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CETUXIMAB Drug Record

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  • Interactions
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  • CETUXIMAB chembl:CHEMBL1201577 ApprovedAntineoplastic

    Alternate Names:

    CETUXIMAB
    CMAB009
    MOAB C225
    CETUXIMAB (GENETICAL RECOMBINATION)
    ABP-494
    IMC-225
    C225
    ERBITUX
    CMAB-009
    C-225
    IMC-C225
    ANTI EGFR
    rxcui:318341
    chemidplus:205923-56-4
    chembl:CHEMBL1201577
    drugbank:00002

    Drug Info:

    FDA Approval Colorectal cancer (KRAS wild type), Squamous cell carcinoma of the head and neck
    Drug Class Therapeutic Antibodies
    Year of Approval 2004
    Drug Class antineoplastic agents
    Pharmaceutical Developer Bristol-Myers Squibb
    Source Reported Drug Name(s) Cetuximab
    Drug Class Monoclonal Antibody
    FDA Approval approved
    Drug Indications antineoplastic agent
    (15 More Sources)

    Publications:

    Zhang et al., 2007, FCGR2A and FCGR3A polymorphisms associated with clinical outcome of epidermal growth factor receptor expressing metastatic colorectal cancer patients treated with single-agent cetuximab., J. Clin. Oncol.
    Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
    Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
    Shepshelovich D et al., 2018, Fc-gamma receptor polymorphisms, cetuximab therapy, and overall survival in the CCTG CO.20 trial of metastatic colorectal cancer., Cancer Med
    Magnes T et al., 2018, The influence of FCGR2A and FCGR3A polymorphisms on the survival of patients with recurrent or metastatic squamous cell head and neck cancer treated with cetuximab., Pharmacogenomics J
    Morgen EK et al., 2017, Germline polymorphisms as biomarkers of tumor response in colorectal cancer patients treated with anti-EGFR monoclonal antibodies: a systematic review and meta-analysis., Pharmacogenomics J
    Negri FV et al., 2014, Role of immunoglobulin G fragment C receptor polymorphism-mediated antibody-dependant cellular cytotoxicity in colorectal cancer treated with cetuximab therapy., Pharmacogenomics J
    Brammeld et al., 2017, Genome-wide chemical mutagenesis screens allow unbiased saturation of the cancer genome and identification of drug resistance mutations., Genome Res.
    Van Cutsem et al., 2015, Fluorouracil, leucovorin, and irinotecan plus cetuximab treatment and RAS mutations in colorectal cancer., J. Clin. Oncol.
    Napolitano et al., 2015, Primary and Acquired Resistance of Colorectal Cancer to Anti-EGFR Monoclonal Antibody Can Be Overcome by Combined Treatment of Regorafenib with Cetuximab., Clin. Cancer Res.
    Ciardiello et al., 2016, Cetuximab continuation after first progression in metastatic colorectal cancer (CAPRI-GOIM): a randomized phase II trial of FOLFOX plus cetuximab versus FOLFOX., Ann. Oncol.
    Allegra CJ et al., 2016, Extended RAS Gene Mutation Testing in Metastatic Colorectal Carcinoma to Predict Response to Anti-Epidermal Growth Factor Receptor Monoclonal Antibody Therapy: American Society of Clinical Oncology Provisional Clinical Opinion Update 2015., J Clin Oncol
    Peeters et al., 2013, Massively parallel tumor multigene sequencing to evaluate response to panitumumab in a randomized phase III study of metastatic colorectal cancer., Clin. Cancer Res.
    De Roock et al., 2010, Effects of KRAS, BRAF, NRAS, and PIK3CA mutations on the efficacy of cetuximab plus chemotherapy in chemotherapy-refractory metastatic colorectal cancer: a retrospective consortium analysis., Lancet Oncol.
    Douillard et al., 2013, Panitumumab-FOLFOX4 treatment and RAS mutations in colorectal cancer., N. Engl. J. Med.
    Benson et al., 2017, Colon Cancer, Version 1.2017, NCCN Clinical Practice Guidelines in Oncology., J Natl Compr Canc Netw
    Sartore-Bianchi et al., 2009, PIK3CA mutations in colorectal cancer are associated with clinical resistance to EGFR-targeted monoclonal antibodies., Cancer Res.
    Xu et al., 2017, PIK3CA Mutations Contribute to Acquired Cetuximab Resistance in Patients with Metastatic Colorectal Cancer., Clin. Cancer Res.
    Souglakos J et al., 2009, Prognostic and predictive value of common mutations for treatment response and survival in patients with metastatic colorectal cancer., Br J Cancer
    Swick et al., 2017, Cotargeting mTORC and EGFR Signaling as a Therapeutic Strategy in HNSCC., Mol. Cancer Ther.
    Hong et al., 2016, Targeting the PI3K signaling pathway in KRAS mutant colon cancer., Cancer Med
    de la Rochefordiere et al., 2015, PIK3CA Pathway Mutations Predictive of Poor Response Following Standard Radiochemotherapy ± Cetuximab in Cervical Cancer Patients., Clin. Cancer Res.
    Hechtman et al., 2015, AKT1 E17K in Colorectal Carcinoma Is Associated with BRAF V600E but Not MSI-H Status: A Clinicopathologic Comparison to PIK3CA Helical and Kinase Domain Mutants., Mol. Cancer Res.
    Berger MD et al., 2018, A Polymorphism within the Vitamin D Transporter Gene Predicts Outcome in Metastatic Colorectal Cancer Patients Treated with FOLFIRI/Bevacizumab or FOLFIRI/Cetuximab., Clin Cancer Res
    Jeong et al., 2017, HER2 Amplification and Cetuximab Efficacy in Patients With Metastatic Colorectal Cancer Harboring Wild-type RAS and BRAF., Clin Colorectal Cancer
    Bertotti et al., 2011, A molecularly annotated platform of patient-derived xenografts ("xenopatients") identifies HER2 as an effective therapeutic target in cetuximab-resistant colorectal cancer., Cancer Discov
    Rexer et al., 2013, Human breast cancer cells harboring a gatekeeper T798M mutation in HER2 overexpress EGFR ligands and are sensitive to dual inhibition of EGFR and HER2., Clin. Cancer Res.
    Yonesaka et al., 2011, Activation of ERBB2 signaling causes resistance to the EGFR-directed therapeutic antibody cetuximab., Sci Transl Med
    Kavuri et al., 2015, HER2 activating mutations are targets for colorectal cancer treatment., Cancer Discov
    Leto et al., 2015, Sustained Inhibition of HER3 and EGFR Is Necessary to Induce Regression of HER2-Amplified Gastrointestinal Carcinomas., Clin. Cancer Res.
    De Roock et al., 2011, KRAS, BRAF, PIK3CA, and PTEN mutations: implications for targeted therapies in metastatic colorectal cancer., Lancet Oncol.
    Skowsky et al., A pilot study of chronic recombinant interferon-alfa 2a for diabetic proliferative retinopathy: metabolic effects and opthalmologic effects., J. Diabetes Complicat.
    Nakamura et al., 2016, Afatinib against Esophageal or Head-and-Neck Squamous Cell Carcinoma: Significance of Activating Oncogenic HER4 Mutations in HNSCC., Mol. Cancer Ther.
    De Roock et al., 2010, Association of KRAS p.G13D mutation with outcome in patients with chemotherapy-refractory metastatic colorectal cancer treated with cetuximab., JAMA
    Janssen et al., 1987, RAS gene mutations in acute and chronic myelocytic leukemias, chronic myeloproliferative disorders, and myelodysplastic syndromes., Proc. Natl. Acad. Sci. U.S.A.
    Lee et al., 2011, Effect of simvastatin on cetuximab resistance in human colorectal cancer with KRAS mutations., J. Natl. Cancer Inst.
    Neumann et al., 2009, Frequency and type of KRAS mutations in routine diagnostic analysis of metastatic colorectal cancer., Pathol. Res. Pract.
    Amado et al., 2008, Wild-type KRAS is required for panitumumab efficacy in patients with metastatic colorectal cancer., J. Clin. Oncol.
    Tyner et al., 2009, High-throughput sequencing screen reveals novel, transforming RAS mutations in myeloid leukemia patients., Blood
    Peeters et al., 2013, Mutant KRAS codon 12 and 13 alleles in patients with metastatic colorectal cancer: assessment as prognostic and predictive biomarkers of response to panitumumab., J. Clin. Oncol.
    Haldar et al., 2011, Epidermal growth factor receptor blockers for the treatment of ovarian cancer., Cochrane Database Syst Rev
    Rowland et al., 2016, Meta-analysis comparing the efficacy of anti-EGFR monoclonal antibody therapy between KRAS G13D and other KRAS mutant metastatic colorectal cancer tumours., Eur. J. Cancer
    Nakayama et al., 2008, KRAS or BRAF mutation status is a useful predictor of sensitivity to MEK inhibition in ovarian cancer., Br. J. Cancer
    Ho et al., 2013, Selumetinib-enhanced radioiodine uptake in advanced thyroid cancer., N. Engl. J. Med.
    Tejpar et al., 2012, Association of KRAS G13D tumor mutations with outcome in patients with metastatic colorectal cancer treated with first-line chemotherapy with or without cetuximab., J. Clin. Oncol.
    Bokemeyer et al., 2009, Fluorouracil, leucovorin, and oxaliplatin with and without cetuximab in the first-line treatment of metastatic colorectal cancer., J. Clin. Oncol.
    Lièvre et al., 2006, KRAS mutation status is predictive of response to cetuximab therapy in colorectal cancer., Cancer Res.
    MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
    Bokemeyer et al., 2011, Efficacy according to biomarker status of cetuximab plus FOLFOX-4 as first-line treatment for metastatic colorectal cancer: the OPUS study., Ann. Oncol.
    Schubbert et al., 2007, Hyperactive Ras in developmental disorders and cancer., Nat. Rev. Cancer
    Kloos et al., 2009, Phase II trial of sorafenib in metastatic thyroid cancer., J. Clin. Oncol.
    Schirripa et al., 2015, Phase II study of single-agent cetuximab in KRAS G13D mutant metastatic colorectal cancer., Ann. Oncol.
    Peeters et al., 2010, Randomized phase III study of panitumumab with fluorouracil, leucovorin, and irinotecan (FOLFIRI) compared with FOLFIRI alone as second-line treatment in patients with metastatic colorectal cancer., J. Clin. Oncol.
    Riely et al., 2008, Frequency and distinctive spectrum of KRAS mutations in never smokers with lung adenocarcinoma., Clin. Cancer Res.
    Bacher et al., 2006, Implications of NRAS mutations in AML: a study of 2502 patients., Blood
    Hoftijzer et al., 2009, Beneficial effects of sorafenib on tumor progression, but not on radioiodine uptake, in patients with differentiated thyroid carcinoma., Eur. J. Endocrinol.
    Migliardi et al., 2012, Inhibition of MEK and PI3K/mTOR suppresses tumor growth but does not cause tumor regression in patient-derived xenografts of RAS-mutant colorectal carcinomas., Clin. Cancer Res.
    Rothenberg et al., 2005, Randomized phase II trial of the clinical and biological effects of two dose levels of gefitinib in patients with recurrent colorectal adenocarcinoma., J. Clin. Oncol.
    Osumi et al., 2015, Cetuximab treatment for metastatic colorectal cancer with KRAS p.G13D mutations improves progression-free survival., Mol Clin Oncol
    Sano et al., 2012, RAS mutations are frequent in FAB type M4 and M5 of acute myeloid leukemia, and related to late relapse: a study of the Japanese Childhood AML Cooperative Study Group., Int. J. Hematol.
    Kumar et al., 2014, KRAS G13D Mutation and Sensitivity to Cetuximab or Panitumumab in a Colorectal Cancer Cell Line Model., Gastrointest Cancer Res
    Douillard et al., 2010, Randomized, phase III trial of panitumumab with infusional fluorouracil, leucovorin, and oxaliplatin (FOLFOX4) versus FOLFOX4 alone as first-line treatment in patients with previously untreated metastatic colorectal cancer: the PRIME study., J. Clin. Oncol.
    Brose et al., 2002, BRAF and RAS mutations in human lung cancer and melanoma., Cancer Res.
    Vogelstein et al., 1990, RAS gene mutations in childhood acute myeloid leukemia: a Pediatric Oncology Group study., Genes Chromosomes Cancer
    Janakiraman et al., 2010, Genomic and biological characterization of exon 4 KRAS mutations in human cancer., Cancer Res.
    Parseghian et al., 2017, Dual Inhibition of EGFR and c-Src by Cetuximab and Dasatinib Combined with FOLFOX Chemotherapy in Patients with Metastatic Colorectal Cancer., Clin. Cancer Res.
    Bertino et al., 2016, A Phase I Trial to Evaluate Antibody-Dependent Cellular Cytotoxicity of Cetuximab and Lenalidomide in Advanced Colorectal and Head and Neck Cancer., Mol. Cancer Ther.
    Venook et al., 2017, Effect of First-Line Chemotherapy Combined With Cetuximab or Bevacizumab on Overall Survival in Patients With KRAS Wild-Type Advanced or Metastatic Colorectal Cancer: A Randomized Clinical Trial., JAMA
    Ramos et al., 2008, Understanding the predictive role of K-ras for epidermal growth factor receptor-targeted therapies in colorectal cancer., Clin Colorectal Cancer
    Osumi et al., 2013, Acquired drug resistance conferred by a KRAS gene mutation following the administration of cetuximab: a case report., BMC Res Notes
    Lièvre et al., 2008, KRAS mutations as an independent prognostic factor in patients with advanced colorectal cancer treated with cetuximab., J. Clin. Oncol.
    Pirazzoli et al., 2016, Afatinib plus Cetuximab Delays Resistance Compared to Single-Agent Erlotinib or Afatinib in Mouse Models of TKI-Naïve EGFR L858R-Induced Lung Adenocarcinoma., Clin. Cancer Res.
    Oddo et al., 2016, Molecular Landscape of Acquired Resistance to Targeted Therapy Combinations in BRAF-Mutant Colorectal Cancer., Cancer Res.
    Deming et al., 2016, A phase I study of selumetinib (AZD6244/ARRY-142866), a MEK1/2 inhibitor, in combination with cetuximab in refractory solid tumors and KRAS mutant colorectal cancer., Invest New Drugs
    Sclafani F et al., 2015, Prognostic role of the LCS6 KRAS variant in locally advanced rectal cancer: results of the EXPERT-C trial., Ann Oncol
    Ying HQ et al., 2014, The involvement of Kras gene 3'-UTR polymorphisms in risk of cancer and influence on patient response to anti-EGFR therapy in metastatic colorectal cancer: a meta-analysis., Onco Targets Ther
    Saridaki Z et al., 2014, A let-7 microRNA-binding site polymorphism in KRAS predicts improved outcome in patients with metastatic colorectal cancer treated with salvage cetuximab/panitumumab monotherapy., Clin Cancer Res
    Sha D et al., 2014, Association study of the let-7 miRNA-complementary site variant in the 3' untranslated region of the KRAS gene in stage III colon cancer (NCCTG N0147 Clinical Trial)., Clin Cancer Res
    Sebio A et al., 2013, The LCS6 polymorphism in the binding site of let-7 microRNA to the KRAS 3'-untranslated region: its role in the efficacy of anti-EGFR-based therapy in metastatic colorectal cancer patients., Pharmacogenet Genomics
    Chen J et al., 2013, Association between KRAS codon 13 mutations and clinical response to anti-EGFR treatment in patients with metastatic colorectal cancer: results from a meta-analysis., Cancer Chemother Pharmacol
    Bando H et al., 2012, Clinical outcome of Japanese metastatic colorectal cancer patients harbouring the KRAS p.G13D mutation treated with cetuximab + irinotecan., Jpn J Clin Oncol
    Gajate P et al., 2012, Influence of KRAS p.G13D mutation in patients with metastatic colorectal cancer treated with cetuximab., Clin Colorectal Cancer
    Kaczirek et al., 2015, FOLFOX4 Plus Cetuximab for Patients With Previously Untreated Metastatic Colorectal Cancer According to Tumor RAS and BRAF Mutation Status: Updated Analysis of the CECOG/CORE 1.2.002 Study., Clin Colorectal Cancer
    Loupakis et al., 2009, KRAS codon 61, 146 and BRAF mutations predict resistance to cetuximab plus irinotecan in KRAS codon 12 and 13 wild-type metastatic colorectal cancer., Br. J. Cancer
    Misale et al., 2012, Emergence of KRAS mutations and acquired resistance to anti-EGFR therapy in colorectal cancer., Nature
    Dunn et al., 2011, Dasatinib sensitizes KRAS mutant colorectal tumors to cetuximab., Oncogene
    Karapetis et al., 2008, K-ras mutations and benefit from cetuximab in advanced colorectal cancer., N. Engl. J. Med.
    Sato N et al., 2012, Cetuximab inhibits the growth of mucinous ovarian carcinoma tumor cells lacking KRAS gene mutations., Oncol Rep
    Valtorta E et al., 2013, KRAS gene amplification in colorectal cancer and impact on response to EGFR-targeted therapy., Int J Cancer
    Ahronian et al., 2015, Clinical Acquired Resistance to RAF Inhibitor Combinations in BRAF-Mutant Colorectal Cancer through MAPK Pathway Alterations., Cancer Discov
    French D et al., 2011, KRAS mutation detection in colorectal cancer by a commercially available gene chip array compares well with Sanger sequencing., Clin Chim Acta
    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
    Graziano F et al., 2008, Pharmacogenetic profiling for cetuximab plus irinotecan therapy in patients with refractory advanced colorectal cancer., J Clin Oncol
    Zhang W et al., 2006, Cyclin D1 and epidermal growth factor polymorphisms associated with survival in patients with advanced colorectal cancer treated with Cetuximab., Pharmacogenet Genomics
    Ansell et al., 2016, Epidermal growth factor is a potential biomarker for poor cetuximab response in tongue cancer cells., J. Oral Pathol. Med.
    Neuman et al., 1999, Predictors of sustained response to alpha interferon therapy in chronic hepatitis C., Clin. Biochem.
    Perrotte et al., 1999, Anti-epidermal growth factor receptor antibody C225 inhibits angiogenesis in human transitional cell carcinoma growing orthotopically in nude mice., Clin. Cancer Res.
    Vallböhmer et al., 2005, Molecular determinants of cetuximab efficacy., J. Clin. Oncol.
    Russo et al., 2016, Tumor Heterogeneity and Lesion-Specific Response to Targeted Therapy in Colorectal Cancer., Cancer Discov
    Ganesan et al., 2016, Epidermal Growth Factor Receptor P753S Mutation in Cutaneous Squamous Cell Carcinoma Responsive to Cetuximab-Based Therapy., J. Clin. Oncol.
    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.
    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.
    Jonker et al., 2007, Cetuximab for the treatment of colorectal cancer., N. Engl. J. Med.
    Personeni et al., 2008, Clinical usefulness of EGFR gene copy number as a predictive marker in colorectal cancer patients treated with cetuximab: a fluorescent in situ hybridization study., 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.
    Cho et al., 2014, Colon cancer-derived oncogenic EGFR G724S mutant identified by whole genome sequence analysis is dependent on asymmetric dimerization and sensitive to cetuximab., Mol. Cancer
    Arena et al., 2015, Emergence of Multiple EGFR Extracellular Mutations during Cetuximab Treatment in Colorectal Cancer., Clin. Cancer Res.
    Braig et al., 2015, Epidermal growth factor receptor mutation mediates cross-resistance to panitumumab and cetuximab in gastrointestinal cancer., Oncotarget
    Hosokawa et al., 1999, Effect of thiazinotrienomycin B, an ansamycin antibiotic, on the function of epidermal growth factor receptor in human stomach tumor cells., J. Antibiot.
    Burke et al., 2001, Regulation of epidermal growth factor receptor signaling by endocytosis and intracellular trafficking., Mol. Biol. Cell
    Suwa et al., Epidermal growth factor receptor-dependent cytotoxic effect of anti-EGFR antibody-ribonuclease conjugate on human cancer cells., Anticancer Res.
    Viloria-Petit et al., 2001, Acquired resistance to the antitumor effect of epidermal growth factor receptor-blocking antibodies in vivo: a role for altered tumor angiogenesis., Cancer Res.
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Wakita et al., 1999, Activation of epidermal growth factor receptor promotes late terminal differentiation of cell-matrix interaction-disrupted keratinocytes., J. Biol. Chem.
    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.
    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.
    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.
    Mok et al., 2009, Gefitinib or carboplatin-paclitaxel in pulmonary adenocarcinoma., N. Engl. J. Med.
    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.
    Maemondo et al., 2010, Gefitinib or chemotherapy for non-small-cell lung cancer with mutated EGFR., 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
    Bell et al., 2005, Inherited susceptibility to lung cancer may be associated with the T790M drug resistance mutation in EGFR., Nat. Genet.
    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.
    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
    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.
    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.
    Kobayashi et al., 2005, EGFR mutation and resistance of non-small-cell lung cancer to gefitinib., N. Engl. J. Med.
    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.
    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
    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.
    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
    Sequist et al., 2011, Genotypic and histological evolution of lung cancers acquiring resistance to EGFR inhibitors., Sci Transl Med
    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
    Li et al., 2014, Response to pemetrexed rechallenge after acquired resistance of EGFR-TKI in a patient with advanced NSCLC., Lung Cancer
    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.
    Fu et al., 2008, EGFR mutants found in non-small cell lung cancer show different levels of sensitivity to suppression of Src: implications in targeting therapy., Oncogene
    Kancha et al., 2009, Functional analysis of epidermal growth factor receptor (EGFR) mutations and potential implications for EGFR targeted therapy., Clin. Cancer Res.
    Guo et al., 2006, Gefitinib-sensitizing mutations in esophageal carcinoma., N. Engl. J. Med.
    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.
    Eberhard et al., 2005, Mutations in the epidermal growth factor receptor and in KRAS are predictive and prognostic indicators in patients with non-small-cell lung cancer treated with chemotherapy alone and in combination with erlotinib., J. Clin. Oncol.
    Sequist et al., 2008, First-line gefitinib in patients with advanced non-small-cell lung cancer harboring somatic EGFR mutations., J. Clin. Oncol.
    Kobayashi et al., 2013, Compound EGFR mutations and response to EGFR tyrosine kinase inhibitors., J Thorac Oncol
    Schick et al., 1990, Effects of marine oil-enriched diets on guinea pig megakaryocyte and platelet lipids: effects on thromboxane synthesis and platelet function., Biochim. Biophys. Acta
    Berge et al., 2013, Erlotinib response in an NSCLC patient with a novel compound G719D+L861R mutation in EGFR., J Thorac Oncol
    Jiang et al., 2005, Epidermal growth factor-independent transformation of Ba/F3 cells with cancer-derived epidermal growth factor receptor mutants induces gefitinib-sensitive cell cycle progression., Cancer Res.
    Greulich et al., 2005, Oncogenic transformation by inhibitor-sensitive and -resistant EGFR mutants., PLoS Med.
    Gilmer et al., 2008, Impact of common epidermal growth factor receptor and HER2 variants on receptor activity and inhibition by lapatinib., Cancer Res.
    Ramalingam et al., 2012, Randomized phase II study of dacomitinib (PF-00299804), an irreversible pan-human epidermal growth factor receptor inhibitor, versus erlotinib in patients with advanced non-small-cell lung cancer., J. Clin. Oncol.
    Sequist et al., 2010, Neratinib, an irreversible pan-ErbB receptor tyrosine kinase inhibitor: results of a phase II trial in patients with advanced non-small-cell lung cancer., J. Clin. Oncol.
    Paez et al., 2004, EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy., Science
    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.
    Huang et al., 2013, MEK inhibitors reverse resistance in epidermal growth factor receptor mutation lung cancer cells with acquired resistance to gefitinib., Mol Oncol
    Mitsudomi et al., 2010, Epidermal growth factor receptor in relation to tumor development: EGFR gene and cancer., FEBS J.
    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.
    Tam et al., 2009, Double EGFR mutants containing rare EGFR mutant types show reduced in vitro response to gefitinib compared with common activating missense mutations., Mol. Cancer Ther.
    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.
    Han et al., 2005, Predictive and prognostic impact of epidermal growth factor receptor mutation in non-small-cell lung cancer patients treated with gefitinib., J. Clin. Oncol.
    Chang et al., 2016, Identifying recurrent mutations in cancer reveals widespread lineage diversity and mutational specificity., Nat. Biotechnol.
    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
    Bahassi et al., 2013, A patient-derived somatic mutation in the epidermal growth factor receptor ligand-binding domain confers increased sensitivity to cetuximab in head and neck cancer., Eur. J. Cancer
    Konduri et al., 2016, EGFR Fusions as Novel Therapeutic Targets in Lung Cancer., Cancer Discov
    Cho et al., 2013, Cetuximab response of lung cancer-derived EGF receptor mutants is associated with asymmetric dimerization., Cancer Res.
    Pirazzoli et al., 2014, Acquired resistance of EGFR-mutant lung adenocarcinomas to afatinib plus cetuximab is associated with activation of mTORC1., Cell Rep
    Wang et al., 2016, Recurrent Olfactory Neuroblastoma Treated With Cetuximab and Sunitinib: A Case Report., Medicine (Baltimore)
    Ercan et al., 2015, EGFR Mutations and Resistance to Irreversible Pyrimidine-Based EGFR Inhibitors., Clin. Cancer Res.
    Jia et al., 2016, Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors., Nature
    Zhang et al., 2013, A subset of gastric cancers with EGFR amplification and overexpression respond to cetuximab therapy., Sci Rep
    Keller et al., 2016, A Novel EGFR Extracellular Domain Mutant, EGFRΔ768, Possesses Distinct Biological and Biochemical Properties in Neuroblastoma., Mol. Cancer Res.
    Arena et al., 2016, MM-151 overcomes acquired resistance to cetuximab and panitumumab in colorectal cancers harboring EGFR extracellular domain mutations., Sci Transl Med
    Uchibori et al., 2017, Brigatinib combined with anti-EGFR antibody overcomes osimertinib resistance in EGFR-mutated non-small-cell lung cancer., Nat Commun
    Luber B et al., 2011, Biomarker analysis of cetuximab plus oxaliplatin/leucovorin/5-fluorouracil in first-line metastatic gastric and oesophago-gastric junction cancer: results from a phase II trial of the Arbeitsgemeinschaft Internistische Onkologie (AIO)., BMC Cancer
    Strickler JH et al., 2018, Genomic Landscape of Cell-Free DNA in Patients with Colorectal Cancer., Cancer Discov
    Takano et al., 1984, Disappearance of terminal deoxynucleotidyltransferase in human malignant T-lymphoblasts treated with a human alpha interferon preparation., Microbiol. Immunol.
    Cushman et al., 2015, Gene expression markers of efficacy and resistance to cetuximab treatment in metastatic colorectal cancer: results from CALGB 80203 (Alliance)., Clin. Cancer Res.
    Pentheroudakis et al., 2013, Biomarkers of benefit from cetuximab-based therapy in metastatic colorectal cancer: interaction of EGFR ligand expression with RAS/RAF, PIK3CA genotypes., BMC Cancer
    Desai, 1991, Drug interaction between alpha interferon and erythropoietin., J. Clin. Oncol.
    Hyman et al., 2015, Vemurafenib in Multiple Nonmelanoma Cancers with BRAF V600 Mutations., N. Engl. J. Med.
    van Geel et al., 2017, A Phase Ib Dose-Escalation Study of Encorafenib and Cetuximab with or without Alpelisib in Metastatic BRAF-Mutant Colorectal Cancer., Cancer Discov
    Yao et al., 2017, Tumours with class 3 BRAF mutants are sensitive to the inhibition of activated RAS., Nature
    Prahallad et al., 2012, Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR., Nature
    Connolly et al., 2014, Anticancer activity of combination targeted therapy using cetuximab plus vemurafenib for refractory BRAF (V600E)-mutant metastatic colorectal carcinoma., Curr Oncol
    Tang et al., 2015, BGB-283, a Novel RAF Kinase and EGFR Inhibitor, Displays Potent Antitumor Activity in BRAF-Mutated Colorectal Cancers., Mol. Cancer Ther.
    Waizenegger et al., 2016, A Novel RAF Kinase Inhibitor with DFG-Out-Binding Mode: High Efficacy in BRAF-Mutant Tumor Xenograft Models in the Absence of Normal Tissue Hyperproliferation., Mol. Cancer Ther.
    Nicolaides et al., 2011, Targeted therapy for BRAFV600E malignant astrocytoma., Clin. Cancer Res.
    Rad et al., 2013, A genetic progression model of Braf(V600E)-induced intestinal tumorigenesis reveals targets for therapeutic intervention., Cancer Cell
    Maldonado et al., 2003, Determinants of BRAF mutations in primary melanomas., J. Natl. Cancer Inst.
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    Villanueva et al., 2010, Acquired resistance to BRAF inhibitors mediated by a RAF kinase switch in melanoma can be overcome by cotargeting MEK and IGF-1R/PI3K., Cancer Cell
    Tiacci et al., 2011, BRAF mutations in hairy-cell leukemia., N. Engl. J. Med.
    Sosman et al., 2012, Survival in BRAF V600-mutant advanced melanoma treated with vemurafenib., N. Engl. J. Med.
    Gupta-Abramson et al., 2008, Phase II trial of sorafenib in advanced thyroid cancer., J. Clin. Oncol.
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    Lovly et al., 2012, Routine multiplex mutational profiling of melanomas enables enrollment in genotype-driven therapeutic trials., PLoS ONE
    Falchook et al., 2013, BRAF mutant gastrointestinal stromal tumor: first report of regression with BRAF inhibitor dabrafenib (GSK2118436) and whole exomic sequencing for analysis of acquired resistance., Oncotarget
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    Nagore et al., 2014, Prognostic value of BRAF mutations in localized cutaneous melanoma., J. Am. Acad. Dermatol.
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    De Roock et al., 2009, Clinical biomarkers in oncology: focus on colorectal cancer., Mol Diagn Ther
    Penna et al., 2016, Primary cross-resistance to BRAFV600E-, MEK1/2- and PI3K/mTOR-specific inhibitors in BRAF-mutant melanoma cells counteracted by dual pathway blockade., Oncotarget
    Corcoran et al., 2012, EGFR-mediated re-activation of MAPK signaling contributes to insensitivity of BRAF mutant colorectal cancers to RAF inhibition with vemurafenib., Cancer Discov
    Xing et al., 2014, BRAF V600E and TERT promoter mutations cooperatively identify the most aggressive papillary thyroid cancer with highest recurrence., J. Clin. Oncol.
    Tejpar et al., 2010, Prognostic and predictive biomarkers in resected colon cancer: current status and future perspectives for integrating genomics into biomarker discovery., Oncologist
    Faber et al., 2014, mTOR inhibition specifically sensitizes colorectal cancers with KRAS or BRAF mutations to BCL-2/BCL-XL inhibition by suppressing MCL-1., Cancer Discov
    Agaimy et al., 2009, V600E BRAF mutations are alternative early molecular events in a subset of KIT/PDGFRA wild-type gastrointestinal stromal tumours., J. Clin. Pathol.
    Ponti et al., 2012, Overwhelming response to Dabrafenib in a patient with double BRAF mutation (V600E; V600M) metastatic malignant melanoma., J Hematol Oncol
    Paraiso et al., 2012, The HSP90 inhibitor XL888 overcomes BRAF inhibitor resistance mediated through diverse mechanisms., Clin. Cancer Res.
    Kirkwood et al., 2012, Phase II, open-label, randomized trial of the MEK1/2 inhibitor selumetinib as monotherapy versus temozolomide in patients with advanced melanoma., Clin. Cancer Res.
    Cardarella et al., 2013, Clinical, pathologic, and biologic features associated with BRAF mutations in non-small cell lung cancer., Clin. Cancer Res.
    Nissan et al., 2014, Loss of NF1 in cutaneous melanoma is associated with RAS activation and MEK dependence., Cancer Res.
    Greger et al., 2012, Combinations of BRAF, MEK, and PI3K/mTOR inhibitors overcome acquired resistance to the BRAF inhibitor GSK2118436 dabrafenib, mediated by NRAS or MEK mutations., Mol. Cancer Ther.
    Flaherty et al., 2012, Combined BRAF and MEK inhibition in melanoma with BRAF V600 mutations., N. Engl. J. Med.
    Jalili et al., 2012, Dual suppression of the cyclin-dependent kinase inhibitors CDKN2C and CDKN1A in human melanoma., J. Natl. Cancer Inst.
    Gandhi et al., 2009, Alterations in genes of the EGFR signaling pathway and their relationship to EGFR tyrosine kinase inhibitor sensitivity in lung cancer cell lines., PLoS ONE
    Rudin et al., 2013, Molecular characterization of acquired resistance to the BRAF inhibitor dabrafenib in a patient with BRAF-mutant non-small-cell lung cancer., J Thorac Oncol
    Hauschild et al., 2012, Dabrafenib in BRAF-mutated metastatic melanoma: a multicentre, open-label, phase 3 randomised controlled trial., Lancet
    Boulalas et al., Mutational analysis of the BRAF gene in transitional cell carcinoma of the bladder., Int. J. Biol. Markers
    Sarker et al., 2015, First-in-human phase I study of pictilisib (GDC-0941), a potent pan-class I phosphatidylinositol-3-kinase (PI3K) inhibitor, in patients with advanced solid tumors., Clin. Cancer Res.
    Crescenzi et al., 2014, Immunohistochemistry for BRAF(V600E) antibody VE1 performed in core needle biopsy samples identifies mutated papillary thyroid cancers., Horm. Metab. Res.
    Andrulis et al., 2013, Targeting the BRAF V600E mutation in multiple myeloma., Cancer Discov
    Rubinstein et al., 2010, Incidence of the V600K mutation among melanoma patients with BRAF mutations, and potential therapeutic response to the specific BRAF inhibitor PLX4032., J Transl Med
    Kim et al., 2013, Clinical responses to vemurafenib in patients with metastatic papillary thyroid cancer harboring BRAF(V600E) mutation., Thyroid
    Dienstmann et al., 2011, BRAF as a target for cancer therapy., Anticancer Agents Med Chem
    Chapman et al., 2011, Improved survival with vemurafenib in melanoma with BRAF V600E mutation., N. Engl. J. Med.
    Tol et al., 2010, Markers for EGFR pathway activation as predictor of outcome in metastatic colorectal cancer patients treated with or without cetuximab., Eur. J. Cancer
    Ji et al., 2013, Vemurafenib synergizes with nutlin-3 to deplete survivin and suppresses melanoma viability and tumor growth., Clin. Cancer Res.
    Morris et al., 2013, Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors., Cancer Discov
    Sen et al., 2012, Kinase-impaired BRAF mutations in lung cancer confer sensitivity to dasatinib., Sci Transl Med
    Patel et al., 2013, Clinical responses to selumetinib (AZD6244; ARRY-142886)-based combination therapy stratified by gene mutations in patients with metastatic melanoma., Cancer
    He et al., 2014, Prognostic value of the BRAF V600E mutation in papillary thyroid carcinoma., Oncol Lett
    Menzies et al., 2014, Dabrafenib and trametinib, alone and in combination for BRAF-mutant metastatic melanoma., Clin. Cancer Res.
    Lam et al., 2010, Phase II clinical trial of sorafenib in metastatic medullary thyroid cancer., J. Clin. Oncol.
    Di Nicolantonio et al., 2008, Wild-type BRAF is required for response to panitumumab or cetuximab in metastatic colorectal cancer., J. Clin. Oncol.
    Zecchin et al., 2013, BRAF V600E is a determinant of sensitivity to proteasome inhibitors., Mol. Cancer Ther.
    Hayes et al., 2012, Phase II efficacy and pharmacogenomic study of Selumetinib (AZD6244; ARRY-142886) in iodine-131 refractory papillary thyroid carcinoma with or without follicular elements., Clin. Cancer Res.
    Meckbach et al., 2014, BRAF-V600 mutations have no prognostic impact in stage IV melanoma patients treated with monochemotherapy., PLoS ONE
    Ascierto et al., 2013, Phase II trial (BREAK-2) of the BRAF inhibitor dabrafenib (GSK2118436) in patients with metastatic melanoma., J. Clin. Oncol.
    Walczyk et al., 2014, The BRAF(V600E) mutation in papillary thyroid microcarcinoma: does the mutation have an impact on clinical outcome?, Clin. Endocrinol. (Oxf)
    Howell et al., 2011, Both BRAF V600E mutation and older age (≥ 65 years) are associated with recurrent papillary thyroid cancer., Ann. Surg. Oncol.
    Wan et al., 2004, Mechanism of activation of the RAF-ERK signaling pathway by oncogenic mutations of B-RAF., Cell
    Flaherty et al., 2012, Improved survival with MEK inhibition in BRAF-mutated melanoma., N. Engl. J. Med.
    Coffee et al., 2013, Concomitant BRAF and PI3K/mTOR blockade is required for effective treatment of BRAF(V600E) colorectal cancer., Clin. Cancer Res.
    Kurman et al., 2011, Molecular pathogenesis and extraovarian origin of epithelial ovarian cancer--shifting the paradigm., Hum. Pathol.
    Falchook et al., 2012, Activity of the oral MEK inhibitor trametinib in patients with advanced melanoma: a phase 1 dose-escalation trial., Lancet Oncol.
    Hatzivassiliou et al., 2013, Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers., Nature
    Rowland et al., 2015, Meta-analysis of BRAF mutation as a predictive biomarker of benefit from anti-EGFR monoclonal antibody therapy for RAS wild-type metastatic colorectal cancer., Br. J. Cancer
    Flaherty et al., 2010, Inhibition of mutated, activated BRAF in metastatic melanoma., N. Engl. J. Med.
    Ohashi et al., 2012, Lung cancers with acquired resistance to EGFR inhibitors occasionally harbor BRAF gene mutations but lack mutations in KRAS, NRAS, or MEK1., Proc. Natl. Acad. Sci. U.S.A.
    Falchook et al., 2012, Dabrafenib in patients with melanoma, untreated brain metastases, and other solid tumours: a phase 1 dose-escalation trial., Lancet
    Paik et al., 2011, Clinical characteristics of patients with lung adenocarcinomas harboring BRAF mutations., J. Clin. Oncol.
    Naoki et al., 2002, Missense mutations of the BRAF gene in human lung adenocarcinoma., Cancer Res.
    Gautschi et al., 2012, A patient with BRAF V600E lung adenocarcinoma responding to vemurafenib., J Thorac Oncol
    Davies et al., 2002, Mutations of the BRAF gene in human cancer., Nature
    Hsu HC et al., 2016, Mutations of KRAS/NRAS/BRAF predict cetuximab resistance in metastatic colorectal cancer patients., Oncotarget
    Hong et al., 2016, Phase IB Study of Vemurafenib in Combination with Irinotecan and Cetuximab in Patients with Metastatic Colorectal Cancer with BRAFV600E Mutation., Cancer Discov
    Kopetz S et al., 2019, Encorafenib, Binimetinib, and Cetuximab in <i>BRAF</i> V600E-Mutated Colorectal Cancer., N Engl J Med
    Tol J et al., 2009, BRAF mutation in metastatic colorectal cancer., N Engl J Med
    Yaeger R et al., 2019, Response to Anti-EGFR Therapy in Patients with BRAF non-V600-Mutant Metastatic Colorectal Cancer., Clin Cancer Res
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    Wittinger et al., 2011, hVps37A Status affects prognosis and cetuximab sensitivity in ovarian cancer., Clin. Cancer Res.
    Wu et al., 2006, Perinatal epidermal growth factor receptor blockade prevents peripheral nerve disruption in a mouse model reminiscent of benign world health organization grade I neurofibroma., Am. J. Pathol.
    Pander J et al., 2015, Genome Wide Association Study for Predictors of Progression Free Survival in Patients on Capecitabine, Oxaliplatin, Bevacizumab and Cetuximab in First-Line Therapy of Metastatic Colorectal Cancer., PLoS One
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    Sclafani et al., 2014, TP53 mutational status and cetuximab benefit in rectal cancer: 5-year results of the EXPERT-C trial., J. Natl. Cancer Inst.
    Cheng et al., 2015, Decreased SMAD4 expression is associated with induction of epithelial-to-mesenchymal transition and cetuximab resistance in head and neck squamous cell carcinoma., Cancer Biol. Ther.
    Kasper et al., 2013, Oncogenic RAS simultaneously protects against anti-EGFR antibody-dependent cellular cytotoxicity and EGFR signaling blockade., Oncogene
    Lv S et al., 2011, Correlation between IDH1 gene mutation status and survival of patients treated for recurrent glioma., Anticancer Res
  • CETUXIMAB   EGF

    Interaction Score: 3.36

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27897268 23959273 18349392 16788380 25677871


    Sources:
    CIViC PharmGKB

  • CETUXIMAB   VPS37A

    Interaction Score: 2.88

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22016507


    Sources:
    CIViC

  • CETUXIMAB   EREG

    Interaction Score: 2.16

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23374602


    Sources:
    CIViC PharmGKB

  • CETUXIMAB   FCGR2A

    Interaction Score: 1.64

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17704420 17016423 17139284 30318772 28719596 27897268 23296156


    Sources:
    PharmGKB

  • CETUXIMAB   BRAF

    Interaction Score: 1.6

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Cetuximab + PLX4720
    combination therapy Vemurafenib + Cetuximab
    combination therapy Cetuximab + Dabrafenib + SCH772984

    PMIDs:
    26287849 28363909 28783719 22270724 22281684 24523613 26208524 26916115 27312529 25838391 27002107 25714871 23325582 21163703 20619739 22038996 19773371 23845441 14679157 22180495 21156289 21663470 22356324 12460918 18541894 23406027 21129611 22536370 23470635 23251002 24594804 19018267 22586120 24388723 19010912 24508103 20857202 19537845 21975775 26678033 22448344 25024077 20350999 24163374 19561230 19255327 23031422 22351686 22048237 23833300 24576830 22389471 23020132 22997239 19238210 23524406 22735384 19404918 25370471 24570209 23612012 20630094 23489023 21426297 21639808 20413299 23812671 23614898 22649091 22972589 24396464 24583796 20368568 19001320 24107445 22241789 26619011 24586605 23918947 24354346 21594703 15035987 22663011 23549875 21683865 22805292 23934108 25157968 25989278 20818844 22773810 22608338 21483012 12460919 22743296 12068308 26989027 19603024 27729313 19603018 31566309 19571295 31515458 28972961


    Sources:
    JAX-CKB DoCM CIViC OncoKB

  • CETUXIMAB   PTP4A3

    Interaction Score: 1.44

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23867504


    Sources:
    CIViC

  • CETUXIMAB   EPO

    Interaction Score: 1.44

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    2016633


    Sources:
    NCI

  • CETUXIMAB   AREG

    Interaction Score: 1.15

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23959273 23374602


    Sources:
    CIViC PharmGKB

  • CETUXIMAB   EGFR

    Interaction Score: 0.92

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

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

    PMIDs:
    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 MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions TEND DoCM CIViC CancerCommons TTD FDA

  • CETUXIMAB   KRAS

    Interaction Score: 0.83

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Clinical Status late trials
    Pathway activation
    Variant Effect gain-of-function

    PMIDs:
    20978259 3122217 21398618 19679400 18316791 19075190 23182985 21975775 26812186 19018267 23406027 22734028 19114683 16618717 25157968 21228335 17384584 19255327 26371285 20921462 18794081 16434492 19773371 22392911 16361624 26623049 22407852 24558511 20921465 12460918 2278970 20570890 28179366 28280091 27458141 28632865 19064407 25714871 27002107 24304820 25605843 26715098 25838391 18202412 26341921 27312529 26666244 27897268 26438111 26162609 25210463 25183481 24727325 23324806 23090619 23071293 22537608 25666295 19603018 22722830 28275037 22586653 20956938 19223544 19603024 20619739 18946061 22246397 23404247 25673644 21575616


    Sources:
    ClearityFoundationBiomarkers JAX-CKB DoCM CIViC PharmGKB OncoKB

  • CETUXIMAB   MGAT4A

    Interaction Score: 0.72

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26222057


    Sources:
    PharmGKB

  • CETUXIMAB   NRG2

    Interaction Score: 0.72

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • CETUXIMAB   TGFA

    Interaction Score: 0.72

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • CETUXIMAB   BTC

    Interaction Score: 0.72

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • CETUXIMAB   DNTT

    Interaction Score: 0.72

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    6335218


    Sources:
    NCI

  • CETUXIMAB   FCGR3A

    Interaction Score: 0.54

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17704420 17016423 17139284 30318772 28719596 27897268 23296156


    Sources:
    NCI PharmGKB

  • CETUXIMAB   HBEGF

    Interaction Score: 0.48

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • CETUXIMAB   NRG3

    Interaction Score: 0.48

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • CETUXIMAB   GC

    Interaction Score: 0.41

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    29208668


    Sources:
    PharmGKB

  • CETUXIMAB   NRAS

    Interaction Score: 0.4

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Cetuximab + FOLFOX
    Indication/Tumor Type colorectal cancer
    Response Type predicted – sensitive

    PMIDs:
    28179366 25605843 25838391 27002107 26438111 23325582 20619739 24024839 28275037


    Sources:
    JAX-CKB CIViC PharmGKB OncoKB

  • CETUXIMAB   CCND1

    Interaction Score: 0.29

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22117530 18349392 16788380


    Sources:
    PharmGKB

  • CETUXIMAB   SMAD4

    Interaction Score: 0.24

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26046389


    Sources:
    CIViC

  • CETUXIMAB   NT5E

    Interaction Score: 0.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25520391


    Sources:
    CIViC

  • CETUXIMAB   HNF4A

    Interaction Score: 0.19

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    8777337


    Sources:
    NCI

  • CETUXIMAB   NRG1

    Interaction Score: 0.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21900593


    Sources:
    CIViC PharmGKB

  • CETUXIMAB   MAP2K1

    Interaction Score: 0.14

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Vemurafenib + Cetuximab
    Indication/Tumor Type colorectal cancer
    Response Type sensitive

    PMIDs:
    26644315 28179366 27312529


    Sources:
    JAX-CKB CIViC

  • CETUXIMAB   PIK3CA

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    20619739 19223544 28424201 19603024 28446642 27002107 26715098 25838391 25724520 25714871


    Sources:
    JAX-CKB CIViC

  • CETUXIMAB   CXCL8

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10614716 10037173 15908664


    Sources:
    NCI

  • CETUXIMAB   RARA

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    8857944


    Sources:
    NCI

  • CETUXIMAB   ERBB3

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25520391


    Sources:
    CIViC

  • CETUXIMAB   HRAS

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    22797062


    Sources:
    JAX-CKB

  • CETUXIMAB   ERBB4

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type head and neck squamous cell carcinoma
    Response Type resistant
    Approval Status Preclinical - Cell culture

    PMIDs:
    27207775


    Sources:
    JAX-CKB

  • CETUXIMAB   ERBB2

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type colorectal cancer
    Response Type resistant
    Approval Status Preclinical - Cell line xenograft

    PMIDs:
    28223103 22586653 23948973 21900593 26243863 26296355


    Sources:
    JAX-CKB CIViC

  • CETUXIMAB   MYC

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    3085922


    Sources:
    NCI

  • CETUXIMAB   PTEN

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    19223544 21163703


    Sources:
    ClearityFoundationBiomarkers CIViC

  • CETUXIMAB   FGFR2

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    27149458


    Sources:
    JAX-CKB

  • CETUXIMAB   RET

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    27149458


    Sources:
    JAX-CKB

  • CETUXIMAB   BDNF

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16651634


    Sources:
    NCI

  • CETUXIMAB   MET

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Response Type sensitive
    combination therapy Cetuximab + JNJ 38877605
    Approval Status Preclinical - Cell culture

    PMIDs:
    23729478


    Sources:
    JAX-CKB CIViC

  • CETUXIMAB   AKT1

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    25714871


    Sources:
    JAX-CKB

  • CETUXIMAB   KDR

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    27149458


    Sources:
    JAX-CKB

  • CETUXIMAB   TP53

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24957073


    Sources:
    CIViC

  • CETUXIMAB   IDH1

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22199315


    Sources:
    CIViC

  • MyCancerGenome: CETUXIMAB

    • Version: 20-Jun-2017

    Alternate Names:
    IMC-C225 Development Name
    CETUXIMAB Generic Name
    ERBITUX Trade Name

    Drug Info:
    Drug Class Therapeutic Antibodies
    FDA Approval Colorectal cancer (KRAS wild type), Squamous cell carcinoma of the head and neck

    Publications:

  • TEND: CETUXIMAB

    • Version: 01-August-2011

    Alternate Names:
    CETUXIMAB Primary Drug Name

    Drug Info:
    Drug Class antineoplastic agents
    Year of Approval 2004

    Publications:

  • CancerCommons: CETUXIMAB

    • Version: 25-July-2013

    Alternate Names:
    IFL Protocol PubChem Drug Name
    56842117 PubChem Drug ID
    Erbitux Drug Trade Name

    Drug Info:
    Drug Class Monoclonal Antibody
    Source Reported Drug Name(s) Cetuximab
    Pharmaceutical Developer Bristol-Myers Squibb

    Publications:

  • TdgClinicalTrial: CETUXIMAB

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications antineoplastic agent
    Drug Class monoclonal antibody
    FDA Approval approved

    Publications:

  • NCI: C225

    • Version: 14-September-2017

    Alternate Names:
    C1723 NCI drug code

    Drug Info:

    Publications:
    Perrotte et al., 1999, Anti-epidermal growth factor receptor antibody C225 inhibits angiogenesis in human transitional cell carcinoma growing orthotopically in nude mice., Clin. Cancer Res.

  • NCI: ALPHA INTERFERON

    • Version: 14-September-2017

    Alternate Names:
    C225 NCI drug code

    Drug Info:

    Publications:
    Skowsky et al., A pilot study of chronic recombinant interferon-alfa 2a for diabetic proliferative retinopathy: metabolic effects and opthalmologic effects., J. Diabetes Complicat.
    Takano et al., 1984, Disappearance of terminal deoxynucleotidyltransferase in human malignant T-lymphoblasts treated with a human alpha interferon preparation., Microbiol. Immunol.
    Desai, 1991, Drug interaction between alpha interferon and erythropoietin., J. Clin. Oncol.

  • NCI: CETUXIMAB

    • Version: 14-September-2017

    Alternate Names:
    C1723 NCI drug code

    Drug Info:

    Publications:
    Vallböhmer et al., 2005, Molecular determinants of cetuximab efficacy., J. Clin. Oncol.
    Zhang et al., 2007, FCGR2A and FCGR3A polymorphisms associated with clinical outcome of epidermal growth factor receptor expressing metastatic colorectal cancer patients treated with single-agent cetuximab., J. Clin. Oncol.
    Wu et al., 2006, Perinatal epidermal growth factor receptor blockade prevents peripheral nerve disruption in a mouse model reminiscent of benign world health organization grade I neurofibroma., Am. J. Pathol.

  • NCI: LEUKOCYTE INTERFERON

    • Version: 14-September-2017

    Alternate Names:
    C225 NCI drug code

    Drug Info:

    Publications:
    Bepler et al., 1986, Additive and differential biological activity of alpha-interferon A, difluoromethylornithine, and their combination on established human lung cancer cell lines., Cancer Res.

  • PharmGKB: cetuximab

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Berger MD et al., 2018, A Polymorphism within the Vitamin D Transporter Gene Predicts Outcome in Metastatic Colorectal Cancer Patients Treated with FOLFIRI/Bevacizumab or FOLFIRI/Cetuximab., Clin Cancer Res
    Pander J et al., 2015, Genome Wide Association Study for Predictors of Progression Free Survival in Patients on Capecitabine, Oxaliplatin, Bevacizumab and Cetuximab in First-Line Therapy of Metastatic Colorectal Cancer., PLoS One
    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

  • JAX-CKB: Cetuximab

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Napolitano et al., 2015, Primary and Acquired Resistance of Colorectal Cancer to Anti-EGFR Monoclonal Antibody Can Be Overcome by Combined Treatment of Regorafenib with Cetuximab., Clin. Cancer Res.
    Ciardiello et al., 2016, Cetuximab continuation after first progression in metastatic colorectal cancer (CAPRI-GOIM): a randomized phase II trial of FOLFOX plus cetuximab versus FOLFOX., Ann. Oncol.
    Brammeld et al., 2017, Genome-wide chemical mutagenesis screens allow unbiased saturation of the cancer genome and identification of drug resistance mutations., Genome Res.

  • DoCM: CETUXIMAB

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Flaherty et al., 2012, Combined BRAF and MEK inhibition in melanoma with BRAF V600 mutations., N. Engl. J. Med.
    Falchook et al., 2012, Dabrafenib in patients with melanoma, untreated brain metastases, and other solid tumours: a phase 1 dose-escalation trial., Lancet
    Chang et al., 2016, Identifying recurrent mutations in cancer reveals widespread lineage diversity and mutational specificity., Nat. Biotechnol.

  • CIViC: CETUXIMAB

    • Version: 14-September-2020

    Alternate Names:

    Drug Info:

    Publications:
    Di Nicolantonio et al., 2008, Wild-type BRAF is required for response to panitumumab or cetuximab in metastatic colorectal cancer., J. Clin. Oncol.
    Loupakis et al., 2009, KRAS codon 61, 146 and BRAF mutations predict resistance to cetuximab plus irinotecan in KRAS codon 12 and 13 wild-type metastatic colorectal cancer., Br. J. Cancer
    Kopetz S et al., 2019, Encorafenib, Binimetinib, and Cetuximab in <i>BRAF</i> V600E-Mutated Colorectal Cancer., N Engl J Med

  • TALC: CETUXIMAB

    • Version: 12-May-2016

    Alternate Names:
    CETUXIMAB Primary Drug Name
    CETUXIMAB Drug Generic Name
    ERBITUX Drug Trade Name

    Drug Info:

    Publications:

  • TTD: Cetuximab

    • Version: 2020.06.01

    Alternate Names:
    D0N5OV TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL1201577

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • FDA: Cetuximab

    • Version: 04-September-2020

    Alternate Names:

    Drug Info:

    Publications:

  • ClearityFoundationBiomarkers: CETUXIMAB

    • Version: 26-July-2013

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL1201577

    • Version: chembl_23

    Alternate Names:

    Drug Info:

    Publications:

  • OncoKB: Cetuximab

    • Version: 23-July-2020

    Alternate Names:

    Drug Info:

    Publications:

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

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

The dgidb.org website does not provide any medical or healthcare products, services or advice, and is not for medical emergencies or urgent situations. IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY, CALL YOUR DOCTOR OR 911 IMMEDIATELY. Information contained on this website is not a substitute for a doctor's medical judgment or advice. We recommend that you discuss your specific, individual health concerns with your doctor or health care professional.

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