DGIdb - EGFR Gene Record

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
Pirazzoli et al., 2016, Afatinib plus Cetuximab Delays Resistance Compared to Single-Agent Erlotinib or Afatinib in Mouse Models of TKI-Naïve EGFR L858R-Induced Lung Adenocarcinoma., Clin. Cancer Res.
Wu et al., 2014, Afatinib versus cisplatin plus gemcitabine for first-line treatment of Asian patients with advanced non-small-cell lung cancer harbouring EGFR mutations (LUX-Lung 6): an open-label, randomised phase 3 trial., Lancet Oncol.
Jensen KV et al., 2020, EGFR blockade in GBM brain tumor stem cells synergizes with JAK2/STAT3 pathway inhibition to abrogate compensatory mechanisms in vitro and in vivo., Neurooncol Adv
Cross et al., 2014, AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer., Cancer Discov
Tsai et al., 2015, Synergistic Blockade of EGFR and HER2 by New-Generation EGFR Tyrosine Kinase Inhibitor Enhances Radiation Effect in Bladder Cancer Cells., Mol. Cancer Ther.
Ai et al., 2014, A systematic profile of clinical inhibitors responsive to EGFR somatic amino acid mutations in lung cancer: implication for the molecular mechanism of drug resistance and sensitivity., Amino Acids
Gilmer et al., 2008, Impact of common epidermal growth factor receptor and HER2 variants on receptor activity and inhibition by lapatinib., Cancer Res.
Park et al., 2016, Afatinib versus gefitinib as first-line treatment of patients with EGFR mutation-positive non-small-cell lung cancer (LUX-Lung 7): a phase 2B, open-label, randomised controlled trial., Lancet Oncol.
Mitsudomi et al., 2010, Epidermal growth factor receptor in relation to tumor development: EGFR gene and cancer., FEBS J.
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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:

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

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

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

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

Novel drug target	Established target
Trial Name	HuMax-EGFr
Notes

Trial Name	rindopepimut, CDX-110
Novel drug target	Established target

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

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

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

Direct Interaction?	True
Direct Interaction?	False
Endogenous Drug?	False

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

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

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

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

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

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

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

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

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

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

EGFR Gene Record

EGFR 1956 Druggable GenomeClinically ActionableDrug Resistance

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

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

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

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

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

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

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

Interaction Types & Directionality: n/a

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

PMIDs: 25586468

Sources: TdgClinicalTrial CIViC TTD DrugBank

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

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

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

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

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

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: 22018877

Sources: DTC ChemblInteractions

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

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

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

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

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

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

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

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

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Clinical Status NCCN/ CAP guidelines

Clinical Status early trials

Variant Effect gain-of-function

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

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

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

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

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

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

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name rindopepimut, CDX-110

Novel drug target Established target

PMIDs:
25586468

Sources:
TdgClinicalTrial CIViC TTD DrugBank

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

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

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

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

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Epidermal growth factor receptor erbB1 inhibitor

Direct Interaction yes

PMIDs:
22018877

Sources:
DTC ChemblInteractions

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

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

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

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

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

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

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

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

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

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

Interaction Types & Directionality:

antibody (inhibitory)

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Notes

Mechanism of Interaction Epidermal growth factor receptor erbB1 inhibitor

Direct Interaction yes

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

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

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

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

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

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

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

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

combination therapy	Gefitinib + Sonidegib
Response Type	no benefit
Evidence Type	Actionable

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

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