afatinib.docx

afatinib.docx

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afatinib

AccessionNo:

42195

MainDetails

DrugNameWorldStatusPharmaStatus

afatinibPre-registrationActive

afatinibdimaleate

BIBW2992

BIBW-2992

BIBW-2992MA2

Tomtovok

Tovok

LatestChange

UpdatedOnByLatestChange

12Mar2013AD134EnrollmentcompletionofPhaseIItrial（Lux-Breast3）forbreastcancerreported

CompanyStatusData

OriginatorCountryDevelopmentStage

BoehringerIngelheimGermanyPre-registration

ActivityData

TherapyDescriptionCodeStatus

COPDtreatmentR4ANoDevelopmentReported

Anticancer,otherK6ZPre-registration

PharmacologyDescriptionCode

Tyrosinekinaseinhibitor（TKI）KI-TYR-

ErbB-1tyrosinekinaseinhibitorKI-TYE1-

ErbB-2tyrosinekinaseinhibitorKI-TYE2-

ProteinkinaseinhibitorKI-PR-

TherapyCodePharmacologyCode

K6Z

R4AKI-PR-,KI-TYR-,KI-TYE2-,KI-TYE1-

KI-PR-,KI-TYR-,KI-TYE2-,KI-TYE1-

RouteofAdministrationRouteofAdministrationCode

Alimentary,poA-PO

IndicationStatus

Cancer,pancreaticPhaseIClinicalTrial

Cancer,solid,unspecifiedPhaseIIClinicalTrial

Cancer,sarcoma,unspecifiedPhaseIClinicalTrial

Cancer,breastPhaseIIIClinicalTrial

Cancer,lung,non-smallcellPre-registration

Cancer,prostatePhaseIIClinicalTrial

Cancer,headandneckPhaseIIIClinicalTrial

Cancer,brainPhaseIIClinicalTrial

Cancer,bladderNoDevelopmentReported

Cancer,endometrialPhaseIIClinicalTrial

Cancer,colorectalPhaseIIClinicalTrial

Cancer,gastrointestinal,stomachPhaseIClinicalTrial

Cancer,ovarianPhaseIIIClinicalTrial

Cancer,oesophagealPhaseIClinicalTrial

Cancer,renalPhaseIClinicalTrial

Cancer,melanomaPhaseIClinicalTrial

Cancer,cervicalPhaseIClinicalTrial

ChronicobstructivepulmonarydiseaseNoDevelopmentReported

Pharmacokinetics

Human（10-100mgpo）

MTD-70mg

ChemicalData

OriginofMaterialCodeDescription

CH-SYChemical,synthetic

CASRegistryNumberMolecularWeightMolecularFormula

439081-18-2

850140-72-6

850140-73-7485.95C24H25ClFN5O3

ChemicalName

2-Butenamide,N-（4-（（3-chloro-4-fluorophenyl）amino）-7-（（（3S）-tetrahydro-3-furanyl）oxy）-6-quinazolinyl）-4-（dimethylamino）-

Structure

CountryData

CountryNameStatusYearLaunchedLicensingOp.

ArgentinaPhaseIIIClinicalTrialNo

AustraliaPhaseIIIClinicalTrialNo

AustriaPre-registrationNo

BelgiumPre-registrationNo

BrazilPhaseIIIClinicalTrialNo

CanadaPhaseIIIClinicalTrialNo

ChilePhaseIIIClinicalTrialNo

ChinaPhaseIIIClinicalTrialNo

ColombiaPhaseIIIClinicalTrialNo

DenmarkPre-registrationNo

FinlandPre-registrationNo

FrancePre-registrationNo

GermanyPre-registrationNo

GreecePre-registrationNo

HongKongPhaseIIIClinicalTrialNo

IndiaPhaseIIIClinicalTrialNo

IrelandPre-registrationNo

IsraelPhaseIIIClinicalTrialNo

ItalyPre-registrationNo

JapanPhaseIIIClinicalTrialNo

Luxembourg-No

MalaysiaPhaseIIIClinicalTrialNo

MexicoPhaseIIIClinicalTrialNo

NetherlandsPre-registrationNo

NewZealand-No

NorwayPhaseIIClinicalTrialNo

PeruPhaseIIIClinicalTrialNo

PhilippinesPhaseIIIClinicalTrialNo

PortugalPhaseIIIClinicalTrialNo

RussianFederationPhaseIIIClinicalTrialNo

SouthAfricaPhaseIIIClinicalTrialNo

SouthKoreaPhaseIIIClinicalTrialNo

SpainPre-registrationNo

SwedenPre-registrationNo

SwitzerlandPhaseIIIClinicalTrialNo

ThailandPhaseIIIClinicalTrialNo

TurkeyPhaseIIIClinicalTrialNo

UKPre-registrationNo

USAPre-registrationNo

Venezuela-No

MajorEvents

EventDateAct/EstEventDetails

3Dec2012EOrphanDrugStatusGrantedTheUS;Cancer,lung,non-smallcell

20Sep2012ERegistrationSubmissionsTheEU;Cancer,lung,non-smallcell

1Jun2012EOrphanDrugStatusGrantedAustralia;Cancer,lung,non-smallcell

16May2012ENewIndicationCancer,pancreatic

16Nov2011EChangeinIndicationStatusCancer,headandneck;PhaseIIIClinicalTrial

29Apr2011ENewIndicationCancer,squamouscell

17Sep2010ANamesGrantedBIBW-2992

21Aug2010AChangeinIndicationStatusCancer,breast;PhaseIIIClinicalTrial

29Jul2010ENewIndicationCancer,solid,general

16Dec2009AChangeinIndicationStatusCancer,ovarian;PhaseIIIClinicalTrial

9Apr2008EstChangeinStatusPhaseIIIClinicalTrial

3Jan2008ActNewChemicalStructureNew

9Aug2007EChangeinIndicationStatusCancer,squamouscell;PhaseIIClinicalTrial

7Jun2007EstNewIndicationCancer,prostate

15Nov2006ActChangeinStatusPhaseIIClinicalTrial

5Jun2006ActNewProductinPharmaprojects

Ratings

NoveltyMarketSizeSpeedTotal

2nd,3rdor4thCompound（5）US$2001-5000million（3）FasterthanAverage（4）12

DetailedInformation

Afatinib（BIBW-2992）isanirreversibledualtyrosinekinaseinhibitorofepidermalgrowthfactorreceptor（EGFR）1and2（HER2）,underdevelopmentbyBoehringerIngelheim（BI）forthetreatmentofcancer.BIwasalsoinvestigatingthepotentialofEGFRinhibitorsfortreatmentofchronicobstructivepulmonarydisease（COPD）（ScripDailyOnline,23Oct2008,S01011964）.Tomtovokistheproposedtradename（Pressrelease,BI,17Sep2010,http:

//www.boehringer-AcompaniondiagnostichasbeendevelopedtoidentifyEGFRmutationsinpatientswithnsclc（CompanyPressrelease,BoehringerIngelheim,29May2009,http:

//www.boehringer-

Marketing

Filings

________________

Cancer,lung,non-smallcell

EU;anMAAfilinghasbeensubmittedforthetreatmentofpatientswithEGFR（ErbB1）mutationpositivenon-smallcelllungcancer（Pressrelease,BI,20Sep2012,http:

//www.boehringer-

USA;ithasUSfast-trackstatusfornsclc（Pressrelease,BI,14Feb2008）.Anopen-label,USexpandedaccessprogramme（EAP）forafatinibhasbeeninitiated.TheEAPwillbeavailabletoeligiblepatientswithlocallyadvancedormetastaticnsclcwhohaveanepidermalgrowthfactorreceptor（EGFR）mutation（Pressrelease,BI,13Sep2012,AnNDAfilingwasacceptedforreviewandpriorityreviewstatuswasgranted.ThePDUFAdateisexpectedinthe3rdqtrof2013（Pressrelease,BI,16Jan2013,http:

//www.boehringer-

OrphanDrugStatus

________________

Cancer,lung,non-smallcell

Australia;forthetreatmentofpatientswithlocallyadvancedormetastaticnsclcwithEGFRmutations（AustralianTGAOrphanDrugWebPage,25Jul2012,http:

//www.tga.gov.au/industry/pm-orphan-drugs.htm）.

USA;forthetreatmentofepidermalgrowthfactorreceptormutationpositivenon-smallcelllungcancer（FDAOrphanDrugList,3Dec2012,http:

//www.accessdata.fda.gov/scripts/opdlisting/oopd/OOPD_Results_2.cfm?

Index_Number=375712）.

Clinical

PhaseIII

Cancer,breast

Itisinanopen-label,randomized,pivotal,parallelassignmentPhaseIIItrial（LUX-Breast1）inArgentina,Australia,Austria,Belarus,Belgium,Brazil,Canada,Chile,China,Colombia,Croatia,theCzechRepublic,Egypt,France,Germany,India,Israel,Italy,Japan,Jordan,Latvia,Lebanon,Lithuania,Mexico,theNetherlands,Norway,Peru,Poland,Portugal,Russia,SAfrica,SKorea,Saudi-Arabia,Singapore,Slovakia,Slovenia,SAfrica,Spain,SriLanka,Taiwan,Turkey,theUKandtheUSin780HER2overexpressingmetastaticbreastcancerpatientsafterfailingtrastuzumabtreatment,toassesstheefficacyofafatinibtabletsonce-daily+vinorelbinevsvinorelbine+trastuzumab,onPFS.Overallsurvival,tolerabilityandsafetywillalsobeassessed.CompletionisexpectedinMay2016（ClinicalTrials.gov,21Aug2011&7Jun2012,http:

//www.clinicaltrials.gov/show/NCT01125566;Pressrelease,BI,17Sep2010,http:

//www.boehringer-&8Dec2010,Companypipeline,BI,Apr2011&Apr2012,http:

//www.boehringer-48thASCO（Chicago）,2012,AbsTPS649,http:

//abstract.asco.org/AbstView_114_91790.html）.

Cancer,headandneck

Itisinarandomized,double-blind,placebo-controlled,parallelassignmentPhaseIIItrial（1200.131;LUX-Head&Neck2）inArgentina,Australia,Austria,Belgium,Brazil,Canada,Chile,Denmark,Finland,France,Germany,Greece,Ireland,Italy,Japan,Mexico,theNetherlands,Spain,Sweden,Switzerland,theUKandtheUSin669primaryunresectedpatientswithstageIII,IVa,orIVbloco-regionallyadvancedheadandnecksquamouscellcarcinoma,toevaluatetheefficacyandsafetyofafatinibonce-dailyasadjuvanttherapyafterchemo-radiotherapy.CompletionisexpectedinFeb2016（ClinicalTrials.gov,19Nov2011,http:

//www.clinicaltrials.gov/show/NCT01345669;Pressrelease,BI,26Jan2012,http:

//www.boehringer-Theprimaryendpointisdisease-freesurvival（DFS）andsecondaryendpointsareDFSat2yr,overallsurvival,health-relatedqualityoflifeandsafety（48thASCO（Chicago）,2012,AbsTPS5599,http:

//www.asco.org/ASCOv2/Meetings/Abstracts?

&vmview=abst_detail_view&confID=114&abstractID=91801）.

Itisinanopen-label,randomized,parallel-assignmentPhaseIIItrial（1200.43;LUX-Head&Neck1）inArgentina,