[1]Patent:WO2013/52157,2013,A1.Locationinpatent:Page/Pagecolumn13;14
[2]Patent:US2005/85495,2005,A1.Locationinpatent:Page/Pagecolumn6-7
[3]Patent:CN108358900,2018,A.Locationinpatent:Paragraph0045-0050
[4]Patent:CN106243092,2016,A.Locationinpatent:Paragraph0026;0049-0052;0061-0064;0073-0076;0085-0088
[5]Patent:WO2012/121764,2012,A1.Locationinpatent:Page/Pagecolumn52-53
[6]Patent:WO2016/51380,2016,A1.Locationinpatent:Page/Pagecolumn5;6
[7]Patent:WO2017/33107,2017,A1.Locationinpatent:Page/Pagecolumn27;28;29;30;31
[8]Patent:WO2017/93789,2017,A1.Locationinpatent:Page/Pagecolumn19
[9]Patent:US2018/30038,2018,A1.Locationinpatent:Paragraph0212;0213-0218;0221-0228;0231;0232;0234-0243
[10]Patent:US2018/297989,2018,A1.Locationinpatent:Paragraph0210;0215;0216;0250;0281;0282;0282;0283
[1]Patent:WO2007/85638,2007,A1.Locationinpatent:Page/Pagecolumn23
[1]Patent:WO2012/121764,2012,A1.Locationinpatent:Page/Pagecolumn49-50
[2]Patent:US2005/85495,2005,A1.Locationinpatent:Page/Pagecolumn6
[3]Patent:WO2016/166720,2016,A2.Locationinpatent:Page/Pagecolumn16
[1]Patent:WO2012/121764,2012,A1.Locationinpatent:Page/Pagecolumn57-58
Title: YM155 as an inhibitor of cancer stemness simultaneously inhibits autophosphorylation of epidermal growth factor receptor and G9a-mediated stemness in lung cancer cells.
Journal: PloS one 20170101
Title: Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants for the Treatment of EGFR Mutant Non-Small-Cell Lung Cancers.
Journal: Journal of medicinal chemistry 20160728
Title: EGF816 Exerts Anticancer Effects in Non-Small Cell Lung Cancer by Irreversibly and Selectively Targeting Primary and Acquired Activating Mutations in the EGF Receptor.
Journal: Cancer research 20160315
Title: Treatment approaches for EGFR-inhibitor-resistant patients with non-small-cell lung cancer.
Journal: The Lancet. Oncology 20150901
Title: Targeted therapies: Afatinib--new therapy option for EGFR-mutant lung cancer.
Journal: Nature reviews. Clinical oncology 20131001
Title: Identification of novel scaffold of benzothiazepinones as non-ATP competitive glycogen synthase kinase-3β inhibitors through virtual screening.
Journal: Bioorganic & medicinal chemistry letters 20121201
Title: Target binding properties and cellular activity of afatinib (BIBW 2992), an irreversible ErbB family blocker.
Journal: The Journal of pharmacology and experimental therapeutics 20121101
Title: Activation of IL-6R/JAK1/STAT3 signaling induces de novo resistance to irreversible EGFR inhibitors in non-small cell lung cancer with T790M resistance mutation.
Journal: Molecular cancer therapeutics 20121001
Title: Second-generation irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs): a better mousetrap? A review of the clinical evidence.
Journal: Critical reviews in oncology/hematology 20120901
Title: Monitoring reversible and irreversible EGFR inhibition with erlotinib and afatinib in a patient with EGFR-mutated non-small cell lung cancer (NSCLC) using sequential [18F]fluorothymidine (FLT-)PET.
Journal: Lung cancer (Amsterdam, Netherlands) 20120901
Title: New therapies in HER2-positive breast cancer: a major step towards a cure of the disease?
Journal: Cancer treatment reviews 20120801
Title: A phase II trial to assess efficacy and safety of afatinib in extensively pretreated patients with HER2-negative metastatic breast cancer.
Journal: Breast cancer research and treatment 20120801
Title: Irreversible protein kinase inhibitors: balancing the benefits and risks.
Journal: Journal of medicinal chemistry 20120726
Title: Structural analysis of the EGFR TK domain and potential implications for EGFR targeted therapy.
Journal: International journal of oncology 20120601
Title: A phase II study of afatinib (BIBW 2992), an irreversible ErbB family blocker, in patients with HER2-positive metastatic breast cancer progressing after trastuzumab.
Journal: Breast cancer research and treatment 20120601
Title: Afatinib for patients with lung adenocarcinoma and epidermal growth factor receptor mutations (LUX-Lung 2): a phase 2 trial.
Journal: The Lancet. Oncology 20120501
Title: Afatinib 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 trial.
Journal: The Lancet. Oncology 20120501
Title: Phase I study of continuous afatinib (BIBW 2992) in patients with advanced non-small cell lung cancer after prior chemotherapy/erlotinib/gefitinib (LUX-Lung 4).
Journal: Cancer chemotherapy and pharmacology 20120401
Title: Afatinib pharmacokinetics and metabolism after oral administration to healthy male volunteers.
Journal: Cancer chemotherapy and pharmacology 20120401
Title: Clinical activity of afatinib (BIBW 2992) in patients with lung adenocarcinoma with mutations in the kinase domain of HER2/neu.
Journal: Lung cancer (Amsterdam, Netherlands) 20120401
Title: EGFR exon 19 insertions: a new family of sensitizing EGFR mutations in lung adenocarcinoma.
Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20120315
Title: The EGFR T790M mutation in acquired resistance to an irreversible second-generation EGFR inhibitor.
Journal: Molecular cancer therapeutics 20120301
Title: Targeting the epidermal growth factor receptor in non-small cell lung cancer cells: the effect of combining RNA interference with tyrosine kinase inhibitors or cetuximab.
Journal: BMC medicine 20120101
Title: Anti-tumour activity of afatinib, an irreversible ErbB family blocker, in human pancreatic tumour cells.
Journal: British journal of cancer 20111108
Title: Comprehensive analysis of kinase inhibitor selectivity.
Journal: Nature biotechnology 20111030
Title: EGFR- and VEGF(R)-targeted small molecules show synergistic activity in colorectal cancer models refractory to combinations of monoclonal antibodies.
Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20111015
Title: Growth response of human colorectal tumour cell lines to treatment with afatinib (BIBW2992), an irreversible erbB family blocker, and its association with expression of HER family members.
Journal: International journal of oncology 20110801
Title: Afatinib (BIBW 2992) development in non-small-cell lung cancer.
Journal: Future oncology (London, England) 20110701
Title: The search for improved systemic therapy of non-small cell lung cancer--what are today's options?
Journal: Lung cancer (Amsterdam, Netherlands) 20110601
Title: Phase II trial of weekly alternating sequential BIBF 1120 and afatinib for advanced colorectal cancer.
Journal: Anticancer research 20110601
Title: The LUX-Lung clinical trial program of afatinib for non-small-cell lung cancer.
Journal: Expert review of anticancer therapy 20110501
Title: Genotype-driven therapies for non-small cell lung cancer: focus on EGFR, KRAS and ALK gene abnormalities.
Journal: Therapeutic advances in medical oncology 20110501
Title: Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors.
Journal: Journal of medicinal chemistry 20110310
Title: BIBW 2992 in non-small cell lung cancer.
Journal: Expert opinion on investigational drugs 20110301
Title: Irreversible EGFR inhibitor EKB-569 targets low-LET γ-radiation-triggered rel orchestration and potentiates cell death in squamous cell carcinoma.
Journal: PloS one 20110101
Title: EGFR inhibitors in non-small cell lung cancer (NSCLC): the emerging role of the dual irreversible EGFR/HER2 inhibitor BIBW 2992.
Journal: Targeted oncology 20101201
Title: New drugs in advanced non-small-cell lung cancer: searching for the correct clinical development.
Journal: Expert opinion on investigational drugs 20101201
Title: Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry.
Journal: Chemistry & biology 20101124
Title: Phase I trial of the irreversible EGFR and HER2 kinase inhibitor BIBW 2992 in patients with advanced solid tumors.
Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20100901
Title: Fast-forwarding hit to lead: aurora and epidermal growth factor receptor kinase inhibitor lead identification.
Journal: Journal of medicinal chemistry 20100708
Title: Enhanced anticancer effect of the combination of BIBW2992 and thymidylate synthase-targeted agents in non-small cell lung cancer with the T790M mutation of epidermal growth factor receptor.
Journal: Molecular cancer therapeutics 20100601
Title: The role of irreversible EGFR inhibitors in the treatment of non-small cell lung cancer: overcoming resistance to reversible EGFR inhibitors.
Journal: Cancer investigation 20100501
Title: Chemogenomic profiling provides insights into the limited activity of irreversible EGFR Inhibitors in tumor cells expressing the T790M EGFR resistance mutation.
Journal: Cancer research 20100201
Title: Irreversible pan-ErbB tyrosine kinase inhibitors and breast cancer: current status and future directions.
Journal: Cancer treatment reviews 20091201
Title: Dual targeting of EGFR can overcome a major drug resistance mutation in mouse models of EGFR mutant lung cancer.
Journal: The Journal of clinical investigation 20091001
Title: Acquired resistance to epidermal growth factor receptor tyrosine kinase inhibitors in non-small-cell lung cancers dependent on the epidermal growth factor receptor pathway.
Journal: Clinical lung cancer 20090701
Title: Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors.
Journal: Bioorganic & medicinal chemistry letters 20090101
Title: BIBW-2992, a dual receptor tyrosine kinase inhibitor for the treatment of solid tumors.
Journal: Current opinion in investigational drugs (London, England : 2000) 20081201
Title: Acquired resistance to epidermal growth factor receptor kinase inhibitors associated with a novel T854A mutation in a patient with EGFR-mutant lung adenocarcinoma.
Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20081115
Title: BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models.
Journal: Oncogene 20080807
Title: A 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 tumours.
Journal: British journal of cancer 20080115