MedKooCat#:201500
Name:Imexon
CAS#:59643-91-3
ChemicalFormula:C4H5N3O
ExactMass:111.04326
MolecularWeight:111.1
ElementalAnalysis:C,43.24;H,4.54;N,37.82;O,14.40
Synonym:BM06002;BM-06002;BM06002;NSC313425;NSC313425;NSC-313425;Imexon;Amplimexon.
IUPAC/ChemicalName:4-amino-1,3-diazABIcyclo[3.1.0]hex-3-en-2-one
InChiKey:BIXBBIPTYBJTRY-UHFFFAOYSA-N
InChiCode:InChI=1S/C4H5N3O/c5-3-2-1-7(2)4(8)6-3/h2H,1H2,(H2,5,6,8)
SMILESCode:O=C1N2CC2C(N)=N1
TechnicalData
AdditionalInformation
PhaseIstudyofImexon:Onehundredfivepatientsreceived340treatmentcycles(median2,range1-16).Patientcharacteristics:medianage63,61%male,ECOGPS0/150%/50%,93%metastatic.DLTwasaBDominalcrampingandpain,oftenwithtransient,acutediarrhea.Bestresponsewasconfirmedpartialresponse(PR)in11.4%,8.9%unconfirmedPR,and48.1%withstabledisease.TherewasadoseproportionalincreaseinimexonAUCacrossthedosestestedwithterminalhalflife69minattheMTDandnoalterationofgemcitabinepharmacokinetics.TherecommendedphaseIIdoseofimexonis875mg/m(2)withgemcitabine1,000mg/m(2).DLTwasacuteabdominalpainandcramping.Encouragingantitumorresponsessupportfurtherevaluationofthiscombinationinadvancedpancreaticcancer.(source:CancerChemotherPharmacol.2010Jul;66(2):287-94.).
PhaseIstudyofImexon:Onehundredfivepatientsreceived340treatmentcycles(median2,range1-16).Patientcharacteristics:medianage63,61%male,ECOGPS0/150%/50%,93%metastatic.DLTwasabdominalcrampingandpain,oftenwithtransient,acutediarrhea.Bestresponsewasconfirmedpartialresponse(PR)in11.4%,8.9%unconfirmedPR,and48.1%withstabledisease.TherewasadoseproportionalincreaseinimexonAUCacrossthedosestestedwithterminalhalflife69minattheMTDandnoalterationofgemcitabinepharmacokinetics.TherecommendedphaseIIdoseofimexonis875mg/m(2)withgemcitabine1,000mg/m(2).DLTwasacuteabdominalpainandcramping.Encouragingantitumorresponsessupportfurtherevaluationofthiscombinationinadvancedpancreaticcancer.(source:CancerChemotherPharmacol.2010Jul;66(2):287-94.).
CombinedPhaseI/IIstudyofImexon:Imexonbelongstoanovelclassofpromisinganticanceragentsthatinducetumorapoptosisthroughoxidativestress.Clinicalexperiencesincethelate1960shasprovidedinitialevidenceforaclinicalantitumoractivity. Preliminaryantimyelomaefficacyof Imexonwasobservedwith1minimalresponse,12(36%)stablediseaseresponses,andallotherevaluablepatientshadprogressivedisease.Remarkably,thepatientwithminimalresponsealsoexperiencedacompleteclinicalresolutionofmyeloma-associatedpolyneuropathy.Overall,Imexonwassafeandwelltoleratedinthedoserangeinvestigated.Imexonshowedminorclinicalactivityasasingleagentinheavilypretreatedmyelomapatients.Onaccountofitsuniquemechanismofaction,favorabletoxicityprofile,initialclinicalevidenceforantimyelomaactivity,anditsknownsynergisticactivityincombinationwithapprovedagentsformyelomatreatment,Imexon isrecommendedforfutureclinicalstudiesincombinationregimensinmultiplemyeloma.(AnticancerDrugs.2010Aug;21(7):708-15.).
CombinedPhaseI/IIstudyofImexon:
(AnticancerDrugs.2010Aug;21(7):708-15.).
References
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