DGIdb - ERLOTINIB Drug Record

ERLOTINIB chembl:CHEMBL553 ApprovedAntineoplastic

Alternate Names:

OSI-774
CP-358774
R-1415
CP-35877401
ERLOTINIB
TARCEVA
CP-358,774
RG-1415
RO-508231
OSI 744
TARCEVA®
NSC 718781
R 1415
[6,7-BIS-(2-METHOXY-ETHOXY)-QUINAZOLIN-4-YL]-(3-ETHYNYL-PHENYL)-AMINE
drugbank:00530
chemidplus:183321-74-6
rxcui:337525
pubchem.compound:176870
chembl:CHEMBL553

Drug Info:

Pharmaceutical Developer	Roche
Source Reported Drug Name(s)	Erlotinib
Drug Class	EGFR Inhibitor
FDA Approval	Non-small cell lung cancer (with EGFR exon 19 deletions or exon 21 substitution (L858R) mutations), Pancreatic cancer
Drug Class	Kinase Inhibitors
Drug Class	antineoplastic agents, protein kinase inhibitors
Year of Approval	2004
FDA Approval	not approved
Drug Class	Small Molecule
Drug Indications	antineoplastic agent

(15 More Sources)

Publications:

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.
Marchetti et al., 2008, Effect of the ATP-binding cassette drug transporters ABCB1, ABCG2, and ABCC2 on erlotinib hydrochloride (Tarceva) disposition in in vitro and in vivo pharmacokinetic studies employing Bcrp1-/-/Mdr1a/1b-/- (triple-knockout) and wild-type mice., Mol. Cancer Ther.
Bahcall et al., 2016, Acquired METD1228V Mutation and Resistance to MET Inhibition in Lung Cancer., Cancer Discov
Niu et al., 2014, Novel agents and strategies for overcoming EGFR TKIs resistance., Exp Hematol 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.
Frattini et al., 2013, The integrated landscape of driver genomic alterations in glioblastoma., Nat. Genet.
Khozin et al., 2014, U.S. Food and Drug Administration approval summary: Erlotinib for the first-line treatment of metastatic non-small cell lung cancer with epidermal growth factor receptor exon 19 deletions or exon 21 (L858R) substitution mutations., Oncologist
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
Rosell et al., 2017, Erlotinib and bevacizumab in patients with advanced non-small-cell lung cancer and activating EGFR mutations (BELIEF): an international, multicentre, single-arm, phase 2 trial., Lancet Respir Med
Kelly et al., 2015, Adjuvant Erlotinib Versus Placebo in Patients With Stage IB-IIIA Non-Small-Cell Lung Cancer (RADIANT): A Randomized, Double-Blind, Phase III Trial., J. Clin. Oncol.
Park et al., 2016, First-Line Erlotinib Therapy Until and Beyond Response Evaluation Criteria in Solid Tumors Progression in Asian Patients With Epidermal Growth Factor Receptor Mutation-Positive Non-Small-Cell Lung Cancer: The ASPIRATION Study., JAMA Oncol
Johnson et al., 2015, Phase I/II Study of HSP90 Inhibitor AUY922 and Erlotinib for EGFR-Mutant Lung Cancer With Acquired Resistance to Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors., J. Clin. Oncol.
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.
Konduri et al., 2016, EGFR Fusions as Novel Therapeutic Targets in Lung Cancer., Cancer Discov
Kotschy et al., 2016, The MCL1 inhibitor S63845 is tolerable and effective in diverse cancer models., Nature
Wen et al., 2014, Phase I/II study of erlotinib and temsirolimus for patients with recurrent malignant gliomas: North American Brain Tumor Consortium trial 04-02., Neuro-oncology
Bean et al., 2008, Acquired resistance to epidermal growth factor receptor kinase inhibitors associated with a novel T854A mutation in a patient with EGFR-mutant lung adenocarcinoma., 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.
Keller et al., 2016, A Novel EGFR Extracellular Domain Mutant, EGFRΔ768, Possesses Distinct Biological and Biochemical Properties in Neuroblastoma., Mol. Cancer Res.
He et al., 2012, EGFR exon 19 insertions: a new family of sensitizing EGFR mutations in lung adenocarcinoma., Clin. Cancer Res.
Foster et al., 2010, Clinical implications of novel activating EGFR mutations in malignant peritoneal mesothelioma., World J Surg Oncol
Gallant et al., 2015, EGFR Kinase Domain Duplication (EGFR-KDD) Is a Novel Oncogenic Driver in Lung Cancer That Is Clinically Responsive to Afatinib., Cancer Discov
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
Tang et al., 2009, Disruption of the EGFR E884-R958 ion pair conserved in the human kinome differentially alters signaling and inhibitor sensitivity., Oncogene
Neal et al., 2016, Erlotinib, cabozantinib, or erlotinib plus cabozantinib as second-line or third-line treatment of patients with EGFR wild-type advanced non-small-cell lung cancer (ECOG-ACRIN 1512): a randomised, controlled, open-label, multicentre, phase 2 trial., Lancet Oncol.
Lee et al., 2006, Epidermal growth factor receptor activation in glioblastoma through novel missense mutations in the extracellular domain., PLoS Med.
Costa et al., 2008, Effects of erlotinib in EGFR mutated non-small cell lung cancers with resistance to gefitinib., Clin. Cancer Res.
Smith et al., 2015, The HSP90 inhibitor ganetespib potentiates the antitumor activity of EGFR tyrosine kinase inhibition in mutant and wild-type non-small cell lung cancer., Target Oncol
Yasuda et al., 2013, Structural, biochemical, and clinical characterization of epidermal growth factor receptor (EGFR) exon 20 insertion mutations in lung cancer., Sci Transl Med
Kim et al., 2015, Differential Effects of Tyrosine Kinase Inhibitors on Normal and Oncogenic EGFR Signaling and Downstream Effectors., Mol. Cancer Res.
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.
Kancha et al., 2009, Functional analysis of epidermal growth factor receptor (EGFR) mutations and potential implications for EGFR targeted therapy., Clin. Cancer Res.
Lara et al., 2015, Phase II Study of the AKT Inhibitor MK-2206 plus Erlotinib in Patients with Advanced Non-Small Cell Lung Cancer Who Previously Progressed on Erlotinib., Clin. Cancer Res.
Udager et al., 2015, High-Frequency Targetable EGFR Mutations in Sinonasal Squamous Cell Carcinomas Arising from Inverted Sinonasal Papilloma., Cancer Res.
Peters et al., 2017, Compound Uncommon EGFR Mutations in a Patient with Advanced NSCLC and Durable Response to Sequential EGFR Targeted Therapies., J Thorac Oncol
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.
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
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
Guo et al., 2006, Gefitinib-sensitizing mutations in esophageal carcinoma., N. Engl. J. Med.
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.
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
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.
MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
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
Delbaldo et al., 2003, [Epidermal growth factor inhibitors]., Rev Med Interne
Akita et al., 2003, Preclinical studies with Erlotinib (Tarceva)., Semin. Oncol.
Kim et al., 2002, Erlotinib OSI/Roche/Genentech., Curr Opin Investig Drugs
Bulgaru et al., 2003, Erlotinib (Tarceva): a promising drug targeting epidermal growth factor receptor tyrosine kinase., Expert Rev Anticancer Ther
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Laird et al., 2003, Small molecule tyrosine kinase inhibitors: clinical development of anticancer agents., Expert Opin Investig Drugs
Zhu YC et al., 2018, EGFR-RAD51 fusion variant in lung adenocarcinoma and response to erlotinib: A case report., Lung Cancer
Klughammer et al., 2016, Examining Treatment Outcomes with Erlotinib in Patients with Advanced Non-Small Cell Lung Cancer Whose Tumors Harbor Uncommon EGFR Mutations., J Thorac Oncol
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.
Hellmann et al., 2014, Clinical and in vivo evidence that EGFR S768I mutant lung adenocarcinomas are sensitive to erlotinib., J Thorac Oncol
Brugger et al., 2011, Prospective molecular marker analyses of EGFR and KRAS from a randomized, placebo-controlled study of erlotinib maintenance therapy in advanced non-small-cell lung cancer., J. Clin. Oncol.
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.
Mellinghoff et al., 2005, Molecular determinants of the response of glioblastomas to EGFR kinase inhibitors., N. Engl. J. Med.
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.
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.
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.
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.
de Gunst et al., 2007, Functional analysis of cancer-associated EGFR mutants using a cellular assay with YFP-tagged EGFR intracellular domain., Mol. Cancer
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
Ban HS et al., 2010, Enhancement of EGFR tyrosine kinase inhibition by C-C multiple bonds-containing anilinoquinazolines., Bioorg Med Chem
Ji X et al., 2014, Design, synthesis and biological evaluation of novel 6-alkenylamides substituted of 4-anilinothieno[2,3-d]pyrimidines as irreversible epidermal growth factor receptor inhibitors., Bioorg Med Chem
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
Cadranel J et al., 2012, Impact of systematic EGFR and KRAS mutation evaluation on progression-free survival and overall survival in patients with advanced non-small-cell lung cancer treated by erlotinib in a French prospective cohort (ERMETIC project--part 2)., J Thorac Oncol
Cho SH et al., 2012, Efficacy of EGFR tyrosine kinase inhibitors for non-adenocarcinoma NSCLC patients with EGFR mutation., Cancer Chemother Pharmacol
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
Onitsuka T et al., 2010, Acquired resistance to gefitinib: the contribution of mechanisms other than the T790M, MET, and HGF status., 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
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
Puyo S et al., 2008, Impact of EGFR gene polymorphisms on anticancer drug cytotoxicity in vitro., Mol Diagn Ther
Miller VA et al., 2008, Molecular characteristics of bronchioloalveolar carcinoma and adenocarcinoma, bronchioloalveolar carcinoma subtype, predict response to erlotinib., J Clin Oncol
Rudin CM et al., 2008, Pharmacogenomic and pharmacokinetic determinants of erlotinib toxicity., J Clin Oncol
Sequist et al., 2007, Response to treatment and survival of patients with non-small cell lung cancer undergoing somatic EGFR mutation testing., Oncologist
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
Perez-Soler R, 2004, The role of erlotinib (Tarceva, OSI 774) in 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.
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
De Pas T et al., 2011, Activity of epidermal growth factor receptor-tyrosine kinase inhibitors in patients with non-small cell lung cancer harboring rare epidermal growth factor receptor mutations., J Thorac Oncol
Pérez-Soler R et al., 2004 Aug 15, Determinants of tumor response and survival with erlotinib in patients with non--small-cell lung cancer., J Clin Oncol
Tsao MS et al., 2005, Erlotinib in lung cancer - molecular and clinical predictors of outcome., N Engl J Med
Starrett JH et al., 2020, Drug Sensitivity and Allele Specificity of First-Line Osimertinib Resistance <i>EGFR</i> Mutations., Cancer Res
Cecchini M et al., 2017, <i>EGFR</i> Exon 19 Deletion in Pancreatic Adenocarcinoma Responds to Erlotinib, Followed by <i>T790M</i>-Mediated Resistance., J Natl Compr Canc Netw
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
Hammerman et al., 2011, Mutations in the DDR2 kinase gene identify a novel therapeutic target in squamous cell lung cancer., Cancer Discov
Pitini et al., 2013, Response to dasatinib in a patient with SQCC of the lung harboring a discoid-receptor-2 and synchronous chronic myelogenous leukemia., Lung Cancer
Day et al., 2008, Inhibition of collagen-induced discoidin domain receptor 1 and 2 activation by imatinib, nilotinib and dasatinib., Eur. J. Pharmacol.
Rosen et al., 2017, A First-in-Human Phase I Study of a Bivalent MET Antibody, Emibetuzumab (LY2875358), as Monotherapy and in Combination with Erlotinib in Advanced Cancer., Clin. Cancer Res.
Spigel et al., 2013, Randomized phase II trial of Onartuzumab in combination with erlotinib in patients with advanced non-small-cell lung cancer., J. Clin. Oncol.
Marchetti et al., 2009, Clinical implications of KRAS mutations in lung cancer patients treated with tyrosine kinase inhibitors: an important role for mutations in minor clones., Neoplasia
Fiala et al., The dominant role of G12C over other KRAS mutation types in the negative prediction of efficacy of epidermal growth factor receptor tyrosine kinase inhibitors in non-small cell lung cancer., Cancer Genet
Pao et al., 2005, KRAS mutations and primary resistance of lung adenocarcinomas to gefitinib or erlotinib., PLoS Med.
Kim et al., 2011, Impact of KRAS mutations on clinical outcomes in pancreatic cancer patients treated with first-line gemcitabine-based chemotherapy., Mol. Cancer Ther.
Zhu et al., 2008, Role of KRAS and EGFR as biomarkers of response to erlotinib in National Cancer Institute of Canada Clinical Trials Group Study BR.21., J. Clin. Oncol.
Papadimitrakopoulou et al., 2016, The BATTLE-2 Study: A Biomarker-Integrated Targeted Therapy Study in Previously Treated Patients With Advanced Non-Small-Cell Lung Cancer., J. Clin. Oncol.
Horn et al., 2016, High-Order Drug Combinations Are Required to Effectively Kill Colorectal Cancer Cells., Cancer Res.
Ko et al., 2016, A Multicenter, Open-Label Phase II Clinical Trial of Combined MEK plus EGFR Inhibition for Chemotherapy-Refractory Advanced Pancreatic Adenocarcinoma., Clin. Cancer Res.
Biswas et al., 2016, Genomic profiling of multiple sequentially acquired tumor metastatic sites from an "exceptional responder" lung adenocarcinoma patient reveals extensive genomic heterogeneity and novel somatic variants driving treatment response., Cold Spring Harb Mol Case Stud
Choi HG et al., 2015, Pharmacokinetic properties of two erlotinib 150 mg formulations with a genetic effect evaluation in healthy Korean subjects., Clin Drug Investig
Van Allen et al., 2015, Genomic Correlate of Exceptional Erlotinib Response in Head and Neck Squamous Cell Carcinoma., JAMA Oncol
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
Vinik et al., 2016, Patient-Reported Outcomes and Quality of Life with Sunitinib Versus Placebo for Pancreatic Neuroendocrine Tumors: Results From an International Phase III Trial., Target Oncol
Yang et al., 2012, Antitumor activity of BRAF inhibitor vemurafenib in preclinical models of BRAF-mutant colorectal cancer., Cancer Res.
Li Y et al., 2011, Genetic variations in multiple drug action pathways and survival in advanced stage non-small cell lung cancer treated with chemotherapy., Clin Cancer Res
Morgillo et al., 2006, Heterodimerization of insulin-like growth factor receptor/epidermal growth factor receptor and induction of survivin expression counteract the antitumor action of erlotinib., Cancer Res.
Kadera et al., 2015, Low expression of the E3 ubiquitin ligase CBL confers chemoresistance in human pancreatic cancer and is targeted by epidermal growth factor receptor inhibition., Clin. Cancer Res.
Li et al., 2007, Differential metabolism of gefitinib and erlotinib by human cytochrome P450 enzymes., Clin. Cancer Res.
Buchanan et al., 2007, Targeting cyclooxygenase-2 and the epidermal growth factor receptor for the prevention and treatment of intestinal cancer., Cancer Res.
Quintanal-Villalonga A et al., 2019, FGFR4 increases EGFR oncogenic signaling in lung adenocarcinoma, and their combined inhibition is highly effective., Lung Cancer
Borad et al., 2014, Integrated genomic characterization reveals novel, therapeutically relevant drug targets in FGFR and EGFR pathways in sporadic intrahepatic cholangiocarcinoma., PLoS Genet.
Heining C et al., 2018, <i>NRG1</i> Fusions in <i>KRAS</i> Wild-Type Pancreatic Cancer., Cancer Discov

ERLOTINIB ERRFI1

Interaction Score: 2.58

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24550739

Sources:
CIViC
ERLOTINIB EGFR

Interaction Score: 1.34

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

combination therapy MGCD265 + Erlotinib

Approval Status Phase III

combination therapy AUY922 + Erlotinib

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 MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB TEND DoCM COSMIC CIViC CancerCommons PharmGKB TTD FDA OncoKB
ERLOTINIB DDR2

Interaction Score: 1.29

Interaction Types & Directionality:

n/a

Interaction Info:

Clinical Status case report

Pathway activation

Variant Effect gain-of-function

PMIDs:
22328973 23932362 18938156

Sources:
DoCM CIViC
ERLOTINIB CDH1

Interaction Score: 0.52

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Erlotinib + Selumetinib

Indication/Tumor Type pancreatic ductal adenocarcinoma

Response Type sensitive

PMIDs:
26251290

Sources:
JAX-CKB
ERLOTINIB CBL

Interaction Score: 0.43

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Emerging

Approval Status Preclinical - Cell line xenograft

Response Type predicted – sensitive

PMIDs:
25348515

Sources:
JAX-CKB
ERLOTINIB MAP3K1

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21636554

Sources:
PharmGKB
ERLOTINIB ERBB4

Interaction Score: 0.16

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:
DTC JAX-CKB PharmGKB
ERLOTINIB APC

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Erlotinib + Ibuprofen

Indication/Tumor Type colorectal cancer

Response Type sensitive

PMIDs:
17909047

Sources:
JAX-CKB
ERLOTINIB KRAS

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy ABT-263 + Alpelisib + Erlotinib + Trametinib

Indication/Tumor Type colorectal cancer

Response Type sensitive

PMIDs:
21969500 21258250 19794967 23313110 15696205 21862683 18626007 16043828 27480147 27659046

Sources:
ClearityFoundationBiomarkers JAX-CKB CIViC
ERLOTINIB NRG1

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
29802158

Sources:
CIViC
ERLOTINIB FGFR4

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
31027687

Sources:
CIViC
ERLOTINIB HIPK4

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ERLOTINIB MKNK2

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ERLOTINIB BRAF

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Erlotinib + PLX4720

Indication/Tumor Type melanoma

Response Type sensitive

PMIDs:
27659046 22448344 27924459 22180495

Sources:
JAX-CKB CIViC
ERLOTINIB MET

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Onartuzumab + Erlotinib

Indication/Tumor Type non-small cell lung carcinoma

Response Type conflicting

PMIDs:
27694386 27803065 24101053

Sources:
DTC JAX-CKB OncoKB
ERLOTINIB BIRC5

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17047074

Sources:
NCI
ERLOTINIB PKN2

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ERLOTINIB LTK

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ERLOTINIB MINK1

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ERLOTINIB SYK

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ERLOTINIB FRK

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ERLOTINIB SLK

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ERLOTINIB ERBB3

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
ERLOTINIB ABCG2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18723475

Sources:
NCI
ERLOTINIB PTEN

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16282176

Sources:
ClearityFoundationBiomarkers CIViC
ERLOTINIB BLK

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ERLOTINIB PRKD2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ERLOTINIB ERBB2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type lung adenocarcinoma

Response Type resistant

Approval Status Clinical Study

PMIDs:
27900369

Sources:
DTC JAX-CKB PharmGKB
ERLOTINIB UGT1A1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
ERLOTINIB LYN

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ERLOTINIB CLK4

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ERLOTINIB ALK

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ERLOTINIB AURKB

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ERLOTINIB JAK2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ERLOTINIB RET

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ERLOTINIB ABL1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ERLOTINIB PIK3CA

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21258250

Sources:
CIViC
ERLOTINIB FLT1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ERLOTINIB MAPK1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26181029

Sources:
CIViC
ERLOTINIB FLT4

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ERLOTINIB KDR

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ERLOTINIB TP53

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy ABT-263 + Alpelisib + Dabrafenib + Erlotinib

Indication/Tumor Type colorectal cancer

Response Type sensitive

PMIDs:
27659046

Sources:
JAX-CKB
ERLOTINIB YES1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ERLOTINIB ABCB1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
ERLOTINIB CYP1A2

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25408262

Sources:
PharmGKB
ERLOTINIB CYP2D6

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17575239

Sources:
NCI
ERLOTINIB AR

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ERLOTINIB CYP3A4

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB

CancerCommons: ERLOTINIB
- Version: 25-July-2013
Alternate Names:

Erlotinib PubChem Drug Name

176870 PubChem Drug ID

Tarceva Drug Trade Name

Drug Info:

Drug Class EGFR Inhibitor

Source Reported Drug Name(s) Erlotinib

Pharmaceutical Developer Roche

Publications:
MyCancerGenome: ERLOTINIB
- Version: 20-Jun-2017
Alternate Names:

OSI-774 Development Name

CP-258 Development Name

774 Development Name

Drug Info:

Drug Class Kinase Inhibitors

FDA Approval Non-small cell lung cancer (with EGFR exon 19 deletions or exon 21 substitution (L858R) mutations), Pancreatic cancer

Publications:
TEND: ERLOTINIB
- Version: 01-August-2011
Alternate Names:

ERLOTINIB Primary Drug Name

Drug Info:

Year of Approval 2004

Drug Class antineoplastic agents, protein kinase inhibitors

Publications:
TdgClinicalTrial: ERLOTINIB
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small Molecule

FDA Approval not approved

Publications:

NCI: ERLOTINIB

Version: 14-September-2017

Alternate Names:

C2693 NCI drug code

Drug Info:

Publications:

Morgillo et al., 2006, Heterodimerization of insulin-like growth factor receptor/epidermal growth factor receptor and induction of survivin expression counteract the antitumor action of erlotinib., Cancer Res.

Li et al., 2007, Differential metabolism of gefitinib and erlotinib by human cytochrome P450 enzymes., Clin. Cancer Res.

NCI: OSI-774

Version: 14-September-2017

Alternate Names:

C2693 NCI drug code

Drug Info:

Publications:

Marchetti et al., 2008, Effect of the ATP-binding cassette drug transporters ABCB1, ABCG2, and ABCC2 on erlotinib hydrochloride (Tarceva) disposition in in vitro and in vivo pharmacokinetic studies employing Bcrp1-/-/Mdr1a/1b-/- (triple-knockout) and wild-type mice., Mol. Cancer Ther.

DTC: ERLOTINIB

Version: 02-September-2020

Alternate Names:

CHEMBL553 ChEMBL Drug ID

Drug Info:

Publications:

Ban HS et al., 2010, Enhancement of EGFR tyrosine kinase inhibition by C-C multiple bonds-containing anilinoquinazolines., Bioorg Med Chem

Ji X et al., 2014, Design, synthesis and biological evaluation of novel 6-alkenylamides substituted of 4-anilinothieno[2,3-d]pyrimidines as irreversible epidermal growth factor receptor inhibitors., Bioorg Med Chem

DoCM: ERLOTINIB

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

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

Rajasekaran et al., 2010, In silico identification of significant detrimental missense mutations of EGFR and their effect with 4-anilinoquinazoline-based drugs., Appl. Biochem. Biotechnol.

Miller et al., 2012, Afatinib versus placebo for patients with advanced, metastatic non-small-cell lung cancer after failure of erlotinib, gefitinib, or both, and one or two lines of chemotherapy (LUX-Lung 1): a phase 2b/3 randomised trial., Lancet Oncol.

JAX-CKB: Erlotinib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Horn et al., 2016, High-Order Drug Combinations Are Required to Effectively Kill Colorectal Cancer Cells., Cancer Res.

Bahcall et al., 2016, Acquired METD1228V Mutation and Resistance to MET Inhibition in Lung Cancer., Cancer Discov

Rosen et al., 2017, A First-in-Human Phase I Study of a Bivalent MET Antibody, Emibetuzumab (LY2875358), as Monotherapy and in Combination with Erlotinib in Advanced Cancer., Clin. Cancer Res.

PharmGKB: erlotinib

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Choi HG et al., 2015, Pharmacokinetic properties of two erlotinib 150 mg formulations with a genetic effect evaluation in healthy Korean subjects., Clin Drug Investig

Li Y et al., 2011, Genetic variations in multiple drug action pathways and survival in advanced stage non-small cell lung cancer treated with chemotherapy., Clin Cancer Res

Puyo S et al., 2008, Impact of EGFR gene polymorphisms on anticancer drug cytotoxicity in vitro., Mol Diagn Ther

CIViC: ERLOTINIB

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

Yang et al., 2012, Antitumor activity of BRAF inhibitor vemurafenib in preclinical models of BRAF-mutant colorectal cancer., Cancer Res.

de Gunst et al., 2007, Functional analysis of cancer-associated EGFR mutants using a cellular assay with YFP-tagged EGFR intracellular domain., Mol. Cancer

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

TALC: ERLOTINIB
- Version: 12-May-2016
Alternate Names:

ERLOTINIB Primary Drug Name

ERLOTINIB Drug Generic Name

TARCEVA Drug Trade Name

Drug Info:

Publications:
TTD: Erlotinib
- Version: 2020.06.01
Alternate Names:

D07POC TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL553
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ClearityFoundationBiomarkers: ERLOTINIB
- Version: 26-July-2013
Alternate Names:

Drug Info:

Publications:
FDA: Erlotinib
- Version: 04-September-2020
Alternate Names:

Drug Info:

Publications:
OncoKB: Erlotinib
- Version: 23-July-2020
Alternate Names:

Drug Info:

Publications:
ClearityFoundationClinicalTrial: ERLOTINIB
- Version: 15-June-2013
Alternate Names:

Drug Info:

Publications:
COSMIC: Erlotinib
- Version: 4-Sep-2020
Alternate Names:

Drug Info:

Publications:

combination therapy	MGCD265 + Erlotinib
Approval Status	Phase III
combination therapy	AUY922 + Erlotinib

Clinical Status	case report
Pathway	activation
Variant Effect	gain-of-function

combination therapy	Erlotinib + Selumetinib
Indication/Tumor Type	pancreatic ductal adenocarcinoma
Response Type	sensitive

Evidence Type	Emerging
Approval Status	Preclinical - Cell line xenograft
Response Type	predicted – sensitive

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

combination therapy	Erlotinib + Ibuprofen
Indication/Tumor Type	colorectal cancer
Response Type	sensitive

combination therapy	ABT-263 + Alpelisib + Erlotinib + Trametinib
Indication/Tumor Type	colorectal cancer
Response Type	sensitive

combination therapy	Erlotinib + PLX4720
Indication/Tumor Type	melanoma
Response Type	sensitive

combination therapy	Onartuzumab + Erlotinib
Indication/Tumor Type	non-small cell lung carcinoma
Response Type	conflicting

Indication/Tumor Type	lung adenocarcinoma
Response Type	resistant
Approval Status	Clinical Study

antagonist (inhibitory)
inhibitor (inhibitory)

combination therapy	ABT-263 + Alpelisib + Dabrafenib + Erlotinib
Indication/Tumor Type	colorectal cancer
Response Type	sensitive

Erlotinib	PubChem Drug Name
176870	PubChem Drug ID
Tarceva	Drug Trade Name

OSI-774	Development Name
CP-258	Development Name
774	Development Name

ERLOTINIB	Primary Drug Name
ERLOTINIB	Drug Generic Name
TARCEVA	Drug Trade Name

ERLOTINIB Drug Record

ERLOTINIB chembl:CHEMBL553 ApprovedAntineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24550739

Sources: CIViC

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

Interaction Info: combination therapy MGCD265 + Erlotinib Approval Status Phase III combination therapy AUY922 + Erlotinib

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

Interaction Types & Directionality: n/a

Interaction Info: Clinical Status case report Pathway activation Variant Effect gain-of-function

PMIDs: 22328973 23932362 18938156

Sources: DoCM CIViC

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Erlotinib + Selumetinib Indication/Tumor Type pancreatic ductal adenocarcinoma Response Type sensitive

PMIDs: 26251290

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: Evidence Type Emerging Approval Status Preclinical - Cell line xenograft Response Type predicted – sensitive

PMIDs: 25348515

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 21636554

Sources: PharmGKB

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: DTC JAX-CKB PharmGKB

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Erlotinib + Ibuprofen Indication/Tumor Type colorectal cancer Response Type sensitive

PMIDs: 17909047

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: combination therapy ABT-263 + Alpelisib + Erlotinib + Trametinib Indication/Tumor Type colorectal cancer Response Type sensitive

PMIDs: 21969500 21258250 19794967 23313110 15696205 21862683 18626007 16043828 27480147 27659046

Sources: ClearityFoundationBiomarkers JAX-CKB CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 29802158

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 31027687

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Erlotinib + PLX4720 Indication/Tumor Type melanoma Response Type sensitive

PMIDs: 27659046 22448344 27924459 22180495

Sources: JAX-CKB CIViC

Interaction Types & Directionality: n/a

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

PMIDs: 27694386 27803065 24101053

Sources: DTC JAX-CKB OncoKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 17047074

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality:

n/a

PMIDs:
24550739

Sources:
CIViC

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

combination therapy MGCD265 + Erlotinib

Approval Status Phase III

combination therapy AUY922 + Erlotinib

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

Interaction Types & Directionality:

n/a

Interaction Info:

Clinical Status case report

Pathway activation

Variant Effect gain-of-function

PMIDs:
22328973 23932362 18938156

Sources:
DoCM CIViC

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Erlotinib + Selumetinib

Indication/Tumor Type pancreatic ductal adenocarcinoma

Response Type sensitive

PMIDs:
26251290

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Emerging

Approval Status Preclinical - Cell line xenograft

Response Type predicted – sensitive

PMIDs:
25348515

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

PMIDs:
21636554

Sources:
PharmGKB

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:
DTC JAX-CKB PharmGKB

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Erlotinib + Ibuprofen

Indication/Tumor Type colorectal cancer

Response Type sensitive

PMIDs:
17909047

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy ABT-263 + Alpelisib + Erlotinib + Trametinib

Indication/Tumor Type colorectal cancer

Response Type sensitive

PMIDs:
21969500 21258250 19794967 23313110 15696205 21862683 18626007 16043828 27480147 27659046

Sources:
ClearityFoundationBiomarkers JAX-CKB CIViC

Interaction Types & Directionality:

n/a

PMIDs:
29802158

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
31027687

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Erlotinib + PLX4720

Indication/Tumor Type melanoma

Response Type sensitive

PMIDs:
27659046 22448344 27924459 22180495

Sources:
JAX-CKB CIViC

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Onartuzumab + Erlotinib

Indication/Tumor Type non-small cell lung carcinoma

Response Type conflicting

PMIDs:
27694386 27803065 24101053

Sources:
DTC JAX-CKB OncoKB

Interaction Types & Directionality:

n/a

PMIDs:
17047074

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
18723475

Sources:
NCI