,iinnMeeisHHsCCoLIur--i.BBiiooCCeeuuttiicc LLaabboorraattoorriieess,, IInncc..,, St. Joseph, Missouri. 11119911..00001133 33MMAA1100006655001166 | interiational Rescarch and Developnieni Corporation rage 11 Page ii 5. sam: B. 1. Gress .R_~SULTS: Pathoiosy (Isble 14) an orsen tielshes (Sable it): i. GYroosgsrosPsathloeisoi~oyns (cToanbsleide14r)ed soandmpOorugnadn-sWeeiigshttesd w(eTraebls~eIe~n$:fn male and fematNeo Tghreosssus lmeosnioknesyscwohnsiicdherdeidedcoormowceurned-rsealcartiefdicweedrfenseeexncraicnismaloer waenrde fesmaaclreifircheedsusatcer 30 monkeysdwahysichofdisecdalyo.r were sacrificed in extremis or were sacrJiofiscteadtiasfttiecrall9y0 dsaiygsnifoifcesntutdyv.ariacions in sex group sesn wetghes Noof csrtgaatnisstciecsalelryretsibgenmimfiaceenntthevarciuantiiroenlsenidn esnepxergtreosunptemleangroups: 2. weights mofisccorgmaancsholoocscuyr(rTeadblbeet1w6e)en the control and experimental groups. 2. 1Hi1stomgalaethoanldo=yfem(aTlaebleso1n6k)e:ys at he 4.5 my/ka/day dosage level nad sasiedAlldimfalfeuseandpifedmaldeeplmeotnikeoyns iant thtehead4.r5enamlgs!.kg/dOaney dmaolseageandlevteol hfaedmslmeas~keadt dtiheff4u.s5e slgi/pikdp/ddaeypledtoisoagne inLevtehle haaddrenoadlesr.sieOnedifmfaulsee ansdcrotpwhoy offematlheespaantcrtehaeti4c.5exmogc!rkign/deayceldloss.ageThleevelleshiaodn mcoodnesriastteeddoifffudseecreastsreodphy ocfeithesipreancarnteatliocssexofocrsiynseogecnellgsr.anvTihees To lesionmecloensiasndtedoneof fami decreased cell size and !oss of zymogen granules. Two male and one female comofonnkkteehyyess saeattrouttshheea44l..v55eolmmaggr//kkagc/!eddllaasyy ddcoohssaaargBaeectellreeivvzeeleldhhabadyd mmdoeodcderereraaatsteeedddiicffeffluulsseesizaaertrrooeppndhhyy oLfosstheofseeryocuesplaaslmviecolagrrancuellelss. These micro characterizedscboypidcecrfeiansdeidngscewlelresizceonseindelroessd comaund-relaces. of cytoplasmic granules. These microscopic findings were considered Yo nisroseopis compound-related. changes which vere considered corpound-seleted "ere seenNo imnictrheoscaodpriecnalcsh,angpeasncrwehaisch owrerseubcsoannsdiidbeurleadr csoamlpiovuanrdy-rgelleantdesd wIenremalseeenandin ftehmealeadrseonnaklesy,s paatnctrheeas0.5oransdubm1.a5ndgib/uklga/rdasyaldiovsaargye gllaenvdelss. Jion mmai!cerosacnodpifcemalleesiomnosnkeiyns taitssutehse o0.t5herandcha1.n5 tmheg/ksgd/rdenaaylsd,osapgaencrleesvselsa.nd Nsoubmziacnriobsucloepric salleisivoanrsy ginlantdisssuoefs saolteherandthafnematlhee madormekmea!ss,atpatnhcere4a.s3 efand Ksugb/mdaenydidbouslaagre slaelveilvavreyreglacnodnssidoefremdalecoamnpdoinfde-mraelleatmeodn.keys at the 4.5 mg! kg/day dosage level were considered compound-related.. 7-002 137-092 11119911..00001144 33MMAA1100006655001177 | International Research and Development Corporation | sefersaces References 1. HCCiooauulllettaeehrr, HHeeFmzioaagtg!iisooebb.iinnoomnestteerr,, Coslier Coulter Tieccrontcs, Electronics, 330 590 .W. 20ch 20~h Strsec, Street, 2. HMCMiieoacrnlroeoohahnehen,,msattF5ao.lcaorrriiiisstdh,,a.. JJoohhnn 3. B. Male, Miala, 3rd 3rd Sd,Ed., 1967, ~967, The The C. C. T. V. Yosby 5. CCSCo3oom0uuplla7tt.neeyrr,2JP0ea~h.rrs:iiS1cc1e!l5r4eea.ssSS,iizzeeHaCCtooeuunnstt,eerr,,FrMoMrooeddceeall. 7a, ZB, Coulter Coulter Slestronics, Electronics, 4. R5GGe9rri0aatddmWwea.hhnoo,ll2''0sstEhiiCCtllSoitirrnnsetiecetasS,llthLHLiaa2abb0loo.erraaahtt1,oo9rr63yyF,!YoMreeTichtdehhaoo.ddCss. Vaa.nnddtaDDsiieaasggnnooCssoiimsspanFFyrrsaavnkkpeerll 11aa3nn5dd. 5. R2CCeoo0iuuhtl!mt~aeeSnrri,rfPeeaErrd,itiiitoccHrlilsaeeteSS6aii~nzzh,eeEdFCC.loo,ouurnnitt1dee9arr6.,,3, fMooTddheeellC4.A,, V.CGooMuuollstibeeyrr Elscsronics, 530 f. Company, p. !~32. Electronics, 590 W. 5. G2e0ntehraSltreDeita,gmHoisatliecash,-- fFalroariedra.Chileort Laboratories Revised April 1965. 7. General Gfenreral General Disgoscics Diagnostics Di~Enostics -- - Harner Warner Warner Chicos Chilcott Chilcott Laborscories Laboratories Laboratories vised Revised Revised Januaty April 1965. January 5. T1e9c67h.micon auto Analyser 6/60 Histo Vethodology. 5. MTeecrhoniAcuotnoAAuntoalyAsnearlyzIe1,r 66//6600 MMiiacrroo MNeetchhooddoollooggsy.. 109.. MaciocsrtoeAuAtbossrApneailoynzerILIIY,ode6l/60393M.icro Metho~o!ogy. I101.. AStiogmaiacTAebcshaoircpatlionSutIlLecMtondel3653,53.Signa Chem. Co., Sc. Louis, Missouri. i1i2.. SSiiggemaa TTeeccthmniiccaall SBuulllleettiinn 552495,, SSiiggmnaa CChheemm.. CCoo..,, SStt.. LLoouuiiss,, Miissssoouurrii.. 1132.. BSiigimlaabTsescihxnicCailmesBuRlelaegteinnt 52S0e,ripSei)g.ma Chem. Co., St. Louis, Missouri. Leo13. 14. BoSSftitee!eeSille!,,laebts~Ri..tciix6Gt..s(,DDA..mMeseaannaddRreaaTTngoonrreirrniiitLee,,,St.rJY.iepusH.).T.or((k11,996600.)),, T-PPrriisncciiool!eess and and Procedures Procedures 15. 15. BDDofuounmenSmceternsrtit,,icsstCC,i..csWS5,.i,,peM.cNNGeers~1a9wT5T-0aa,Hbbillleelss, forNew for Weitiple York, N. >~ltiple CCYoo.mmppaarriissoonnss Wich With a a CCoonnttrrooll,, Biometrics, Sept. 1964. J 137-092 11119911..00001155 33MMAA1100006655001188 iI ! Dl gizmag smaan sssns li 38% 3amz sansa Li gases seams asses i lel s$s33s 33332 z333% ol sasmz esssa ssa 1 | 7) Rid SERAFE addA a z $10 LU asses assez gmsse 31 PLLHBF HIfEA7) dHlipb)) PP3330E)b1 k Bssmmes uoesmssmoosnmmamzo piagn?s wseEesomsmeers o smm n apans s3m3m3a8s1 EssMmnIc AraEmRs Eshasne mazEarr oEosmsmTag osmasta oagnen 200 LD gssza aman: sseas sama i Piji lf| l| PPlRd] PDillgL]l z#a2sz3z maazz m222E33 s#. s8e=3s oszaze so3s3mm:e s2m m0sz3a r Bzsuasss amas ozmasz asgmmie:r os: mna P1IE1Ph3y)! zRgE2m2man smamssme sossmsan:n ssaasmzss les ddd 1| g3 33g 33 HEF 12148 EHIeTn3t REonn PeyREIL FERP Nuves3 Hoven 11119911..00001166 Page 13 Page 13 i 1 ! i | i ! i: ii iii |i I 1I11H Iis I5IHE PIE | i|; 5 1[I % 33MMAA1100006655001199 ress sesscstony Corgmereen, [Th-- ea sem:pre, Pla1cghtecs, restestoerses, rrTasecoasia Tne, seEstSmeus rT -- Te =T,o "Te EiSon Sinuca-Bur Subacute Shem Sooke Toxicity Sadr. Ninety-Day Subacute Rhesus Monkey Toxicity Study. MALF.~: .~eaus and Si~nflcance of Hematolozlcal Values. Nr Month Conceal C~n=rol ] 3 oct Control i1 33 Gn Control 7! ]3 ne ~onrrol 1 33 Conceal Control 7I 3 PR Con=rol 3T3 cme Control I 33 onceet Cou~rol 71 3 GaT mi 33 aol outrol T[ 53 cme Control +l 33 cemerel Control an~. 93 ~,.67 ~ .63 123~Z.3 jos12.& i12.3 3Hl35 37 39 129 i181 05205 osO. 5 oa0.3 0.2 ii ii12 n29 i24 i25 v.007.03 wa 10.59 8.67 n379 "84 325 827 527 x%36 34 32 05 sires 0.5 mg/kg/day 5.26 5.36 :.81 :, .,~ 112.7 i13.0 i12.~ 38 337 539 wo140 Ed226 Ed226 05O. 9 ao0.3 0.3 u!i iinzII 28 i25 i22 re10.29 toil I0.-~i 7.06 n777 80 x2~ 529 x26 xy. 37 333 Ls mialeer 1.5 mB/k~i~ay so5.0~ ~.66 4.45 us12.3 Jed13.2 ii11.6 37 37 336 1114 joy161 =223 0s0.6 a30.2 0.I u11 iiII 29 i24 B28 oz8.22 ed8-'~9 9.0~ n~o =o25 a28 H26 x34 Hi36 i32 Page 14 Page 14 5 said ~.5 mg!k~iday sa 4.71 - a!3.7 3i:12.8 uiw 177 oLfaI .{3 O.Z - 2ui:26 529 ?oa6.39 id i t .37 - a78 5:25 327 *136 335 2- 137-092 - No~ available 11119911..00001177 33MMAA1100006655002200 Sone Tpzesasstony poe a ps EE hs ) =T,ow rs ce pan sy cs ~inecy-Day ~ubacuce ~hes~.s Monkey Toxicity To: mo me psi Seog FE~.ALES: ~eans and $1gni~Icance of Hematological vaZues. rTI EE Y~n~h Control 1 ees Control 5.66 5.02 3 ~ .71 Co~=rol =1 3 Control ~ ~ Control 1 3 1~, 1 1~.1 12.0 g39 ~0 38 og1 ~ 6 , 151 232 oceiwin 0.5 mg/kg/d~ 5.56 4.56 4.79 1~.6 13.~ 12.2 i38 38 39 #16~ 177 236 issn i.5 ~,"k~iday 15. !i 5.~5 -~.37 12. 12.0 11.7 53~ 35 37 %L 6~ 15~ Z29 Control 0.4 O.S O. 3 rul 8 4 ~ 0.2 0.i 0.2 3 0.I 0.I Co~tr~l I i I0 I i I II II II Control og i i 3 ra: i Control I 27 ~5 7.39 8.77 27 29 i0.31 7.82 ~6 8. Sl 9.~4 3 ~. 62 9.09** Control I 68 79 6=9 82 a67 88 3 3 3 Control 2~ 23 25 rod i ~ 28 30 31 ) 26 26 27 ul x 3i 33 ~u=rol 34 33 37 I 36 36 35 3 32 31 32 re 5 Page 15 sie ~.5 mgikgi~ay ig5.08 5.00 - 12.9 E3d182 194 O.S 40.~ ii 12 27 i112.71 I~.2S E68E 75 223 325 - 5535 - sr137-092 E rrS Ee IROEn TnEm A different from Control Stoup aean, p<O.05. different from Control Stoup ~ean, p<O.Ol. 1I 119911..00001188 33MMAA1100006655002211 | ! 2HH3) greaeze22 n wer snxonn RsRaAnasa snsexsa | ED 88332 RARE 248A meanoe | Tu sezza sssss massa seers ETRE I d I) E Hel i hi oi l i$3;lkgu] seems 22am: eases 23ammmzam 2 - sexs messe os sseee 2_RL7 R:RR A 1i5n:e $148 SIE sxx: osmses zazzz ozzens H|YgH]l sEaEssEy soymmenrs osemanmis oseness PIiie# s S333: s3Eeld EEE R BEE: TDlegede HE CEE [D[I|liEEgsl| mses sma amen sims oz:ziomEni mio: Emamnre mmem ine ssmsns asemas Li Bee Feren {een FE i2al5|i05 s3831 n1l)JaBdmaanrs$1:8asoanyn 11 3daBunsens 3 Haennes! 11119911..00001199 Page 16 Page 16 ii i | | |: | || | i i :i | i| | | ||| | i| d#3 33MMAA1100006655002222 I Hy samza maga i i) ARRAN ERE A hi LE EE TEI ll EE a[1 Hal svenr comes Hl $i] smsrc zsszs $| 0 TL i j.| ILHigsi)a THHIiiE sEy|i 130150, sssas EseEsRsE szema sess: sams: osgmnsi: anus see 2 mess a Bg 200 if] | |= 533 32233 233s RRIF asa =mRT I EE sass gEmaan TT sewn sons sass aasas assza ssn: osgsemssEisoemsms agaa menanes seen ossdsw smn: sIRER goEss Le iaHla) smrzomser mmr oma: |] gd] ssa sssz osssza dss H$E1H2E0 FTE ESIY. FH Homer I Mogee funn: J Ragec 11119911..00002200 Page 17 | { + | i || | | | | : |1Ii1: i[F 33MMAA1100006655002233 1IiB]T! sess amas meas Fl osszes esses sssss DPinE] ess sasee sess sil] HE i seams ssiRa =mase RI FDEil3ill| cazmays mmsmszma mmaanggee | ie] cover me sos HDiEgE! sssse maser mema ih En 3p1i31e38 mzmza szzza ozzazs F iH d| oswmees mommssyn zozsems: CPaYl maz: amar szzza Dlgee] memes sxsnn mases Hy SEEfd SEEIE ZEEE: I fdgl)) smsma omoesrm aomsss: moumn 3 eld 33 i? $8... 0 HE FETTERPRL PPT 11119911..000021 rage 18 Page 18 | ; | 1 | | i| iJ : || || i| iPfi 33MMAA1100006655024 po~C-9~: som TABLE 6. Bioche~.~s=~y Gluco~e, mg/l-O0 ~ B.CUma.zNsi.!i,0o0 ~at EEE .~llne ?hospda=~e, i~'l un1=sil 5.G.O.T., In~'l ~i~s/l ewxn. Cholesterol, m~/100 ~ aapn Total Protein, ~/I00 ~ sosg/l~o ~ _Sodi~, meq/l _ ?OCaSSI~, meq/! Chloride, =meq/l ssgoon i~rga~e P~spha~e, mE/100 ~ smn v - Glu~l Transpep=i~ase sam Si~ ~s/~ pi pepe, Creaci~ne Phospho~se, ro S~ ~=s/~ st cs sg sss ~Ine~y-Da~ Subacuce Rhesus Monke~ To~ic!~! Study. Hom cmww H~L~S: $ cudy ~on~h S,~'r7 of ~un BiochenLlcal Valuee. Control 0.5 ~g/kg/day name ~.S m~/kgiday Control 118 331 9"776 Canrirreml n2233..y73 3 2B.2 v Conrro! l pt 1070 1113 3 Control Cd 3 Tg I 3 A ul SE Control l 3 wm w Eta Control ~ 3 ww l 3 3 Con=rol 1 3 ot ~CZOl 1095 22 56 42 35 183 198 162 8.38 8.46 7.85 4.75 4.70 LbO 161 153 4.9 1 4.9 3 ~mcrol TB l 3 [RA ~n~rol ~31 om~n~rol rodog 1 3 csoo Coa~rol 4.2 I12 117 112 6.8 8T7..e14 56 42 56 25 1 62 3 20 106 92 80 32n39..338 26.5 wr680 897 747* 23 349 i27 28 3172 200 152 ai8.74 8.59 8.07 im5.~7 4.69 5L56 160 151 25.6 &.6 4.2 ~14 #LL8 ~i0 ws~.4 &~3..~5 336 ii45 29 Hi44 34 40 I02 w1o1r5 107 33aI2..sA8 I~.6 i1I0ii3io50 89L 18 3g38 28 #@tSS 213 Lia8.68 8.74 .8.~8 in5.22 4.98 5156 160 150 5.4 ~.7 #~.8 116 iZl Iii 6.0 x86..~0 5~0 I855 45 3i1] 67 40 se 19 Pa~e 19 wwe ~,3 n~ikg/da? --99 29.1 - 1T30e0 25 ]:27 53190 ius8.90 8.90 - "in160 153 us- 4.7 z.- ~i~ 105 - 4.-=9* %46 326 - 2313 - --137-092 i iS eTO e~sL~nlflcen~17 di~feren~ from Control - = No~ available Elgroup mean, p<O.O1. 11119911..00002222 33MMAA1100006655002255 renFC-95: We TABLE 6. Cont. -- 3iochem~s~ry -- Glucose, i =8/I00 =i seB.U.N., Simg.' :00 ~ site rospacte, .~i=e Phcspha~a~e, ing'l uni~a/! een S.~.O.T., Fi tn in~'l uni ts/i Ee lesan 5.~.P.T., inc'l unlts/l Cater, Chafes ~er~l, we mg/i00 m! fos proce, ~oral Proren, iiag/IO0 ml fr.~5~n, Ta gilO0 ~ fom, Sodi~, uameq/l rami, P= :assi~m, avierse, meq/l Sarsperce, ~eq/1 ~=orga~= Phosp~e, ~/00 ~ Co Gum tian -, - Glut~l Transpe~tidase path Si~ u~s/~ Copnrcrisoeelmiomnpokisae, Creaul~ne Phosphoki~se, acc Some Bane Soka Toney sr. Ninety-Day ~ubacuce Rhesus .~onkey Toxlc!t7 Study. run sm sven vem FLMALE$: S,-,mmr7 of Mean Biochemical Values. Study BE owe Month 1 Courrol TR l 8 3 Cot Control ; Bt 1 Pow 3 Cort Con~r=l I 5 C~n~rol ol 1 Con=rol 107 163 88 25.6 25.2 28.7 1173 ~092 16 &6 3 36 ose 0.~ mg/kg/day wo119 %98 #97 io22.0 #325.5 i21.5 wn1013 942 bi39 355 36 swe 1.5 3g/kgiday PY113 Fe:19 f0d:20.7 a26.~ i22.6 =770 753 Hon20 ~5 27 Control 1 PB i 3 co 0 on Control om @ ! OW fi 3 Cra 0 Control i bo il I 3 5 i 3 et an pre ~==rol ; pe WW [ 3 pd i 3 et 1 Control Cl i [ 3 i 3 [ 22 Co==rol T i 3 I 5 1i" TM4] ~ o2Zh33 29 180 198 165 7.70 7.66 7.&9 4.71 &.86 &.77 156 155 152 4.8 4.7 4.6 342 37 27 208 221 169 8.77 8.47 8.02 5.27 5.&l &.82 158 162 ~51 5.3 5.1 ~.1 i32 35 334 Py204 i~69 4100 wio~ .67 8.63 isae5.20 pd5.42 fe5.21 pe157 i157 iI~9 55.2 i3.8 us33.7 i 3 4 is 3 Control 33I ce 3 a ~=~rol ol 2 # 1 3s i 3 3 Goel 10 x Con=rol 3TR3 32 $}e 3 111 113 6.4 D66X..)55 38 41 32 I0 5 116 111 7.5 787..332 50 ~7 40 20 i0 113 109 5.4 p45x..]77 43 ~8 30 Z& 7 Page 20 Page 20 ewe 4.~ mBik~!day wjeo16,'. :aSei3[.6 - os875 615 i57 75* i37 45 ue2176 i112" 5is5a8.82* sae5. bE5.39 8ww159 #[56 - 55.3 ue350llO 6 5:5.=z6 i530 - won !37-092 "mySH Iey E ry n ed ."Significantly different from Control ~zoup mean, p*O.O$. eeSignlfican~ly differ~n~ from Com~rol Stoup ~ean, p~0.01. available 1119911..00002233 33MMAA1100006655002266 [| mere sme mre aes [[EEiS seems smsss sma aes P=] THE zsavs maszs amin: sma i {43} U[liHssE] |i i $1.1 ol HsEiB dHaEoE HE 3P1 HE1S35)8] PJoiIllaisy]l sEmEs ozmmgs Emmzs zm: smgmanos somas ss mso wamsiwmesss 83353 32333 3333 IEE GERomI mD EE Ems m 33338osm 3snz osmtEmny mgaEma TssEsReEs SsEsRmRaEs sRzEsEtSrE mess REERR $1355] i187 iHolic|) ammzs $3ea83 A mmees AAs a semen AREER zamss RsEam F185] | |3ig| sens EERE GsRmEsReEs EsEeseEs asopsems EE I] EEE EI HEI mn Cl PPEE]E zmsez 3 osmsss 4 asses 5 amass dPalorgi]a ee ETTeen ETJenn ETdames HEHE EER EERE REFE 11119911..00002244 Page 21 Ta~,e 21 : i i i i | | i| i i | |i Le [IE 33MMAA1100006655002277 VLE] EIE}E EE] iHH i 2i 1:53]) IH Ici i De E| FE i i F3iEglRiEieD| 33 HE EEE a HieE HEEL] i 135) isl | Ha Li EE3 D UEE sesas samen somns meses esses sspze amen mame amor om: mma oma zzz oszzza oma: asm: menaonse ssemncse mcommmon osmmaonees spas sass sERas sms = mmeommoamnnomus s3m323zReE oeEsIaiioIsmanmiein 3 ozss zi3ze g3%z: EEE: seme RSTERm amRRE Ramm2 mmaza sams ssssa wsszs 2fzsa 333F SIRE BBESR lugs aErmRanIi omzaEziioommmaa:l omnmls: pi ail sez: Soro sEges Yu zR@Ei EEE RDEEEITEemRer LoaPneSe d|f qpF annAduSaOne?| 11119911..00002255 rage 22 Page 22 | | :i i| i | ii |} | | | Ii | i | || !i | [II E 33MMAA1100006655002288 Hi:_EH-_.] sens creza geen 3 saras smaza sees LilHiH i iy. 1|4g5]%)] Polis) i5 J 13 HdHI HdEsH UE Bfi il HFiElMdSe) HH 3h$11i1:1e5180 2) |g5| IV| lIedS|s mmr mmr =B2RssEcE: sure 23332 FREER sss smemenr: szzze sens ware: Sgg3e3r2s mann mms 388R2I2i2 oman 3283 REERE ame gmmmonrs ossmss amman wares sapnaszis a mon mm GI3EIEEEEE:S amin PERIE EEESS aml omsoems mame: mames samme EssRssEz rage23 PaSe 23 ! } i i !| | |: | - ; |! i || PP| a30 ZEEE: ERIia ERRiz I LB] zemze sesss ssszs 111 HBEERIGIEE PEAEERE NHOEISFENS E| RE HESEIT PEi 11119911..00002266 33MMAA1100006655002299 FrCe--9955:: TTAHBLLEE 1I00.. UUreitnnaallyysstiss VVooollyuummee,, mi "pH SGprSeapecvciiifcfiyicc Gravity NNitnaeetcyy--DDaayy SSuubbaaccuuttee RRhheessuuss MMoonnkkeeyy TTooxxiicciittyy SSttuuddyy.. MMAALLEESS:: SS-u-m~,aarryy ooff MMeeaann UUrriinnaallyyssiiss VVaalluueess.. oSSttauutddhyy Control 0.5 mg/kg/day 1.5 mg/kg/day Month Con=rol 0.5 mg/kg/day 1.5 mg/kg/day CCoonn=t1rrooll 33 1 CCoomnet1rrooll 331 CCoonmte1rrooll 31 3 232022 13i000 767..622 677...4000~ 11i ...000323282 Li.o02m8a 1.034a 2222 33235 885..s33 5T7..a52ea L1L.0o02a2r77 IL.o02n7e 1.033a "2208 477s50 885.'s5s 885...900a0 11L..o00a3300 1t.o0a21 1.024 Page 2 44..55 mmeg//kkag//ddaayy 535888 38-p88..o44 6-.-4 IlL.oo03xx4 i. 0--33 137-082 137-092 a-2ssi=tggnaNlottffiicacavaanniccleeabnnlooect ddeetteerrmmiinneedd dduuee =too oonnllyy oonnee vvaalluuee iinn tthhee CCoonnctrrooll ggrroouupp.. - - Not availaSle 11119911..00002277 33MMAA1100006655003300 ze-95: FC-95: TTAABBLLEE 1I00.. rUrtinnaallyyssiiss VVoollauusmee,, pFHl GesSappveeiccetityfiicc Gravity Nisecy-day Subacuce Rhesus Monkey Toxicity Study. Nine=y-Day Subacu=e Rhesus Monkey Toxicity Study. CCoonntt.. FFEIMMAALLESSS:: SSuummmaarryy ooff MMeeaann UUrriinnaallyyssiiss VVaalluueess.. oSSetnuutddhyy Control 0.5 mg/kg/day 1.5 mp/g/day Mon=h Conmrol 0.5 mE/kg/day 1.5 mg/kg/day CCoonntt1rrooll 331 cCoonnttIrrooll 331 CCoonntt1rrooll 33 1 233522 88205 885..811 885..080 111..000333211 L1i..o00z23i12 5533 33103 757.'.99s 995...005 LL1.000322277 Li1.l.0o02z3112 22200 "42008 ap8.3n3 06.~ L8.0031 111i...00002322s188 1.025 Page 25 Page 25 ~4..55 amgg//kkagl/ddaayy 3330 23-886..s88 6.35 1.- 027 11i...00-0233766 - 137-082 137-092 - = Not avatlable - - Not availaSle 11119911..00002288 33MMAA1100006655003311 IEe La CEE ee pepe ep ees ELL LLL iDUEi e5e et eee ee J P1oE 8gB Bly Torem ooip or8 n p own i How oor ow op Fil $3 5F #: ITH ee if FHMHEEI]IHH315] sete eer tems eee were eee waiz oem :ilP| EHsl aete rene sess cous UL sess sess szer sass U[sa|] if3e2nn amteEs zszmaas nmaamm EOE ORR Bn By | i|b sees Fass seer gas [175 wenn aman een ee IB 4 Hela 3 3 11119911..0000229 Page 26 I ii 2 | | 11[3i3Fs,E3E: aii |i! Lil R[J ieiHtelit | | [IEEH, Lud 1[8a8533 | lz 33MMAA11000066550032 [| Pillado 2: Hep ee gp i]PE | i sD Ime mnrown pny sSiedb oewesr ooops 1 zor oossne fil HE To op HE see ssn saan eens iFE3I 00 HE PEL ID eeee eeee eeme are is o o |} p| F "2 osgs yy sm: ms sweamee o29u5s8 iCBDR ONE sm onm | 5 amzz mses =ssr sans i 3| rr a res eens SJ EE d3eers Jzaan di unn d: em 11119911..00003300 rage 22 Page 27 LE iH H3H; HH | A hn [jEiE :i | L| a2ala {2582 loasiid i D| E3 [| iEtHhH aisid | i:H 33MMAA1100006655003333 |J HEE ET i lyad iE) Car pee amg EH fue gee eens gl $F0E3.Toon HE HH # Fry Fer as Tiger ao 1P H5E H rori eeeer oeese iE3E70OH ver seer meee 2i UH eet seen eee i| i i(|iBil E2 E2E2 O$E2E3E8E E35E:E3 Poel rao osm ES EES &es2 2232 sgan 3II3 i i i Eras rEas rzas xzas il NINE i i3 i3 E SlEaEnlHYE e BER eEe E EMRogsRBiOnEaEs 11119911..00003311 Page 28 PaEe 28 if o, iit it ; i L HHREM je Fi4H E [[JnraEiei2EgsasEee ! : i| 3 [1] HE lesnss | i i PiE 33MMAA1100006655003344 rage 29 Page 29 FC-95 : sefue Agrenals enlarged brown Ln color Necropsy Observations, Ter~nel $~c~ce and Deaths. _ Simi. deus dss fHilee:rz2r:23s:3e8 ss83ss35s3a83i3i83i2d: Lun~ ~ellowish mi:e lesions dark red area pleurel adhesions dark red raiJed focus aodule accessory splenic tissue Thymus x x S~omach raised edema, nodules glandular =ucosa Sh ete, dar~ yei!ow ~.hick fluid, VILL aie void of on~en~s IIeocoli~ orifice ongestion LAver accea=uaced lobulacions yellowish focus/area brown Ln color uo::Led whhe~orrhaEe, bindli~bs abscess, riEh~ hand . I. . - sacrificed in excre~is. 11119911..00003322 33MMAA1100006655003355 | | 323333 3832223 ssanag id {| IND HIND Bind bd i 522324 f3sEeR 224323 z3az LY| lE)=! Ec HegIrNesDs NnezIasIz msaiznasts = uczmez rage30 Page 30 HE fl 234223 s3zags gaaszs Hg ay oaag|B i Hi:AA) sSsEzNemDs sZzEzNenEs h wssE enn RomneEs L|if { iy iH] i| I 355332 s3sass SERSER 2233828 2333s szszze ddddid 231313 ssasms sassas did4ssd zzsazy gas [EDF mess|i EEE1 i: grag (EL | $$ii) 392333:313 3sIzAsaInE: ssIsMan:s osw3ang 0s ar EE J ; El lgmratgntag 4; 5 ian inindus 5 3 11119911..00003333 33MMAA1100006655003366 Page 1 Page 31 TA3LE 16. H~c~os~op~ Observations. SpE ipa shy -itn i$H1 232335%2 3353%F TF2i32z2 $Erii:st ~razn Peripheral Ne.-ve Sn Eye f~c~ of l~hoid ~f~ra~es ~!an/ ~ys~ic ~arsal ~l~ds Piiuip i=aryToac ot tras mtsence a ~ar~ =e~osa ~renals focus of i~pnoid ~filtra~e /Lffuse ~on~es~ion aci/o?h~ic desenera~on of Sy see ~ s~l! ~roups o cells Eseir -- diffuse lipid depletiou focus of In~mrs~itla! lymphoid sien: : > sas a : riCsaasa TTT I rr Ti as Parathyroid Tongue Terps, oca_i hzalin de~enera=iou o muscle focl of i~fi~anor7 cell infil~raues ~ ~ osa! epi:he!i~ and l~i~ ~ropr~ SEE arin loci of ~fi*~o~ call ~ muscle ~nEylo~ s~. i~ ~ucosal epi~heli~ 1 1 i 3114 3 2 2 1 1- '3 , : 2 2 x - -1 3 ' R : 1 !1 ` , 3 GREED wn. 000 rr re : loci of iafl:-~=~ory cell a --atl he shat > i Esophagus TEE ttm cnt tics in fccl of i~flam=a=or7 cell ~-f!i'~ra~es in 4 3 2 3 1 1 2 2 ~ 2 222 3 ! 1 1 1 2 1 1 ! I lamina ;r~pria 3 2 3 3 2 2 4 32 EE ~ear: loci of ~nters=tial lymphoid iufil~rates small focus of myocardial necrosis I 2 3 3 I 3 2 3 2 1 3 2 2 2 apSim es Code: x - condition present 1 - not remarkabie 2 - very. sii~ht ame 3 - slight & - moderate Ee 5 - marked usm 6 - ~treme - - nc~ available ET... ome * - died or sacrificed in !37-092 11119911..00003344 33MMAA1100006655003377 nage 32 Page 32 te TTT ~aivary ~$and 7 -- foc~ of in=srs=i:ial L~phoi~ md ss infiltrates decreased cell size, loss of ~ycoplasmic Ecanules dila=ed duc:s fm eye raw ssa ff sz: 33s TTT ress 2 2 3 2 ICo soI a 3 2 sss iii TT av1os l : 2 2 4 ~ 3 1fo5ca1! preertivvuassctualiatrsnepecurtoroppsshlll isnafuitlctrrsacteess re ~oca! aggregates of alveolar ~rop~ges acarlan ~i~e~= (peri~ronchlclar, Serenata, Bertvaseutae ~erib ronchi~, perlvascular a,Rl pes loci of per~vascular l~pho~4 ~f~ra~es a a snp Zhe1Srekthola 1aen foot of perlbronchial/peribronchiolar i~phold aggregates lun~ mica in bronchlolar l~en acute focal brouchcpne~on~ =hroRic focal plauri=is STaINnEiahet 1 seri focal acc~lation of blood and n~roph~s ~ alveoli coin emia, foe tszemaisial tibeonss focal n~rrhase, focal ~uersi~ fibrosis p21 z 2 2 2 EE 3 3 3 3 Tonsil ksracin-fi!!ed cyet BITES wn ween fo~ of ~nfl=~:ory cell infil=ranes in muoosal epithelium and lamina proprta LR Sm e m focl of !nfl~m~ory c~ll ~~tra~es nielemn mai, surface epi~he!i~ and ~ons~la~ 3 4 mE Th.~-~u~ Lye.oh Nodes diffuse re=iculoendo~hellal ce!l hyp erp las ia ir EEE Fa Stomach totiamaceny cot atti tn toci ko~ f Spriopra~ r wit tattieaces dn "lasine propriasod subsucosa ~oci of infl~=~o~ call ~f~raues LEN ei ctsnion of mtn l~a ~ropria and serosa S~II mui~ifocal cystic d~ata~io~ of glands ' `4 23 35 J?3 ,3 2122 ! 3 Z 2 Z 3 3 3 2 3 3 : : : ni 222: 222 2 3 3 3 3 3 : 22 22 22 22 3i+2 ?2 s s 3 ss ia 2P3rone . , 3 : Pr 3 . aeCode: won 137-092 pigemepe x - condi:iou present i - not r~markable EES 2 - very slight giage slisht EEE marked time not available Elena died or sacrificed in extramls 11119911..00003355 33MMAA1100006655003388 - TAz~L~ ~6. Con. at th vor 4 nS Microlcop~c Observations. raze 3 Page 33 SEL ewe Lie i. 5 mglk~Iday see &.5 ",, HY z23s gees pss 3iii i np -x , x X x CoiDn 1 11 1 1 1 focal mucosa! hemorrhage 3 paras&t!c ~ranuloma Ln muscularLs and EE rr-- : parasitic ~ranulo~a in serosa and f~ci of inflammatory cell Infil=races Ln muscularis and serosa loci of inflammatory cell n11tra~es loci of in1=~ory cell i=~il=rates i Em , in muscularis, serosa and mesen=e:'y parasitic granuloma in mesen=er7 parasitic ~ranulo~.a in =uscuiaris FEES RR : chronic focal seros~=is a rl TT ETE ETET fool of Infl=--'~:o~T, cell infilcra~es TE EooTsE tpLiE i mtRoE t. res F:;1e,: oa f:: + 3tesCo , A, tn ~uscularis I i 1 i 3 2 2 3 1 1 3 3 1 1 1 x xx x 2 3 3 2 3 Een L amT e Cn0 in roams amt a arin ety 3 3 E3 L3 3E2 ES2 EE3 3 . IRE 3 2 2 5 & 4 4 3 3 = 3 3 rT focal ly~phold infll:rates i~ ~eripanc~eatic fat ~issue Je : decreased cell size, loss of z~aogen te ST . Lots ~ranules i i 1 3 1 4 4 focal ince~s=i~ial izmphold infiltrates 3 2 3 P PDoEmEmST e CmET Be E tse ee i - ~o: r~mar~able 3 - sll~hc 4 - moderate - = not available 2 - yew s!iEh * - died or sacriced in exCr~mis 137-092 a - autolyzed 11119911..00003366 33MMAA1100006655003399 roFC-95: T.~LE 16. C~nc. oy ip pin wn ou ey Hp Niuer7 Day Subacuts Rhesus ~nkey Toxiclcy ~croscopic Observations. Page 3 Page 34 Es Samer lgser sie ~idney LC ---- m~l;inuclea=ed iL~ epi;~e!i~m L~ papillar> ducts LE amen f~al interstitial iTmphoid focus of g!omeru!ar fibrosis nn Be ~icroli~h in rerml tubules ill we cystic ~lomerull Tage : 113s . aaa s Co a as i2 e2s2 4 3 3 3 fy wt atten Urinary ~ladder in lamima prcpria of SmI. loci of inf!=~-cory cell loci of ~fi=~ory cell ss 1 3 3 3 : ars 2 2 ] aaa 2 3 2 1 1 s 4 omnes 2 1 loci of interstitial 17~phoid infil=Tates 3 3 LF~phoid modules/infilc:a:es in corpu~ 3 2 Sa~ ocys~is sp. ~n =uscle 1 uUer~ne ~lands smal! ~oci of hemorrhage smn endomecri~ ne sim 5 is focus of L BTT st sr pa prepuberal development 2 : 3 : " tI s 3 : " ig : i K X : 2 p vr EE of eis ations a meen i i . epi=helium and lamina pr~ri~ 4 3 pry -- i $1 1 3 loci of lymphoi4 infil~ra~es in musc'olarls 2 2 ~ocus of ~ucosal epi~hellmm 2 r Meme ar in ~kel~al muscl~ Sar=ocys~is sp. Eea ramen eit : fool of in~ers=l~lal i~i=.-~=~ory cell SL sci 1: i : infil~rates i 1 1 1 ! 1 3 2 3 4 i 1 small loci of necrosis : me omens NEE. NEE C~de: 27 vnveeorr:yys:s~ilmLgagrnhkueable 3 - slgh: ~55 -- s~~aoardr~eeredace -+== tnoitedaovrailsaabclreifices fo mezents 137--092 11119911..00003377 33MMAA1100006655004400 FC-95: TASLE 16. Cont. N~necy Day Subacute Rhesus ~onkey Toxicity Study. Microscopic.Observatlon~ page 35 Page 35 Sm nage Lise sae Site BY raz zzz: ssi: id EE Pe i ki EAoreaime .x C2it 2 " 7?3 2 ro i3 3 M=~ry Gland dermal nflan=~=ory cell infla~r~cory ~xuda~e in d~c~s 32 3 2 2 ~i!a~sd ~uc~s ETE se 1535 fsey Qr,r ges hyperkera~osis ET TTT TT T TTT ~one/3one ~rro~ (R~b ~ :Lou) TEL St h~ocellular ~ov ~Lff~e conEesclon L37-092 TRImERSOIIINDY Coda: ~ - condition present ~ - ~oc :emarlu~le 2 - very slight ~ - ~dera~e 5 - ~arked STILT wees - = uoC available * - died or sacrificed n ex~reeis i 11119911..00003388 33MMAA1100006655004411