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Medchemexpress/Oseltamivir acid(Synonyms: GS 4071; Ro 64-0802; oseltamivir carboxylate)/HY-13318/5mg
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Medchemexpress/Oseltamivir acid(Synonyms: GS 4071; Ro 64-0802; oseltamivir carboxylate)/HY-13318/5mg
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OseltamiviracidisanactivemetaboliteofOseltamivir,whichisapotentandselectiveinhibitorofinfluenzaAandBvirusneuraminidases.

CustomerValidation

  • •ACSNano.2014Jun24;8(6):5468-77.
  • •Oncotarget.2017Sep15;8(47):83142-83154.
  • •EurJMedChem.2017Dec1;141:648-656.
  • •AntimicrobAgentsChemother.2015Aug;59(8):4962-73.
  • •AntiviralRes.2017Jul;143:106-112.
  • •AntiviralRes.2016May;129:81-92.
  • •AntiviralRes.2016Mar;127:68-78.
  • •AntiviralRes.2014Nov;111:69-77.
  • •JEnvironManage.2015Oct1;162:326-33.
  • •EurJPharmSci.2017Sep28;111:167-176.
  • •EurJPharmSci.2015Jul8;78:47-53.
  • •Molecules.2017Nov18;22(11).pii:E1998.
  • •Molecules.2016Aug26;21(9).pii:E1133.
  • •PLoSOne.2016May27;11(5):e0156400.
  • •PLoSOne.2014Oct21;9(10):e110631.
  • •BiomedPharmacother.2017Oct27;97:385-394.
  • •BiomedPharmacother.2017Jul5;93:636-645.
  • •FEBSOpenBio.2013Oct29;3:484-9.
  • •ArchVirol.2014Dec;159(12):3269-78.
  • •EvidBasedComplementAlternatMed.2015;2015:917670.
Description

OseltamiviracidisanactivemetaboliteofOseltamivir,whichisapotentandselectiveinhibitorofinfluenzaAandBvirusneuraminidases.

IC50&Target

InfluenzaAandB[1]

InVitro

Oseltamiviracidinhibitsvirusreplicationinvitroandinvivo.InfluenzaBandA/H1N1virusesappearetobesensitivetoOseltamivir(meanBIC50value:13nM;meanH1N1IC50value:1.34nM),whileA/H1N2andA/H3N2virusesaremoresensitivetoOseltamivir(meanH3N2IC50value:0.67nM;meanH1N2IC50value:0.9nM)[1].InneuraminidasesinhibitionassayswithinfluenzaAviruses,themedian50%inhibitoryconcentration(IC50)ofRWJ-270201(approximately0.34nM)iscomparabletothatofOseltamivircarboxylate(0.45nM)ForinfluenzaBvirusisolates,theIC50ofRWJ-270201(1.36nM)iscomparabletothatofZanamivir(2.7nM)andlessthanthatofOseltamivircarboxylate(8.5nM)[2].

InVivo

Oseltamivir(0.1,1,or10mg/kg/day,twicedailybyoralgavage)producesadose-dependentantiviraleffectagainstVietnam/1203/04(VN1203/04)virus.The5-dayregimenat10mg/kg/dayprotects50%ofmice;deathsinthistreatmentgrouparedelayedandindicatedthereplicationofresidualvirusafterthecompletionoftreatment.Eight-dayregimensimprovedOseltamivirefficacy,anddosagesof1and10mg/kg/daysignificantlyreducedvirustitersinorgansandprovided60%and80%survivalrates,respectively[3].Inthepharmacokineticstudy,aftertheoraladmiNISTrationof1,000mg/kgOseltamivir,peakplasmaconcentrationsarereachedat2hpostdoseforOseltamivirand8hforOseltamivircarboxylate(OC).RatsareexposedtoOseltamiviroverthewholesamplingintervalandhada~2.7-fold-higherrateofexposuretoOCthanOseltamivir.InCSF,peakconcentrationsarereachedat2hpostdoseforOseltamivirand6hforOC.CSF/plasmaexposureratios(AUC0-8h)are~0.07forOseltamivirand0.007forOC.Inperfusedbrainsamples,peakconcentrationsarereachedat8hpostdoseforOseltamivirand6hforOC.Brain/plasmaexposureratios(AUC0-8h)of~0.12forOseltamivirand0.01forOCarerecorded.CorrespondingCSF/brainexposureratiosrangedbetween~0.55and0.64forbothanalytes.AfurthergroupofanimalsthatreceivedasingleoraladministrationofOseltamiviratalowerdoseproducedsimilarresults[4].

ClinicalTrial
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References

  • [1].FerrarisO,etal.Sensitivityofinfluenzavirusestozanamivirandoseltamivir:astudyperformedonvirusescirculatinginFrancepriortotheintroductionofneuraminidaseinhibitorsinclinicalpractice.AntiviralRes.2005Oct;68(1):43-8.

    [2].GubarevaLV,etal.Comparisonoftheactivitiesofzanamivir,oseltamivir,andRWJ-270201againstclinicalisolatesofinfluenzavirusandneuraminidaseinhibitor-resistantvariants.AntimicrobAgentsChemother.2001Dec;45(12):3403-8.

    [3].YenHL,etal.VirulencemaydeterminethenecessarydurationanddosageofoseltamivirtreatmentforhighlypathogenicA/Vietnam/1203/04influenzavirusinmice.JInfectDis.2005Aug15;192(4):665-72.

    [4].HoffmannG,etal.Nonclinicalpharmacokineticsofoseltamivirandoseltamivircarboxylateinthecentralnervoussystem.AntimicrobAgentsChemother.2009Nov;53(11):4753-61.

AnimalAdministration
[3][4]

OseltamivirisdissolvedinsterilePBS(Mice)[3].

Mice[3]
Female6-week-oldBALB/cmiceareanesthetizedwithisofluoraneandintranasallyinoculatedwith50μLof10-foldserialdilutionsofVN1203/04virusinPBS.Themouselethaldose(MLD50)iscalculatedaftera16-dayobservationperiod.Oseltamivirisadministeredbyoralgavagetwicedailyfor5or8daystogroupsof10miceatdosagesof0.1,1,and10mg/kg/day.Control(infectedbutuntreated)micereceivedsterilePBS(placebo)onthesameschedule.FourhoursafterthefirstdoseofOseltamivir,themiceareinoculatedintranasallywith5MLD50ofVN1203/04virusin50μLofPBS.Survivalandweightchangeareobservedfor24days.Virustitersinthemouseorgansaredeterminedondays3,6,and9afterinoculation.Threemicefromeachexperimentalandplacebogrouparekilled,andthelungsandbrainsareremoved.TheorgansarehomogenizedandsUSPendedin1mLofPBS.Thecellulardebrisisclearedbycentrifugationat2000gfor5min.Thelimitofvirusdetectionis0.75log10EID50.Forcalculationofthemean,sampleswithavirustiter<0.75>10EID50/mLareassignedavalueof0.VirustitersineachorganarecalculatedbyuseofthemethodofReedandMuenchandareexpressedasmeanlog10EID50/mL±SE.
Rat[4]
SeveralstudiesareperformedtocharacterizethepharmacokineticsofOseltamivirandOCintheplasma,cerebrospinalfluid(CSF),andbrainofSprague-Dawleyratsfollowingsingle-dosebolusadministrationofOseltamivir(intravenous[i.v.]andoral)andOC(i.v.).Inthei.v.studies,nonfastedadultrats(twogroupsof35animalsforeachtestsubstance)receivedadoseof30mg/kgbodyweightofeitherOseltamivirorOseltamivircarboxylate(OC)inaqueoussolutionwithsodiumchloride(0.9%;pH4.0)viaslowinjectionintothetailveinover20to30s.Inbothi.v.studies,pharmacokineticsamplingtookplaceat5minandat0.25,0.5,1,2,4,and8hpostdose(fourorfiverats/timepoint).MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].FerrarisO,etal.Sensitivityofinfluenzavirusestozanamivirandoseltamivir:astudyperformedonvirusescirculatinginFrancepriortotheintroductionofneuraminidaseinhibitorsinclinicalpractice.AntiviralRes.2005Oct;68(1):43-8.

    [2].GubarevaLV,etal.Comparisonoftheactivitiesofzanamivir,oseltamivir,andRWJ-270201againstclinicalisolatesofinfluenzavirusandneuraminidaseinhibitor-resistantvariants.AntimicrobAgentsChemother.2001Dec;45(12):3403-8.

    [3].YenHL,etal.VirulencemaydeterminethenecessarydurationanddosageofoseltamivirtreatmentforhighlypathogenicA/Vietnam/1203/04influenzavirusinmice.JInfectDis.2005Aug15;192(4):665-72.

    [4].HoffmannG,etal.Nonclinicalpharmacokineticsofoseltamivirandoseltamivircarboxylateinthecentralnervoussystem.AntimicrobAgentsChemother.2009Nov;53(11):4753-61.

MolecularWeight

284.35

Formula

C₁₄H₂₄N₂O₄

CASNo.

187227-45-8

Storage
Powder-20°C3years
 4°C2years
Insolvent-80°C6months
 -20°C1month
Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

H2O:≥56mg/mL

*"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">

Purity:98.60%

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