Afatinib: emerging next-generation tyrosine kinase inhibitor for NSCLC

References

• National Comprehensive Cancer NetworkNCCN Clinical Practice Guidelines in Oncology: Non-Small Cell Lung Cancer2012 Available from: http://www.nccn.org/professionals/physician_gls/f_guidelines.aspAccessed October 14, 2012
   Google Scholar
• DollRGrayRHafnerBPetoRMortality in relation to smoking: 22 years’ observations on female British doctorsBMJ198028062199679717417764
   PubMed Web of Science ®Google Scholar
• JanerichDTThompsonWDVarelaLRLung cancer and exposure to tobacco smoke in the householdN Engl J Med1990323106326362385268
   PubMed Web of Science ®Google Scholar
• TurnerMCKrewskiDChenYPopeCA3rdGapsturSThunMJRadon and lung cancer in the American Cancer Society cohortCancer Epidemiol Biomarkers Prev201120343844821212062
   PubMed Web of Science ®Google Scholar
• HeintzNHJanssen-HeiningerYMMossmanBTAsbestos, lung cancers, and mesotheliomas: from molecular approaches to targeting tumor survival pathwaysAm J Respir Cell Mol Biol201042213313920068227
   PubMed Web of Science ®Google Scholar
• SandlerAGrayRPerryMCPaclitaxel-carboplatin alone or with bevacizumab for non-small-cell lung cancerN Engl J Med2006355242542255017167137
   PubMed Web of Science ®Google Scholar
• ReidAVidalLShawHde BonoJDual inhibition of ErbB1 (EGFR/HER1) and ErbB2 (HER2/neu)Eur J Cancer200743348148917208435
   PubMed Web of Science ®Google Scholar
• HerbstRSHeymachJVLippmanSMLung cancerN Engl J Med2008359131367138018815398
   PubMed Web of Science ®Google Scholar
• SpicerJFRudmanSMEGFR inhibitors in non-small cell lung cancer (NSCLC): the emerging role of the dual irreversible EGFR/HER2 inhibitor BIBW 2992Target Oncol20105424525520574858
   PubMed Web of Science ®Google Scholar
• GazdarAFActivating and resistance mutations of EGFR in non-small-cell lung cancer: role in clinical response to EGFR tyrosine kinase inhibitorsOncogene200928Suppl 1S24S3119680293
   PubMed Web of Science ®Google Scholar
• RayMSalgiaRVokesEEThe role of EGFR inhibition in the treatment of non-small cell lung cancerOncologist200914111116113019892771
   PubMed Web of Science ®Google Scholar
• MurraySDahabrehIJLinardouHManoloukosMBafaloukosDKosmidisPSomatic mutations of the tyrosine kinase domain of epidermal growth factor receptor and tyrosine kinase inhibitor response to TKIs in non-small cell lung cancer: an analytical databaseJ Thorac Oncol20083883283918670300
   PubMed Web of Science ®Google Scholar
• RielyGJPolitiKAMillerVAPaoWUpdate on epidermal growth factor receptor mutations in non-small cell lung cancerClin Cancer Res200612247232724117189394
   PubMed Web of Science ®Google Scholar
• EngelmanJAJannePAMechanisms of acquired resistance to epidermal growth factor receptor tyrosine kinase inhibitors in non-small cell lung cancerClin Cancer Res200814102895289918483355
   PubMed Web of Science ®Google Scholar
• SharmaSVBellDWSettlemanJHaberDAEpidermal growth factor receptor mutations in lung cancerNat Rev Cancer20077316918117318210
   PubMed Web of Science ®Google Scholar
• ShepherdFARodrigues PereiraJCiuleanuTErlotinib in previously treated non-small-cell lung cancerN Engl J Med2005353212313216014882
   PubMed Web of Science ®Google Scholar
• JackmanDMMillerVACioffrediLAImpact of epidermal growth factor receptor and KRAS mutations on clinical outcomes in previously untreated non-small cell lung cancer patients: results of an online tumor registry of clinical trialsClin Cancer Res200915165267527319671843
   PubMed Web of Science ®Google Scholar
• RosellRMoranTQueraltCScreening for epidermal growth factor receptor mutations in lung cancerN Engl J Med20093611095896719692684
   PubMed Web of Science ®Google Scholar
• InoueASuzukiTFukuharaTProspective phase II study of gefitinib for chemotherapy-naive patients with advanced non-small-cell lung cancer with epidermal growth factor receptor gene mutationsJ Clin Oncol200624213340334616785471
   PubMed Web of Science ®Google Scholar
• JannePAWangXSocinskiMARandomized phase II trial of erlotinib alone or with carboplatin and paclitaxel in patients who were never or light former smokers with advanced lung adenocarcinoma: CALGB 30406 trialJ Clin Oncol201230172063206922547605
   PubMed Web of Science ®Google Scholar
• JackmanDMYeapBYSequistLVExon 19 deletion mutations of epidermal growth factor receptor are associated with prolonged survival in non-small cell lung cancer patients treated with gefitinib or erlotinibClin Cancer Res200612133908391416818686
   PubMed Web of Science ®Google Scholar
• RosellRCarcerenyEGervaisRErlotinib versus standard chemotherapy as first-line treatment for European patients with advanced EGFR mutation-positive non-small-cell lung cancer (EURTAC): a multicentre, open-label, randomised phase 3 trialLancet Oncol201213323924622285168
   PubMed Web of Science ®Google Scholar
• ZhouCWuYLChenGErlotinib versus chemotherapy as first-line treatment for patients with advanced EGFR mutationpositive non-small-cell lung cancer (OPTIMAL, CTONG-0802): a multicentre, open-label, randomised, phase 3 studyLancet Oncol201112873574221783417
   PubMed Web of Science ®Google Scholar
• GridelliCDe MarinisFDi MaioMCortinovisDCappuzzoFMokTGefitinib as first-line treatment for patients with advanced non-small-cell lung cancer with activating epidermal growth factor receptor mutation: review of the evidenceLung Cancer201171324925721216486
   PubMed Web of Science ®Google Scholar
• MokTSWuYLThongprasertSGefitinib or carboplatin-paclitaxel in pulmonary adenocarcinomaN Engl J Med20093611094795719692680
   PubMed Web of Science ®Google Scholar
• MaemondoMInoueAKobayashiKGefitinib or chemotherapy for non-small-cell lung cancer with mutated EGFRN Engl J Med2010362252380238820573926
   PubMed Web of Science ®Google Scholar
• MitsudomiTMoritaSYatabeYGefitinib versus cisplatin plus docetaxel in patients with non-small-cell lung cancer harbouring mutations of the epidermal growth factor receptor (WJTOG3405): an open label, randomised phase 3 trialLancet Oncol201011212112820022809
   PubMed Web of Science ®Google Scholar
• Paz-AresLSoulieresDMelezinekIClinical outcomes in non-small-cell lung cancer patients with EGFR mutations: pooled analysisJ Cell Mol Med2010141–2516920015198
   PubMed Web of Science ®Google Scholar
• JackmanDPaoWRielyGJClinical definition of acquired resistance to epidermal growth factor receptor tyrosine kinase inhibitors in non-small-cell lung cancerJ Clin Oncol201028235736019949011
   PubMed Web of Science ®Google Scholar
• PaoWMillerVAPolitiKAAcquired resistance of lung adenocarcinomas to gefitinib or erlotinib is associated with a second mutation in the EGFR kinase domainPLoS Med200523e7315737014
   PubMed Web of Science ®Google Scholar
• ArcilaMEOxnardGRNafaKRebiopsy of lung cancer patients with acquired resistance to EGFR inhibitors and enhanced detection of the T790M mutation using a locked nucleic acid-based assayClin Cancer Res20111751169118021248300
   PubMed Web of Science ®Google Scholar
• SequistLVWaltmanBADias-SantagataDGenotypic and histological evolution of lung cancers acquiring resistance to EGFR inhibitorsSci Transl Med201137575ra26
   PubMed Web of Science ®Google Scholar
• OuSHSecond-generation irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs): a better mousetrap? A review of the clinical evidenceCrit Rev Oncol Hematol201283340742122257651
   PubMed Web of Science ®Google Scholar
• BalakMNGongYRielyGJNovel D761Y and common secondary T790M mutations in epidermal growth factor receptor-mutant lung adenocarcinomas with acquired resistance to kinase inhibitorsClin Cancer Res200612216494650117085664
   PubMed Web of Science ®Google Scholar
• BeanJRielyGJBalakMAcquired resistance to epidermal growth factor receptor kinase inhibitors associated with a novel T854A mutation in a patient with EGFR-mutant lung adenocarcinomaClin Cancer Res200814227519752519010870
   PubMed Web of Science ®Google Scholar
• CostaDBHalmosBKumarABIM mediates EGFR tyrosine kinase inhibitor-induced apoptosis in lung cancers with oncogenic EGFR mutationsPLoS Med200741016691679 discussion 168017973572
   PubMed Web of Science ®Google Scholar
• EngelmanJAZejnullahuKMitsudomiTMET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signalingScience200731658271039104317463250
   PubMed Web of Science ®Google Scholar
• SudaKTomizawaKFujiiMEpithelial to mesenchymal transition in an epidermal growth factor receptor-mutant lung cancer cell line with acquired resistance to erlotinibJ Thorac Oncol2011671152116121597390
   PubMed Web of Science ®Google Scholar
• MaheswaranSSequistLVNagrathSDetection of mutations in EGFR in circulating lung-cancer cellsN Engl J Med2008359436637718596266
   PubMed Web of Science ®Google Scholar
• RosellRMolinaMACostaCPretreatment EGFR T790M mutation and BRCA1 mRNA expression in erlotinib-treated advanced non-small-cell lung cancer patients with EGFR mutationsClin Cancer Res20111751160116821233402
   PubMed Web of Science ®Google Scholar
• SuKYChenHYLiKCPretreatment epidermal growth factor receptor (EGFR) T790M mutation predicts shorter EGFR tyrosine kinase inhibitor response duration in patients with non-small-cell lung cancerJ Clin Oncol201230443344022215752
   PubMed Web of Science ®Google Scholar
• RielyGJKrisMGZhaoBProspective assessment of discontinuation and reinitiation of erlotinib or gefitinib in patients with acquired resistance to erlotinib or gefitinib followed by the addition of everolimusClin Cancer Res200713175150515517785570
   PubMed Web of Science ®Google Scholar
• CostaDBNguyenKSChoBCEffects of erlotinib in EGFR mutated non-small cell lung cancers with resistance to gefitinibClin Cancer Res200814217060706718981003
   PubMed Web of Science ®Google Scholar
• ChaftJEOxnardGRSimaCSKrisMGMillerVARielyGJDisease fare after tyrosine kinase inhibitor discontinuation in patients with EGFR-mutant lung cancer and acquired resistance to erlotinib or gefitinib: implications for clinical trial designClin Cancer Res201117196298630321856766
   PubMed Web of Science ®Google Scholar
• PietanzaMCLynchTJJrLaraPNJrXL647 – a multitargeted tyrosine kinase inhibitor: results of a phase II study in subjects with non-small cell lung cancer who have progressed after responding to treatment with either gefitinib or erlotinibJ Thorac Oncol20127121922622011666
   PubMed Web of Science ®Google Scholar
• JohnsonMLRielyGJRizviNAPhase II trial of dasatinib for patients with acquired resistance to treatment with the epidermal growth factor receptor tyrosine kinase inhibitors erlotinib or gefitinibJ Thorac Oncol2011661128113121623279
   PubMed Web of Science ®Google Scholar
• SequistLVBesseBLynchTJNeratinib, an irreversible pan-ErbB receptor tyrosine kinase inhibitor: results of a phase II trial in patients with advanced non-small-cell lung cancerJ Clin Oncol201028183076308320479403
   PubMed Web of Science ®Google Scholar
• JanjigianYYAzzoliCGKrugLMPhase I/II trial of cetuximab and erlotinib in patients with lung adenocarcinoma and acquired resistance to erlotinibClin Cancer Res20111782521252721248303
   PubMed Web of Science ®Google Scholar
• LiDAmbrogioLShimamuraTBIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer modelsOncogene200827344702471118408761
   PubMed Web of Science ®Google Scholar
• YapTAVidalLAdamJPhase I trial of the irreversible EGFR and HER2 kinase inhibitor BIBW 2992 in patients with advanced solid tumorsJ Clin Oncol201028253965397220679611
   PubMed Web of Science ®Google Scholar
• MetroGCrinoLThe LUX-Lung clinical trial program of afatinib for non-small-cell lung cancerExpert Rev Anticancer Ther201111567368221554040
   PubMed Web of Science ®Google Scholar
• KwakELSordellaRBellDWIrreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinibProc Natl Acad Sci USA2005102217665767015897464
   PubMed Web of Science ®Google Scholar
• MurakamiHTamuraTTakahashiTPhase I study of continuous afatinib (BIBW 2992) in patients with advanced non-small cell lung cancer after prior chemotherapy/erlotinib/gefitinib (LUX-Lung 4)Cancer Chemother Pharmacol201269489189922071596
   PubMed Web of Science ®Google Scholar
• AgusDBTerlizziEStopferPAmelsbergAGordonMSA phase I dose escalation study of BIBW 2992, an irreversible dual EGFR/HER2 receptor tyrosine kinase inhibitor, in a continuous schedule in patients with advanced solid tumoursJ Clin Oncol2006241897S97S
   Web of Science ®Google Scholar
• YangJCShihJYSuWCAfatinib for patients with lung adenocarcinoma and epidermal growth factor receptor mutations (LUX-Lung 2): a phase 2 trialLancet Oncol201213553954822452895
   PubMed Web of Science ®Google Scholar
• SchulerMAwadaAHarterPA phase II trial to assess efficacy and safety of afatinib in extensively pretreated patients with HER2-negative metastatic breast cancerBreast Cancer Res Treat201213431149115922763464
   PubMed Web of Science ®Google Scholar
• EskensFAMomCHPlantingASA phase I dose escalation study of BIBW 2992, an irreversible dual inhibitor of epidermal growth factor receptor 1 (EGFR) and 2 (HER2) tyrosine kinase in a 2-week on, 2-week off schedule in patients with advanced solid tumoursBr J Cancer2008981808518026190
   PubMed Web of Science ®Google Scholar
• CohenMHJohnsonJRChenYFSridharaRPazdurRFDA drug approval summary: erlotinib (Tarceva) tabletsOncologist200510746146616079312
   PubMed Web of Science ®Google Scholar
• LinNUWinerEPWheatleyDA phase II study of afatinib (BIBW 2992), an irreversible ErbB family blocker, in patients with HER2-positive metastatic breast cancer progressing after trastuzumabBreast Cancer Res Treat201213331057106522418700
   PubMed Web of Science ®Google Scholar
• BarberNAGantiAKPulmonary toxicities from targeted therapies: a reviewTarget Oncol20116423524322076388
   PubMed Web of Science ®Google Scholar
• 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
   PubMed Web of Science ®Google Scholar
• YangCHSchulerMHYamamotoNLUX-Lung 3: a randomized, open-label, phase III study of afatinib versus pemetrexed and cisplatin as first-line treatment for patients with advanced adenocarcinoma of the lung harboring EGFR-activating mutationsJ Clin Oncol201230SupplLBA7500
   Web of Science ®Google Scholar
• Boehringer Ingelheim PharmaceuticalsA phase II trail of afatinib (BIBW 2992) in third-line treatment for patients with stage IIIB/IV adenocarcinoma of the lung harbouring wild-type epidermal growth factor receptor (EGFR)ClinicalTrialsgov [website on the Internet]Bethesda, MDUS National Library of Medicine2012 [updated April 13, 2012]. Available from: http://clinicaltrials.gov/ct2/show/NCT01003899 NLM identifier: NCT01003899. Accessed October 14, 2012
   Google Scholar
• JanjigianYY GHHornLSmitEFActivity and tolerability of afatinib (BIBW 2992) and cetuximab in NSCLC patients with acquired resistance to erlotinib and gefitinibJ Clin Oncol201129Suppl7525
   Web of Science ®Google Scholar
• SequistLVSchulernYamamotoMLUX-Lung 3: Symptom and health-related quality of life results from a randomized phase III study in 1st-line advanced NSCLC patients harbouring EGFR mutations37th ESMO CongressSeptember 28–October 2, 2012Vienna, Austria
   Google Scholar