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Technology|AegisTherapeuticsLLC

IntravailTechnology
Intravailcomprisesabroadclassofchemicallysynthesizabletransmucosalabsorptionenhancementagentsthatallownoninvasive
systemicdeliveryofpotentpeptide,protein,nucleotiderelated,andothersmallandlargemoleculedrugsthatwerepreviouslyonly
deliverablebyinjection.

IntravailisSafe
AegisIntravailabsorptionenhancementagentsaremildandnonirritatingtomucosalmembranes.Theyaresafe,odorless,
tasteless,nontoxic,nonirritating,nondenaturing,andnonmutagenic,chemicallysynthesizedmoleculesthatmetabolizetoCO2
andH2O.Thesemoleculesarecloselyrelatedtomildsurfactantswidelyusedinpersonalcareandfoodproductsinsignificantly
higherconcentrationsthanthoseusedinAegisformulationsandarerecognizedasGRASsubstancesformanyapplications.

IntravailisEffective
Intravailabsorptionenhancementagentsprovideexceptionallyhighandunmatchedbioavailabilityperformance,comparablein
efficiencytosubcutaneousinjection,viatheintranasal,buccal,intestinal,andothermucosalmembraneadministrationroutes,
deliveringpotentpeptide,protein,andlargemoleculedrugsthatcancurrentlyonlybedeliveredbyinjection(SeeFigure1).

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Figure1Intranasalbioavailabilitycomparedwithinjectionofequalamountsofproteinandpeptidetherapeuticsofdifferent
molecularweightsupto30kDaasafunctionofIntravailenhancementagentconcentration.

IntravailisBroadlyApplicable
Wehaveprovenfeasibilityforabroadrangeoftherapeuticsupto30,000Daltonsmolecularweightincludingcalcitonin,growth
hormone,leptin,PTH,insulin,erythropoietin,PYY336,GLP1relatedpeptides,glucagon,antisensedrugs,andlowmolecular
weightheparins.WhileourprimaryfocusisontheintranasalapplicationofIntravail,thetechnologycanalsodramatically
improvethebioavailabilityoftherapeuticsthroughanyofthefollowingmodesofadministration:
Intranasal
Oral&OralCavity
Ocular
Rectal
Transdermal
Vaginal
Pulmonary

SimpletoUse
Intravailtechnologyiscompatiblewithsimpleofftheshelfnasalspraydeliverydevicesandstandardhomogeneousmanufacturing
formulationanddispensingprocessesnoparticles,powders,liposomes,orchemicalmodifications,andnoneedforcomplicated
andexpensivedispensersrequiringpatienttraining.Ourcustomersarenotrequiredtoinvestinanyspecialmanufacturing
equipmentordeliverydevices.

IntravailisGoodBusiness
Creationofintranasalformulationsofexistinginjectableproductsprovidesaccesstonewandexpandedmarkets,broaderclinical
applicationsofexistingtherapeutics,andgreaterpatientconvenienceandacceptance.Confirmingthis,salesofnasallydelivered
therapeuticshavedemonstrated5to33foldincreasesinsalesovertheoriginalequivalentinjectableformulation.Newnon
invasiveformulationsofexistingpeptideandproteintherapeuticscanprovideopportunitiesformaximizingvalueextractionfroman
existingdrugfranchiseandwillallowforpatentlifeextensionandproductlifecyclemanagement.Withareported600700
peptidetherapeuticsinclinicalorpreclinicaldevelopment(Frost&Sullivan)noninvasiveIntravailbasedformulationsofnew
peptideorproteindrugswillfacilitatemarketintroductionoffirstinclasstherapeutics,capitalizinguponthegrowingtrendtoward
broadscaleacceptanceofpeptidedrugs.

SummaryofIntravailPropertiesandBenefits:
Mildandnonirritatingtomucosalmembranes
Exceptionallyhighandunmatchedbioavailabilitycomparableinefficiencyto
subcutaneousinjection,viatheintranasaladministrationroute
Deliveryofpotentpeptide,protein,andlargemoleculedrugsthatcan
currentlyonlybedeliveredbyinjection
Noalterationofthechemicalformorbiologicalintegrityofthedrugi.e.,no
liposomesparticles,pumps,patchesoremulsions
Rapiddrugabsorptionandonsetofaction
Controlledtransientpermeationofthenasalmucosalbarrier
Avoidanceofgastrichydrolysisandfirstpasseffectelimination
Greaterpatientconvenienceandcompliance
Eliminationofneedlestickinjuriesandassociatedtransmissionof
bloodbornepathogens
Compatibilitywithcurrentnasaldeliverydevices
Easeofformulationandcompatibilitywithroutinehomogeneousformulation

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Technology|AegisTherapeuticsLLC
anddispensingmanufacturingprocessesforeaseofscaleupandproduction
Extensionofpatentprotectionandproductlifecycle
Broadlyapplicabletoothertransmucosalandtransdermaladministrationroutes

AdditionalLinks:
Increasedbioavailabilityviamultipleroutesofadministration
Morerapidonsetofdrugaction
EnhancedCNSDelivery
ModeofactionOpeningtightjunctionsandinducingtranscytosis
Intravailfunctionsreversiblyandindependentlyofdrug

ProTekTechnology
AegisProTekproteinstabilizationtechnologycomprisestheuseofproprietaryGRASexcipientsthatpreventaggregationof
proteinsandpeptidestherebystabilizingthemandreducingimmunogenicity.ProTekallowscreationofproprietary,easily
manufacturable,homogeneous,stable,aqueousorlyophilizeddosageformsforpeptideorproteintherapeuticsthatmaintainthe
structuralintegrityandphysiologicalactivityofmanyproteinandpeptidedrugs.ProTekformulationsareapplicabletoinjectable,
intranasal,andotherdosageforms.ProTekexcipientsmayalsobeincorporatedintomanufacturingprocessesrequiringproducing
ormanipulatingconcentratedproteinorpeptidesolutionswhichresultinunwantedorirreversibleaggregation.
Figure2demonstratesthelongtermpreventionofhumaninsulindenaturationatelevatedtemperatureuponcontinuousagitation
at150rpm,37C.Lightscattering,aquantitativemeasureofsolutioncloudinessarisingupondenaturation,wasmonitoredovera
periodof60daysinthisparticularstudy.BioassayconfirmsthelossofactivityintheabsenceofProTekexcipient.Without
inclusionofaProTekexcipient,insulinbecomesperceptiblycloudyinamatterofhoursunderthesestressingconditions.The
stabilizationeffectisevenmoredramaticatpHvaluesbelowpH7whereinsulinincompletelydenaturedintwodaysorlessinthe
absenceofProTekexcipient.Completestabilizationhasbeendemonstratedtocontinueforuptothreemonthsofcontinuous
shakingat37C.StructurallyrelatednonProTekalkylsaccharidesfailtoprovidesimilarprotectionasshownbythecontrols.
2090

Figure2Extended60daystabilityofhumaninsulin(pH7.5)withProTekIcomparedwithanonProTekalkylsaccharidecontrol
(at37C,150rpm).

AdditionalLinks:
Aggregationpreventionforpeptidesandproteins
Eliminationofoxidativedamageandunwantedimmunogenicity

AegisHydrogelTechnology
AegisHydrogelsareproprietaryabsorptionenhancingselfassemblingaqueoushydrogelsusefulfortransdermaldrugdelivery,or
fortransmucosalapplicationsbenefitingfromextendedresidencetime.AegisHydrogelsservesimultaneouslyasbothdelivery
vehicleandabsorptionenhancer.Indermalapplications,thesehydrogelsleavetheskinfeelingsoftwithnosenseofanyresidue
whenrubbedontotheskin.Indispensingapplications,includingdepotorsustainedreleaseapplications,thethixotropicnatureof
thesegelspreventdrippingorrunningandallowsresumptionofthestablegelformassoonastheshearforceofdispensing
terminates.

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