A comprehensive review of the preclinical efficacy profile of the ErbB family blocker afatinib in cancer

scientific article

A comprehensive review of the preclinical efficacy profile of the ErbB family blocker afatinib in cancer is …
instance of (P31):
review articleQ7318358
scholarly articleQ13442814

External links are
P6179Dimensions Publication ID1013528465
P356DOI10.1007/S00210-014-0967-3
P932PMC publication ID4019832
P698PubMed publication ID24643470
P5875ResearchGate publication ID260916184

P50authorHelmout ModjtahediQ55475854
Martin Christian MichelQ57055217
P2093author name stringFlavio Solca
Byoung Chul Cho
P2860cites workComputational Studies of Epidermal Growth Factor Receptor: Docking Reliability, Three-Dimensional Quantitative Structure−Activity Relationship Analysis, and Virtual Screening StudiesQ59171683
The primary structure of epidermal growth factorQ69387018
Isolation of a mouse submaxillary gland protein accelerating incisor eruption and eyelid opening in the new-born animalQ79368389
Oncogenic ERBB3 mutations in human cancersQ24293022
An allosteric mechanism for activation of the kinase domain of epidermal growth factor receptorQ24293598
EGFR-mutant lung adenocarcinomas treated first-line with the novel EGFR inhibitor, XL647, can subsequently retain moderate sensitivity to erlotinibQ24606177
ErbB3/HER3 intracellular domain is competent to bind ATP and catalyze autophosphorylationQ24621754
The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATPQ24649549
BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer modelsQ24649935
ErbB receptors: from oncogenes to targeted cancer therapiesQ24683709
Acquired resistance of lung adenocarcinomas to gefitinib or erlotinib is associated with a second mutation in the EGFR kinase domainQ24794765
Target binding properties and cellular activity of afatinib (BIBW 2992), an irreversible ErbB family blockerQ27681964
EGFR mutation and resistance of non-small-cell lung cancer to gefitinibQ27824829
HER2YVMA drives rapid development of adenosquamous lung tumors in mice that are sensitive to BIBW2992 and rapamycin combination therapyQ27851461
Analysis of the tyrosine kinome in melanoma reveals recurrent mutations in ERBB4.Q27851483
Randomized study of Lapatinib alone or in combination with trastuzumab in women with ErbB2-positive, trastuzumab-refractory metastatic breast cancerQ27851549
Genotypic and histological evolution of lung cancers acquiring resistance to EGFR inhibitorsQ27851633
Activating HER2 mutations in HER2 gene amplification negative breast cancerQ27851987
Untangling the ErbB signalling networkQ27860884
An open-and-shut case? Recent insights into the activation of EGF/ErbB receptorsQ28207289
PTEN loss contributes to erlotinib resistance in EGFR-mutant lung cancer by activation of Akt and EGFRQ28240702
The ErbB/HER family of protein-tyrosine kinases and cancerQ28302611
Analysis of compound synergy in high-throughput cellular screens by population-based lifetime modelingQ28472663
Loss of activating EGFR mutant gene contributes to acquired resistance to EGFR tyrosine kinase inhibitors in lung cancer cellsQ28481370
Comprehensive analysis of kinase inhibitor selectivityQ29616719
EGFR antagonists in cancer treatmentQ29616740
Chemogenomic profiling provides insights into the limited activity of irreversible EGFR Inhibitors in tumor cells expressing the T790M EGFR resistance mutationQ33526744
Activating and resistance mutations of EGFR in non-small-cell lung cancer: role in clinical response to EGFR tyrosine kinase inhibitorsQ33769838
Amplification of EGFR T790M causes resistance to an irreversible EGFR inhibitorQ33810574
ErbB-2, the preferred heterodimerization partner of all ErbB receptors, is a mediator of lateral signalingQ33886341
EGFR exon 20 insertion mutations in non-small-cell lung cancer: preclinical data and clinical implicationsQ33963199
Four-year follow-up of trastuzumab plus adjuvant chemotherapy for operable human epidermal growth factor receptor 2-positive breast cancer: joint analysis of data from NCCTG N9831 and NSABP B-31.Q33964848
Irreversible EGFR inhibitor EKB-569 targets low-LET γ-radiation-triggered rel orchestration and potentiates cell death in squamous cell carcinomaQ34126513
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.Q34205052
Treatment with a combination of the ErbB (HER) family blocker afatinib and the IGF-IR inhibitor, NVP-AEW541 induces synergistic growth inhibition of human pancreatic cancer cells.Q34569071
Anti-p185HER2 monoclonal antibodies: biological properties and potential for immunotherapy.Q35271691
Anti-tumour activity of afatinib, an irreversible ErbB family blocker, in human pancreatic tumour cellsQ35623056
ErbB receptors: directing key signaling networks throughout lifeQ35639126
Subtype and pathway specific responses to anticancer compounds in breast cancerQ35779241
Hedgehog-EGFR cooperation response genes determine the oncogenic phenotype of basal cell carcinoma and tumour-initiating pancreatic cancer cellsQ35835273
Deubiquitination of EGFR by Cezanne-1 contributes to cancer progression.Q35889217
Mechanisms of Resistance to Trastuzumab and Novel Therapeutic Strategies in HER2-Positive Breast CancerQ35977527
Dual kinase inhibition of EGFR and HER2 overcomes resistance to cetuximab in a novel in vivo model of acquired cetuximab resistance.Q36185012
Functional analysis of receptor tyrosine kinase mutations in lung cancer identifies oncogenic extracellular domain mutations of ERBB2.Q36221780
HER2 amplification: a potential mechanism of acquired resistance to EGFR inhibition in EGFR-mutant lung cancers that lack the second-site EGFRT790M mutationQ36322762
Personalized medicine and treatment approaches in non-small-cell lung carcinomaQ36441548
Epidermal growth factor receptor inhibitors and antiangiogenic agents for the treatment of non-small cell lung cancerQ36482542
Noncovalent wild-type-sparing inhibitors of EGFR T790MQ36622817
Afatinib: emerging next-generation tyrosine kinase inhibitor for NSCLC.Q36673751
Acquired resistance to EGFR tyrosine kinase inhibitors in cancer cells is mediated by loss of IGF-binding proteinsQ36726112
The role of the EGFR signaling in tumor microenvironment.Q36951215
Acquired resistance to epidermal growth factor receptor kinase inhibitors associated with a novel T854A mutation in a patient with EGFR-mutant lung adenocarcinomaQ37000611
Epidermal growth factor receptor inhibition in mutation-positive non-small-cell lung cancer: is afatinib better or simply newer?Q47692335
Glycolysis inhibition sensitizes non-small cell lung cancer with T790M mutation to irreversible EGFR inhibitors via translational suppression of Mcl-1 by AMPK activation.Q47943383
Clinical implications of T790M mutation in patients with acquired resistance to EGFR tyrosine kinase inhibitors.Q53316003
EGFR- and VEGF(R)-targeted small molecules show synergistic activity in colorectal cancer models refractory to combinations of monoclonal antibodies.Q54564313
Genetic and chemical targeting of epithelial-restricted with serine box reduces EGF receptor and potentiates the efficacy of afatinibQ37101367
Acquired resistance to tyrosine kinase inhibitors during cancer therapyQ37104243
Structure and clinical relevance of the epidermal growth factor receptor in human cancerQ37122918
Monitoring afatinib treatment in HER2-positive gastric cancer with 18F-FDG and 89Zr-trastuzumab PET.Q37141350
Role of lapatinib alone or in combination in the treatment of HER2-positive breast cancerQ37355762
Dual targeting of EGFR can overcome a major drug resistance mutation in mouse models of EGFR mutant lung cancerQ37363050
Acquired resistance to epidermal growth factor receptor tyrosine kinase inhibitors in non-small-cell lung cancers dependent on the epidermal growth factor receptor pathway.Q37379113
HER-2/neu oncogene amplification and expression in breast and ovarian cancersQ37605489
Resistance to Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors in Non-Small Cell Lung CancerQ37653443
Potential of ErbB4 antibodies for cancer therapy.Q37658764
The receptor for EGF and its ligands - expression, prognostic value and target for therapy in cancer (review).Q37874958
Irreversible protein kinase inhibitors: balancing the benefits and risksQ38012518
Expression pattern and targeting of HER family members and IGF-IR in pancreatic cancer.Q38015157
Prognostic significance and targeting of HER family in colorectal cancerQ38070499
Trastuzumab emtansine (T-DM1) for HER2-positive breast cancer.Q38080898
Erlotinib resistance in lung cancer cells mediated by integrin β1/Src/Akt-driven bypass signaling.Q39122768
Afatinib prolongs survival compared with gefitinib in an epidermal growth factor receptor-driven lung cancer modelQ39188098
Genotype-selective combination therapies for melanoma identified by high-throughput drug screeningQ39226193
Structural optimization and structure-activity relationships of N2-(4-(4-Methylpiperazin-1-yl)phenyl)-N8-phenyl-9H-purine-2,8-diamine derivatives, a new class of reversible kinase inhibitors targeting both EGFR-activating and resistance mutations.Q39250868
Preclinical and clinical development of afatinib: a focus on breast cancer and squamous cell carcinoma of the head and neckQ39297048
Activation of IL-6R/JAK1/STAT3 signaling induces de novo resistance to irreversible EGFR inhibitors in non-small cell lung cancer with T790M resistance mutationQ39297840
Combined therapy with mutant-selective EGFR inhibitor and Met kinase inhibitor for overcoming erlotinib resistance in EGFR-mutant lung cancer.Q39306353
SKLB1206, a novel orally available multikinase inhibitor targeting EGFR activating and T790M mutants, ErbB2, ErbB4, and VEGFR2, displays potent antitumor activity both in vitro and in vivo.Q39399335
Met kinase inhibitor E7050 reverses three different mechanisms of hepatocyte growth factor-induced tyrosine kinase inhibitor resistance in EGFR mutant lung cancer.Q39399655
The EGFR T790M mutation in acquired resistance to an irreversible second-generation EGFR inhibitorQ39415296
The irreversible pan-HER inhibitor PF00299804 alone or combined with gemcitabine has an antitumor effect in biliary tract cancer cell linesQ39422598
Evaluation of the antitumor effects and mechanisms of PF00299804, a pan-HER inhibitor, alone or in combination with chemotherapy or targeted agents in gastric cancerQ39434209
Antitumor activity of HM781-36B, a highly effective pan-HER inhibitor in erlotinib-resistant NSCLC and other EGFR-dependent cancer modelsQ39512157
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 membersQ39535457
Antitumor activity of HM781-36B, an irreversible Pan-HER inhibitor, alone or in combination with cytotoxic chemotherapeutic agents in gastric cancerQ39595342
The effect of acquired cisplatin resistance on sensitivity to EGFR tyrosine kinase inhibitors in EGFR mutant lung cancer cellsQ39614263
Structural analysis of the EGFR TK domain and potential implications for EGFR targeted therapyQ39656288
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 receptorQ39695840
Combination of EGFR/HER2 tyrosine kinase inhibition by BIBW 2992 and BIBW 2669 with irradiation in FaDu human squamous cell carcinoma.Q40133869
Somatic mutations of the HER2 kinase domain in lung adenocarcinomas.Q40449400
Mechanisms of Resistance to Epidermal Growth Factor Receptor Inhibitors and Novel Therapeutic Strategies to Overcome Resistance in NSCLC PatientsQ42043613
Phase I trial of intratumoral liposome E1A gene therapy in patients with recurrent breast and head and neck cancerQ43606249
P275copyright licenseCreative Commons Attribution 4.0 InternationalQ20007257
P6216copyright statuscopyrightedQ50423863
P433issue6
P921main subjectcancerQ12078
enzymeQ8047
heterocyclic compoundQ193430
membrane proteinQ423042
neoplasmQ1216998
cell surface receptorQ2476074
antineoplasticQ2853144
P304page(s)505-521
P577publication date2014-03-19
2014-06-01
P1433published inNaunyn-Schmiedeberg's Archives of PharmacologyQ1468251
P1476titleA comprehensive review of the preclinical efficacy profile of the ErbB family blocker afatinib in cancer
P478volume387

Reverse relations

cites work (P2860)
Q36571455Acquired resistance of pancreatic cancer cells to treatment with gemcitabine and HER-inhibitors is accompanied by increased sensitivity to STAT3 inhibition.
Q53402902Adverse kidney effects of epidermal growth factor receptor inhibitors.
Q33649260Afatinib ameliorates osteoclast differentiation and function through downregulation of RANK signaling pathways.
Q27853078Afatinib demonstrates remarkable activity against HER2-amplified uterine serous endometrial cancer in vitro and in vivo.
Q26749005Afatinib in Non-Small Cell Lung Cancer
Q52655265Afatinib in advanced NSCLC: a profile of its use.
Q33591405Afatinib radiosensitizes head and neck squamous cell carcinoma cells by targeting cancer stem cells
Q60050170Afatinib reverses ceritinib resistance (CR) in ALK/ROS1-positive non-small-cell lung cancer cell (NSCLC) via suppression of NRG1 pathway
Q38646686Afatinib-based combination regimens for the treatment of solid tumors: rationale, emerging strategies and recent progress
Q39016290Afatinib: A Review in Advanced Non-Small Cell Lung Cancer
Q54979771Application of molecular targeted therapies in the treatment of head and neck squamous cell carcinoma.
Q57818008Appropriate Sequence for Afatinib and Cisplatin Combination Improves Anticancer Activity in Head and Neck Squamous Cell Carcinoma
Q37008862Arylfluorosulfates Inactivate Intracellular Lipid Binding Protein(s) through Chemoselective SuFEx Reaction with a Binding Site Tyr Residue
Q39156722Biological determinants of radioresistance and their remediation in pancreatic cancer
Q38262804Class act: safety comparison of approved tyrosine kinase inhibitors for non-small-cell lung carcinoma.
Q37650711Clinical Pharmacokinetics and Pharmacodynamics of Afatinib
Q64055605Clinical development of targeted and immune based anti-cancer therapies
Q60193666Covalent inhibitors of EGFR family protein kinases induce degradation of human Tribbles 2 (TRIB2) pseudokinase in cancer cells.
Q71098757Design and synthesis of novel 6-substituted quinazoline-2-thiols
Q37004934Digital Gene Expression Analysis of Populus simonii × P. nigra Pollen Germination and Tube Growth
Q36095074Down-regulation of neutrophil gelatinase-associated lipocalin in head and neck squamous cell carcinoma correlated with tumorigenesis, not with metastasis
Q43604978Evaluating the cost-effectiveness of afatinib after platinum-based therapy for the treatment of squamous non-small-cell lung cancer in France
Q89834325How Different Substitution Positions of F, Cl Atoms in Benzene Ring of 5-Methylpyrimidine Pyridine Derivatives Affect the Inhibition Ability of EGFRL858R/T790M/C797S Inhibitors: A Molecular Dynamics Simulation Study
Q38969795Ibrutinib (ImbruvicaTM) potently inhibits ErbB receptor phosphorylation and cell viability of ErbB2-positive breast cancer cells
Q91726663Inhibition of cisplatin-resistant head and neck squamous cell carcinoma by combination of Afatinib with PD0325901, a MEK inhibitor
Q31028700Longitudinal trends and subgroup analysis in publication patterns for preclinical data of newly approved drugs
Q54166640Management Strategies for Adverse Events Associated With EGFR TKIs in Non-Small Cell Lung Cancer.
Q50064748Molecular Correlates of In Vitro Responses to Dacomitinib and Afatinib in Bladder Cancer
Q41021890Molecular Profiling of Thymoma and Thymic Carcinoma: Genetic Differences and Potential Novel Therapeutic Targets
Q89278505Naunyn-Schmiedeberg's Archives of Pharmacology under new editorship: change and continuity
Q35807946Next-Generation Covalent Irreversible Kinase Inhibitors in NSCLC: Focus on Afatinib
Q37702126Novel multi-targeted ErbB family inhibitor afatinib blocks EGF-induced signaling and induces apoptosis in neuroblastoma
Q28076506Opportunities and Challenges for Drug Development: Public-Private Partnerships, Adaptive Designs and Big Data
Q52591096Osimertinib: A Novel Dermatologic Adverse Event Profile in Patients with Lung Cancer.
Q50026716Phase I open-label study of afatinib plus vinorelbine in patients with solid tumours overexpressing EGFR and/or HER2.
Q38411081Preclinical research strategies for newly approved drugs as reflected in early publication patterns
Q38848784Restoration of CBX7 expression increases the susceptibility of human lung carcinoma cells to irinotecan treatment.
Q90371930Safety Profile of Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors: A Disproportionality Analysis of FDA Adverse Event Reporting System
Q104111327Selective inhibition of stemness through EGFR/FOXA2/SOX9 axis reduces pancreatic cancer metastasis
Q40862682Selectivity profile of afatinib for EGFR-mutated non-small-cell lung cancer.
Q91143046Small-molecule targeting of brachyury transcription factor addiction in chordoma
Q26745776Spotlight on afatinib and its potential in the treatment of squamous cell lung cancer: the evidence so far
Q33822560Synergistic effects of various Her inhibitors in combination with IGF-1R, C-MET and Src targeting agents in breast cancer cell lines
Q47138128The efficacy of 40 mg versus dose de-escalation to less than 40 mg of afatinib (Giotrif) as the first-line therapy for patients with primary lung adenocarcinoma harboring favorable epidermal growth factor mutations.

Search more.