References
- SharmaSVBellDWSettlemanJHaberDAEpidermal growth factor receptor mutations in lung cancerNat Rev Cancer20077316918117318210
- EckMJYunCHStructural and mechanistic underpinnings of the differential drug sensitivity of EGFR mutations in non-small cell lung cancerBiochim Biophys Acta20101804355956620026433
- StamosJSliwkowskiMXEigenbrotCStructure of the epidermal growth factor receptor kinase domain alone and in complex with a 4-anilinoquinazoline inhibitorJ Biol Chem200227748462654627212196540
- YunCHBoggonTJLiYStructures of lung cancer-derived EGFR mutants and inhibitor complexes: mechanism of activation and insights into differential inhibitor sensitivityCancer Cell200711321722717349580
- ZhangXGureaskoJShenKColePAKuriyanJAn allosteric mechanism for activation of the kinase domain of epidermal growth factor receptorCell200612561137114916777603
- NingJWuQLiuZWangJLinXMapping inhibitor response to the in-frame deletions, insertions and duplications of epidermal growth factor receptor (EGFR) in non-small cell lung cancerJ Recept Signal Transduct Res2016361374426096169
- WuJYWuSGYangCHLung cancer with epidermal growth factor receptor exon 20 mutations is associated with poor gefitinib treatment responseClin Cancer Res200814154877488218676761
- ChoJChenLSangjiNCetuximab response of lung cancer-derived EGF receptor mutants is associated with asymmetric dimerizationCancer Res201373226770677924063894
- 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
- JiangJGreulichHJännePASellersWRMeyersonMGriffinJDEpidermal growth factor-independent transformation of Ba/F3 cells with cancer-derived epidermal growth factor receptor mutants induces gefitinib-sensitive cell cycle progressionCancer Res200565198968897416204070
- ParkSJKimHTLeeDHEfficacy of epidermal growth factor receptor tyrosine kinase inhibitors for brain metastasis in non-small cell lung cancer patients harboring either exon 19 or 21 mutationLung Cancer201277355656022677429
- PortaRSánchez-TorresJMPaz-AresLBrain metastases from lung cancer responding to erlotinib: The importance of EGFR mutationEur Respir J201137362463120595147
- ZhangYShengJYangYOptimized selection of three major EGFR-TKIs in advanced EGFR-positive non-small cell lung cancer: a network meta-analysisOncotarget2016715200932010826933807
- WhelerJJTsimberidouAMFalchookGSCombining erlotinib and cetuximab is associated with activity in patients with non-small cell lung cancer (including squamous cell carcinomas) and wild-type EGFR or resistant mutationsMol Cancer Ther201312102167217523963360
- NaidooJSimaCSRodriguezKEpidermal growth factor receptor exon 20 insertions in advanced lung adenocarcinomas: clinical outcomes and response to erlotinibCancer2015121183212322026096453
- PiotrowskaZBotelho CostaDHubermanMActivity of AUY922 in NSCLC patients with EGFR exon 20 insertionsJ Clin Oncol201533Suppl abstract 8015
- BeanJRielyGJBalakMAcquired resistance to epidermal growth factor receptor kinase inhibitors associated with a novel T854A mutation in a patient with EGFR-mutant lung adenocarcinomaClin Cancer Res200814227519752619010870
- CostaDBSchumerSTTenenDGKobayashiSDifferential responses to erlotinib in epidermal growth factor receptor (EGFR)-mutated lung cancers with acquired resistance to gefitinib carrying the L747S or T790M secondary mutationsJ Clin Oncol20082671182118418309959
- BalakMNGongYRielyGJNovel D761Yand common secondary T790M mutations in epidermal growth factor receptor-mutant lung adenocarcinomas with acquired resistance to kinase inhibitorsClin Cancer Res200612216494650217085664
- KlughammerBBruggerWCappuzzoFExamining treatment outcomes with erlotinib in patients with advanced non-small-cell lung cancer whose tumors harbor uncommon epidermal growth factor receptors mutationsJ Thorac Oncol201611454555526773740
- YunCHMengwasserKETomsAVThe T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATPProc Natl Acad Sci U S A200810562070207518227510
- EngelmanJAZejnullahuKMitsudomiTMET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signalingScience200731658271039104317463250
- SolcaFDahlGZoephelATarget binding properties and cellular activity of afatinib (BIBW 2992), an irreversible ErbB family blockerJ Pharmacol Exp Ther2012343234235022888144
- LiDAmbrogioLShimamuraTBIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer modelsOncogene200827344702471118408761
- HoffknechtPTufmanAWehlerTEfficacy of the irreversible ErbB family blocker afatinib in epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI)-pretreated non-small-cell lung cancer patients with brain metastases or leptomeningeal diseaseJ Thorac Oncol201510115616325247337
- LandiLTiseoMChiariRActivity of the EGFR-HER2 dual inhibitor afatinib in EGFR-mutant lung cancer patients with acquired resistance to reversible EGFR tyrosine kinase inhibitorsClin Lung Cancer201415641141725242668
- ParkKTanEHO’ByrneKAfatinib versus gefitinib as first-line treatment of patients with EGFR mutation-positive non-small-cell lung cancer (LUX-Lung 7): A phase 2B, open-label, randomised controlled trialLancet Oncol201617557758927083334
- YangJCSequistLVGeaterSLClinical activity of afatinib in patients with advanced non-small-cell lung cancer harbouring uncommon EGFR mutations: a combined post-hoc analysis of LUX-Lung 2, LUX-Lung 3, and LUX-Lung 6Lancet Oncol201516783083826051236
- WalterAOSjinRTHaringsmaHJDiscovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M mediated resistance in NSCLCCancer Discov20133121404141524065731
- PiotrowskaZNiederstMJKarlovichCAHeterogeneity underlies the emergence of EGFRT790 wild-type clones following treatment of T790M-positive cancers with a third-generation EGFR inhibitorCancer Discov20155771372325934077
- DhingraKRociletinib: has the TIGER lost a few of its stripes?Ann Oncol201627611611164 Epub 2016 Apr 427045101
- SequistLVSoriaJCGoldmanJWRociletinib in EGFR-mutated non-small-cell lung cancerN Engl J Med2015372181700170925923550
- SimmonsADJaw-TsaiSHaringsmaHJAllenAHardingTCInsulin-like growth factor 1 (IGF1R)/insulin receptor (INSR) inhibitory activity of rociletinib (CO-1686) and its metabolites in nonclinical models. In: Proceedings of the 106th Annual Meeting of the American Association for Cancer Research; 2015 Apr 18–22; Philadelphia, PACancer Res201575Suppl 15 abstract 793
- WheatonWWWeinbergSEHamanakaRBMetformin inhibits mitochondrial complex I of cancer cells to reduce tumorigenesisElife20143e0224224843020
- GallagherEJLeRoithDThe proliferation role of insulin and insulin-like growth factors in cancerTrends Endocrinol Metab2010211061061820663687
- ViolletBGuigasBSanz GarciaNLeclercJForetzMAndreelliFCellular and molecular mechanisms of metformin: an overviewClin Sci (Lond)2012122625327022117616
- OtaSHorigomeKIshiiTMetformin suppresses glucose-6-phosphatase expression by a complex I inhibition and AMPK activation-independent mechanismBiochem Biophys Res Commun2009388231131619664596
- CrossDAAshtonSEGhiorghiuSAZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancerCancer Discov2014491046106124893891
- GalvaniESunJLeonLGNF-κB drives acquired resistance to a novel mutant-selective EGFR inhibitorOncotarget2015640427174273226015408
- ErcanDChoiHGYunCHEGFR mutations and resistance to irreversible pyrimidine-based EGFR inhibitorsClin Cancer Res201521173913392325948633
- YuHATianSKDrilonAEAcquired resistance of EGFR-mutant lung cancer to aT790M-specific EGFR inhibitor: emergence of a third mutation (C797S) in the EGFR tyrosine kinase domainJAMA Oncol20151798298426181354
- PenzelRSersCChenYEGFR mutation detection in NSCLC-assessment of diagnostic application and recommendations of the German Panel for Mutation Testing in NSCLCVirchows Arch20114581959821057810
- TaronMIchinoseYRosellRActivating mutations in the tyrosine kinase domain of the epidermal growth factor receptor are associated with improved survival in gefitinib-treated chemorefractory lung adenocarcinomasClin Cancer Res200511165878588516115929
- Locatelli-SanchezMCouraudSArpinDRiouRBringuierPPSouquetPJRoutine EGFR molecular analysis in non-small-cell lung cancer patients is feasible: Exons 18–21 sequencing results of 753 patients and subsequent clinical outcomesLung2013191549149923749122
- LiuYWuBQZhongHHHuiPFangWGScreening for EGFR and KRAS mutations in non-small cell lung carcinomas using DNA extraction by hydrothermal pressure coupled with PCR-based direct sequencingInt J Clin Exp Pathol2013691880188924040454
- NiederstMJSequistLVPoirierJTRB loss in resistant EGFR mutant lung adenocarcinomas that transform to small-cell lung cancerNat Commun20156637725758528
- SequistLVPiotrowskaZNiederstMJOsimertinib responses after disease progression in patients who had been receiving rociletinibJAMA Oncol20162454154326720284
- SequistLVGoldmanJWWakeleeHAEfficacy of rociletinib (CO-1686) in plasma-genotyped T790M-positive non-small cell lung cancer (NSCLC) patients (pts)J Clin Oncol201533Suppl 15 abstract 8001
- GoldmanJWSoriaJ-CWakeleeHAUpdated results from TIGER-X, a phase I/II open label study of rociletinib in patients (pts) with advanced, recurrent T790M-positive non-small cell lung cancer (NSCLC)J Clin Oncol201634Suppl 15 abstract 9045
- Clovis Oncology IncTIGER-2: A Phase 2, Open-label, Multicenter, Safety and Efficacy Study of Oral CO-1686 as 2nd Line EGFR-directed TKI in Patients With Mutant EGFR Non-small Cell Lung Cancer (NSCLC). NCT02147990Boulder, CO, USAClovis Oncology, Inc
- Clovis Oncology IncTIGER-3: Open Label, Multicenter Study of Rociletinib (CO-1686) Mono Therapy Versus Single-agent Cytotoxic Chemotherapy in Patients With Mutant EGFR NSCLC Who Have Failed at Least One Previous EGFR-Directed TKI and Platinum-doublet Chemothera. NCT02322281Boulder, CO, USAClovis Oncology, Inc
- Clovis Oncology IncTIGER-1: Safety and Efficacy Study of Rociletinib (CO-1686) or Erlotinib in Patients With EGFR-mutant/Metastatic NSCLC Who Have Not Had Any Previous EGFR Directed Therapy. NCT02186301Boulder, CO, USAClovis Oncology, Inc
- WalkerKGinsbergGHattisDJohnsDOGuytonKZSonawaneBGenetic polymorphism in N-acetyltransferase (NAT): population distribution of NAT1 and NAT2 activityJ Toxicol Environ Health B Crit Rev2009125–644047220183529
- JännePAYangJCKimDWAZD9291 in EGFR inhibitor-resistant non-small-cell lung cancerN Engl J Med2015372181689169925923549
- DickinsonPACantariniMVCollierJMetabolic disposition of osimertinib in rat, dog, and man: insights into a drug designed to bind covalently to a cysteine residue of EGFRDrug Metab Dispos20164481201121227226351
- PlanchardDBrownKHKimDWOsimertinib Western and Asian clinical pharmacokinetics in patients and healthy volunteers: implications for formulation, dose, and dosing frequency in pivotal clinical studiesCancer Chemother Pharmacol201677476777626902828
- BallardPYatesJWYangZPreclinical comparison of osimertinib with other EGFR-TKIs in EGFR-mutant NSCLC brain metastases models, and early evidence of clinical brain metastases activityClin Cancer Res Epub2016719
- AhnMJTsaiCMYangJCAZD9291 activity in patients with EGFR-mutant advanced non-small cell lung cancer (NSCLC) and brain metastases: data from Phase II studiesEur J Cancer201551Suppl 3S625S626
- SequistLVSoriaJCCamidgeDRUpdate to rociletinib data with the RECIST confirmed response rateN Engl J Med2016374232296229727195670
- RamalingamSSYangJC-HLeeCKAZD9291, a mutant-selective EGFR inhibitor, as first-line treatment for EGFR mutation-positive advanced non-small cell lung cancer (NSCLC): Results from a phase 1 expansion cohortJ Clin Oncol201533Suppl abstract 8000
- JannePARamalingamSSYangJC-HClinical activity of the mutant-selective EGFR inhibitor AZD9291 in patients (pts) with EGFR inhibitor-resistant non-small cell lung cancer (NSCLC)J Clin Oncol201432Suppl abstract 8009
- RamalingamSSRukazenkovYThomasKSoriaJCA randomized, phase III study (FLAURA) of AZD9291, a novel EGFR-TKI, versus gefitinib or erlotinib in treatment-naïve patients with advanced non-small cell lung cancer and an EGFR-TKI-sensitizing mutationJ Clin Oncol201533Suppl abstract TPS8102
- SequistLVGoldmanJWWakeleeHAEfficacy of rociletinib (CO-1686) in plasma-genotyped T790M-positive non-small cell lung cancer (NSCLC) patients (pts)Journal of Clinical Oncology – ASCO Annual meeting201533Suppl 158001
- FDAFDA Briefing Document Oncologic Drugs Advisory Committee Meeting NDA 208542 Rociletinib2016