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
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
Yasuda et al., 2012, EGFR exon 20 insertion mutations in non-small-cell lung cancer: preclinical data and clinical implications., Lancet Oncol.
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.
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.
Ma et al., 2016, InsR/IGF1R Pathway Mediates Resistance to EGFR Inhibitors in Glioblastoma., Clin. Cancer Res.
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.
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.
Kosaka et al., 2017, Response Heterogeneity of EGFR and HER2 Exon 20 Insertions to Covalent EGFR and HER2 Inhibitors., Cancer Res.
Gerber et al., 2014, Management and future directions in non-small cell lung cancer with known activating mutations., Am Soc Clin Oncol Educ Book
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
Sequist et al., 2011, Genotypic and histological evolution of lung cancers acquiring resistance to EGFR inhibitors., Sci Transl Med
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.
Brzezniak C et al., 2013, Dacomitinib, a new therapy for the treatment of non-small cell lung cancer., Expert Opin Pharmacother
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.
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.
Lynch et al., 2002, Therapeutic potential of ABX-EGF: a fully human anti-epidermal growth factor receptor monoclonal antibody for cancer treatment., Semin. Oncol.
Heymach et al., 2006, Epidermal growth factor receptor inhibitors in development for the treatment of non-small cell lung cancer., Clin. Cancer Res.
Yang et al., 2001, Development of ABX-EGF, a fully human anti-EGF receptor monoclonal antibody, for cancer therapy., Crit. Rev. Oncol. Hematol.
Keating, 2010, Panitumumab: a review of its use in metastatic colorectal cancer., Drugs
Wu et al., 2008, Panitumumab: human monoclonal antibody against epidermal growth factor receptors for the treatment of metastatic colorectal cancer., Clin Ther
Jean et al., 2008, Epidermal growth factor receptor monoclonal antibodies for the treatment of metastatic colorectal cancer., Pharmacotherapy
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.
Saadeh et al., 2007, Panitumumab: a fully human monoclonal antibody with activity in metastatic colorectal cancer., Ann Pharmacother
Keating, 2010, Spotlight on panitumumab in metastatic colorectal cancer., BioDrugs
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Segaert et al., 2005, Clinical signs, pathophysiology and management of skin toxicity during therapy with epidermal growth factor receptor inhibitors., Ann. Oncol.
Cohen, 2003, Epidermal growth factor receptor as a therapeutic target in colorectal cancer., Clin Colorectal Cancer
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
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
Mayo C et al., 2012, Pharmacogenetics of EGFR in lung cancer: perspectives and clinical applications., Pharmacogenomics
Van Cutsem et al., 2009, Cetuximab and chemotherapy as initial treatment for metastatic colorectal cancer., N. Engl. J. Med.
Vermorken JB et al., 2008, Platinum-based chemotherapy plus cetuximab in head and neck cancer., N Engl J Med
Funke S et al., 2008, Pharmacogenetics in colorectal cancer: a systematic review., Pharmacogenomics
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
Jonker et al., 2007, Cetuximab for the treatment of colorectal cancer., N. Engl. J. Med.
Bonner JA et al., 2006, Radiotherapy plus cetuximab for squamous-cell carcinoma of the head and neck., N Engl J Med
Normanno N et al., 2006, Epidermal growth factor receptor (EGFR) signaling in cancer., Gene
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
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
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
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.
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.
Arena et al., 2016, MM-151 overcomes acquired resistance to cetuximab and panitumumab in colorectal cancers harboring EGFR extracellular domain mutations., Sci Transl Med
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.
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.
Uchibori et al., 2017, Brigatinib combined with anti-EGFR antibody overcomes osimertinib resistance in EGFR-mutated non-small-cell lung cancer., Nat Commun
Strickler JH et al., 2018, Genomic Landscape of Cell-Free DNA in Patients with Colorectal Cancer., Cancer Discov
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
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
Cho SH et al., 2012, Efficacy of EGFR tyrosine kinase inhibitors for non-adenocarcinoma NSCLC patients with EGFR mutation., Cancer Chemother Pharmacol
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
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.
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
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.
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
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
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.
Maemondo et al., 2010, Gefitinib or chemotherapy for non-small-cell lung cancer with mutated EGFR., N. Engl. J. Med.
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.
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.
Mok et al., 2009, Gefitinib or carboplatin-paclitaxel in pulmonary adenocarcinoma., N. Engl. J. Med.
Onitsuka T et al., 2010, Acquired resistance to gefitinib: the contribution of mechanisms other than the T790M, MET, and HGF status., Lung 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
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
Ma F et al., 2009, Polymorphisms of EGFR predict clinical outcome in advanced non-small-cell lung cancer patients treated with Gefitinib., Lung Cancer
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
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
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
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
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
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
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
Sequist et al., 2007, Response to treatment and survival of patients with non-small cell lung cancer undergoing somatic EGFR mutation testing., 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
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.
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
Han SW et al., 2006, Clinical predictors versus epidermal growth factor receptor mutation in gefitinib-treated non-small-cell lung cancer patients., Lung Cancer
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.
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
Bell et al., 2005, Inherited susceptibility to lung cancer may be associated with the T790M drug resistance mutation in EGFR., Nat. Genet.
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
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
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.
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.
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.
Ban HS et al., 2010, Enhancement of EGFR tyrosine kinase inhibition by C-C multiple bonds-containing anilinoquinazolines., Bioorg Med Chem
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
Carmi C et al., 2010, Novel irreversible epidermal growth factor receptor inhibitors by chemical modulation of the cysteine-trap portion., J Med Chem
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
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.
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.
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
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.
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.
Mellinghoff et al., 2005, Molecular determinants of the response of glioblastomas to EGFR kinase inhibitors., N. Engl. J. Med.
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.
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
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.
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.
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.
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
Belchis et al., 2016, Heterogeneity of resistance mutations detectable by nextgeneration sequencing in TKI-treated lung adenocarcinoma., Oncotarget
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.
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.
Kobayashi et al., 2005, EGFR mutation and resistance of non-small-cell lung cancer to gefitinib., N. Engl. J. Med.
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.
Paez et al., 2004, EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy., Science
Fukihara et al., 2014, Clinical predictors of response to EGFR tyrosine kinase inhibitors in patients with EGFR-mutant non-small cell lung cancer., Oncology
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
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.
Engelman et al., 2007, MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling., Science
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
Niu et al., 2014, Novel agents and strategies for overcoming EGFR TKIs resistance., Exp Hematol Oncol
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.
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.
Ma et al., 2011, T790M and acquired resistance of EGFR TKI: a literature review of clinical reports., J Thorac Dis
Koole et al., 2016, FGFR1 Is a Potential Prognostic Biomarker and Therapeutic Target in Head and Neck Squamous Cell Carcinoma., Clin. 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.
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.
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.
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.
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
Peters et al., 2012, Metastatic non-small-cell lung cancer (NSCLC): ESMO Clinical Practice Guidelines for diagnosis, treatment and follow-up., Ann. Oncol.
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.
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
Foster et al., 2010, Clinical implications of novel activating EGFR mutations in malignant peritoneal mesothelioma., World J Surg Oncol
Ercan et al., 2015, EGFR Mutations and Resistance to Irreversible Pyrimidine-Based EGFR Inhibitors., Clin. Cancer Res.
Costa et al., 2008, Effects of erlotinib in EGFR mutated non-small cell lung cancers with resistance to gefitinib., 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
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.
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.
Okada-Iwasaki et al., 2016, The Discovery and Characterization of K-756, a Novel Wnt/β-Catenin Pathway Inhibitor Targeting Tankyrase., Mol. Cancer Ther.
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.
Kim et al., 2015, Differential Effects of Tyrosine Kinase Inhibitors on Normal and Oncogenic EGFR Signaling and Downstream Effectors., Mol. Cancer Res.
Lou et al., 2014, Combination of gefitinib and DNA methylation inhibitor decitabine exerts synergistic anti-cancer activity in colon cancer cells., PLoS ONE
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.
Udager et al., 2015, High-Frequency Targetable EGFR Mutations in Sinonasal Squamous Cell Carcinomas Arising from Inverted Sinonasal Papilloma., Cancer Res.
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
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.
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.
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.
Arteaga et al., 2001, Tyrosine kinase inhibitors-ZD1839 (Iressa)., Curr Opin Oncol
Nicholson et al., 2001, Modulation of epidermal growth factor receptor in endocrine-resistant, oestrogen receptor-positive breast cancer., Endocr. Relat. Cancer
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
Lewis et al., 2012, A phase II study of gefitinib for aggressive cutaneous squamous cell carcinoma of the head and neck., Clin. Cancer Res.
Geoerger B et al., 2008, EGFR tyrosine kinase inhibition radiosensitizes and induces apoptosis in malignant glioma and childhood ependymoma xenografts., Int J Cancer
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
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
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
Liao BC et al., 2015, Second and third-generation epidermal growth factor receptor tyrosine kinase inhibitors in advanced nonsmall cell lung cancer., Curr Opin Oncol
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.
Shi et al., 2013, Icotinib versus gefitinib in previously treated advanced non-small-cell lung cancer (ICOGEN): a randomised, double-blind phase 3 non-inferiority trial., Lancet Oncol.
Rosell et al., 2012, Erlotinib versus standard chemotherapy as first-line treatment for European patients with advanced EGFR mutation-positive non-small-cell lung cancer (EURTAC): a multicentre, open-label, randomised phase 3 trial., Lancet Oncol.
Sequist et al., 2013, Phase III study of afatinib or cisplatin plus pemetrexed in patients with metastatic lung adenocarcinoma with EGFR mutations., J. Clin. Oncol.
Fukuoka et al., 2011, Biomarker analyses and final overall survival results from a phase III, randomized, open-label, first-line study of gefitinib versus carboplatin/paclitaxel in clinically selected patients with advanced non-small-cell lung cancer in Asia (IPASS)., J. Clin. Oncol.
Kosaka et al., 2009, Prognostic implication of EGFR, KRAS, and TP53 gene mutations in a large cohort of Japanese patients with surgically treated lung adenocarcinoma., J Thorac Oncol
Marks et al., 2008, Prognostic and therapeutic implications of EGFR and KRAS mutations in resected lung adenocarcinoma., J Thorac Oncol
Yang et al., 2012, Afatinib for patients with lung adenocarcinoma and epidermal growth factor receptor mutations (LUX-Lung 2): a phase 2 trial., Lancet Oncol.
Rosell et al., 2009, Screening for epidermal growth factor receptor mutations in lung cancer., N. Engl. J. Med.
Zhou et al., 2011, Erlotinib versus chemotherapy as first-line treatment for patients with advanced EGFR mutation-positive non-small-cell lung cancer (OPTIMAL, CTONG-0802): a multicentre, open-label, randomised, phase 3 study., Lancet Oncol.
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.
Mulloy et al., 2007, Epidermal growth factor receptor mutants from human lung cancers exhibit enhanced catalytic activity and increased sensitivity to gefitinib., Cancer Res.
Walter et al., 2013, Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC., Cancer Discov
Zhou et al., 2009, Novel mutant-selective EGFR kinase inhibitors against EGFR T790M., Nature
Jänne et al., 2015, AZD9291 in EGFR inhibitor-resistant non-small-cell lung cancer., N. Engl. J. Med.
Hirano et al., 2015, In vitro modeling to determine mutation specificity of EGFR tyrosine kinase inhibitors against clinically relevant EGFR mutants in non-small-cell lung cancer., Oncotarget
Ding et al., 2014, The predictive role of pretreatment epidermal growth factor receptor T790M mutation on the progression-free survival of tyrosine-kinase inhibitor-treated non-small cell lung cancer patients: a meta-analysis., Onco Targets 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
Katakami et al., 2013, LUX-Lung 4: a phase II trial of afatinib in patients with advanced non-small-cell lung cancer who progressed during prior treatment with erlotinib, gefitinib, or both., J. Clin. Oncol.
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.
Cross et al., 2014, AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer., Cancer Discov
Oxnard et al., 2012, Screening for germline EGFR T790M mutations through lung cancer genotyping., J Thorac Oncol
Sequist et al., 2016, Osimertinib Responses After Disease Progression in Patients Who Had Been Receiving Rociletinib., JAMA Oncol
Li et al., 2014, Primary concomitant EGFR T790M mutation predicted worse prognosis in non-small cell lung cancer patients., Onco Targets Ther
Denis et al., 2015, EGFR T790M resistance mutation in non small-cell lung carcinoma., Clin. Chim. Acta
Sequist et al., 2015, Rociletinib in EGFR-mutated non-small-cell lung cancer., N. Engl. J. Med.
Watanabe et al., 2011, Clinical responses to EGFR-tyrosine kinase inhibitor retreatment in non-small cell lung cancer patients who benefited from prior effective gefitinib therapy: a retrospective analysis., BMC Cancer
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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.
Markham A, 2017, Brigatinib: First Global Approval., Drugs
Iragavarapu C et al., 2015, Novel ALK inhibitors in clinical use and development., J Hematol Oncol
Ceccon M et al., 2013, Crizotinib-resistant NPM-ALK mutants confer differential sensitivity to unrelated Alk inhibitors., Mol Cancer Res
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:
25611025 11255078 23022519 22594511 19339720 18784101 18681783 18316547 18003960 16467544 16377102 16257339 14990633 14990632 12648464 19455431 23948351 20022809 22285168 19692680 23816960 21670455 19096302 18303429 22452895 19692684 20573926 21783417 22452896 17332364 24065731 16258541 15737014 20033049 25923549 26515464 24623981 18227510 16912157 15728811 21531810 24658966 22215752 23816963 20068085 24893891 21430269 22588155 26720284 24729716 25668228 25923550 21194487 24636847 21233402 17653080 19147750 16707764 16043828 18458038 23242437 2302402 23945392 16204070 24894453 16187797 18199554 25157968 22753918 20479403 15118125 15329413 23102728 19922469 15118073 19671738 16115929 15710947 26619011 16011858 26051236 27083334 25589191 24035188 27304188 23982599 24439929 23930994 24565969 27694386 27102076 23991291 25870145 24813888 25077897 26341921 28145866 26862733 22190593 21617858 25589492 25964297 27207775 25559287 27044931 26286086 26206867 23344264 17349580 27913578 25948633 24353160 28363995 26354527 24790411 32226941 32193290

Sources:
TALC DTC DrugBank MyCancerGenome TdgClinicalTrial JAX-CKB CGI DoCM COSMIC CIViC GuideToPharmacology MyCancerGenomeClinicalTrial PharmGKB FDA OncoKB
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:
25939061 28202511 27959700 26729184 26720284 25923549 24893891 27694386 27102076 24410791 27252416 27393507 27216193 27435396 25870145 26286086 28343545 26206867 25948633 28416483 26522274 32193290 31825714 31254668

Sources:
DrugBank MyCancerGenome JAX-CKB ChemblInteractions CGI COSMIC CIViC GuideToPharmacology PharmGKB TTD FDA OncoKB
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:
23930994 21764376 18089823 25456362 25939761 26561558 26206867 27913578 28363995 24857124 28958502 21430269 26768165 23294134 9751783

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

Interaction Score: 1.88

Interaction Types & Directionality:

inhibitor (inhibitory)

antagonist (inhibitory)

Interaction Info:

combination therapy [Rociletinib,HM61713]

Drug family [EGFR inhibitor 3rd gen]

Alteration EGFR:T790M

PMIDs:
26898616

Sources:
DrugBank JAX-CKB ChemblInteractions CGI GuideToPharmacology

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 2394835 25261231 24438614 23372346

Sources:
TALC DrugBank MyCancerGenome JAX-CKB GuideToPharmacology MyCancerGenomeClinicalTrial

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:
TALC DrugBank TdgClinicalTrial ChemblInteractions TTD
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:
DrugBank TdgClinicalTrial CIViC TTD
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:
MyCancerGenome JAX-CKB TTD
NECITUMUMAB EGFR

Interaction Score: 1.26

Interaction Types & Directionality:

antibody (inhibitory)

inhibitor (inhibitory)

antagonist (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:
TALC DrugBank MyCancerGenome TdgClinicalTrial ChemblInteractions GuideToPharmacology TTD
ERLOTINIB EGFR

Interaction Score: 1.05

Interaction Types & Directionality:

inhibitor (inhibitory)

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

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

Sources:
TALC DTC ClearityFoundationBiomarkers DrugBank MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB CGI TEND DoCM COSMIC CIViC GuideToPharmacology CancerCommons PharmGKB TTD FDA OncoKB
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:
DrugBank ChemblInteractions TTD
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:
TALC DrugBank MyCancerGenome JAX-CKB ChemblInteractions GuideToPharmacology TTD
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:
28202511 24065731 25923550

Sources:
MyCancerGenome ChemblInteractions CGI CIViC GuideToPharmacology TTD
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:
TALC MyCancerGenome TdgClinicalTrial JAX-CKB 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:
11255078 23022519 22594511 19339720 18784101 18681783 18316547 18003960 16467544 16377102 16257339 14990633 14990632 12648464 21325073 17085664 25931286 26206867 20479403 25948633

Sources:
TALC DrugBank TdgClinicalTrial JAX-CKB ChemblInteractions GuideToPharmacology PharmGKB TTD
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 ChemblInteractions TTD
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:
TALC DTC MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions GuideToPharmacology TTD
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:
TALC MyCancerGenome JAX-CKB ChemblInteractions GuideToPharmacology
PANITUMUMAB EGFR

Interaction Score: 0.73

Interaction Types & Directionality:

inhibitor (inhibitory)

antibody (inhibitory)

suppressor (inhibitory)

Interaction Info:

Mechanism of Interaction Epidermal growth factor receptor erbB1 inhibitor

Direct Interaction yes

Novel drug target Established target

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

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

Interaction Score: 0.71

Interaction Types & Directionality:

antibody (inhibitory)

inhibitor (inhibitory)

antagonist (inhibitory)

Interaction Info:

Notes

Mechanism of Interaction Epidermal growth factor receptor erbB1 inhibitor

Direct Interaction yes

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

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

Interaction Score: 0.65

Interaction Types & Directionality:

inhibitor (inhibitory)

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Direct Interaction? False

Endogenous Drug? False

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

Sources:
TALC DTC ClearityFoundationBiomarkers DrugBank MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions CGI TEND DoCM COSMIC CIViC GuideToPharmacology MyCancerGenomeClinicalTrial PharmGKB TTD FDA OncoKB
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 23988354 10346932 10592235

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:
26846818 24424355

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:
TALC MyCancerGenome JAX-CKB
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:
DrugBank TdgClinicalTrial ChemblInteractions TTD
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:
12214266 16894399 14751502 20110044 20658522 15374980 11752352 14633707 15163842 14737100 14967461 18803986 18408761 25305330 24355130 23917401 18199554 20215545 27595477 22885469 11255078 23022519 22594511 19339720 18784101 18681783 18316547 18003960 16467544 16377102 16257339 14990633 14990632 12648464

Sources:
TALC DTC DrugBank TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB CGI TEND DoCM CIViC GuideToPharmacology CancerCommons PharmGKB TTD OncoKB
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:
DrugBank TdgClinicalTrial JAX-CKB 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 GuideToPharmacology TTD
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 DrugBank MyCancerGenome CIViC GuideToPharmacology TTD
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:
MyCancerGenome TTD
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:
ChemblInteractions GuideToPharmacology TTD
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:
TALC MyCancerGenome JAX-CKB ChemblInteractions GuideToPharmacology TTD
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:
ChemblInteractions GuideToPharmacology
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:
JAX-CKB ChemblInteractions GuideToPharmacology MyCancerGenomeClinicalTrial OncoKB
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:
TALC MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions GuideToPharmacology
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:
TALC JAX-CKB MyCancerGenomeClinicalTrial
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:
28287083 28597393 25888090 23239810

Sources:
DrugBank ChemblInteractions CIViC GuideToPharmacology
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:
23542356 24165158 26124204

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:
ChemblInteractions GuideToPharmacology TTD
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:
MyCancerGenome JAX-CKB ChemblInteractions GuideToPharmacology
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:
27225694 31086949

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:
TALC TdgClinicalTrial JAX-CKB ChemblInteractions GuideToPharmacology TTD
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:
25910950 11255078 23022519 22594511 19339720 18784101 18681783 18316547 18003960 16467544 16377102 16257339 14990633 14990632 12648464

Sources:
TALC ClearityFoundationBiomarkers DrugBank MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB ChemblInteractions GuideToPharmacology MyCancerGenomeClinicalTrial PharmGKB TTD
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:
27225694 28407039 31086949

Sources:
JAX-CKB CIViC PharmGKB FDA
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:
27225694 31086949

Sources:
JAX-CKB CIViC PharmGKB FDA
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:
PharmGKB FDA
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:
27393507 27283993 27595477 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:
27225694 31086949

Sources:
JAX-CKB CIViC PharmGKB FDA
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:
ChemblInteractions TTD
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:
24636847 31605797

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 28416483 25870145 27287717 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:
DrugBank TdgClinicalTrial
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 18089823 25157968

Sources:
JAX-CKB CGI DoCM CIViC
CARBOPLATIN EGFR

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22581822 22370314 22285168 21900837 21783417 20573926 20022809 19692680 22139083

Sources:
CIViC PharmGKB
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:
21325073 19238632 16731747

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 22581822 22370314 22285168 21900837 21783417 20573926 20022809 19692680 22139083

Sources:
JAX-CKB CIViC PharmGKB
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 27312529 26582713 26036643

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:
JAX-CKB PharmGKB
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 24166906 26318998

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:
24939055 23629727

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:
22323597 28762371

Sources:
JAX-CKB PharmGKB
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:
25185971 23209031

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:
22285168 21783417

Sources:
PharmGKB
DOCETAXEL EGFR

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22285168 21783417

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:

Jorissen RN et al., 2003, Epidermal growth factor receptor: mechanisms of activation and signalling., Exp Cell Res

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

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

CIViC: EGFR

Version: 14-September-2020

Alternate Names:

1956 Entrez Gene ID

19 CIViC Gene ID

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE, DRUG RESISTANCE

Publications:

Kancha et al., 2009, Functional analysis of epidermal growth factor receptor (EGFR) mutations and potential implications for EGFR targeted therapy., Clin. Cancer Res.

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.

Sequist et al., 2015, Rociletinib in EGFR-mutated non-small-cell lung cancer., N. Engl. J. Med.

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.

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.

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids 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:

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.

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.

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:

Lee et al., 2006, Epidermal growth factor receptor activation in glioblastoma through novel missense mutations in the extracellular domain., PLoS Med.

Rosell et al., 2005, Mutations in the tyrosine kinase domain of the EGFR gene associated with gefitinib response in non-small-cell lung cancer., Lung Cancer

Chang et al., 2016, Identifying recurrent mutations in cancer reveals widespread lineage diversity and mutational specificity., Nat. Biotechnol.

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

Smaill JB et al., 1999, Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding site of the epidermal growth factor receptor., J Med Chem

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

Interaction Types & Directionality: inhibitor (inhibitory)

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

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

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

Interaction Types & Directionality: inhibitor (inhibitory)

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

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

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

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

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

PMIDs: 26898616

Sources: DrugBank JAX-CKB ChemblInteractions CGI GuideToPharmacology

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 2394835 25261231 24438614 23372346

Sources: TALC DrugBank MyCancerGenome JAX-CKB GuideToPharmacology MyCancerGenomeClinicalTrial

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

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

PMIDs: 15383606

Sources: TALC DrugBank TdgClinicalTrial ChemblInteractions TTD

Interaction Types & Directionality: n/a

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

PMIDs: 25586468

Sources: DrugBank TdgClinicalTrial CIViC TTD

Interaction Types & Directionality: antibody (inhibitory)

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

PMIDs: 25895099

Sources: MyCancerGenome JAX-CKB TTD

Interaction Types & Directionality: antibody (inhibitory) inhibitor (inhibitory) antagonist (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: TALC DrugBank MyCancerGenome TdgClinicalTrial ChemblInteractions GuideToPharmacology TTD

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

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

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

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: DrugBank ChemblInteractions TTD

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: TALC DrugBank MyCancerGenome JAX-CKB ChemblInteractions GuideToPharmacology TTD

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: 28202511 24065731 25923550

Sources: MyCancerGenome ChemblInteractions CGI CIViC GuideToPharmacology TTD

Interaction Types & Directionality: antibody (inhibitory)

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

PMIDs: 25185971

Sources: TALC MyCancerGenome TdgClinicalTrial JAX-CKB CGI

Interaction Types & Directionality: inhibitor (inhibitory)

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

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

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

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 ChemblInteractions TTD

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: 19821562 21576284

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

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: 24886365 20145185

Sources: TALC MyCancerGenome JAX-CKB ChemblInteractions GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Clinical Status NCCN/ CAP guidelines

Clinical Status early trials

Variant Effect gain-of-function

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

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

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

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

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

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

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

Interaction Types & Directionality:

inhibitor (inhibitory)

antagonist (inhibitory)

Interaction Info:

combination therapy [Rociletinib,HM61713]

Drug family [EGFR inhibitor 3rd gen]

Alteration EGFR:T790M

PMIDs:
26898616

Sources:
DrugBank JAX-CKB ChemblInteractions CGI GuideToPharmacology

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 2394835 25261231 24438614 23372346

Sources:
TALC DrugBank MyCancerGenome JAX-CKB GuideToPharmacology MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

antibody (inhibitory)

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name HuMax-EGFr

Notes

PMIDs:
15383606

Sources:
TALC DrugBank TdgClinicalTrial ChemblInteractions TTD

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name rindopepimut, CDX-110

Novel drug target Established target

PMIDs:
25586468

Sources:
DrugBank TdgClinicalTrial CIViC TTD

Interaction Types & Directionality:

antibody (inhibitory)

Interaction Info:

Evidence Type Actionable

Response Type predicted – sensitive

Indication/Tumor Type Advanced Solid Tumor

PMIDs:
25895099

Sources:
MyCancerGenome JAX-CKB TTD

Interaction Types & Directionality:

antibody (inhibitory)

inhibitor (inhibitory)

antagonist (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:
TALC DrugBank MyCancerGenome TdgClinicalTrial ChemblInteractions GuideToPharmacology TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

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

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:
DrugBank ChemblInteractions TTD

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:
TALC DrugBank MyCancerGenome JAX-CKB ChemblInteractions GuideToPharmacology TTD

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:
28202511 24065731 25923550

Sources:
MyCancerGenome ChemblInteractions CGI CIViC GuideToPharmacology TTD

Interaction Types & Directionality:

antibody (inhibitory)

Interaction Info:

Notes

Novel drug target Established target

Trial Name Nimotuzumab

PMIDs:
25185971

Sources:
TALC MyCancerGenome TdgClinicalTrial JAX-CKB CGI

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

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

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

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 ChemblInteractions TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
19821562 21576284

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

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
24886365 20145185

Sources:
TALC MyCancerGenome JAX-CKB ChemblInteractions GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

antibody (inhibitory)

suppressor (inhibitory)

Interaction Info:

Mechanism of Interaction Epidermal growth factor receptor erbB1 inhibitor

Direct Interaction yes

Novel drug target Established target

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

Interaction Types & Directionality:

antibody (inhibitory)

inhibitor (inhibitory)

antagonist (inhibitory)

Interaction Info:

Notes

Mechanism of Interaction Epidermal growth factor receptor erbB1 inhibitor

Direct Interaction yes

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

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