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IntJHematol.2008Jul88(1):7381.doi:10.1007/s1218500801152.Epub2008Jul4.

Asafety,pharmacokineticandpharmacodynamicinvestigationof
deferasirox(Exjade,ICL670)inpatientswithtransfusiondependentanemias
andironoverload:aPhaseIstudyinJapan.
MiyazawaK1,OhyashikiK,UrabeA,HataT,NakaoS,OzawaK,IshikawaT,KatoJ,TatsumiY,MoriH,
KondoM,TaniguchiJ,TaniiH,RojkjaerL,OmineM.

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Abstract
Thepharmacokinetics(PK)andpharmacodynamics(PD)oftheoncedaily,oralironchelatingagent,
deferasirox(Exjade,ICL670),havebeenevaluatedfurtherinaPhaseI,openlabel,multicenter,dose
escalationstudyinJapanesepatientswithmyelodysplasticsyndromes,aplasticanemia,andother
anemias.Deferasiroxwasinitiallyadministeredasasingledoseof5(n=6),10(n=7),20(n=6)or
30(n=7)mg/(kgday)andthenafter7dayssevendailydoseswereadministered.LinearPK(C
(max)andAUC)wereobservedatalldosesafterasingledoseandatsteadystate,anddose
dependentironexcretionwasobserved.Pharmacokinetic/pharmacodynamicparameterswere
similartothosereportedinaCaucasianbetathalassemiacohort.Followingthesingleandmultiple
dosephases,21of26patientsprogressedtoa3yearextensionphaseofthestudy,wheredose
reductionsandincreases[530mg/(kgday)]wereallowedfollowingsafetyandefficacyassessments.
Intheinterim,1yeardatashowthatdeferasiroxwaswelltolerated,withgenerallyinfrequentandmild
adverseevents.Reductionsinserumferritinlevelswereobservedandanegativeironbalance
achievedatdosesof2030mg/(kgday).Thesedatasuggestthatdeferasiroxhasastableand
predictablePK/PDprofile,irrespectiveofunderlyingdiseaseorrace,andapredictableand
manageablesafetyprofilesuitableforchronicadministration.
PMID:18597054 DOI:10.1007/s1218500801152
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