DGIdb - GEFITINIB Drug Record

GEFITINIB chembl:CHEMBL939 ApprovedAntineoplastic

Alternate Names:

ZD-1839
IRESSA
GEFITINIB
N-(3-CHLORO-4-FLUOROPHENYL)-7-METHOXY-6-(3-(4-MORPHOLINYL)PROPOXY)-4-QUINAZOLINAMINE
IRESSA®
ZD1839
ZD 1839
4-(3'-CHLORO-4'-FLUOROANILINO)-7-METHOXY-6-(3-MORPHOLINOPROPOXY)QUINAZOLINE
rxcui:328134
chemidplus:184475-35-2
drugbank:00317
pubchem.compound:123631
chembl:CHEMBL939

Drug Info:

FDA Approval	approved
Drug Class	Small Molecule
Drug Indications	antineoplastic agent
Drug Class	antineoplastic agents, protein kinase inhibitors
Year of Approval	2003
FDA Approval	Non-small cell lung cancer (with EGFR exon 19 deletions or exon 21 substitution (L858R) mutations)
Drug Class	Kinase Inhibitors
Drug Categories	cytochrome p-450 cyp2c19 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 cyp2c9 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 cyp3a inhibitors
Drug Categories	cytochrome p-450 cyp3a substrates
Drug Categories	cytochrome p-450 cyp3a4 inhibitors
Drug Categories	cytochrome p-450 cyp3a4 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 cyp3a5 substrates
Drug Categories	cytochrome p-450 enzyme inhibitors
Drug Categories	cytochrome p-450 substrates
Drug Categories	heterocyclic compounds, fused-ring
Drug Categories	kinase inhibitor
Drug Categories	p-glycoprotein inhibitors
Drug Categories	p-glycoprotein substrates
Drug Categories	quinazolines
Drug Categories	tyrosine kinase inhibitors

(18 More Sources)

Publications:

Liang et al., 2014, Network meta-analysis of erlotinib, gefitinib, afatinib and icotinib in patients with advanced non-small-cell lung cancer harboring EGFR mutations., PLoS ONE
Chen et al., 2016, Clinical efficacy of first-generation EGFR-TKIs in patients with advanced non-small-cell lung cancer harboring EGFR exon 20 mutations., Onco Targets Ther
Ludovini V et al., 2011, Phosphoinositide-3-kinase catalytic alpha and KRAS mutations are important predictors of resistance to therapy with epidermal growth factor receptor tyrosine kinase inhibitors in patients with advanced non-small cell lung cancer., J Thorac Oncol
Lin et al., 2017, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor-sensitive Exon 19 Insertion and Exon 20 Insertion in Patients With Advanced Non-Small-cell Lung Cancer., Clin Lung Cancer
Funke S et al., 2008, Pharmacogenetics in colorectal cancer: a systematic review., Pharmacogenomics
Liu G et al., 2008, Epidermal growth factor receptor polymorphisms and clinical outcomes in non-small-cell lung cancer patients treated with gefitinib., Pharmacogenomics J
Yu et al., 2013, Analysis of tumor specimens at the time of acquired resistance to EGFR-TKI therapy in 155 patients with EGFR-mutant lung cancers., Clin. Cancer Res.
Zhang X et al., 2017, EGFR gene copy number as a predictive/biomarker for patients with non-small-cell lung cancer receiving tyrosine kinase inhibitor treatment: a systematic review and meta-analysis., J Investig Med
Han et al., 2012, First-SIGNAL: first-line single-agent iressa versus gemcitabine and cisplatin trial in never-smokers with adenocarcinoma of the lung., J. Clin. Oncol.
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
Zhang D et al., 2013, Synthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors., Bioorg Med Chem
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
Hirsch FR et al., 2007, Combination of EGFR gene copy number and protein expression predicts outcome for advanced non-small-cell lung cancer patients treated with gefitinib., Ann Oncol
Ciardiello et al., 2000, Antitumor effect and potentiation of cytotoxic drugs activity in human cancer cells by ZD-1839 (Iressa), an epidermal growth factor receptor-selective tyrosine kinase inhibitor., Clin. Cancer Res.
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
Takeuchi et al., 2012, Dual inhibition of Met kinase and angiogenesis to overcome HGF-induced EGFR-TKI resistance in EGFR mutant lung cancer., Am. J. Pathol.
Vermorken JB et al., 2008, Platinum-based chemotherapy plus cetuximab in head and neck cancer., N Engl J Med
Ban HS et al., 2010, Enhancement of EGFR tyrosine kinase inhibition by C-C multiple bonds-containing anilinoquinazolines., Bioorg Med Chem
Kosaka T et al., 2006, Analysis of epidermal growth factor receptor gene mutation in patients with non-small cell lung cancer and acquired resistance to gefitinib., Clin Cancer Res
Albanell et al., 2001, Activated extracellular signal-regulated kinases: association with epidermal growth factor receptor/transforming growth factor alpha expression in head and neck squamous carcinoma and inhibition by anti-epidermal growth factor receptor treatments., Cancer Res.
Murray et al., 2010, Screening for EGFR Mutations in Patients with Head and Neck Cancer Treated with Gefitinib on a Compassionate-Use Program: A Hellenic Cooperative Oncology Group Study., J Oncol
Koole et al., 2016, FGFR1 Is a Potential Prognostic Biomarker and Therapeutic Target in Head and Neck Squamous Cell Carcinoma., Clin. Cancer Res.
Yang JC et al., 2020, A Randomized Phase 2 Study of Gefitinib With or Without Pemetrexed as First-line Treatment in Nonsquamous NSCLC With EGFR Mutation: Final Overall Survival and Biomarker Analysis., J Thorac Oncol
Geoerger B et al., 2008, EGFR tyrosine kinase inhibition radiosensitizes and induces apoptosis in malignant glioma and childhood ependymoma xenografts., Int J Cancer
Tiseo M et al., 2010, Predictors of gefitinib outcomes in advanced non-small cell lung cancer (NSCLC): study of a comprehensive panel of molecular markers., Lung Cancer
Niu et al., 2014, Novel agents and strategies for overcoming EGFR TKIs resistance., Exp Hematol Oncol
Nakamura T et al., 2011, A noninvasive system for monitoring resistance to epidermal growth factor receptor tyrosine kinase inhibitors with plasma DNA., J Thorac Oncol
Chang et al., Early radiographic response to epidermal growth factor receptor-tyrosine kinase inhibitor in non-small cell lung cancer patients with epidermal growth factor receptor mutations: A prospective study., Biomed J
Inukai et al., 2006, Presence of epidermal growth factor receptor gene T790M mutation as a minor clone in non-small cell lung cancer., Cancer Res.
Onitsuka T et al., 2010, Acquired resistance to gefitinib: the contribution of mechanisms other than the T790M, MET, and HGF status., Lung Cancer
Lewis et al., 2012, A phase II study of gefitinib for aggressive cutaneous squamous cell carcinoma of the head and neck., Clin. Cancer Res.
Moasser et al., 2001, The tyrosine kinase inhibitor ZD1839 ("Iressa") inhibits HER2-driven signaling and suppresses the growth of HER2-overexpressing tumor cells., Cancer Res.
Engelman et al., 2007, MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling., Science
Kobayashi et al., 2005, EGFR mutation and resistance of non-small-cell lung cancer to gefitinib., N. Engl. J. Med.
Maemondo et al., 2010, Gefitinib or chemotherapy for non-small-cell lung cancer with mutated EGFR., N. Engl. J. Med.
Bell et al., 2005, Inherited susceptibility to lung cancer may be associated with the T790M drug resistance mutation in EGFR., Nat. Genet.
Mok et al., 2009, Gefitinib or carboplatin-paclitaxel in pulmonary adenocarcinoma., N. Engl. J. Med.
Paez et al., 2004, EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy., Science
Yun et al., 2008, The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP., Proc. Natl. Acad. Sci. U.S.A.
Rho et al., 2014, MET and AXL inhibitor NPS-1034 exerts efficacy against lung cancer cells resistant to EGFR kinase inhibitors because of MET or AXL activation., Cancer Res.
Dahabreh et al., 2011, EGFR gene copy number as a predictive biomarker for patients receiving tyrosine kinase inhibitor treatment: a systematic review and meta-analysis in non-small-cell lung cancer., Ann. Oncol.
Oizumi S et al., 2012, Quality of life with gefitinib in patients with EGFR-mutated non-small cell lung cancer: quality of life analysis of North East Japan Study Group 002 Trial., Oncologist
Ichihara S et al., 2007, The impact of epidermal growth factor receptor gene status on gefitinib-treated Japanese patients with non-small-cell lung cancer., Int J Cancer
Niederst et al., 2015, The Allelic Context of the C797S Mutation Acquired upon Treatment with Third-Generation EGFR Inhibitors Impacts Sensitivity to Subsequent Treatment Strategies., Clin. Cancer Res.
Okada-Iwasaki et al., 2016, The Discovery and Characterization of K-756, a Novel Wnt/β-Catenin Pathway Inhibitor Targeting Tankyrase., Mol. Cancer Ther.
Tomizawa Y et al., 2005, Clinicopathologic significance of the mutations of the epidermal growth factor receptor gene in patients with non-small cell lung cancer., Clin Cancer Res
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
Han SW et al., 2007, Intron 1 CA dinucleotide repeat polymorphism and mutations of epidermal growth factor receptor and gefitinib responsiveness in non-small-cell lung cancer., Pharmacogenet Genomics
Dziadziuszko et al., 2006, Epidermal growth factor receptor messenger RNA expression, gene dosage, and gefitinib sensitivity in non-small cell lung cancer., Clin. Cancer Res.
Rakhit A et al., 2008, The effects of CYP3A4 inhibition on erlotinib pharmacokinetics: computer-based simulation (SimCYP) predicts in vivo metabolic inhibition., Eur J Clin Pharmacol
Goss et al., 2013, Gefitinib versus placebo in completely resected non-small-cell lung cancer: results of the NCIC CTG BR19 study., J. Clin. Oncol.
Wang et al., 2012, Phosphorylated EGFR expression may predict outcome of EGFR-TKIs therapy for the advanced NSCLC patients with wild-type EGFR., J. Exp. Clin. Cancer Res.
Balak et al., 2006, Novel D761Y and common secondary T790M mutations in epidermal growth factor receptor-mutant lung adenocarcinomas with acquired resistance to kinase inhibitors., Clin. Cancer Res.
Verma et al., 2017, Targeting of PYK2 Synergizes with EGFR Antagonists in Basal-like TNBC and Circumvents HER3-Associated Resistance via the NEDD4-NDRG1 Axis., Cancer Res.
Yasuda et al., 2013, Structural, biochemical, and clinical characterization of epidermal growth factor receptor (EGFR) exon 20 insertion mutations in lung cancer., Sci Transl Med
Kim et al., 2015, Differential Effects of Tyrosine Kinase Inhibitors on Normal and Oncogenic EGFR Signaling and Downstream Effectors., Mol. Cancer Res.
Otsuka et al., 2015, Effectiveness of Tyrosine Kinase Inhibitors in Japanese Patients with Non-small Cell Lung Cancer Harboring Minor Epidermal Growth Factor Receptor Mutations: Results from a Multicenter Retrospective Study (HANSHIN Oncology Group 0212)., Anticancer Res.
Jonker et al., 2007, Cetuximab for the treatment of colorectal cancer., N. Engl. J. Med.
Eberlein et al., 2015, Acquired Resistance to the Mutant-Selective EGFR Inhibitor AZD9291 Is Associated with Increased Dependence on RAS Signaling in Preclinical Models., Cancer Res.
Lim et al., 2014, Comparison of clinical outcomes following gefitinib and erlotinib treatment in non-small-cell lung cancer patients harboring an epidermal growth factor receptor mutation in either exon 19 or 21., J Thorac Oncol
Pao et al., 2004, EGF receptor gene mutations are common in lung cancers from "never smokers" and are associated with sensitivity of tumors to gefitinib and erlotinib., Proc. Natl. Acad. Sci. U.S.A.
Ma et al., 2011, T790M and acquired resistance of EGFR TKI: a literature review of clinical reports., J Thorac Dis
Chen HJ et al., 2009, Clinicopathologic and molecular features of epidermal growth factor receptor T790M mutation and c-MET amplification in tyrosine kinase inhibitor-resistant Chinese non-small cell lung cancer., Pathol Oncol Res
Costa et al., 2008, Effects of erlotinib in EGFR mutated non-small cell lung cancers with resistance to gefitinib., Clin. Cancer Res.
Wu YL et al., 2007, Epidermal growth factor receptor mutations and their correlation with gefitinib therapy in patients with non-small cell lung cancer: a meta-analysis based on updated individual patient data from six medical centers in mainland China., J Thorac Oncol
Yun et al., 2007, Structures of lung cancer-derived EGFR mutants and inhibitor complexes: mechanism of activation and insights into differential inhibitor sensitivity., Cancer Cell
Nicholson et al., 2001, Modulation of epidermal growth factor receptor in endocrine-resistant, oestrogen receptor-positive breast cancer., Endocr. Relat. Cancer
Chou et al., 2005, Mutation in the tyrosine kinase domain of epidermal growth factor receptor is a predictive and prognostic factor for gefitinib treatment in patients with non-small cell lung cancer., Clin. Cancer Res.
Mellinghoff et al., 2005, Molecular determinants of the response of glioblastomas to EGFR kinase inhibitors., N. Engl. J. Med.
Ma et al., 2016, InsR/IGF1R Pathway Mediates Resistance to EGFR Inhibitors in Glioblastoma., Clin. Cancer Res.
Arteaga et al., 2001, Tyrosine kinase inhibitors-ZD1839 (Iressa)., Curr Opin Oncol
Fukuoka et al., 2003, Multi-institutional randomized phase II trial of gefitinib for previously treated patients with advanced non-small-cell lung cancer (The IDEAL 1 Trial) [corrected]., J. Clin. Oncol.
Su et al., 2012, Pretreatment epidermal growth factor receptor (EGFR) T790M mutation predicts shorter EGFR tyrosine kinase inhibitor response duration in patients with non-small-cell lung cancer., J. Clin. Oncol.
Sheng M et al., 2016, Comparison of clinical outcomes of patients with non-small-cell lung cancer harbouring epidermal growth factor receptor exon 19 or exon 21 mutations after tyrosine kinase inhibitors treatment: a meta-analysis., Eur J Clin Pharmacol
Della Corte et al., 2015, SMO Gene Amplification and Activation of the Hedgehog Pathway as Novel Mechanisms of Resistance to Anti-Epidermal Growth Factor Receptor Drugs in Human Lung Cancer., Clin. Cancer Res.
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
Yeh et al., 2013, DNA-Mutation Inventory to Refine and Enhance Cancer Treatment (DIRECT): a catalog of clinically relevant cancer mutations to enable genome-directed anticancer therapy., Clin. Cancer Res.
Goto K et al., 2012, Epidermal growth factor receptor mutation status in circulating free DNA in serum: from IPASS, a phase III study of gefitinib or carboplatin/paclitaxel in non-small cell lung cancer., J Thorac Oncol
Foster et al., 2010, Clinical implications of novel activating EGFR mutations in malignant peritoneal mesothelioma., World J Surg Oncol
Xu JM et al., 2009, EGFR mutations and HER2/3 protein expression and clinical outcome in Chinese advanced non-small cell lung cancer patients treated with gefitinib., J Cancer Res Clin Oncol
Douillard et al., 2010, Molecular predictors of outcome with gefitinib and docetaxel in previously treated non-small-cell lung cancer: data from the randomized phase III INTEREST trial., J. Clin. Oncol.
Endo K et al., 2006, Evaluation of the epidermal growth factor receptor gene mutation and copy number in non-small cell lung cancer with gefitinib therapy., Oncol Rep
Lou et al., 2014, Combination of gefitinib and DNA methylation inhibitor decitabine exerts synergistic anti-cancer activity in colon cancer cells., PLoS ONE
Yang et al., 2001, Development of ABX-EGF, a fully human anti-EGF receptor monoclonal antibody, for cancer therapy., Crit. Rev. Oncol. Hematol.
Sequist et al., 2007, Response to treatment and survival of patients with non-small cell lung cancer undergoing somatic EGFR mutation testing., Oncologist
Lynch et al., 2004, Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib., N. Engl. J. Med.
Mitsudomi et al., 2010, Gefitinib versus cisplatin plus docetaxel in patients with non-small-cell lung cancer harbouring mutations of the epidermal growth factor receptor (WJTOG3405): an open label, randomised phase 3 trial., Lancet Oncol.
Taron et al., 2005, Activating mutations in the tyrosine kinase domain of the epidermal growth factor receptor are associated with improved survival in gefitinib-treated chemorefractory lung adenocarcinomas., Clin. Cancer Res.
Yang et al., 2011, Good response to gefitinib in a lung adenocarcinoma harboring a heterozygous complex mutation of L833V and H835L in epidermal growth factor receptor gene., J. Clin. Oncol.
Van Cutsem et al., 2009, Cetuximab and chemotherapy as initial treatment for metastatic colorectal cancer., N. Engl. J. Med.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Giusti RM et al., 2008, U.S. Food and Drug Administration approval: panitumumab for epidermal growth factor receptor-expressing metastatic colorectal carcinoma with progression following fluoropyrimidine-, oxaliplatin-, and irinotecan-containing chemotherapy regimens., Clin Cancer Res
Ercan et al., 2015, EGFR Mutations and Resistance to Irreversible Pyrimidine-Based EGFR Inhibitors., Clin. Cancer Res.
Ma F et al., 2009, Polymorphisms of EGFR predict clinical outcome in advanced non-small-cell lung cancer patients treated with Gefitinib., Lung Cancer
Peters et al., 2012, Metastatic non-small-cell lung cancer (NSCLC): ESMO Clinical Practice Guidelines for diagnosis, treatment and follow-up., Ann. Oncol.
Cho SH et al., 2012, Efficacy of EGFR tyrosine kinase inhibitors for non-adenocarcinoma NSCLC patients with EGFR mutation., Cancer Chemother Pharmacol
Bell DW et al., 2005, Epidermal growth factor receptor mutations and gene amplification in non-small-cell lung cancer: molecular analysis of the IDEAL/INTACT gefitinib trials., J Clin Oncol
Kancha et al., 2009, Functional analysis of epidermal growth factor receptor (EGFR) mutations and potential implications for EGFR targeted therapy., Clin. Cancer Res.
Yang et al., 2008, Specific EGFR mutations predict treatment outcome of stage IIIB/IV patients with chemotherapy-naive non-small-cell lung cancer receiving first-line gefitinib monotherapy., J. Clin. Oncol.
Han SW et al., 2006, Clinical predictors versus epidermal growth factor receptor mutation in gefitinib-treated non-small-cell lung cancer patients., Lung Cancer
Nie Q et al., 2007, The epidermal growth factor receptor intron1 (CA) n microsatellite polymorphism is a potential predictor of treatment outcome in patients with advanced lung cancer treated with Gefitinib., Eur J Pharmacol
Fukihara et al., 2014, Clinical predictors of response to EGFR tyrosine kinase inhibitors in patients with EGFR-mutant non-small cell lung cancer., Oncology
Jorissen RN et al., 2003, Epidermal growth factor receptor: mechanisms of activation and signalling., Exp Cell Res
Szerlip et al., 2012, Intratumoral heterogeneity of receptor tyrosine kinases EGFR and PDGFRA amplification in glioblastoma defines subpopulations with distinct growth factor response., Proc. Natl. Acad. Sci. U.S.A.
Oddo et al., 2016, Molecular Landscape of Acquired Resistance to Targeted Therapy Combinations in BRAF-Mutant Colorectal Cancer., Cancer Res.
Pao et al., 2005, Acquired resistance of lung adenocarcinomas to gefitinib or erlotinib is associated with a second mutation in the EGFR kinase domain., PLoS Med.
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.
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.
Sugio K et al., 2009, Prospective phase II study of gefitinib in non-small cell lung cancer with epidermal growth factor receptor gene mutations., Lung Cancer
Udager et al., 2015, High-Frequency Targetable EGFR Mutations in Sinonasal Squamous Cell Carcinomas Arising from Inverted Sinonasal Papilloma., Cancer Res.
Shien et al., 2013, Acquired resistance to EGFR inhibitors is associated with a manifestation of stem cell-like properties in cancer cells., Cancer Res.
Belchis et al., 2016, Heterogeneity of resistance mutations detectable by nextgeneration sequencing in TKI-treated lung adenocarcinoma., Oncotarget
Yamaoka et al., 2016, Acquired Resistance Mechanisms to Combination Met-TKI/EGFR-TKI Exposure in Met-Amplified EGFR-TKI-Resistant Lung Adenocarcinoma Harboring an Activating EGFR Mutation., Mol. Cancer Ther.
Liu G et al., 2012, Pharmacogenetic analysis of BR.21, a placebo-controlled randomized phase III clinical trial of erlotinib in advanced non-small cell lung cancer., J Thorac Oncol
Wu et al., 2011, Effectiveness of tyrosine kinase inhibitors on "uncommon" epidermal growth factor receptor mutations of unknown clinical significance in non-small cell lung cancer., Clin. Cancer Res.
Carmi C et al., 2010, Novel irreversible epidermal growth factor receptor inhibitors by chemical modulation of the cysteine-trap portion., J Med Chem
Jackman et al., 2006, Exon 19 deletion mutations of epidermal growth factor receptor are associated with prolonged survival in non-small cell lung cancer patients treated with gefitinib or erlotinib., Clin. Cancer Res.
Yu H et al., 2014, A phase II randomized trial evaluating gefitinib intercalated with pemetrexed/platinum chemotherapy or pemetrexed/platinum chemotherapy alone in unselected patients with advanced non-squamous non-small cell lung cancer., Cancer Biol Ther
Mayo C et al., 2012, Pharmacogenetics of EGFR in lung cancer: perspectives and clinical applications., Pharmacogenomics
Ji et al., 2006, The impact of human EGFR kinase domain mutations on lung tumorigenesis and in vivo sensitivity to EGFR-targeted therapies., Cancer Cell
Pao et al., 2005, KRAS mutations and primary resistance of lung adenocarcinomas to gefitinib or erlotinib., PLoS Med.
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
Manchado et al., 2016, A combinatorial strategy for treating KRAS-mutant lung cancer., Nature
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
Xin S et al., 2020, Polymorphisms of NF-κB pathway genes influence adverse drug reactions of gefitinib in NSCLC patients., Pharmacogenomics J
Mitsudomi et al., 2005, Mutations of the epidermal growth factor receptor gene predict prolonged survival after gefitinib treatment in patients with non-small-cell lung cancer with postoperative recurrence., J. Clin. Oncol.
Ehmann F et al., 2014, European Medicines Agency initiatives and perspectives on pharmacogenomics., Br J Clin Pharmacol
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
Li et al., 2007, Differential metabolism of gefitinib and erlotinib by human cytochrome P450 enzymes., Clin. Cancer Res.
Girotti et al., 2013, Inhibiting EGF receptor or SRC family kinase signaling overcomes BRAF inhibitor resistance in melanoma., Cancer Discov
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
Prahallad et al., 2012, Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR., Nature
Kobayashi H et al., 2015, Relationship Among Gefitinib Exposure, Polymorphisms of Its Metabolizing Enzymes and Transporters, and Side Effects in Japanese Patients With Non-Small-Cell Lung Cancer., Clin Lung Cancer
Lemos C et al., 2011, Impact of ABCG2 polymorphisms on the clinical outcome and toxicity of gefitinib in non-small-cell lung cancer patients., Pharmacogenomics
Akasaka K et al., 2010, Impact of functional ABCG2 polymorphisms on the adverse effects of gefitinib in Japanese patients with non-small-cell lung cancer., Cancer Chemother Pharmacol
Cusatis G et al., 2006, Pharmacogenetics of ABCG2 and adverse reactions to gefitinib., J Natl Cancer Inst
Li et al., 2016, TOPK promotes lung cancer resistance to EGFR tyrosine kinase inhibitors by phosphorylating and activating c-Jun., Oncotarget
Desbois-Mouthon et al., 2006, Impact of IGF-1R/EGFR cross-talks on hepatoma cell sensitivity to gefitinib., Int. J. Cancer
Sun et al., 2014, Intrinsic resistance to MEK inhibition in KRAS mutant lung and colon cancer through transcriptional induction of ERBB3., Cell Rep
Leggas et al., 2006, Gefitinib modulates the function of multiple ATP-binding cassette transporters in vivo., Cancer Res.
Ma Y et al., 2017, Determinants of Gefitinib toxicity in advanced non-small cell lung cancer (NSCLC): a pharmacogenomic study of metabolic enzymes and transporters., Pharmacogenomics J
Ozvegy-Laczka et al., 2004, High-affinity interaction of tyrosine kinase inhibitors with the ABCG2 multidrug transporter., Mol. Pharmacol.
Judde et al., 2007, Gefitinib and chemotherapy combination studies in five novel human non small cell lung cancer xenografts. Evidence linking EGFR signaling to gefitinib antitumor response., Int. J. Cancer
Suzawa et al., 2016, Antitumor effect of afatinib, as a human epidermal growth factor receptor 2-targeted therapy, in lung cancers harboring HER2 oncogene alterations., Cancer Sci.
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Piechocki et al., 2007, Breast cancer expressing the activated HER2/neu is sensitive to gefitinib in vitro and in vivo and acquires resistance through a novel point mutation in the HER2/neu., Cancer Res.
Erjala et al., 2006, Signaling via ErbB2 and ErbB3 associates with resistance and epidermal growth factor receptor (EGFR) amplification with sensitivity to EGFR inhibitor gefitinib in head and neck squamous cell carcinoma cells., Clin. Cancer Res.
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GEFITINIB EMP1

Interaction Score: 1.67

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16087880

Sources:
NCI
GEFITINIB NFKBIB

Interaction Score: 1.67

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
31664190

Sources:
PharmGKB
GEFITINIB TAB2

Interaction Score: 1.67

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
31664190

Sources:
PharmGKB
GEFITINIB CRKL

Interaction Score: 0.84

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22586683

Sources:
CIViC
GEFITINIB EGFR

Interaction Score: 0.65

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Direct Interaction? False

Endogenous Drug? False

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

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

Interaction Score: 0.33

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26745678

Sources:
CIViC
GEFITINIB CEACAM5

Interaction Score: 0.33

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15738541

Sources:
NCI
GEFITINIB SIRT2

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
31664190

Sources:
PharmGKB
GEFITINIB SMO

Interaction Score: 0.17

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Gefitinib + Sonidegib

Indication/Tumor Type non-small cell lung carcinoma

Response Type sensitive

PMIDs:
26124204

Sources:
JAX-CKB CIViC
GEFITINIB NFKBIA

Interaction Score: 0.15

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
31664190

Sources:
PharmGKB
GEFITINIB MAP3K1

Interaction Score: 0.15

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21636554

Sources:
PharmGKB
GEFITINIB IKBKE

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
31664190

Sources:
PharmGKB
GEFITINIB IGF2

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16988945

Sources:
NCI
GEFITINIB ERBB3

Interaction Score: 0.11

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
24685132

Sources:
MyCancerGenomeClinicalTrial PharmGKB CIViC
GEFITINIB NR1H2

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
31664190

Sources:
PharmGKB
GEFITINIB SIK2

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GEFITINIB PHKG2

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GEFITINIB ABCG2

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25554506 21332310 20035425 17148776

Sources:
PharmGKB
GEFITINIB IKBKB

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
31664190

Sources:
PharmGKB
GEFITINIB MET

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

Approval Status Preclinical - Cell culture

combination therapy Gefitinib + NPS-1034

Approval Status Preclinical - Cell line xenograft

PMIDs:
23993328 17463250 24165158 23542356 27612490

Sources:
DTC OncoKB JAX-CKB CIViC
GEFITINIB ERBB4

Interaction Score: 0.06

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial DTC PharmGKB
GEFITINIB HIPK4

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GEFITINIB KRAS

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Gefitinib + Trametinib

Indication/Tumor Type lung cancer

Response Type no benefit

PMIDs:
21258250 15696205 19794967 27338794 25870145 23313110

Sources:
ClearityFoundationBiomarkers JAX-CKB CIViC
GEFITINIB ERBB2

Interaction Score: 0.05

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type breast cancer

Response Type resistant

Approval Status Preclinical

PMIDs:
26545934 23220880 17638894 20151670 16818711

Sources:
MyCancerGenomeClinicalTrial NCI DTC PharmGKB JAX-CKB
GEFITINIB BRAF

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

combination therapy Gefitinib + PLX4720

Evidence Type Actionable

PMIDs:
23242808 22448344 22281684 27312529

Sources:
JAX-CKB CIViC
GEFITINIB MKNK2

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GEFITINIB CAMK2D

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GEFITINIB PIM3

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GEFITINIB PTEN

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Gefitinib + Linsitinib

Indication/Tumor Type glioblastoma multiforme

Response Type sensitive

PMIDs:
16282176 26561558

Sources:
ClearityFoundationBiomarkers JAX-CKB CIViC
GEFITINIB BRSK1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GEFITINIB IRAK1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GEFITINIB IRAK4

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GEFITINIB CAMK2G

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GEFITINIB TNK2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
GEFITINIB CSNK1D

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GEFITINIB NRAS

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type non-small cell lung carcinoma

Response Type resistant

Approval Status Preclinical

PMIDs:
25870145

Sources:
JAX-CKB
GEFITINIB MAPK8

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17205515

Sources:
NCI
GEFITINIB HCK

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GEFITINIB LIMK1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GEFITINIB RELA

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
31664190

Sources:
PharmGKB
GEFITINIB FGFR2

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell culture

Response Type sensitive

PMIDs:
26936917

Sources:
JAX-CKB
GEFITINIB AXL

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GEFITINIB CHEK2

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GEFITINIB MINK1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GEFITINIB FRK

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GEFITINIB PRKD2

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GEFITINIB SLK

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GEFITINIB PDGFRA

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Gefitinib + Imatinib

Indication/Tumor Type glioblastoma multiforme

Response Type sensitive

PMIDs:
22323597

Sources:
JAX-CKB
GEFITINIB MAP4K5

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GEFITINIB MAPK9

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GEFITINIB PRKD3

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GEFITINIB BLK

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GEFITINIB MAP4K4

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GEFITINIB ABCB1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25554506 16651435 27089937 15155841

Sources:
NCI PharmGKB
GEFITINIB LYN

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GEFITINIB FGFR1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy AZD4547 + Gefitinib

Indication/Tumor Type head and neck squamous cell carcinoma

Response Type sensitive

PMIDs:
26936917

Sources:
JAX-CKB
GEFITINIB MAPK10

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GEFITINIB PIM1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GEFITINIB CYP3A5

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17575239

Sources:
NCI
GEFITINIB LCK

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GEFITINIB PIK3CA

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21258250

Sources:
CIViC
GEFITINIB FLT4

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GEFITINIB MAPK14

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GEFITINIB YES1

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GEFITINIB CYP2C9

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24433361

Sources:
PharmGKB
GEFITINIB MAPT

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GEFITINIB GMNN

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GEFITINIB CYP2D6

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
FDA

DrugBank: DB00317

Version: 5.1.7

Alternate Names:

GEFITINIB DrugBank Drug Name

184475-35-2 CAS Number

Apo-gefitinib Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups investigational

Publications:

Ciardiello et al., 2000, Antitumor effect and potentiation of cytotoxic drugs activity in human cancer cells by ZD-1839 (Iressa), an epidermal growth factor receptor-selective tyrosine kinase inhibitor., Clin. Cancer Res.

Albanell et al., 2001, Activated extracellular signal-regulated kinases: association with epidermal growth factor receptor/transforming growth factor alpha expression in head and neck squamous carcinoma and inhibition by anti-epidermal growth factor receptor treatments., Cancer Res.

Moasser et al., 2001, The tyrosine kinase inhibitor ZD1839 ("Iressa") inhibits HER2-driven signaling and suppresses the growth of HER2-overexpressing tumor cells., Cancer Res.

TEND: GEFITINIB
- Version: 01-August-2011
Alternate Names:

GEFITINIB Primary Drug Name

Drug Info:

Year of Approval 2003

Drug Class antineoplastic agents, protein kinase inhibitors

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

ZD1839 Development Name

GEFITINIB Generic Name

IRESSA Trade 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)

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

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small Molecule

FDA Approval approved

Publications:
NCI: ZD1839
- Version: 14-September-2017
Alternate Names:

C1855 NCI drug code

Drug Info:

Publications:

Ozvegy-Laczka et al., 2004, High-affinity interaction of tyrosine kinase inhibitors with the ABCG2 multidrug transporter., Mol. Pharmacol.

DTC: GEFITINIB

Version: 02-September-2020

Alternate Names:

CHEMBL939 ChEMBL Drug ID

Drug Info:

Publications:

Zhang D et al., 2013, Synthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors., Bioorg Med Chem

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

Carmi C et al., 2010, Novel irreversible epidermal growth factor receptor inhibitors by chemical modulation of the cysteine-trap portion., J Med Chem

NCI: GEFITINIB

Version: 14-September-2017

Alternate Names:

C1855 NCI drug code

Drug Info:

Publications:

Jain et al., 2005, Epithelial membrane protein-1 is a biomarker of gefitinib resistance., Proc. Natl. Acad. Sci. U.S.A.

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

Judde et al., 2007, Gefitinib and chemotherapy combination studies in five novel human non small cell lung cancer xenografts. Evidence linking EGFR signaling to gefitinib antitumor response., Int. J. Cancer

JAX-CKB: Gefitinib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Pao et al., 2005, KRAS mutations and primary resistance of lung adenocarcinomas to gefitinib or erlotinib., PLoS Med.

Manchado et al., 2016, A combinatorial strategy for treating KRAS-mutant lung cancer., Nature

Eberlein et al., 2015, Acquired Resistance to the Mutant-Selective EGFR Inhibitor AZD9291 Is Associated with Increased Dependence on RAS Signaling in Preclinical Models., Cancer Res.

CGI: Gefitinib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Murray et al., 2010, Screening for EGFR Mutations in Patients with Head and Neck Cancer Treated with Gefitinib on a Compassionate-Use Program: A Hellenic Cooperative Oncology Group Study., J Oncol

Lewis et al., 2012, A phase II study of gefitinib for aggressive cutaneous squamous cell carcinoma of the head and neck., Clin. Cancer Res.

DoCM: GEFITINIB

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Murray et al., 2010, Screening for EGFR Mutations in Patients with Head and Neck Cancer Treated with Gefitinib on a Compassionate-Use Program: A Hellenic Cooperative Oncology Group Study., J Oncol

PharmGKB: gefitinib

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Funke S et al., 2008, Pharmacogenetics in colorectal cancer: a systematic review., Pharmacogenomics

Liu G et al., 2008, Epidermal growth factor receptor polymorphisms and clinical outcomes in non-small-cell lung cancer patients treated with gefitinib., Pharmacogenomics J

Han et al., 2012, First-SIGNAL: first-line single-agent iressa versus gemcitabine and cisplatin trial in never-smokers with adenocarcinoma of the lung., J. Clin. Oncol.

CIViC: GEFITINIB

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

Prahallad et al., 2012, Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR., Nature

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

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.

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

ZD1839 Drug Trade Name

Drug Info:

Publications:
GuideToPharmacology: 178101639
- Version: 29-September-2020
Alternate Names:

GEFITINIB GuideToPharmacology Ligand Name

Drug Info:

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

D01RYO TTD Drug ID

D09XZB TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL939
- Version: ChEMBL_27
Alternate Names:

Drug Info:

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

Drug Info:

Publications:
MyCancerGenomeClinicalTrial: GEFITINIB
- Version: 30-February-2014
Alternate Names:

Drug Info:

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

Drug Info:

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

Drug Info:

Publications:
ChemblInteractions: CHEMBL939
- Version: chembl_23
Alternate Names:

Drug Info:

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

Drug Info:

Publications:

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

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

Approval Status	Preclinical - Cell culture
combination therapy	Gefitinib + NPS-1034
Approval Status	Preclinical - Cell line xenograft

combination therapy	Gefitinib + Trametinib
Indication/Tumor Type	lung cancer
Response Type	no benefit

Indication/Tumor Type	breast cancer
Response Type	resistant
Approval Status	Preclinical

Indication/Tumor Type	melanoma
combination therapy	Gefitinib + PLX4720
Evidence Type	Actionable

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

combination therapy	Gefitinib + Imatinib
Indication/Tumor Type	glioblastoma multiforme
Response Type	sensitive

combination therapy	AZD4547 + Gefitinib
Indication/Tumor Type	head and neck squamous cell carcinoma
Response Type	sensitive

GEFITINIB	DrugBank Drug Name
184475-35-2	CAS Number
Apo-gefitinib	Drug Brand

antagonist (inhibitory)
inhibitor (inhibitory)

Drug Type	small molecule
Drug Groups	approved
Drug Groups	investigational

GEFITINIB Drug Record

GEFITINIB chembl:CHEMBL939 ApprovedAntineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16087880

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 31664190

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 31664190

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22586683

Sources: CIViC

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

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

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

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 26745678

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15738541

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 31664190

Sources: PharmGKB

Interaction Types & Directionality: n/a

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

PMIDs: 26124204

Sources: JAX-CKB CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 31664190

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 21636554

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 31664190

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16988945

Sources: NCI

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 24685132

Sources: MyCancerGenomeClinicalTrial PharmGKB CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 31664190

Sources: PharmGKB

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: 25554506 21332310 20035425 17148776

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 31664190

Sources: PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
16087880

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
31664190

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
31664190

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
22586683

Sources:
CIViC

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Direct Interaction? False

Endogenous Drug? False

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

Interaction Types & Directionality:

n/a

PMIDs:
26745678

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
15738541

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
31664190

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Gefitinib + Sonidegib

Indication/Tumor Type non-small cell lung carcinoma

Response Type sensitive

PMIDs:
26124204

Sources:
JAX-CKB CIViC

Interaction Types & Directionality:

n/a

PMIDs:
31664190

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
21636554

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
31664190

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
16988945

Sources:
NCI

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
24685132

Sources:
MyCancerGenomeClinicalTrial PharmGKB CIViC

Interaction Types & Directionality:

n/a

PMIDs:
31664190

Sources:
PharmGKB

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:
25554506 21332310 20035425 17148776

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
31664190

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

Interaction Info:

Approval Status Preclinical - Cell culture

combination therapy Gefitinib + NPS-1034

Approval Status Preclinical - Cell line xenograft

PMIDs:
23993328 17463250 24165158 23542356 27612490

Sources:
DTC OncoKB JAX-CKB CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial DTC PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Gefitinib + Trametinib

Indication/Tumor Type lung cancer

Response Type no benefit

PMIDs:
21258250 15696205 19794967 27338794 25870145 23313110

Sources:
ClearityFoundationBiomarkers JAX-CKB CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type breast cancer

Response Type resistant

Approval Status Preclinical

PMIDs:
26545934 23220880 17638894 20151670 16818711

Sources:
MyCancerGenomeClinicalTrial NCI DTC PharmGKB JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

combination therapy Gefitinib + PLX4720

Evidence Type Actionable

PMIDs:
23242808 22448344 22281684 27312529

Sources:
JAX-CKB CIViC