LC Labs/R8024 Regorafenib, Free Base, >99%/R8024/500 mg

• RegorafenibdemonstratedtolerABIlityandantitumouractivityinpatientswithmetastaticcolorectalcancer(CRC)inaphase1clinicaltrail.StrumbergD.,etal."Regorafenib(BAY73-4506)inadvancedcolorectalcancer:aphaseIstudy."Br.J.Cancer106:1722-1727(2012).
• Incombinationchemotherapy,regorafenibshowedacceptabletolerabilitywithSN-38andirinotecanbutshowednosignificanteffectonoxaliplatinor5-fluorouracilpharmacokinetics.SchultheisB.,etal."RegorafenibincombinationwithFOLFOXorFOLFIRIasfirst-orsecond-linetreatmentofcolorectalcancer:resultsofamulticenter,phaseIbstudy."Ann.Oncol.24:1560-1567(2013).
• RegorafenibshowedsignificantactivityinpatientswithadvancedandmetastaticGIstromaltumor(GIST)afterfailureofbothimatinibandsunitinibinaphase2clinicaltrial.GeorgeS.,etal."Efficacyandsafetyofregorafenibinpatientswithmetastaticand/orunresectableGIstromaltumorafterfailureofimatinibandsunitinib:amulticenterphaseIItrial."J.Clin.Oncol.30:2401-2407(2012).
• Inaphase2clinicaltrial,regorafenibdemonstratedacceptabletolerabilityandantitumouractivityinpatientswithintermediateoradvancedhepatocellularcarcinoma(HCC)afterfailureoffirst-linesorafenib.BruixJ.,etal."Regorafenibassecond-linetherapyforintermediateoradvancedhepatocellularcarcinoma:Multicentre,open-label,phaseIIsafetystudy."Eur.J.Cancer49:3412-3419(2013).
• Inaphase3study,regorafenibdemonstratedprolongedsurvivalofpatientswithmetastaticcolorectalcancerafterstandardtherapiesfailed.GrotheyA.,etal."Regorafenibmonotherapyforpreviouslytreatedmetastaticcolorectalcancer(CORRECT):aninternational,multicentre,randomised,placebo-controlled,phase3trial."Lancet381:303-312(2013).
• Regorafenibdemonstratedantitumouractivityasafirst-linetreatmentformetastaticorunresectablerenal-cellcarcinomainaphase2clinicaltrial.However,thedrugssafetyprofilerequiredclosemonitoring.EisenT.,etal."Regorafenibforpatientswithpreviouslyuntreatedmetastaticorunresectablerenal-cellcarcinoma:asingle-groupphase2trial."LancetOncol.13:1055-1062(2012).
• Oralregorafenibsignificantlyimprovedprogression-freesurvivalwhencomparedwithplaceboinpatientswithmetastaticgastrointestinalstromaltumours(GIST)afterfailureofstandardtreatmentsinaphase3clinicaltrial.DemetriG.D.,etal."Efficacyandsafetyofregorafenibforadvancedgastrointestinalstromaltumoursafterfailureofimatinibandsunitinib(GRID):aninternational,multicentre,randomised,placebo-controlled,phase3trial."Lancet381:295-302(2013).
• RegorafenibistheactiveingredientinthedrugproductsoldunderthetradenameStivarga®.ThisdrugiscurrentlyapprovedinatleastonecountryforuseinpatientswithmetastaticcolorectalcancerandpatientswithadvancedgastrointestinalstromaltumorswhichcannotberemovedsurgicallyandnolongerrespondtootherFDA-approvedtreatmentsforthisdisease.NOTE:THEREGORAFENIB,FREEBASERESEARCHCOMPOUNDSOLDBYLCLaboratoriesISNOTSTIVARGA®,ANDISNOTFORHUMANUSE.
• RelatedCASnumbers:835621-07-3forthehydrochloridesalt.
• OtherCASnumberspreviouslyassignedtoRegorafenib,FreeBase,namely1219951-07-1and1370461-45-2,havebeendeletedbyCASandarenolongerinuse.
• Soldforlaboratoryormanufacturingpurposesonly;notforhuman,veterinary,food,orhouseholduse
• ThisproductisofferedforR&Duseinaccordancewith(i)35USC271(e)+A13(1)intheU.S.;(ii)Section69.1ofJapanesePatentLawinJapan;(iii)Section11,No.2oftheGermanPatentActof1981inGermany;(iv)Section60,Paragraph5boftheU.K.PatentsActof1977intheU.K.;(v)Sections55.2(1)and55.2(6)andothercommonlawexemptionsofCanADIanpatentlaw;(vi)Section68BofthePatentsActof1953inNewZealandtogetherwiththeamendmentofsamebytheStatutesAmendmentBillof2002;(vii)suchrelatedlegislationand/orcaselawasmaybeorbecomeapplicableintheaforementionedcountries;and(viii)suchsimilarlawsandrulesasmayapplyinvariousothercountries.
• Notavailableinsomecountries;notavailabletosomeinstitutions;notavailableforsomeuses.

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