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EGFR Gene Record

  • Summary
  • Interactions
  • Claims
  • EGFR 1956 Druggable GenomeClinically ActionableDrug Resistance

    Alternate Names:

    1956
    EPIDERMAL GROWTH FACTOR RECEPTOR
    EGFR
    ERBB
    ERBB1
    HER1
    NISBD2
    PIG61
    mENA
    131550
    3236
    ENSG00000146648
    OTTHUMG00000023661
    P00533
    EGFR_HUMAN
    19
    Proto-oncogene c-ErbB-1
    Receptor tyrosine-protein kinase erbB-1
    PA7360
    EGFR (HER1/ERBB1)HER2 (ERBB2/neu)HER4 (ERBB4)
    EGFR (HER1/ERBB1)HER2 (ERBB2/neu)HER3 (ERBB3)
    EGFR (HER1/ERBB1)
    1797
    NP_005219
    NM_005228
    EPIDERMAL GROWTH FACTOR RECEPTOR PRECURSOR (EC 2.7.1.112) (RECEPTOR TYROSINE-PROTEIN KINASE ERBB-1). [SOURCE:UNIPROT/SWISSPROT;ACC:P00533]
    BE0000767
    T59328

    Gene Info:

    CancerCommons Reported Gene Name EGFR
    Target Class Receptors
    Target Subclass EC:2.7.10.1
    Target Subclass Kinase
    Target Main Class Receptors
    Transmembrane Helix Count 1
    Target Subclass EGFR
    Initial Gene Query EGFR
    Counted Citations from 1950-2000 12181
    GuideToPharmacology Gene Category Name Type I RTKs: ErbB (epidermal growth factor) receptor family
    GuideToPharmacology Gene Category ID 320
    Human Readable Name DRUGGABLE GENOME
    Interpro Type Domain
    Interpro Acc IPR001245
    Interpro Short Name Ser-Thr/Tyr_kinase_cat_dom
    Interpro Name Serine-threonine/tyrosine-protein kinase catalytic domain
    Uniprot Evidence 1: Evidence at protein level
    Uniprot Status Swiss-Prot
    Human Readable Name KINASE
    Gene Biotype PROTEIN_CODING
    (32 More Sources)

    Gene Categories: Category Details

    CELL SURFACE
    KINASE
    TYROSINE KINASE
    DRUG RESISTANCE
    DRUGGABLE GENOME
    CLINICALLY ACTIONABLE

    Publications:

    Yao et al., 2017, Tumours with class 3 BRAF mutants are sensitive to the inhibition of activated RAS., Nature
    Gerber et al., 2014, Management and future directions in non-small cell lung cancer with known activating mutations., Am Soc Clin Oncol Educ Book
    Ward RA et al., 2013, Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR)., J Med Chem
    Ramalingam et al., 2016, Dacomitinib versus erlotinib in patients with EGFR-mutated advanced nonsmall-cell lung cancer (NSCLC): pooled subset analyses from two randomized trials., Ann. Oncol.
    Wu YL et al., 2017, Dacomitinib versus gefitinib as first-line treatment for patients with EGFR-mutation-positive non-small-cell lung cancer (ARCHER 1050): a randomised, open-label, phase 3 trial., Lancet Oncol
    Kosaka et al., 2017, Response Heterogeneity of EGFR and HER2 Exon 20 Insertions to Covalent EGFR and HER2 Inhibitors., Cancer Res.
    Brzezniak C et al., 2013, Dacomitinib, a new therapy for the treatment of non-small cell lung cancer., Expert Opin Pharmacother
    Yasuda et al., 2012, EGFR exon 20 insertion mutations in non-small-cell lung cancer: preclinical data and clinical implications., Lancet Oncol.
    Fry et al., 1998, Specific, irreversible inactivation of the epidermal growth factor receptor and erbB2, by a new class of tyrosine kinase inhibitor., Proc. Natl. Acad. Sci. U.S.A.
    Ma et al., 2016, InsR/IGF1R Pathway Mediates Resistance to EGFR Inhibitors in Glioblastoma., Clin. Cancer Res.
    Kobayashi et al., 2017, Characterization of EGFR T790M, L792F, and C797S Mutations as Mechanisms of Acquired Resistance to Afatinib in Lung Cancer., Mol. Cancer Ther.
    Jänne et al., 2014, Dacomitinib as first-line treatment in patients with clinically or molecularly selected advanced non-small-cell lung cancer: a multicentre, open-label, phase 2 trial., Lancet Oncol.
    Zahonero et al., 2015, Preclinical Test of Dacomitinib, an Irreversible EGFR Inhibitor, Confirms Its Effectiveness for Glioblastoma., Mol. Cancer Ther.
    Sequist et al., 2011, Genotypic and histological evolution of lung cancers acquiring resistance to EGFR inhibitors., Sci Transl Med
    Kobayashi et al., 2015, EGFR Exon 18 Mutations in Lung Cancer: Molecular Predictors of Augmented Sensitivity to Afatinib or Neratinib as Compared with First- or Third-Generation TKIs., Clin. Cancer Res.
    Engelman et al., 2007, PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefitinib., Cancer Res.
    Saadeh et al., 2007, Panitumumab: a fully human monoclonal antibody with activity in metastatic colorectal cancer., Ann Pharmacother
    Strickler JH et al., 2018, Genomic Landscape of Cell-Free DNA in Patients with Colorectal Cancer., Cancer Discov
    Funke S et al., 2008, Pharmacogenetics in colorectal cancer: a systematic review., Pharmacogenomics
    Shen et al., 2014, EGFR gene copy number as a predictive biomarker for resistance to anti-EGFR monoclonal antibodies in metastatic colorectal cancer treatment: a meta-analysis., Chin. J. Cancer Res.
    Foon et al., 2004, Preclinical and clinical evaluations of ABX-EGF, a fully human anti-epidermal growth factor receptor antibody., Int. J. Radiat. Oncol. Biol. Phys.
    Cohen, 2003, Epidermal growth factor receptor as a therapeutic target in colorectal cancer., Clin Colorectal Cancer
    Herbst RS et al., 2004, Gefitinib in combination with paclitaxel and carboplatin in advanced non-small-cell lung cancer: a phase III trial--INTACT 2., J Clin Oncol
    Bonner JA et al., 2006, Radiotherapy plus cetuximab for squamous-cell carcinoma of the head and neck., N Engl J Med
    Sebio A et al., 2014, Intergenic polymorphisms in the amphiregulin gene region as biomarkers in metastatic colorectal cancer patients treated with anti-EGFR plus irinotecan., Pharmacogenomics J
    Normanno N et al., 2006, Epidermal growth factor receptor (EGFR) signaling in cancer., Gene
    Giaccone G et al., 2004, Gefitinib in combination with gemcitabine and cisplatin in advanced non-small-cell lung cancer: a phase III trial--INTACT 1., J Clin Oncol
    Vermorken JB et al., 2008, Platinum-based chemotherapy plus cetuximab in head and neck cancer., N Engl J Med
    Keating, 2010, Spotlight on panitumumab in metastatic colorectal cancer., BioDrugs
    Sánchez-Martín et al., 2016, The First-in-class Anti-EGFR Antibody Mixture Sym004 Overcomes Cetuximab Resistance Mediated by EGFR Extracellular Domain Mutations in Colorectal Cancer., Clin. Cancer Res.
    Heymach et al., 2006, Epidermal growth factor receptor inhibitors in development for the treatment of non-small cell lung cancer., Clin. Cancer Res.
    Keating, 2010, Panitumumab: a review of its use in metastatic colorectal cancer., Drugs
    Uchibori et al., 2017, Brigatinib combined with anti-EGFR antibody overcomes osimertinib resistance in EGFR-mutated non-small-cell lung cancer., Nat Commun
    Arena et al., 2016, MM-151 overcomes acquired resistance to cetuximab and panitumumab in colorectal cancers harboring EGFR extracellular domain mutations., Sci Transl Med
    Thatcher N et al., 2005, Gefitinib plus best supportive care in previously treated patients with refractory advanced non-small-cell lung cancer: results from a randomised, placebo-controlled, multicentre study (Iressa Survival Evaluation in Lung Cancer)., Lancet
    Sartore-Bianchi et al., 2007, Epidermal growth factor receptor gene copy number and clinical outcome of metastatic colorectal cancer treated with panitumumab., J. Clin. Oncol.
    Lynch et al., 2002, Therapeutic potential of ABX-EGF: a fully human anti-epidermal growth factor receptor monoclonal antibody for cancer treatment., Semin. Oncol.
    Jonker et al., 2007, Cetuximab for the treatment of colorectal cancer., N. Engl. J. Med.
    Montagut et al., 2012, Identification of a mutation in the extracellular domain of the Epidermal Growth Factor Receptor conferring cetuximab resistance in colorectal cancer., Nat. Med.
    Rossi A et al., 2013, Should epidermal growth factor receptor tyrosine kinase inhibitors be considered ideal drugs for the treatment of selected advanced non-small cell lung cancer patients?, Cancer Treat Rev
    Yang et al., 2001, Development of ABX-EGF, a fully human anti-EGF receptor monoclonal antibody, for cancer therapy., Crit. Rev. Oncol. Hematol.
    Van Cutsem et al., 2009, Cetuximab and chemotherapy as initial treatment for metastatic colorectal cancer., N. Engl. J. Med.
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Giusti RM et al., 2008, U.S. Food and Drug Administration approval: panitumumab for epidermal growth factor receptor-expressing metastatic colorectal carcinoma with progression following fluoropyrimidine-, oxaliplatin-, and irinotecan-containing chemotherapy regimens., Clin Cancer Res
    Jean et al., 2008, Epidermal growth factor receptor monoclonal antibodies for the treatment of metastatic colorectal cancer., Pharmacotherapy
    Wu et al., 2008, Panitumumab: human monoclonal antibody against epidermal growth factor receptors for the treatment of metastatic colorectal cancer., Clin Ther
    Jorissen RN et al., 2003, Epidermal growth factor receptor: mechanisms of activation and signalling., Exp Cell Res
    Oddo et al., 2016, Molecular Landscape of Acquired Resistance to Targeted Therapy Combinations in BRAF-Mutant Colorectal Cancer., Cancer Res.
    Segaert et al., 2005, Clinical signs, pathophysiology and management of skin toxicity during therapy with epidermal growth factor receptor inhibitors., Ann. Oncol.
    Mayo C et al., 2012, Pharmacogenetics of EGFR in lung cancer: perspectives and clinical applications., Pharmacogenomics
    Schuster et al., 2015, A phase II, multicenter trial of rindopepimut (CDX-110) in newly diagnosed glioblastoma: the ACT III study., Neuro-oncology
    Rateb ME et al., 2009, Bioactive diterpene derivatives from the marine sponge Spongionella sp., J Nat Prod
    Liang et al., 2014, Network meta-analysis of erlotinib, gefitinib, afatinib and icotinib in patients with advanced non-small-cell lung cancer harboring EGFR mutations., PLoS ONE
    Chen et al., 2016, Clinical efficacy of first-generation EGFR-TKIs in patients with advanced non-small-cell lung cancer harboring EGFR exon 20 mutations., Onco Targets Ther
    Ludovini V et al., 2011, Phosphoinositide-3-kinase catalytic alpha and KRAS mutations are important predictors of resistance to therapy with epidermal growth factor receptor tyrosine kinase inhibitors in patients with advanced non-small cell lung cancer., J Thorac Oncol
    Lin et al., 2017, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor-sensitive Exon 19 Insertion and Exon 20 Insertion in Patients With Advanced Non-Small-cell Lung Cancer., Clin Lung Cancer
    Liu G et al., 2008, Epidermal growth factor receptor polymorphisms and clinical outcomes in non-small-cell lung cancer patients treated with gefitinib., Pharmacogenomics J
    Yu et al., 2013, Analysis of tumor specimens at the time of acquired resistance to EGFR-TKI therapy in 155 patients with EGFR-mutant lung cancers., Clin. Cancer Res.
    Zhang X et al., 2017, EGFR gene copy number as a predictive/biomarker for patients with non-small-cell lung cancer receiving tyrosine kinase inhibitor treatment: a systematic review and meta-analysis., J Investig Med
    Han et al., 2012, First-SIGNAL: first-line single-agent iressa versus gemcitabine and cisplatin trial in never-smokers with adenocarcinoma of the lung., J. Clin. Oncol.
    Zhang D et al., 2013, Synthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors., Bioorg Med Chem
    Hirsch FR et al., 2007, Combination of EGFR gene copy number and protein expression predicts outcome for advanced non-small-cell lung cancer patients treated with gefitinib., Ann Oncol
    Ciardiello et al., 2000, Antitumor effect and potentiation of cytotoxic drugs activity in human cancer cells by ZD-1839 (Iressa), an epidermal growth factor receptor-selective tyrosine kinase inhibitor., Clin. Cancer Res.
    Takeuchi et al., 2012, Dual inhibition of Met kinase and angiogenesis to overcome HGF-induced EGFR-TKI resistance in EGFR mutant lung cancer., Am. J. Pathol.
    Ban HS et al., 2010, Enhancement of EGFR tyrosine kinase inhibition by C-C multiple bonds-containing anilinoquinazolines., Bioorg Med Chem
    Kosaka T et al., 2006, Analysis of epidermal growth factor receptor gene mutation in patients with non-small cell lung cancer and acquired resistance to gefitinib., Clin Cancer Res
    Albanell et al., 2001, Activated extracellular signal-regulated kinases: association with epidermal growth factor receptor/transforming growth factor alpha expression in head and neck squamous carcinoma and inhibition by anti-epidermal growth factor receptor treatments., Cancer Res.
    Murray et al., 2010, Screening for EGFR Mutations in Patients with Head and Neck Cancer Treated with Gefitinib on a Compassionate-Use Program: A Hellenic Cooperative Oncology Group Study., J Oncol
    Koole et al., 2016, FGFR1 Is a Potential Prognostic Biomarker and Therapeutic Target in Head and Neck Squamous Cell Carcinoma., Clin. Cancer Res.
    Yang JC et al., 2020, A Randomized Phase 2 Study of Gefitinib With or Without Pemetrexed as First-line Treatment in Nonsquamous NSCLC With EGFR Mutation: Final Overall Survival and Biomarker Analysis., J Thorac Oncol
    Geoerger B et al., 2008, EGFR tyrosine kinase inhibition radiosensitizes and induces apoptosis in malignant glioma and childhood ependymoma xenografts., Int J Cancer
    Tiseo M et al., 2010, Predictors of gefitinib outcomes in advanced non-small cell lung cancer (NSCLC): study of a comprehensive panel of molecular markers., Lung Cancer
    Niu et al., 2014, Novel agents and strategies for overcoming EGFR TKIs resistance., Exp Hematol Oncol
    Nakamura T et al., 2011, A noninvasive system for monitoring resistance to epidermal growth factor receptor tyrosine kinase inhibitors with plasma DNA., J Thorac Oncol
    Chang et al., Early radiographic response to epidermal growth factor receptor-tyrosine kinase inhibitor in non-small cell lung cancer patients with epidermal growth factor receptor mutations: A prospective study., Biomed J
    Inukai et al., 2006, Presence of epidermal growth factor receptor gene T790M mutation as a minor clone in non-small cell lung cancer., Cancer Res.
    Onitsuka T et al., 2010, Acquired resistance to gefitinib: the contribution of mechanisms other than the T790M, MET, and HGF status., Lung Cancer
    Lewis et al., 2012, A phase II study of gefitinib for aggressive cutaneous squamous cell carcinoma of the head and neck., Clin. Cancer Res.
    Moasser et al., 2001, The tyrosine kinase inhibitor ZD1839 ("Iressa") inhibits HER2-driven signaling and suppresses the growth of HER2-overexpressing tumor cells., Cancer Res.
    Engelman et al., 2007, MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling., Science
    Kobayashi et al., 2005, EGFR mutation and resistance of non-small-cell lung cancer to gefitinib., N. Engl. J. Med.
    Maemondo et al., 2010, Gefitinib or chemotherapy for non-small-cell lung cancer with mutated EGFR., N. Engl. J. Med.
    Bell et al., 2005, Inherited susceptibility to lung cancer may be associated with the T790M drug resistance mutation in EGFR., Nat. Genet.
    Mok et al., 2009, Gefitinib or carboplatin-paclitaxel in pulmonary adenocarcinoma., N. Engl. J. Med.
    Paez et al., 2004, EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy., Science
    Yun et al., 2008, The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP., Proc. Natl. Acad. Sci. U.S.A.
    Rho et al., 2014, MET and AXL inhibitor NPS-1034 exerts efficacy against lung cancer cells resistant to EGFR kinase inhibitors because of MET or AXL activation., Cancer Res.
    Dahabreh et al., 2011, EGFR gene copy number as a predictive biomarker for patients receiving tyrosine kinase inhibitor treatment: a systematic review and meta-analysis in non-small-cell lung cancer., Ann. Oncol.
    Oizumi S et al., 2012, Quality of life with gefitinib in patients with EGFR-mutated non-small cell lung cancer: quality of life analysis of North East Japan Study Group 002 Trial., Oncologist
    Ichihara S et al., 2007, The impact of epidermal growth factor receptor gene status on gefitinib-treated Japanese patients with non-small-cell lung cancer., Int J Cancer
    Niederst et al., 2015, The Allelic Context of the C797S Mutation Acquired upon Treatment with Third-Generation EGFR Inhibitors Impacts Sensitivity to Subsequent Treatment Strategies., Clin. Cancer Res.
    Okada-Iwasaki et al., 2016, The Discovery and Characterization of K-756, a Novel Wnt/β-Catenin Pathway Inhibitor Targeting Tankyrase., Mol. Cancer Ther.
    Tomizawa Y et al., 2005, Clinicopathologic significance of the mutations of the epidermal growth factor receptor gene in patients with non-small cell lung cancer., Clin Cancer Res
    Han SW et al., 2007, Intron 1 CA dinucleotide repeat polymorphism and mutations of epidermal growth factor receptor and gefitinib responsiveness in non-small-cell lung cancer., Pharmacogenet Genomics
    Dziadziuszko et al., 2006, Epidermal growth factor receptor messenger RNA expression, gene dosage, and gefitinib sensitivity in non-small cell lung cancer., Clin. Cancer Res.
    Rakhit A et al., 2008, The effects of CYP3A4 inhibition on erlotinib pharmacokinetics: computer-based simulation (SimCYP) predicts in vivo metabolic inhibition., Eur J Clin Pharmacol
    Goss et al., 2013, Gefitinib versus placebo in completely resected non-small-cell lung cancer: results of the NCIC CTG BR19 study., J. Clin. Oncol.
    Wang et al., 2012, Phosphorylated EGFR expression may predict outcome of EGFR-TKIs therapy for the advanced NSCLC patients with wild-type EGFR., J. Exp. Clin. Cancer Res.
    Balak et al., 2006, Novel D761Y and common secondary T790M mutations in epidermal growth factor receptor-mutant lung adenocarcinomas with acquired resistance to kinase inhibitors., Clin. Cancer Res.
    Verma et al., 2017, Targeting of PYK2 Synergizes with EGFR Antagonists in Basal-like TNBC and Circumvents HER3-Associated Resistance via the NEDD4-NDRG1 Axis., Cancer Res.
    Yasuda et al., 2013, Structural, biochemical, and clinical characterization of epidermal growth factor receptor (EGFR) exon 20 insertion mutations in lung cancer., Sci Transl Med
    Kim et al., 2015, Differential Effects of Tyrosine Kinase Inhibitors on Normal and Oncogenic EGFR Signaling and Downstream Effectors., Mol. Cancer Res.
    Otsuka et al., 2015, Effectiveness of Tyrosine Kinase Inhibitors in Japanese Patients with Non-small Cell Lung Cancer Harboring Minor Epidermal Growth Factor Receptor Mutations: Results from a Multicenter Retrospective Study (HANSHIN Oncology Group 0212)., Anticancer Res.
    Eberlein et al., 2015, Acquired Resistance to the Mutant-Selective EGFR Inhibitor AZD9291 Is Associated with Increased Dependence on RAS Signaling in Preclinical Models., Cancer Res.
    Lim et al., 2014, Comparison of clinical outcomes following gefitinib and erlotinib treatment in non-small-cell lung cancer patients harboring an epidermal growth factor receptor mutation in either exon 19 or 21., J Thorac Oncol
    Pao et al., 2004, EGF receptor gene mutations are common in lung cancers from "never smokers" and are associated with sensitivity of tumors to gefitinib and erlotinib., Proc. Natl. Acad. Sci. U.S.A.
    Ma et al., 2011, T790M and acquired resistance of EGFR TKI: a literature review of clinical reports., J Thorac Dis
    Chen HJ et al., 2009, Clinicopathologic and molecular features of epidermal growth factor receptor T790M mutation and c-MET amplification in tyrosine kinase inhibitor-resistant Chinese non-small cell lung cancer., Pathol Oncol Res
    Costa et al., 2008, Effects of erlotinib in EGFR mutated non-small cell lung cancers with resistance to gefitinib., Clin. Cancer Res.
    Wu YL et al., 2007, Epidermal growth factor receptor mutations and their correlation with gefitinib therapy in patients with non-small cell lung cancer: a meta-analysis based on updated individual patient data from six medical centers in mainland China., J Thorac Oncol
    Yun et al., 2007, Structures of lung cancer-derived EGFR mutants and inhibitor complexes: mechanism of activation and insights into differential inhibitor sensitivity., Cancer Cell
    Nicholson et al., 2001, Modulation of epidermal growth factor receptor in endocrine-resistant, oestrogen receptor-positive breast cancer., Endocr. Relat. Cancer
    Chou et al., 2005, Mutation in the tyrosine kinase domain of epidermal growth factor receptor is a predictive and prognostic factor for gefitinib treatment in patients with non-small cell lung cancer., Clin. Cancer Res.
    Mellinghoff et al., 2005, Molecular determinants of the response of glioblastomas to EGFR kinase inhibitors., N. Engl. J. Med.
    Arteaga et al., 2001, Tyrosine kinase inhibitors-ZD1839 (Iressa)., Curr Opin Oncol
    Fukuoka et al., 2003, Multi-institutional randomized phase II trial of gefitinib for previously treated patients with advanced non-small-cell lung cancer (The IDEAL 1 Trial) [corrected]., J. Clin. Oncol.
    Su et al., 2012, Pretreatment epidermal growth factor receptor (EGFR) T790M mutation predicts shorter EGFR tyrosine kinase inhibitor response duration in patients with non-small-cell lung cancer., J. Clin. Oncol.
    Sheng M et al., 2016, Comparison of clinical outcomes of patients with non-small-cell lung cancer harbouring epidermal growth factor receptor exon 19 or exon 21 mutations after tyrosine kinase inhibitors treatment: a meta-analysis., Eur J Clin Pharmacol
    Della Corte et al., 2015, SMO Gene Amplification and Activation of the Hedgehog Pathway as Novel Mechanisms of Resistance to Anti-Epidermal Growth Factor Receptor Drugs in Human Lung Cancer., Clin. Cancer Res.
    Yeh et al., 2013, DNA-Mutation Inventory to Refine and Enhance Cancer Treatment (DIRECT): a catalog of clinically relevant cancer mutations to enable genome-directed anticancer therapy., Clin. Cancer Res.
    Goto K et al., 2012, Epidermal growth factor receptor mutation status in circulating free DNA in serum: from IPASS, a phase III study of gefitinib or carboplatin/paclitaxel in non-small cell lung cancer., J Thorac Oncol
    Foster et al., 2010, Clinical implications of novel activating EGFR mutations in malignant peritoneal mesothelioma., World J Surg Oncol
    Xu JM et al., 2009, EGFR mutations and HER2/3 protein expression and clinical outcome in Chinese advanced non-small cell lung cancer patients treated with gefitinib., J Cancer Res Clin Oncol
    Douillard et al., 2010, Molecular predictors of outcome with gefitinib and docetaxel in previously treated non-small-cell lung cancer: data from the randomized phase III INTEREST trial., J. Clin. Oncol.
    Endo K et al., 2006, Evaluation of the epidermal growth factor receptor gene mutation and copy number in non-small cell lung cancer with gefitinib therapy., Oncol Rep
    Lou et al., 2014, Combination of gefitinib and DNA methylation inhibitor decitabine exerts synergistic anti-cancer activity in colon cancer cells., PLoS ONE
    Sequist et al., 2007, Response to treatment and survival of patients with non-small cell lung cancer undergoing somatic EGFR mutation testing., Oncologist
    Lynch et al., 2004, Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib., N. Engl. J. Med.
    Mitsudomi et al., 2010, Gefitinib 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 trial., Lancet Oncol.
    Taron et al., 2005, Activating mutations in the tyrosine kinase domain of the epidermal growth factor receptor are associated with improved survival in gefitinib-treated chemorefractory lung adenocarcinomas., Clin. Cancer Res.
    Yang et al., 2011, Good response to gefitinib in a lung adenocarcinoma harboring a heterozygous complex mutation of L833V and H835L in epidermal growth factor receptor gene., J. Clin. Oncol.
    Ercan et al., 2015, EGFR Mutations and Resistance to Irreversible Pyrimidine-Based EGFR Inhibitors., Clin. Cancer Res.
    Ma F et al., 2009, Polymorphisms of EGFR predict clinical outcome in advanced non-small-cell lung cancer patients treated with Gefitinib., Lung Cancer
    Peters et al., 2012, Metastatic non-small-cell lung cancer (NSCLC): ESMO Clinical Practice Guidelines for diagnosis, treatment and follow-up., Ann. Oncol.
    Cho SH et al., 2012, Efficacy of EGFR tyrosine kinase inhibitors for non-adenocarcinoma NSCLC patients with EGFR mutation., Cancer Chemother Pharmacol
    Bell DW et al., 2005, Epidermal growth factor receptor mutations and gene amplification in non-small-cell lung cancer: molecular analysis of the IDEAL/INTACT gefitinib trials., J Clin Oncol
    Kancha et al., 2009, Functional analysis of epidermal growth factor receptor (EGFR) mutations and potential implications for EGFR targeted therapy., Clin. Cancer Res.
    Yang et al., 2008, Specific EGFR mutations predict treatment outcome of stage IIIB/IV patients with chemotherapy-naive non-small-cell lung cancer receiving first-line gefitinib monotherapy., J. Clin. Oncol.
    Han SW et al., 2006, Clinical predictors versus epidermal growth factor receptor mutation in gefitinib-treated non-small-cell lung cancer patients., Lung Cancer
    Nie Q et al., 2007, The epidermal growth factor receptor intron1 (CA) n microsatellite polymorphism is a potential predictor of treatment outcome in patients with advanced lung cancer treated with Gefitinib., Eur J Pharmacol
    Fukihara et al., 2014, Clinical predictors of response to EGFR tyrosine kinase inhibitors in patients with EGFR-mutant non-small cell lung cancer., Oncology
    Szerlip et al., 2012, Intratumoral heterogeneity of receptor tyrosine kinases EGFR and PDGFRA amplification in glioblastoma defines subpopulations with distinct growth factor response., Proc. Natl. Acad. Sci. U.S.A.
    Pao et al., 2005, Acquired resistance of lung adenocarcinomas to gefitinib or erlotinib is associated with a second mutation in the EGFR kinase domain., PLoS Med.
    Rosell et al., 2011, Pretreatment EGFR T790M mutation and BRCA1 mRNA expression in erlotinib-treated advanced non-small-cell lung cancer patients with EGFR mutations., Clin. Cancer Res.
    Sugio K et al., 2009, Prospective phase II study of gefitinib in non-small cell lung cancer with epidermal growth factor receptor gene mutations., Lung Cancer
    Udager et al., 2015, High-Frequency Targetable EGFR Mutations in Sinonasal Squamous Cell Carcinomas Arising from Inverted Sinonasal Papilloma., Cancer Res.
    Shien et al., 2013, Acquired resistance to EGFR inhibitors is associated with a manifestation of stem cell-like properties in cancer cells., Cancer Res.
    Belchis et al., 2016, Heterogeneity of resistance mutations detectable by nextgeneration sequencing in TKI-treated lung adenocarcinoma., Oncotarget
    Yamaoka et al., 2016, Acquired Resistance Mechanisms to Combination Met-TKI/EGFR-TKI Exposure in Met-Amplified EGFR-TKI-Resistant Lung Adenocarcinoma Harboring an Activating EGFR Mutation., Mol. Cancer Ther.
    Liu G et al., 2012, Pharmacogenetic analysis of BR.21, a placebo-controlled randomized phase III clinical trial of erlotinib in advanced non-small cell lung cancer., J Thorac Oncol
    Wu et al., 2011, Effectiveness of tyrosine kinase inhibitors on "uncommon" epidermal growth factor receptor mutations of unknown clinical significance in non-small cell lung cancer., Clin. Cancer Res.
    Carmi C et al., 2010, Novel irreversible epidermal growth factor receptor inhibitors by chemical modulation of the cysteine-trap portion., J Med Chem
    Jackman et al., 2006, Exon 19 deletion mutations of epidermal growth factor receptor are associated with prolonged survival in non-small cell lung cancer patients treated with gefitinib or erlotinib., Clin. Cancer Res.
    Yu H et al., 2014, A phase II randomized trial evaluating gefitinib intercalated with pemetrexed/platinum chemotherapy or pemetrexed/platinum chemotherapy alone in unselected patients with advanced non-squamous non-small cell lung cancer., Cancer Biol Ther
    Ji et al., 2006, The impact of human EGFR kinase domain mutations on lung tumorigenesis and in vivo sensitivity to EGFR-targeted therapies., Cancer Cell
    Chang et al., 2016, Identifying recurrent mutations in cancer reveals widespread lineage diversity and mutational specificity., Nat. Biotechnol.
    Rajasekaran et al., 2010, In silico identification of significant detrimental missense mutations of EGFR and their effect with 4-anilinoquinazoline-based drugs., Appl. Biochem. Biotechnol.
    Miller et al., 2012, 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., Lancet Oncol.
    Dungo et al., 2013, Afatinib: first global approval., Drugs
    Huang et al., 2013, MEK inhibitors reverse resistance in epidermal growth factor receptor mutation lung cancer cells with acquired resistance to gefitinib., Mol Oncol
    Sun et al., 2013, Clinical implications of T790M mutation in patients with acquired resistance to EGFR tyrosine kinase inhibitors., Lung Cancer
    Girard et al., 2010, Analysis of genetic variants in never-smokers with lung cancer facilitated by an Internet-based blood collection protocol: a preliminary report., Clin. Cancer Res.
    Choudhury et al., 2016, Afatinib Activity in Platinum-Refractory Metastatic Urothelial Carcinoma in Patients With ERBB Alterations., J. Clin. Oncol.
    Bahcall et al., 2016, Acquired METD1228V Mutation and Resistance to MET Inhibition in Lung Cancer., Cancer Discov
    Konduri et al., 2016, EGFR Fusions as Novel Therapeutic Targets in Lung Cancer., Cancer Discov
    Guo et al., 2006, Gefitinib-sensitizing mutations in esophageal carcinoma., N. Engl. J. Med.
    Starrett JH et al., 2020, Drug Sensitivity and Allele Specificity of First-Line Osimertinib Resistance <i>EGFR</i> Mutations., Cancer Res
    Fu et al., 2008, EGFR mutants found in non-small cell lung cancer show different levels of sensitivity to suppression of Src: implications in targeting therapy., Oncogene
    Han et al., 2005, Predictive and prognostic impact of epidermal growth factor receptor mutation in non-small-cell lung cancer patients treated with gefitinib., J. Clin. Oncol.
    Sequist et al., 2010, Neratinib, an irreversible pan-ErbB receptor tyrosine kinase inhibitor: results of a phase II trial in patients with advanced non-small-cell lung cancer., J. Clin. Oncol.
    Yang et al., 2015, Afatinib versus cisplatin-based chemotherapy for EGFR mutation-positive lung adenocarcinoma (LUX-Lung 3 and LUX-Lung 6): analysis of overall survival data from two randomised, phase 3 trials., Lancet Oncol.
    Yang et al., 2015, Clinical 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 6., Lancet Oncol.
    Heigener et al., 2015, Afatinib in Non-Small Cell Lung Cancer Harboring Uncommon EGFR Mutations Pretreated With Reversible EGFR Inhibitors., Oncologist
    Denis et al., 2015, EGFR T790M resistance mutation in non small-cell lung carcinoma., Clin. Chim. Acta
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    Paz-Ares et al., 2015, Monotherapy Administration of Sorafenib in Patients With Non-Small Cell Lung Cancer (MISSION) Trial: A Phase III, Multicenter, Placebo-Controlled Trial of Sorafenib in Patients with Relapsed or Refractory Predominantly Nonsquamous Non-Small-Cell Lung Cancer after 2 or 3 Previous Treatment Regimens., J Thorac Oncol
    Diez-Cecilia E et al., 2015, Probing a 3,4'-bis-guanidinium diaryl derivative as an allosteric inhibitor of the Ras pathway., Bioorg Med Chem Lett
    Blumenschein et al., 2013, Comprehensive biomarker analysis and final efficacy results of sorafenib in the BATTLE trial., Clin. Cancer Res.
    Takahashi H et al., 2013, Identification of a candidate single-nucleotide polymorphism related to chemotherapeutic response through a combination of knowledge-based algorithm and hypothesis-free genomic data., J Biosci Bioeng
    Li X et al., 2014, Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity., J Med Chem
    Tan CS et al., 2016, Next-generation epidermal growth factor receptor tyrosine kinase inhibitors in epidermal growth factor receptor -mutant non-small cell lung cancer., Lung Cancer
    Ratner et al., 2012, A KRAS variant is a biomarker of poor outcome, platinum chemotherapy resistance and a potential target for therapy in ovarian cancer., Oncogene
    Hudkins RL et al., 2012, Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-4-one (CEP-11981): a novel oncology therapeutic agent., J Med Chem
    Zhou X et al., 2006, Isolation and inhibitory activity against ERK phosphorylation of hydroxyanthraquinones from rhubarb., Bioorg Med Chem Lett
    Xu et al., 2016, AC0010, an Irreversible EGFR Inhibitor Selectively Targeting Mutated EGFR and Overcoming T790M-Induced Resistance in Animal Models and Lung Cancer Patients., Mol. Cancer Ther.
    Sakaguchi et al., 2006, The antiproliferative effect of lidocaine on human tongue cancer cells with inhibition of the activity of epidermal growth factor receptor., Anesth. Analg.
    Challa et al., 2016, IKBKE Is a Substrate of EGFR and a Therapeutic Target in Non-Small Cell Lung Cancer with Activating Mutations of EGFR., Cancer Res.
    Ceccon M et al., 2013, Crizotinib-resistant NPM-ALK mutants confer differential sensitivity to unrelated Alk inhibitors., Mol Cancer Res
    Markham A, 2017, Brigatinib: First Global Approval., Drugs
    Iragavarapu C et al., 2015, Novel ALK inhibitors in clinical use and development., J Hematol Oncol
    Qu et al., 2014, Antitumor activity of selective MEK1/2 inhibitor AZD6244 in combination with PI3K/mTOR inhibitor BEZ235 in gefitinib-resistant NSCLC xenograft models., J. Exp. Clin. Cancer Res.
    Gozgit et al., 2012, Ponatinib (AP24534), a multitargeted pan-FGFR inhibitor with activity in multiple FGFR-amplified or mutated cancer models., Mol. Cancer Ther.
    Chabon et al., 2016, Circulating tumour DNA profiling reveals heterogeneity of EGFR inhibitor resistance mechanisms in lung cancer patients., Nat Commun
    Sasaki et al., 2011, A novel ALK secondary mutation and EGFR signaling cause resistance to ALK kinase inhibitors., Cancer Res.
    Etienne-Grimaldi MC et al., 2012, Multifactorial pharmacogenetic analysis in colorectal cancer patients receiving 5-fluorouracil-based therapy together with cetuximab-irinotecan., Br J Clin Pharmacol
    Asnavandi M et al., 2017, EGFR rs11506105 and IFNL3 SNPs but not rs8099917 are strongly associated with treatment responses in Iranian patients with chronic hepatitis C., Genes Immun
    Selig R et al., 2012, A frozen analogue approach to aminopyridinylimidazoles leading to novel and promising p38 MAP kinase inhibitors., J Med Chem
    Petch D et al., 2012, Design and synthesis of EGFR dimerization inhibitors and evaluation of their potential in the treatment of psoriasis., Bioorg Med Chem
    Schleissner C et al., 2011, Antitumor actinopyranones produced by Streptomyces albus POR-04-15-053 isolated from a marine sediment., J Nat Prod
    Wu S et al., 2020, <i>EGFR</i> Amplification Induces Increased DNA Damage Response and Renders Selective Sensitivity to Talazoparib (PARP Inhibitor) in Glioblastoma., Clin Cancer Res
    Tam CS et al., 2019, Phase 1 study of the selective BTK inhibitor zanubrutinib in B-cell malignancies and safety and efficacy evaluation in CLL., Blood
    Guo Y et al., 2019, Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase., J Med Chem
    Rolf MG et al., 2015, In vitro pharmacological profiling of R406 identifies molecular targets underlying the clinical effects of fostamatinib., Pharmacol Res Perspect
  • AFATINIB   EGFR

    Interaction Score: 4.14

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Clinical Status NCCN/ CAP guidelines
    Clinical Status early trials
    Variant Effect gain-of-function

    PMIDs:
    26619011 19455431 22452896 23982599 18681783 23102728 23930994 24035188 14990633 16467544 20068085 16377102 27044931 27694386 27102076 14990632 16707764 32193290 18784101 17653080 15710947 20479403 25589191 26051236 26354527 25668228 26341921 24439929 32226941 16912157 24893891 25589492 15728811 20573926 16258541 19692680 15118125 18227510 24658966 18199554 27083334 19922469 20033049 25964297 28363995 26515464 25923549 16257339 21783417 19692684 27207775 22753918 16187797 28145866 24353160 22452895 18003960 25559287 25870145 23945392 24813888 15329413 24636847 23816963 24729716 25611025 23816960 22285168 19096302 17349580 16204070 24894453 16043828 22215752 23022519 23344264 21194487 25077897 24065731 11255078 15118073 20022809 23948351 16115929 18458038 26286086 19339720 18316547 17332364 27913578 25948633 24623981 22190593 24790411 19147750 25157968 16011858 21430269 12648464 2302402 15737014 26720284 21670455 21233402 26206867 24565969 23242437 25923550 27304188 23991291 22588155 21531810 26862733 18303429 19671738 21617858 22594511


    Sources:
    MyCancerGenomeClinicalTrial DTC OncoKB FDA PharmGKB DoCM JAX-CKB TdgClinicalTrial CIViC DrugBank COSMIC TALC MyCancerGenome GuideToPharmacology CGI

  • OSIMERTINIB   EGFR

    Interaction Score: 2.26

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    31825714 26522274 27694386 27102076 32193290 31254668 24410791 24893891 27959700 25923549 25870145 26729184 28202511 28416483 26286086 25948633 27393507 27252416 25939061 26720284 26206867 27216193 28343545 27435396


    Sources:
    OncoKB FDA PharmGKB JAX-CKB CIViC TTD DrugBank COSMIC MyCancerGenome GuideToPharmacology ChemblInteractions CGI

  • DACOMITINIB   EGFR

    Interaction Score: 1.88

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    24857124 23930994 26768165 28958502 28363995 23294134 21764376 9751783 26561558 27913578 25456362 25939761 21430269 26206867 18089823


    Sources:
    CancerCommons MyCancerGenomeClinicalTrial DTC OncoKB FDA PharmGKB JAX-CKB TdgClinicalTrial CIViC TTD DrugBank TALC MyCancerGenome GuideToPharmacology ChemblInteractions

  • OLMUTINIB   EGFR

    Interaction Score: 1.88

    Interaction Types & Directionality:
    antagonist (inhibitory)
    inhibitor (inhibitory)

    Interaction Info:
    combination therapy [Rociletinib,HM61713]
    Drug family [EGFR inhibitor 3rd gen]
    Alteration EGFR:T790M

    PMIDs:
    26898616


    Sources:
    JAX-CKB DrugBank GuideToPharmacology ChemblInteractions CGI

  • ICOTINIB   EGFR

    Interaction Score: 1.88

    Interaction Types & Directionality:
    antagonist (inhibitory)
    inhibitor (inhibitory)

    Interaction Info:
    Details of the Assay for Interaction Inhibition of EGFR-mediated intracellular tyrosine phosphorylation in EGF-stimulated human A431 cells.
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False

    PMIDs:
    24533047 27468240 23372346 2394835 25261231 24438614


    Sources:
    MyCancerGenomeClinicalTrial JAX-CKB DrugBank TALC MyCancerGenome GuideToPharmacology

  • ZALUTUMUMAB   EGFR

    Interaction Score: 1.88

    Interaction Types & Directionality:
    antibody (inhibitory)
    antagonist (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name HuMax-EGFr
    Notes

    PMIDs:
    15383606


    Sources:
    TdgClinicalTrial TTD DrugBank TALC ChemblInteractions

  • RINDOPEPIMUT   EGFR

    Interaction Score: 1.57

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name rindopepimut, CDX-110
    Novel drug target Established target

    PMIDs:
    25586468


    Sources:
    TdgClinicalTrial CIViC TTD DrugBank

  • DEPATUXIZUMAB   EGFR

    Interaction Score: 1.26

    Interaction Types & Directionality:
    antibody (inhibitory)

    Interaction Info:
    Evidence Type Actionable
    Response Type predicted – sensitive
    Indication/Tumor Type Advanced Solid Tumor

    PMIDs:
    25895099


    Sources:
    JAX-CKB TTD MyCancerGenome

  • NECITUMUMAB   EGFR

    Interaction Score: 1.26

    Interaction Types & Directionality:
    antibody (inhibitory)
    antagonist (inhibitory)
    inhibitor (inhibitory)

    Interaction Info:
    Details of the Assay for Interaction Binding affinity of whole IMC-11F8 IgG using BIAcore sensor technology.
    Specific Action of the Ligand Binding
    Endogenous Drug? False

    PMIDs:
    20197484


    Sources:
    TdgClinicalTrial TTD DrugBank TALC MyCancerGenome GuideToPharmacology ChemblInteractions

  • ERLOTINIB   EGFR

    Interaction Score: 1.05

    Interaction Types & Directionality:
    antagonist (inhibitory)
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? True

    PMIDs:
    26619011 26324372 17877814 25870087 19455431 27468240 22452896 21258250 18652519 28089594 18681783 23470965 23102728 27664271 26773740 14990633 16467544 20068085 15310767 16377102 27694386 27102076 14990632 12517254 26768165 16707764 32193290 18784101 19969465 17653080 17020982 15710947 20479403 27216155 21841502 23917401 24410791 21921847 25668228 26341921 19015641 25179728 16912157 19589612 24893891 27760111 18309947 15728811 20573926 16258541 19692680 15118125 18227510 24658966 20826716 12814826 12498017 18199554 19922469 20033049 26106072 26515464 25923549 16257339 21783417 19692684 27207775 22753918 16187797 22901364 17085664 27793840 24353160 22452895 25573954 26124334 18003960 24736073 23945392 15329413 24636847 19381876 23816963 18981003 15217965 24729716 23816960 22285168 22982650 29290255 19096302 17349580 16204070 24894453 16043828 16282176 22215752 26490356 28874593 23022519 23344264 21194487 20942962 25077897 24065731 11255078 17285735 15118073 16014883 20022809 23948351 27825638 16115929 12820772 18458038 26286086 18349398 25521405 19339720 11752352 18316547 17332364 27913578 24623981 22190593 26720423 22760226 19147750 25157968 16011858 24868098 21430269 24457318 12648464 2302402 15737014 26720284 21670455 28408243 21233402 26206867 18992959 25931286 28343545 24565969 23242437 17177598 25923550 27304188 22588155 21531810 21969500 24470557 16818686 18303429 19671738 19010870 12840797 22594511


    Sources:
    ClearityFoundationBiomarkers ClearityFoundationClinicalTrial CancerCommons TEND DTC OncoKB FDA PharmGKB DoCM JAX-CKB TdgClinicalTrial CIViC TTD DrugBank COSMIC TALC MyCancerGenome GuideToPharmacology CGI

  • PKI-166   EGFR

    Interaction Score: 0.94

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Epidermal growth factor receptor erbB1 inhibitor
    Direct Interaction yes

    PMIDs:
    22018877


    Sources:
    DTC ChemblInteractions

  • MATUZUMAB   EGFR

    Interaction Score: 0.94

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Epidermal growth factor receptor erbB1 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    TTD DrugBank ChemblInteractions

  • PELITINIB   EGFR

    Interaction Score: 0.94

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Epidermal growth factor receptor erbB1 inhibitor
    Indication/Tumor Type Advanced Solid Tumor

    PMIDs:
    16710023 16364494


    Sources:
    JAX-CKB TTD DrugBank TALC MyCancerGenome GuideToPharmacology ChemblInteractions

  • ROCILETINIB   EGFR

    Interaction Score: 0.94

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Epidermal growth factor receptor erbB1 inhibitor
    Specific Action of the Ligand Inhibition

    PMIDs:
    24065731 28202511 25923550


    Sources:
    CIViC TTD MyCancerGenome GuideToPharmacology ChemblInteractions CGI

  • NIMOTUZUMAB   EGFR

    Interaction Score: 0.94

    Interaction Types & Directionality:
    antibody (inhibitory)

    Interaction Info:
    Notes
    Novel drug target Established target
    Trial Name Nimotuzumab

    PMIDs:
    25185971


    Sources:
    JAX-CKB TdgClinicalTrial TALC MyCancerGenome CGI

  • NERATINIB   EGFR

    Interaction Score: 0.8

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction? False
    Endogenous Drug? False
    Specific Action of the Ligand Inhibition

    PMIDs:
    18681783 14990633 16467544 16377102 14990632 18784101 20479403 16257339 17085664 18003960 23022519 11255078 19339720 18316547 25948633 12648464 26206867 25931286 21325073 22594511


    Sources:
    PharmGKB JAX-CKB TdgClinicalTrial TTD DrugBank TALC GuideToPharmacology ChemblInteractions

  • S-222611   EGFR

    Interaction Score: 0.78

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Epidermal growth factor receptor erbB1 inhibitor
    Direct Interaction yes
    Indication/Tumor Type Advanced Solid Tumor

    PMIDs:
    24837299 25434923


    Sources:
    JAX-CKB TTD ChemblInteractions

  • AC-480   EGFR

    Interaction Score: 0.78

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    19821562 21576284


    Sources:
    DTC JAX-CKB TdgClinicalTrial TTD TALC MyCancerGenome GuideToPharmacology ChemblInteractions

  • SAPITINIB   EGFR

    Interaction Score: 0.73

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? True

    PMIDs:
    24886365 20145185


    Sources:
    JAX-CKB TALC MyCancerGenome GuideToPharmacology ChemblInteractions

  • PANITUMUMAB   EGFR

    Interaction Score: 0.73

    Interaction Types & Directionality:
    suppressor (inhibitory)
    antibody (inhibitory)
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Epidermal growth factor receptor erbB1 inhibitor
    Direct Interaction yes
    Novel drug target Established target

    PMIDs:
    17355997 29196463 18681783 24653627 14967460 12620146 14990633 16467544 23959273 16377102 14990632 18784101 20623992 26888827 16857825 20481659 28287083 26843189 16257339 17664472 11894013 18003960 22270724 23022519 11255078 19339720 11752352 18316547 18503402 18343240 12648464 27312529 16012181 22594511


    Sources:
    ClearityFoundationBiomarkers TEND FDA PharmGKB DoCM JAX-CKB TdgClinicalTrial CIViC TTD DrugBank TALC MyCancerGenome GuideToPharmacology ChemblInteractions CGI

  • CETUXIMAB   EGFR

    Interaction Score: 0.71

    Interaction Types & Directionality:
    antibody (inhibitory)
    antagonist (inhibitory)
    inhibitor (inhibitory)

    Interaction Info:
    Notes
    Mechanism of Interaction Epidermal growth factor receptor erbB1 inhibitor
    Direct Interaction yes

    PMIDs:
    26619011 27149458 19455431 22452896 29196463 24653627 26059438 24934779 23102728 25623215 20068085 27102076 16707764 17653080 26888827 15710947 20479403 27216155 25668228 26341921 16912157 24893891 15728811 20573926 16258541 19692680 15118125 18227510 24063894 24658966 18199554 28287083 19922469 27251290 10601294 20033049 26515464 26843189 25923549 21783417 19692684 27207775 22753918 16187797 11408594 22452895 18003960 23945392 24813888 15329413 24636847 23816963 24729716 23816960 22285168 19096302 22152101 16204070 22270724 24894453 16043828 22215752 21194487 24065731 15118073 20022809 23948351 16115929 18458038 11752352 17332364 25948633 24623981 18794099 10628369 19147750 25157968 16011858 21430269 23578570 2302402 27312529 15737014 26720284 21670455 21233402 23242437 10480573 25923550 22588155 11431346 21531810 24141978 18303429 19671738 18089823


    Sources:
    ClearityFoundationBiomarkers CancerCommons TEND FDA DoCM JAX-CKB TdgClinicalTrial CIViC TTD DrugBank TALC MyCancerGenome GuideToPharmacology ChemblInteractions CGI

  • GEFITINIB   EGFR

    Interaction Score: 0.65

    Interaction Types & Directionality:
    antagonist (inhibitory)
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction? True
    Direct Interaction? False
    Endogenous Drug? False

    PMIDs:
    24533047 27468240 21258250 28089594 18681783 17375033 23470965 27664271 22370314 14990633 23993328 16467544 16377102 17317677 10815932 14990632 22789825 18784101 19969465 17020982 11522647 21274259 26936917 31605797 18386816 19473722 24410791 21921847 25179728 16912157 19589612 22261807 11585753 17463250 15728811 20573926 16258541 19692680 15118125 18227510 24165158 20826716 22581822 17192902 25964297 27196752 16203769 16257339 17429313 16707605 18000659 23980091 22901364 17085664 27793840 24353160 25573954 26124334 18003960 25870145 24736073 15329413 22263058 19381876 18981003 17473659 17349580 11566608 15897572 16282176 26561558 11673690 12748244 22215752 26490356 26124204 23022519 23344264 21900837 20942962 19020901 20038723 16865253 24874286 11255078 17285735 15118073 20022809 16115929 21422421 19339720 11752352 18316547 25948633 19201048 22997455 22760226 16204011 19147750 18509184 16956694 17597605 24457318 12648464 22323597 27312529 15737014 21233402 26206867 18992959 25931286 23542356 27304188 27612490 22237259 21531810 20151670 16818686 24755888 22594511 16730237


    Sources:
    ClearityFoundationBiomarkers MyCancerGenomeClinicalTrial TEND DTC OncoKB FDA PharmGKB DoCM JAX-CKB TdgClinicalTrial CIViC TTD DrugBank COSMIC TALC MyCancerGenome GuideToPharmacology ChemblInteractions CGI

  • CHEMBL1078000   EGFR

    Interaction Score: 0.63

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    19601607


    Sources:
    DTC

  • EPITINIB   EGFR

    Interaction Score: 0.63

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Epidermal growth factor receptor erbB1 inhibitor
    Direct Interaction yes
    Indication/Tumor Type non-small cell lung carcinoma

    PMIDs:
    None found


    Sources:
    JAX-CKB ChemblInteractions

  • GRACILIN A   EGFR

    Interaction Score: 0.63

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    19601607


    Sources:
    DTC

  • ABIVERTINIB MALEATE   EGFR

    Interaction Score: 0.63

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type lung adenocarcinoma
    Response Type sensitive
    Indication/Tumor Type non-small cell lung carcinoma

    PMIDs:
    27573423


    Sources:
    JAX-CKB

  • CHEMBL472212   EGFR

    Interaction Score: 0.63

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Gefitinib + PF-431396
    Evidence Type Actionable
    Approval Status Preclinical - Cell culture

    PMIDs:
    27793840


    Sources:
    JAX-CKB

  • CHEMBL285063   EGFR

    Interaction Score: 0.63

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17334377 10592235 23988354 10346932


    Sources:
    DTC DrugBank

  • DEPATUXIZUMAB MAFODOTIN   EGFR

    Interaction Score: 0.63

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type lung squamous cell carcinoma
    Indication/Tumor Type glioblastoma multiforme
    Response Type predicted – sensitive

    PMIDs:
    24424355 26846818


    Sources:
    JAX-CKB TTD

  • AZD-3759   EGFR

    Interaction Score: 0.63

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Approval Status Clinical Study
    Approval Status Preclinical - Cell line xenograft
    Response Type sensitive

    PMIDs:
    27928026


    Sources:
    JAX-CKB

  • CHEMBL188762   EGFR

    Interaction Score: 0.63

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    19969465


    Sources:
    DTC

  • IMGATUZUMAB   EGFR

    Interaction Score: 0.63

    Interaction Types & Directionality:
    antibody (inhibitory)

    Interaction Info:
    Notes
    Approval Status Preclinical
    Indication/Tumor Type non-small cell lung carcinoma

    PMIDs:
    23209031


    Sources:
    JAX-CKB TALC MyCancerGenome

  • VARLITINIB   EGFR

    Interaction Score: 0.63

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name ARRY-334543
    Novel drug target Established target
    Mechanism of Interaction Epidermal growth factor receptor erbB1 inhibitor

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial TTD DrugBank ChemblInteractions

  • GRACILIN J   EGFR

    Interaction Score: 0.63

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    19601607


    Sources:
    DTC

  • CHEMBL1077773   EGFR

    Interaction Score: 0.63

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    19601607


    Sources:
    DTC

  • LAPATINIB   EGFR

    Interaction Score: 0.55

    Interaction Types & Directionality:
    antagonist (inhibitory)
    inhibitor (inhibitory)

    Interaction Info:
    Reported Cancer Type Prostate
    Alteration EGFR:E690K
    Drug family ERBB2 inhibitor

    PMIDs:
    25305330 18681783 27595477 12214266 14990633 16467544 16377102 20110044 20215545 14990632 18784101 23917401 15374980 14633707 18199554 16257339 24355130 16894399 18003960 14751502 23022519 11255078 18408761 19339720 11752352 18316547 14737100 18803986 22885469 15163842 12648464 20658522 14967461 22594511


    Sources:
    ClearityFoundationClinicalTrial CancerCommons TEND DTC OncoKB PharmGKB DoCM JAX-CKB TdgClinicalTrial CIViC TTD DrugBank TALC GuideToPharmacology CGI

  • MP-412   EGFR

    Interaction Score: 0.52

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type non-small cell lung carcinoma
    Response Type sensitive
    Approval Status Preclinical

    PMIDs:
    17888033


    Sources:
    JAX-CKB TdgClinicalTrial DrugBank ChemblInteractions

  • NAQUOTINIB   EGFR

    Interaction Score: 0.47

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type non-small cell lung carcinoma
    Response Type sensitive
    Approval Status Phase I

    PMIDs:
    None found


    Sources:
    JAX-CKB TTD GuideToPharmacology

  • JNJ-61186372   EGFR

    Interaction Score: 0.47

    Interaction Types & Directionality:
    antibody (inhibitory)

    Interaction Info:
    Direct Interaction? True
    Endogenous Drug? False
    Specific Action of the Ligand Binding

    PMIDs:
    27216193


    Sources:
    JAX-CKB GuideToPharmacology

  • TAK-285   EGFR

    Interaction Score: 0.47

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Response Type sensitive
    Indication/Tumor Type squamous cell carcinoma
    Approval Status Preclinical - Cell line xenograft

    PMIDs:
    23983820


    Sources:
    JAX-CKB ChemblInteractions

  • CANERTINIB   EGFR

    Interaction Score: 0.36

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Details of the Assay for Interaction Inhibition of kinase activity
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False

    PMIDs:
    23930994 18408761


    Sources:
    DTC CIViC TTD DrugBank MyCancerGenome GuideToPharmacology

  • AVELUMAB   EGFR

    Interaction Score: 0.31

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    31086949


    Sources:
    CIViC

  • ERLOTINIB HYDROCHLORIDE   EGFR

    Interaction Score: 0.31

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Epidermal growth factor receptor erbB1 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • ALFLUTINIB   EGFR

    Interaction Score: 0.31

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • CETUXIMAB SAROTALOCAN   EGFR

    Interaction Score: 0.31

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • SIMOTINIB   EGFR

    Interaction Score: 0.31

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Epidermal growth factor receptor erbB1 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • NAZARTINIB   EGFR

    Interaction Score: 0.31

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Details of the Assay for Interaction Biochemical assay using EGFR L858R/T790M with a 90 minute preincubation with the inhibitor.
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • THELIATINIB   EGFR

    Interaction Score: 0.31

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Epidermal growth factor receptor erbB1 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • TARLOXOTINIB   EGFR

    Interaction Score: 0.31

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • CHEMBL2347958   EGFR

    Interaction Score: 0.31

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Reported Cancer Type Lung, Prostate

    PMIDs:
    None found


    Sources:
    CancerCommons

  • SAVOLITINIB   EGFR

    Interaction Score: 0.31

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy AZD9291 + Savolitinib
    Indication/Tumor Type lung adenocarcinoma
    Response Type sensitive

    PMIDs:
    27694386


    Sources:
    JAX-CKB

  • DULIGOTUZUMAB   EGFR

    Interaction Score: 0.31

    Interaction Types & Directionality:
    antibody (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD MyCancerGenome

  • ALLITINIB   EGFR

    Interaction Score: 0.31

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Epidermal growth factor receptor erbB1 inhibitor
    Direct Interaction yes
    Specific Action of the Ligand Inhibition

    PMIDs:
    None found


    Sources:
    TTD GuideToPharmacology ChemblInteractions

  • BMS-690514   EGFR

    Interaction Score: 0.31

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type non-small cell lung carcinoma
    Response Type predicted – sensitive
    Approval Status Phase II

    PMIDs:
    23490650


    Sources:
    JAX-CKB TTD TALC MyCancerGenome GuideToPharmacology ChemblInteractions

  • PYROTINIB   EGFR

    Interaction Score: 0.31

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Irreversible inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology ChemblInteractions

  • MAVELERTINIB   EGFR

    Interaction Score: 0.31

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • FUTUXIMAB   EGFR

    Interaction Score: 0.31

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • RG-7160   EGFR

    Interaction Score: 0.31

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Epidermal growth factor receptor erbB1 antagonist

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • MAB-425   EGFR

    Interaction Score: 0.31

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Epidermal growth factor receptor erbB1 inhibitor

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • POZIOTINIB   EGFR

    Interaction Score: 0.31

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type lung adenocarcinoma
    Response Type sensitive
    Approval Status Phase II

    PMIDs:
    None found


    Sources:
    MyCancerGenomeClinicalTrial OncoKB JAX-CKB GuideToPharmacology ChemblInteractions

  • AZD-4769   EGFR

    Interaction Score: 0.31

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Epidermal growth factor receptor erbB1 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • TESEVATINIB   EGFR

    Interaction Score: 0.27

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Epidermal growth factor receptor erbB1 inhibitor
    Direct Interaction yes
    Indication/Tumor Type non-small cell lung carcinoma

    PMIDs:
    22722787


    Sources:
    JAX-CKB TdgClinicalTrial TALC MyCancerGenome GuideToPharmacology ChemblInteractions

  • CHEMBL3397300   EGFR

    Interaction Score: 0.26

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Notes
    Approval Status Phase I
    Response Type sensitive

    PMIDs:
    27836716 27780853


    Sources:
    MyCancerGenomeClinicalTrial JAX-CKB TALC

  • BRIGATINIB   EGFR

    Interaction Score: 0.25

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Epidermal growth factor receptor erbB1 inhibitor
    Direct Interaction yes
    Specific Action of the Ligand Inhibition

    PMIDs:
    23239810 28597393 28287083 25888090


    Sources:
    CIViC DrugBank GuideToPharmacology ChemblInteractions

  • PHA-665752   EGFR

    Interaction Score: 0.25

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy PHA-665752 + Sonidegib
    Indication/Tumor Type non-small cell lung carcinoma
    Response Type sensitive

    PMIDs:
    24165158 26124204 23542356


    Sources:
    JAX-CKB

  • FALNIDAMOL   EGFR

    Interaction Score: 0.24

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction? False
    Endogenous Drug? False
    Specific Action of the Ligand Inhibition

    PMIDs:
    None found


    Sources:
    TTD GuideToPharmacology ChemblInteractions

  • AEE-788   EGFR

    Interaction Score: 0.22

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type Advanced Solid Tumor
    Response Type resistant
    Approval Status Preclinical

    PMIDs:
    19147750


    Sources:
    JAX-CKB MyCancerGenome GuideToPharmacology ChemblInteractions

  • CHEMBL1358137   EGFR

    Interaction Score: 0.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22944332


    Sources:
    DTC

  • GOLVATINIB   EGFR

    Interaction Score: 0.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Gefitinib + Golvatinib
    Indication/Tumor Type lung adenocarcinoma
    Response Type sensitive

    PMIDs:
    22789825


    Sources:
    JAX-CKB

  • DURVALUMAB   EGFR

    Interaction Score: 0.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type non-small cell lung carcinoma
    Response Type decreased response
    Approval Status Clinical Study

    PMIDs:
    31086949 27225694


    Sources:
    JAX-CKB CIViC

  • TEGAFUR   EGFR

    Interaction Score: 0.16

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22486600


    Sources:
    PharmGKB

  • METHYLCURCUMIN   EGFR

    Interaction Score: 0.16

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25753330


    Sources:
    DTC

  • MDX-447   EGFR

    Interaction Score: 0.16

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Mechanism of Interaction Epidermal growth factor receptor erbB1 other
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • ALOE-EMODIN   EGFR

    Interaction Score: 0.16

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16275083


    Sources:
    DTC

  • LAPATINIB DITOSYLATE   EGFR

    Interaction Score: 0.16

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Epidermal growth factor receptor erbB1 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • LY-3164530   EGFR

    Interaction Score: 0.16

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • LIFIRAFENIB   EGFR

    Interaction Score: 0.16

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction? False
    Endogenous Drug? False
    Specific Action of the Ligand Inhibition

    PMIDs:
    26208524


    Sources:
    JAX-CKB GuideToPharmacology

  • CUDC-101   EGFR

    Interaction Score: 0.16

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Evidence Type Actionable
    Approval Status Preclinical
    Response Type sensitive

    PMIDs:
    20388807


    Sources:
    JAX-CKB TdgClinicalTrial TTD TALC GuideToPharmacology ChemblInteractions

  • CAPMATINIB   EGFR

    Interaction Score: 0.16

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type collecting duct carcinoma
    Approval Status Preclinical - Pdx
    combination therapy INC280 + Trametinib

    PMIDs:
    28783719


    Sources:
    JAX-CKB

  • VANDETANIB   EGFR

    Interaction Score: 0.15

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name Zactima
    Novel drug target Established target
    combination therapy Vandetanib + Temozolomide

    PMIDs:
    18681783 14990633 16467544 16377102 14990632 18784101 25910950 16257339 18003960 23022519 11255078 19339720 18316547 12648464 22594511


    Sources:
    ClearityFoundationBiomarkers ClearityFoundationClinicalTrial MyCancerGenomeClinicalTrial PharmGKB JAX-CKB TdgClinicalTrial TTD DrugBank TALC MyCancerGenome GuideToPharmacology ChemblInteractions

  • NIVOLUMAB   EGFR

    Interaction Score: 0.15

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type non-small cell lung carcinoma
    Response Type decreased response
    Approval Status Clinical Study

    PMIDs:
    31086949 27225694 28407039


    Sources:
    FDA PharmGKB JAX-CKB CIViC

  • ATEZOLIZUMAB   EGFR

    Interaction Score: 0.14

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type non-small cell lung carcinoma
    Response Type decreased response
    Approval Status Clinical Study

    PMIDs:
    31086949 27225694


    Sources:
    FDA PharmGKB JAX-CKB CIViC

  • PACRITINIB   EGFR

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    32226941


    Sources:
    CIViC

  • SONIDEGIB   EGFR

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Gefitinib + Sonidegib
    Response Type no benefit
    Evidence Type Actionable

    PMIDs:
    26124204


    Sources:
    JAX-CKB

  • YUANHUADINE   EGFR

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21916433


    Sources:
    DTC

  • DIMETHYLCURCUMIN   EGFR

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25753330


    Sources:
    DTC

  • TYRPHOSTIN AG-1478   EGFR

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21718029


    Sources:
    DTC

  • CHEMBL219557   EGFR

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • AFATINIB DIMALEATE   EGFR

    Interaction Score: 0.1

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Epidermal growth factor receptor erbB1 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • CANERTINIB DIHYDROCHLORIDE   EGFR

    Interaction Score: 0.1

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Epidermal growth factor receptor erbB1 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • ABIVERTINIB   EGFR

    Interaction Score: 0.1

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Details of the Assay for Interaction In a biochemical assay.
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • CHEMBL1765740   EGFR

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy GSK2334470 + Osimertinib
    Indication/Tumor Type lung cancer
    Response Type sensitive

    PMIDs:
    28416483


    Sources:
    JAX-CKB

  • RAMUCIRUMAB   EGFR

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    FDA PharmGKB

  • CRIZOTINIB   EGFR

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy CO1686 + Crizotinib
    Indication/Tumor Type non-small cell lung carcinoma
    Indication/Tumor Type lung adenocarcinoma

    PMIDs:
    27595477 27393507 27283993 21791641


    Sources:
    JAX-CKB CIViC

  • PF-00477736   EGFR

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy PF3644022 + PF-477736
    Indication/Tumor Type Advanced Solid Tumor
    Response Type no benefit

    PMIDs:
    26140595


    Sources:
    JAX-CKB

  • PEMBROLIZUMAB   EGFR

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type non-small cell lung carcinoma
    Response Type decreased response
    Approval Status Clinical Study

    PMIDs:
    31086949 27225694


    Sources:
    FDA PharmGKB JAX-CKB CIViC

  • TUCATINIB   EGFR

    Interaction Score: 0.08

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Details of the Assay for Interaction Inhibition of enzyme activity in a biochemical assay.
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • CEP-32496   EGFR

    Interaction Score: 0.08

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Epidermal growth factor receptor erbB1 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • OSIMERTINIB MESYLATE   EGFR

    Interaction Score: 0.08

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Epidermal growth factor receptor inhibitor

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • LINSITINIB   EGFR

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Gefitinib + Linsitinib
    Indication/Tumor Type glioblastoma multiforme
    Response Type sensitive

    PMIDs:
    26561558


    Sources:
    JAX-CKB

  • CHEMBL29197   EGFR

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20095624


    Sources:
    DTC

  • CHEMBL1951415   EGFR

    Interaction Score: 0.08

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction? False
    Endogenous Drug? False
    Specific Action of the Ligand Inhibition

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • ENCORAFENIB   EGFR

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Cetuximab + Encorafenib
    Indication/Tumor Type colorectal cancer
    Response Type resistant

    PMIDs:
    27312529


    Sources:
    JAX-CKB

  • JNJ-26483327   EGFR

    Interaction Score: 0.07

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Epidermal growth factor receptor erbB1 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    TTD ChemblInteractions

  • GANETESPIB   EGFR

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Afatinib + Ganetespib
    combination therapy Erlotinib + Ganetespib
    Indication/Tumor Type non-small cell lung carcinoma

    PMIDs:
    25077897


    Sources:
    JAX-CKB

  • PIMASERTIB   EGFR

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Pimasertib + BEZ235
    Approval Status Preclinical - Cell line xenograft
    combination therapy Pimasertib + Sorafenib

    PMIDs:
    23629727


    Sources:
    JAX-CKB

  • PEMETREXED   EGFR

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    31605797 24636847


    Sources:
    CIViC

  • ZANUBRUTINIB   EGFR

    Interaction Score: 0.06

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    31340982 31381333


    Sources:
    DrugBank

  • ROGARATINIB   EGFR

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • CABOZANTINIB   EGFR

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Evidence Type Actionable
    Approval Status Phase II
    Response Type unknown

    PMIDs:
    27694386 27825638


    Sources:
    JAX-CKB

  • TALAZOPARIB   EGFR

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    31852834


    Sources:
    CIViC

  • SELUMETINIB   EGFR

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Osimertinib + Selumetinib
    Indication/Tumor Type lung adenocarcinoma
    Approval Status Preclinical

    PMIDs:
    24939055 25870145 27287717 28416483 27312529


    Sources:
    JAX-CKB

  • LIDOCAINE   EGFR

    Interaction Score: 0.05

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name PSD502, lidocaine + prilocaine
    Novel drug target Established target

    PMIDs:
    16551906


    Sources:
    TdgClinicalTrial DrugBank

  • DECITABINE   EGFR

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Evidence Type Actionable
    Approval Status Preclinical
    Response Type sensitive

    PMIDs:
    24874286


    Sources:
    JAX-CKB

  • BMS-754807   EGFR

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy BMS-754807 + Dacomitinib
    Indication/Tumor Type glioblastoma multiforme
    Response Type sensitive

    PMIDs:
    26561558


    Sources:
    JAX-CKB

  • SARACATINIB   EGFR

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Evidence Type Actionable
    Approval Status Preclinical - Cell culture
    Response Type sensitive

    PMIDs:
    28416483


    Sources:
    JAX-CKB

  • ERDAFITINIB   EGFR

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type lung cancer
    Response Type resistant
    Approval Status Preclinical - Cell culture

    PMIDs:
    28341788


    Sources:
    JAX-CKB

  • TEMOZOLOMIDE   EGFR

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy ABT-414 + Temozolomide + Radiotherapy
    Indication/Tumor Type glioblastoma multiforme
    Response Type predicted – sensitive

    PMIDs:
    25910950 26846818


    Sources:
    JAX-CKB

  • SIROLIMUS   EGFR

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Alteration EGFR:P753S
    Drug family EGFR mAb inhibitor;MTOR inhibitor
    combination therapy Cetuximab;Sirolimus

    PMIDs:
    24934779 24813888 25157968 18089823


    Sources:
    DoCM JAX-CKB CIViC CGI

  • CARBOPLATIN   EGFR

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22370314 20573926 19692680 22581822 21783417 22285168 21900837 22139083 20022809


    Sources:
    PharmGKB CIViC

  • GEDATOLISIB   EGFR

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Gedatolisib + Neratinib
    Indication/Tumor Type non-small cell lung carcinoma
    Response Type sensitive

    PMIDs:
    16731747 19238632 21325073


    Sources:
    JAX-CKB

  • GELDANAMYCIN   EGFR

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    18652519


    Sources:
    PharmGKB

  • TEMSIROLIMUS   EGFR

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Response Type no benefit
    combination therapy Temsirolimus + Erlotinib
    Indication/Tumor Type malignant glioma

    PMIDs:
    24470557


    Sources:
    JAX-CKB

  • PLUMBAGIN   EGFR

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24355130


    Sources:
    DTC

  • IBRUTINIB   EGFR

    Interaction Score: 0.04

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    24915291


    Sources:
    DTC GuideToPharmacology

  • PACLITAXEL   EGFR

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Sapitinib + Paclitaxel
    Indication/Tumor Type inflammatory breast carcinoma
    Response Type sensitive

    PMIDs:
    24886365 22370314 20573926 19692680 22581822 21783417 22285168 21900837 22139083 20022809


    Sources:
    PharmGKB JAX-CKB CIViC

  • GLESATINIB   EGFR

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy MGCD265 + Erlotinib
    Indication/Tumor Type non-small cell lung carcinoma
    Response Type predicted – sensitive

    PMIDs:
    None found


    Sources:
    JAX-CKB

  • MK-2206   EGFR

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Erlotinib + MK2206
    Indication/Tumor Type non-small cell lung carcinoma
    Response Type sensitive

    PMIDs:
    26106072


    Sources:
    JAX-CKB

  • TRAMETINIB   EGFR

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Approval Status Preclinical - Cell line xenograft
    Indication/Tumor Type collecting duct carcinoma
    Approval Status Preclinical - Pdx

    PMIDs:
    28783719 26036643 26582713 27312529


    Sources:
    JAX-CKB

  • AMLEXANOX   EGFR

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Amlexanox + Selumetinib
    Indication/Tumor Type non-small cell lung carcinoma
    Response Type sensitive

    PMIDs:
    27287717


    Sources:
    JAX-CKB

  • CEP-11981   EGFR

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22148921


    Sources:
    DTC

  • REGORAFENIB   EGFR

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Pimasertib + Regorafenib
    Indication/Tumor Type non-small cell lung carcinoma
    Response Type sensitive

    PMIDs:
    23629727


    Sources:
    PharmGKB JAX-CKB

  • ORANTINIB   EGFR

    Interaction Score: 0.03

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction? False
    Endogenous Drug? False
    Specific Action of the Ligand Inhibition

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • NITROGLYCERIN   EGFR

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • PUQUITINIB   EGFR

    Interaction Score: 0.03

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Epidermal growth factor receptor erbB1 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • ALVOCIDIB   EGFR

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    11752352


    Sources:
    DrugBank

  • BOSUTINIB   EGFR

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Osimertinib + Bosutinib + PF-573328
    Indication/Tumor Type lung cancer
    Response Type sensitive

    PMIDs:
    28416483


    Sources:
    JAX-CKB

  • DABRAFENIB   EGFR

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Trametinib + Dabrafenib
    Indication/Tumor Type colorectal cancer
    Response Type resistant

    PMIDs:
    27312529


    Sources:
    JAX-CKB

  • BUPARLISIB   EGFR

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy BKM120 + Osimertinib
    Indication/Tumor Type lung cancer
    Response Type sensitive

    PMIDs:
    28416483


    Sources:
    JAX-CKB

  • TRASTUZUMAB   EGFR

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    11752352


    Sources:
    TEND

  • SORAFENIB   EGFR

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Pimasertib + Sorafenib
    Approval Status Preclinical - Cell line xenograft
    Indication/Tumor Type non-small cell lung carcinoma

    PMIDs:
    23629727 26743856 26318998 24166906


    Sources:
    DTC JAX-CKB TTD

  • VATALANIB   EGFR

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • LEUCOVORIN   EGFR

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22486600


    Sources:
    PharmGKB

  • ACALABRUTINIB   EGFR

    Interaction Score: 0.02

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction? False
    Endogenous Drug? False
    Specific Action of the Ligand Inhibition

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • PONATINIB   EGFR

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type non-small cell lung carcinoma
    Response Type resistant
    Approval Status Preclinical

    PMIDs:
    22238366


    Sources:
    JAX-CKB

  • DACTOLISIB   EGFR

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Pimasertib + BEZ235
    Indication/Tumor Type non-small cell lung carcinoma
    Response Type sensitive

    PMIDs:
    23629727 24939055


    Sources:
    JAX-CKB

  • VEMURAFENIB   EGFR

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Vemurafenib + Gefitinib
    combination therapy Vemurafenib + Panitumumab
    Response Type sensitive

    PMIDs:
    27312529


    Sources:
    JAX-CKB

  • RIBAVIRIN   EGFR

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    28703131


    Sources:
    PharmGKB

  • IMATINIB   EGFR

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Evidence Type Actionable
    Approval Status Preclinical
    Response Type sensitive

    PMIDs:
    28762371 22323597


    Sources:
    PharmGKB JAX-CKB

  • SB-202190   EGFR

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22951114


    Sources:
    DTC

  • IRINOTECAN   EGFR

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Irinotecan + Nimotuzumab
    Indication/Tumor Type stomach cancer
    Response Type predicted – sensitive

    PMIDs:
    23209031 25185971


    Sources:
    JAX-CKB

  • BEVACIZUMAB   EGFR

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Bevacizumab + Erlotinib
    Indication/Tumor Type lung adenocarcinoma
    Response Type sensitive

    PMIDs:
    28408243


    Sources:
    JAX-CKB

  • EVEROLIMUS   EGFR

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Everolimus + Pimasertib
    Indication/Tumor Type non-small cell lung carcinoma
    Response Type sensitive

    PMIDs:
    23629727


    Sources:
    JAX-CKB

  • SUNITINIB   EGFR

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Cetuximab + Sunitinib
    Indication/Tumor Type olfactory neuroblastoma
    Response Type sensitive

    PMIDs:
    27149458


    Sources:
    JAX-CKB

  • DORAMAPIMOD   EGFR

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • AZD-1152-HQPA   EGFR

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • TAK-715   EGFR

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • ETOPOSIDE   EGFR

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type neuroblastoma
    Response Type resistant
    Approval Status Preclinical - Cell culture

    PMIDs:
    27216155


    Sources:
    JAX-CKB

  • MLN-8054   EGFR

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • GEMCITABINE   EGFR

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21783417 22285168


    Sources:
    PharmGKB

  • DOCETAXEL   EGFR

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21783417 22285168


    Sources:
    PharmGKB

  • CURCUMIN   EGFR

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25753330


    Sources:
    DTC

  • CISPLATIN   EGFR

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy ER2 + Cisplatin
    Indication/Tumor Type non-small cell lung carcinoma
    Response Type sensitive

    PMIDs:
    23764753 27040853


    Sources:
    JAX-CKB CIViC

  • GW843682X   EGFR

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DASATINIB   EGFR

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Dasatinib + Osimertinib
    Indication/Tumor Type lung cancer
    Response Type sensitive

    PMIDs:
    28416483


    Sources:
    JAX-CKB

  • ALISERTIB   EGFR

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • GO-6976   EGFR

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • PD-0166285   EGFR

    Interaction Score: 0.01

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Epidermal growth factor receptor erbB1 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • FLUOROURACIL   EGFR

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23816762


    Sources:
    PharmGKB

  • STAUROSPORINE   EGFR

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • SOTRASTAURIN   EGFR

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • ALCOHOL   EGFR

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10092515


    Sources:
    NCI

  • TOZASERTIB   EGFR

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • R-406   EGFR

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • RG-1530   EGFR

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DOVITINIB   EGFR

    Interaction Score: 0.0

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • CYC-116   EGFR

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • TAE-684   EGFR

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • ILORASERTIB   EGFR

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CENISERTIB   EGFR

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • FOSTAMATINIB   EGFR

    Interaction Score: 0.0

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    26516587


    Sources:
    DrugBank

  • Ensembl: ENSG00000146648

    • Version: 101_38

    Alternate Names:
    EGFR Ensembl Gene Name

    Gene Info:
    Gene Biotype PROTEIN_CODING

    Publications:

  • TdgClinicalTrial: P00533

    • Version: January-2014

    Alternate Names:
    EGFR Gene Symbol

    Gene Info:
    Target Class Receptors
    Target Subclass EC:2.7.10.1

    Publications:

  • CancerCommons: EGFR

    • Version: 25-July-2013

    Alternate Names:
    1956 Entrez Gene ID

    Gene Info:
    CancerCommons Reported Gene Name EGFR

    Publications:

  • TEND: P00533

    • Version: 01-August-2011

    Alternate Names:
    EGFR_HUMAN Uniprot Id
    ENSG00000146648 Ensembl Gene Id
    P00533 Uniprot Accession

    Gene Info:
    Target Subclass Kinase
    Target Main Class Receptors
    Transmembrane Helix Count 1

    Publications:

  • RussLampel: ENSG00000146648

    • Version: 26-July-2011

    Alternate Names:
    EGFR Display Id
    ENSG00000146648 Ensembl Gene Id
    EPIDERMAL GROWTH FACTOR RECEPTOR PRECURSOR (EC 2.7.1.112) (RECEPTOR TYROSINE-PROTEIN KINASE ERBB-1). [SOURCE:UNIPROT/SWISSPROT;ACC:P00533] Description

    Gene Info:
    Human Readable Name DRUGGABLE GENOME

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • BaderLabGenes: EGFR

    • Version: February-2014

    Alternate Names:
    1956 Entrez Gene ID

    Gene Info:
    Initial Gene Query EGFR
    Counted Citations from 1950-2000 12181

    Gene Categories:
    KINASE

    Publications:

  • HopkinsGroom: P00533

    • Version: 11-September-2012

    Alternate Names:
    P00533 Uniprot Accession
    1956 Entrez Gene Id
    EGFR Uniprot Gene Name

    Gene Info:
    Interpro Type Domain
    Interpro Acc IPR001245
    Human Readable Name DRUGGABLE GENOME

    Gene Categories:
    KINASE, DRUGGABLE GENOME

    Publications:

  • GuideToPharmacology: 1956

    • Version: 29-September-2020

    Alternate Names:
    3236 HUGO Gene ID
    3236 HUGO Gene Symbol
    epidermal growth factor receptor HUGO Gene Name

    Gene Info:
    GuideToPharmacology Gene Category Name Type I RTKs: ErbB (epidermal growth factor) receptor family
    GuideToPharmacology Gene Category ID 320

    Publications:

  • JAX-CKB: EGFR

    • Version: 27-September-2017

    Alternate Names:
    1956 CKB Entrez Id
    EGFR CKB Gene Synonym
    ERBB CKB Gene Synonym

    Gene Info:

    Publications:
    Yao et al., 2017, Tumours with class 3 BRAF mutants are sensitive to the inhibition of activated RAS., Nature
    Gainor et al., 2016, EGFR Mutations and ALK Rearrangements Are Associated with Low Response Rates to PD-1 Pathway Blockade in Non-Small Cell Lung Cancer: A Retrospective Analysis., Clin. Cancer Res.
    Suzuki et al., 2007, Pharmacological characterization of MP-412 (AV-412), a dual epidermal growth factor receptor and ErbB2 tyrosine kinase inhibitor., Cancer Sci.

  • PharmGKB: EGFR

    • Version: 18-August-2020

    Alternate Names:
    PA7360 PharmGKB ID

    Gene Info:

    Publications:
    Funke S et al., 2008, Pharmacogenetics in colorectal cancer: a systematic review., Pharmacogenomics
    Liu G et al., 2008, Epidermal growth factor receptor polymorphisms and clinical outcomes in non-small-cell lung cancer patients treated with gefitinib., Pharmacogenomics J
    Han et al., 2012, First-SIGNAL: first-line single-agent iressa versus gemcitabine and cisplatin trial in never-smokers with adenocarcinoma of the lung., J. Clin. Oncol.

  • CIViC: EGFR

    • Version: 14-September-2020

    Alternate Names:
    1956 Entrez Gene ID
    19 CIViC Gene ID

    Gene Info:

    Gene Categories:
    DRUG RESISTANCE, CLINICALLY ACTIONABLE

    Publications:
    Yun et al., 2008, The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP., Proc. Natl. Acad. Sci. U.S.A.
    Kancha et al., 2009, Functional analysis of epidermal growth factor receptor (EGFR) mutations and potential implications for EGFR targeted therapy., Clin. Cancer Res.
    Walter et al., 2013, Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC., Cancer Discov

  • DrugBank: BE0000767

    • Version: 5.1.7

    Alternate Names:
    EGFR DrugBank Gene Name
    P00533 UniProt Accession
    1956 Entrez Gene Id

    Gene Info:

    Publications:
    Sakaguchi et al., 2006, The antiproliferative effect of lidocaine on human tongue cancer cells with inhibition of the activity of epidermal growth factor receptor., Anesth. Analg.
    Ciardiello et al., 2000, Antitumor effect and potentiation of cytotoxic drugs activity in human cancer cells by ZD-1839 (Iressa), an epidermal growth factor receptor-selective tyrosine kinase inhibitor., Clin. Cancer Res.
    Albanell et al., 2001, Activated extracellular signal-regulated kinases: association with epidermal growth factor receptor/transforming growth factor alpha expression in head and neck squamous carcinoma and inhibition by anti-epidermal growth factor receptor treatments., Cancer Res.

  • TTD: Epidermal growth factor receptor

    • Version: 2020.06.01

    Alternate Names:
    EGFR TTD Gene Abbreviation
    T59328 TTD Target ID

    Gene Info:

    Publications:
    Klinguer-Hamour C et al., 2014, World Antibody-Drug Conjugate Summit, October 15-16, 2013, San Francisco, CA., MAbs
    Newman DJ et al., 2014, Marine-sourced anti-cancer and cancer pain control agents in clinical and late preclinical development., Mar Drugs

  • CGI: EGFR

    • Version: 27-September-2017

    Alternate Names:

    Gene Info:

    Publications:
    Braig et al., 2015, Epidermal growth factor receptor mutation mediates cross-resistance to panitumumab and cetuximab in gastrointestinal cancer., Oncotarget
    Arena et al., 2015, Emergence of Multiple EGFR Extracellular Mutations during Cetuximab Treatment in Colorectal Cancer., Clin. Cancer Res.
    Sánchez-Martín et al., 2016, The First-in-class Anti-EGFR Antibody Mixture Sym004 Overcomes Cetuximab Resistance Mediated by EGFR Extracellular Domain Mutations in Colorectal Cancer., Clin. Cancer Res.

  • NCI: EGFR

    • Version: 14-September-2017

    Alternate Names:

    Gene Info:

    Publications:
    Zhang et al., 1999, Chronic ethanol consumption disrupts complexation between EGF receptor and phospholipase C-gamma1: relevance to impaired hepatocyte proliferation., Biochem. Biophys. Res. Commun.

  • DoCM: EGFR

    • Version: 27-September-2017

    Alternate Names:

    Gene Info:

    Publications:
    Chang et al., 2016, Identifying recurrent mutations in cancer reveals widespread lineage diversity and mutational specificity., Nat. Biotechnol.
    Rajasekaran et al., 2010, In silico identification of significant detrimental missense mutations of EGFR and their effect with 4-anilinoquinazoline-based drugs., Appl. Biochem. Biotechnol.
    Miller et al., 2012, 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., Lancet Oncol.

  • DTC: EGFR

    • Version: 02-September-2020

    Alternate Names:

    Gene Info:

    Publications:
    Rateb ME et al., 2009, Bioactive diterpene derivatives from the marine sponge Spongionella sp., J Nat Prod
    Ban HS et al., 2010, Enhancement of EGFR tyrosine kinase inhibition by C-C multiple bonds-containing anilinoquinazolines., Bioorg Med Chem
    Blair JA et al., 2007, Structure-guided development of affinity probes for tyrosine kinases using chemical genetics., Nat Chem Biol

  • TALC: HER1

    • Version: 12-May-2016

    Alternate Names:
    HER1 Gene Symbol

    Gene Info:

    Publications:

  • TALC: EGFR

    • Version: 12-May-2016

    Alternate Names:
    EGFR Gene Symbol

    Gene Info:

    Publications:

  • HingoraniCasas: ENSG00000146648

    • Version: 31-May-2017

    Alternate Names:
    ENSG00000146648 Gene Symbol
    EGFR Ensembl Id

    Gene Info:

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • MyCancerGenome: EGFR

    • Version: 20-Jun-2017

    Alternate Names:
    1956 Entrez Gene Id
    EGFR MyCancerGenome Gene Symbol
    EGFR (HER1/ERBB1) MyCancerGenome Reported Gene Name

    Gene Info:

    Publications:

  • ChemblInteractions: ERBB

    • Version: chembl_23

    Alternate Names:
    ERBB1 GENE_SYMBOL
    HER1 GENE_SYMBOL
    EGFR GENE_SYMBOL

    Gene Info:

    Publications:

  • OncoKB: EGFR

    • Version: 23-July-2020

    Alternate Names:
    ERBB1 OncoKB Gene Synonym
    1956 OncoKB Entrez Id
    PIG61 OncoKB Gene Synonym

    Gene Info:

    Publications:

  • Pharos: EGFR

    • Version: 03-September-2020

    Alternate Names:
    Epidermal growth factor receptor Gene Name
    P00533 UniProt ID

    Gene Info:

    Gene Categories:
    KINASE

    Publications:

  • GO: EGFR

    • Version: 05-September-2020

    Alternate Names:
    ERBB GO Gene Synonym
    ERBB1 GO Gene Synonym
    HER1 GO Gene Synonym

    Gene Info:

    Gene Categories:
    CELL SURFACE, TYROSINE KINASE

    Publications:

  • Tempus: EGFR

    • Version: 11-November-2018

    Alternate Names:
    EGFR Gene Symbol

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • dGene: EGFR

    • Version: 27-Jun-2013

    Alternate Names:
    1956 Gene ID
    ERBB dGene Synonym
    ERBB1 dGene Synonym

    Gene Info:

    Gene Categories:
    KINASE, TYROSINE KINASE

    Publications:

  • ClearityFoundationBiomarkers: EGFR

    • Version: 26-July-2013

    Alternate Names:

    Gene Info:

    Publications:

  • MyCancerGenomeClinicalTrial: EGFR

    • Version: 30-February-2014

    Alternate Names:

    Gene Info:

    Publications:

  • ClearityFoundationClinicalTrial: EGFR

    • Version: 15-June-2013

    Alternate Names:

    Gene Info:

    Publications:

  • MskImpact: EGFR

    • Version: May-2015

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • FoundationOneGenes: EGFR

    • Version: 03-September-2020

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • CarisMolecularIntelligence: EGFR

    • Version: 04-September-2020

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • FDA: EGFR

    • Version: 04-September-2020

    Alternate Names:

    Gene Info:

    Publications:

  • Oncomine: EGFR

    • Version: v3

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • COSMIC: EGFR

    • Version: 4-Sep-2020

    Alternate Names:

    Gene Info:

    Gene Categories:
    DRUG RESISTANCE

    Publications:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

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DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21