317
Views
27
CrossRef citations to date
0
Altmetric
Review

Profile of neratinib and its potential in the treatment of breast cancer

&
Pages 147-162 | Published online: 09 Jun 2015

References

  • BaselgaJSwainSMNovel anticancer targets: revisiting ERBB2 and discovering ERBB3Nat Rev Cancer20099746347519536107
  • SlamonDJClarkGMWongSGLevinWJUllrichAMcGuireWLHuman breast cancer: correlation of relapse and survival with amplification of the HER-2/neu oncogeneScience198723547851771823798106
  • LinggiBCarpenterGErbB receptors: new insights on mechanisms and biologyTrends Cell Biol2006161264965617085050
  • KlapperLNGlatheSVaismanNThe ErbB-2/HER2 oncoprotein of human carcinomas may function solely as a shared coreceptor for multiple stroma-derived growth factorsProc Natl Acad Sci U S A19999694995500010220407
  • ZhangXGureaskoJShenKColePAKuriyanJAn allosteric mechanism for activation of the kinase domain of epidermal growth factor receptorCell200612561137114916777603
  • VivancoISawyersCLThe phosphatidylinositol 3-kinase AKT pathway in human cancerNat Rev Cancer20022748950112094235
  • DankortDMaslikowskiBWarnerNGrb2 and Shc adapter proteins play distinct roles in Neu (ErbB-2)-induced mammary tumorigenesis: implications for human breast cancerMol Cell Biol20012151540155111238891
  • MoasserMMThe oncogene HER2: its signaling and transforming functions and its role in human cancer pathogenesisOncogene200726456469648717471238
  • ChoHSMasonKRamyarKXStructure of the extracellular region of HER2 alone and in complex with the Herceptin FabNature2003421692475676012610629
  • Graus-PortaDBeerliRRDalyJMHynesNEErbB-2, the preferred heterodimerization partner of all ErbB receptors, is a mediator of lateral signalingEMBO J1997167164716559130710
  • WissnerAMansourTSThe development of HKI-272 and related compounds for the treatment of cancerArch Pharm (Weinheim)2008341846547718493974
  • BrittenCDTargeting ErbB receptor signaling: a pan-ErbB approach to cancerMol Cancer Ther20043101335134215486201
  • SolcaFDahlGZoephelATarget binding properties and cellular activity of afatinib (BIBW 2992), an irreversible ErbB family blockerJ Pharmacol Exp Ther2012343234235022888144
  • RabindranSKDiscafaniCMRosfjordECAntitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinaseCancer Res200464113958396515173008
  • EngelmanJAZejnullahuKGaleCMPF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefitinibCancer Res20076724119241193218089823
  • National Center for Biotechnology InformationPubChem Compound Database; CID=208908 Available from: https://pubchem.ncbi.nlm.nih.gov/compound/208908#section=2D-StructureAccessed March 28, 2015
  • National Center for Biotechnology InformationPubChem Compound Database; CID=123631 Available from: https://pubchem.ncbi.nlm.nih.gov/compound/123631#section=2D-StructureAccessed March 28, 2015
  • National Center for Biotechnology InformationPubChem Compound Database; CID=176870 Available from: https://pubchem.ncbi.nlm.nih.gov/compound/176870#section=2D-StructureAccessed March 28, 2015
  • National Center for Biotechnology InformationPubChem Compound Database; CID=9915743 Available from: https://pubchem.ncbi.nlm.nih.gov/compound/9915743#section=2D-StructureAccessed March 28, 2015
  • National Center for Biotechnology InformationPubChem Compound Database; CID=6445562 Available from: https://pubchem.ncbi.nlm.nih.gov/compound/6445562#section=2D-StructureAccessed March 28, 2015
  • National Center for Biotechnology InformationPubChem Compound Database; CID=10184653 Available from: https://pubchem.ncbi.nlm.nih.gov/compound/10184653#section=2D-StructureAccessed March 28, 2015
  • SchwartzPAKuzmicPSolowiejJCovalent EGFR inhibitor analysis reveals importance of reversible interactions to potency and mechanisms of drug resistanceProc Natl Acad Sci U S A2014111117317824347635
  • BosePOzerHNeratinib: an oral, irreversible dual EGFR/HER2 inhibitor for breast and non-small cell lung cancerExpert Opin Investig Drugs2009181117351751
  • TsouHROverbeek-KlumpersEGHallettWAOptimization of 6,7-disubstituted-4-(arylamino)quinoline-3-carbonitriles as orally active, irreversible inhibitors of human epidermal growth factor receptor-2 kinase activityJ Med Chem20054841107113115715478
  • WissnerAOverbeekEReichMFSynthesis and structure-activity relationships of 6,7-disubstituted 4-anilinoquinoline-3-carbonitriles. The design of an orally active, irreversible inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor-2 (HER-2)J Med Chem2003461496312502359
  • CanoniciAGijsenMMulloolyMNeratinib overcomes trastuzumab resistance in HER2 amplified breast cancerOncotarget20134101592160524009064
  • NafiSGeneraliDKramer-MarekGNuclear HER4 mediates acquired resistance to trastuzumab and is associated with poor outcome in HER2 positive breast cancerOncotarget20145155934594925153719
  • SeyhanAAVaradarajanUChoeSA genome-wide RNAi screen identifies novel targets of neratinib sensitivity leading to neratinib and paclitaxel combination drug treatmentsMol Biosyst2011761974198921487605
  • O’NeillFMaddenSFClynesMA gene expression profile indicative of early stage HER2 targeted therapy responseMol Cancer2013126923816254
  • CobleighMAVogelCLTripathyDMultinational study of the efficacy and safety of humanized anti-HER2 monoclonal antibody in women who have HER2-overexpressing metastatic breast cancer that has progressed after chemotherapy for metastatic diseaseJ Clin Oncol19991792639264810561337
  • SlamonDJLeyland-JonesBShakSUse of chemotherapy plus a monoclonal antibody against HER2 for metastatic breast cancer that overexpresses HER2N Engl J Med20013441178379211248153
  • RomondEHPerezEABryantJTrastuzumab plus adjuvant chemotherapy for operable HER2-positive breast cancerN Engl J Med2005353161673168416236738
  • Piccart-GebhartMJProcterMLeyland-JonesBTrastuzumab after adjuvant chemotherapy in HER2-positive breast cancerN Engl J Med2005353161659167216236737
  • PandolfiPPBreast cancer – loss of PTEN predicts resistance to treatmentN Engl J Med2004351222337233815564551
  • NagataYLanKHZhouXPTEN activation contributes to tumor inhibition by trastuzumab, and loss of PTEN predicts trastuzumab resistance in patientsCancer Cell20046211712715324695
  • SaalLHHolmKMaurerMPIK3CA mutations correlate with hormone receptors, node metastasis, and ERBB2, and are mutually exclusive with PTEN loss in human breast carcinomaCancer Res20056572554255915805248
  • NahtaRTakahashiTUenoNTHungMCEstevaFJP27(kip1) downregulation is associated with trastuzumab resistance in breast cancer cellsCancer Res200464113981398615173011
  • ScaltritiMRojoFOcanaAExpression of p95HER2, a truncated form of the HER2 receptor, and response to anti-HER2 therapies in breast cancerJ Natl Cancer Inst200799862863817440164
  • NagyPFriedlanderETannerMDecreased accessibility and lack of activation of ErbB2 in JIMT-1, a Herceptin-resistant, MUC4-expressing breast cancer cell lineCancer Res200565247348215695389
  • Palyi-KrekkZBarokMIsolaJTammiMSzollosiJNagyPHyaluronan-induced masking of ErbB2 and CD44-enhanced trastuzumab internalisation in trastuzumab resistant breast cancerEur J Cancer200743162423243317911008
  • ShattuckDLMillerJKCarrawayKL3rdSweeneyCMet receptor contributes to trastuzumab resistance of Her2-overexpressing breast cancer cellsCancer Res20086851471147718316611
  • GijsenMKingPPereraTHER2 phosphorylation is maintained by a PKB negative feedback loop in response to anti-HER2 Herceptin in breast cancerPloS Biol2010812e100056321203579
  • FeldingerKGeneraliDKramer-MarekGADAM10 mediates trastuzumab resistance and is correlated with survival in HER2 positive breast cancerOncotarget20145166633664624952873
  • XiaWPetricoinEF3rdZhaoSAn heregulin-EGFR-HER3 autocrine signaling axis can mediate acquired lapatinib resistance in HER2+ breast cancer modelsBreast Cancer Res2013155R8524044505
  • LeungWYRoxanisISheldonHCombining lapatinib and pertuzumab to overcome lapatinib resistance due to NRG1-mediated signaling in HER2 amplified breast cancerOncotarget1212015 Epub ahead of print
  • Sanchez-MartinMPandiellaADifferential action of small molecule HER kinase inhibitors on receptor heterodimerization: therapeutic implicationsInt J Cancer2012131124425221826647
  • MallonRFeldbergLRLucasJAntitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitorClin Cancer Res201117103193320321325073
  • PierceAMcGowanPMCotterMComparative antiproliferative effects of iniparib and olaparib on a panel of triple-negative and non-triple-negative breast cancer cell linesCancer Biol Ther201314653754523760496
  • ModiSStopeckALindenHHSP90 inhibition is effective in breast cancer: a phase II trial of tanespimycin (17-AAG) plus trastuzumab in patients with HER2-positive metastatic breast cancer progressing on trastuzumabClin Cancer Res201117155132513921558407
  • MehtaAIBrufskyAMSampsonJHTherapeutic approaches for HER2-positive brain metastases: circumventing the blood-brain barrierCancer Treat Rev201339326126922727691
  • PolliJWHumphreysJEHarmonKAThe role of efflux and uptake transporters in [N-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-([2-(methylsulfonyl)ethyl]amino }methyl)-2-furyl]-4-quinazolinamine (GW572016, lapatinib) disposition and drug interactionsDrug Metab Dispos200836469570118216274
  • ZhaoXQXieJDChenXGNeratinib reverses ATP-binding cassette B1-mediated chemotherapeutic drug resistance in vitro, in vivo, and ex vivoMol Pharmacol2012821475822491935
  • HegedusCTruta-FelesKAntalffyGInteraction of the EGFR inhibitors gefitinib, vandetanib, pelitinib and neratinib with the ABCG2 multidrug transporter: implications for the emergence and reversal of cancer drug resistanceBiochem Pharmacol201284326026722548830
  • FreedmanRAGelmanRSWefelJSTBCRC 022: Phase II trial of neratinib for patients (Pts) with human epidermal growth factor receptor 2 (HER2+) breast cancer and brain metastases (BCBM)J Clin Oncol2014325 Suppl Abstr 528
  • BirnerPOberhuberGStaniJEvaluation of the United States Food and Drug Administration-approved scoring and test system of HER-2 protein expression in breast cancerClin Cancer Res2001761669167511410505
  • WolffACHammondMESchwartzJNAmerican Society of Clinical Oncology/College of American Pathologists guideline recommendations for human epidermal growth factor receptor 2 testing in breast cancerArch Pathol Lab Med20071311184319548375
  • WolffACHammondMEHicksDGRecommendations for human epidermal growth factor receptor 2 testing in breast cancer: American Society of Clinical Oncology/College of American Pathologists clinical practice guideline updateJ Clin Oncol201331313997401324101045
  • AllisonMThe HER2 testing conundrumNat Biotechnol201028211711920139941
  • PaikSKimCWolmarkNHER2 status and benefit from adjuvant trastuzumab in breast cancerN Engl J Med2008358131409141118367751
  • RobidouxATangGRastogiPEvaluation of lapatinib as a component of neoadjuvant therapy for HER2+operable breast cancer: NSABP protocol B-41J Clin Oncol201230Suppl 18 Abstr LBA506
  • Puma Biotechnology IncPuma Biotechnology announces presentation of positive PB272 Phase II data from I-SPY 2 trial: neratinib graduates from I-SPY 2 trial2014 Available from: http://www.pumabiotechnology.com/pr20140407.htmlAccessed March 28, 2015
  • CorkeryBCrownJClynesMO’DonovanNEpidermal growth factor receptor as a potential therapeutic target in triple-negative breast cancerAnn Oncol200920586286719150933
  • McGowanPMMulloolyMCaiazzaFADAM-17: a novel therapeutic target for triple negative breast cancerAnn Oncol201324236236922967992
  • CarlsonRHI-SPY 2 trial: neoadjuvant neratinib improves pathologic complete response in HR-/HER2+ breast cancerOncology Times201436102526
  • CareyLARugoHSMarcomPKTBCRC 001: randomized phase II study of cetuximab in combination with carboplatin in stage IV triple-negative breast cancerJ Clin Oncol201230212615262322665533
  • BaselgaJGomezPGreilRRandomized phase II study of the anti-epidermal growth factor receptor monoclonal antibody cetuximab with cisplatin versus cisplatin alone in patients with metastatic triple-negative breast cancerJ Clin Oncol201331202586259223733761
  • PaoWMillerVZakowskiMEGF receptor gene mutations are common in lung cancers from “never smokers” and are associated with sensitivity of tumors to gefitinib and erlotinibProc Natl Acad Sci U S A200410136133061331115329413
  • YunCHMengwasserKETomsAVThe T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATPProc Natl Acad Sci U S A200810562070207518227510
  • KatakamiNAtagiSGotoKLUX-Lung 4: a phase II trial of afatinib in patients with advanced non-small-cell lung cancer who progressed during prior treatment with erlotinib, gefitinib, or bothJ Clin Oncol201331273335334123816963
  • MillerVAHirshVCadranelJAfatinib versus placebo for patients with advanced, metastatic non-small-cell lung cancer after failure of erlotinib, gefitinib, or both, and one or two lines of chemotherapy (LUX-Lung 1): a phase 2b/3 randomised trialLancet Oncol201213552853822452896
  • SequistLVYangJCYamamotoNPhase III study of afatinib or cisplatin plus pemetrexed in patients with metastatic lung adenocarcinoma with EGFR mutationsJ Clin Oncol201331273327333423816960
  • BoseRKavuriSMSearlemanACActivating HER2 mutations in HER2 gene amplification negative breast cancerCancer Discov20133222423723220880
  • JaiswalBSKljavinNMStawiskiEWOncogenic ERBB3 mutations in human cancersCancer Cell201323560361723680147
  • PrickettTDAgrawalNSWeiXAnalysis of the tyrosine kinome in melanoma reveals recurrent mutations in ERBB4Nat Genet200941101127113219718025
  • SeyhanAAVaradarajanUChoeSLiuWRyanTEA genome-wide RNAi screen identifies novel targets of neratinib resistance leading to identification of potential drug resistant genetic markersMol Biosyst2012851553157022446932
  • CorcoranCRaniSBreslinSmiR-630 targets IGF1R to regulate response to HER-targeting drugs and overall cancer cell progression in HER2 over-expressing breast cancerMol Cancer2014137124655723
  • RaniSCorcoranCShielsLNeuromedin U: a candidate biomarker and therapeutic target to predict and overcome resistance to HER-tyrosine kinase inhibitorsCancer Res201474143821383324876102
  • WongKKFracassoPMBukowskiRMA phase I study with neratinib (HKI-272), an irreversible pan ErbB receptor tyrosine kinase inhibitor, in patients with solid tumorsClin Cancer Res20091572552255819318484
  • BursteinHJSunYDirixLYNeratinib, an irreversible ErbB receptor tyrosine kinase inhibitor, in patients with advanced ErbB2-positive breast cancerJ Clin Oncol20102881301130720142587
  • AwadaADirixLManso SanchezLSafety and efficacy of neratinib (HKI-272) plus vinorelbine in the treatment of patients with ErbB2-positive metastatic breast cancer pretreated with anti-HER2 therapyAnn Oncol201324110911622967996
  • ChowLWXuBGuptaSCombination neratinib (HKI-272) and paclitaxel therapy in patients with HER2-positive metastatic breast cancerBr J Cancer2013108101985199323632474
  • JankowitzRCAbrahamJTanARSafety and efficacy of neratinib in combination with weekly paclitaxel and trastuzumab in women with metastatic HER2-positive breast cancer: an NSABP Foundation Research Program phase I studyCancer Chemother Pharmacol20137261205121224077916
  • GandhiLBahledaRTolaneySMPhase I study of neratinib in combination with temsirolimus in patients with human epidermal growth factor receptor 2-dependent and other solid tumorsJ Clin Oncol2014322687524323026
  • AbbasRHugBALeisterCSonnichsenDA double-blind, randomized, multiple-dose, parallel-group study to characterize the occurrence of diarrhea following two different dosing regimens of neratinib, an irreversible pan-ErbB receptor tyrosine kinase inhibitorCancer Chemother Pharmacol201270119119922418773
  • HugBAbbasRLeisterCBurnsJSonnichsenDA single-dose, crossover, placebo- and moxifloxacin-controlled study to assess the effects of neratinib (HKI-272) on cardiac repolarization in healthy adult subjectsClin Cancer Res201016154016402320647478
  • MartinMBonneterreJGeyerCEJrA phase two randomised trial of neratinib monotherapy versus lapatinib plus capecitabine combination therapy in patients with HER2+ advanced breast cancerEur J Cancer201349183763377223953056
  • Puma Biotechnology IncPuma Biotechnology announces positive top line results from phase III PB272 trial in adjuvant breast cancer (ExteNET Trial)2014 Available from: http://www.pumabiotechnology.com/pr2014072202.htmlAccessed March 28, 2015
  • Puma Biotechnology IncPuma Biotechnology expands cohort in phase II trial of PB272 (neratinib) in HER2 mutation-positive solid tumor patients2014 Available from: http://investor.pumabiotechnology.com/press-release/puma-biotechnology-expands-cohort-phase-ii-trial-pb272-neratinib-her2-mutation-positivAccessed March 28, 2015
  • ItoYSuenagaMHatakeKSafety, efficacy and pharmacokinetics of neratinib (HKI-272) in Japanese patients with advanced solid tumors: a phase 1 dose-escalation studyJpn J Clin Oncol201242427828622371427