Therapeutic Targets Database
BIDD Pharmainformatics Databases


TTD Target ID: TTDS00355

Target Information
NameEpidermal growth factor receptor    
Type of targetSuccessful target    
Epidermal growth factor receptor ErbB-1    
Epidermal growth factor receptor-tyrosine kinase    
Receptor protein-tyrosine kinase ErbB-1    
DiseaseBreast cancer
[ICD9: 174, 175   ICD10: C50]
Cancer, unspecific
[ICD9: 140-229   ICD10: C00-C96]
Colorectal cancer
[ICD9: 153, 154   ICD10: C18-C21]
Glioblastoma multiforme
[ICD9: 191   ICD10: C71]
HCV infection
[ICD9: 070.4, 070.5, 070.70   ICD10: B17.1, B18.2]
Head and neck tumors
[ICD9: 140-199, 210-229   ICD10: C00-C75, C7A, C7B, D10-D36, D3A]
Nonsmall cell lung cancer
[ICD9: 140-229, 162, 204.0   ICD10: C00-C96, C33-C34, C91.0]
Ovarian cancer
[ICD9: 183   ICD10: C56]
Pancreatic cancer
[ICD9: 157   ICD10: C25]
Solid tumor
[ICD9: 140-199, 210-229   ICD10: C00-C75, C7A, C7B, D10-D36, D3A]
Squamous cell carcinoma
[ICD9: 199   ICD10: C44]
[ICD9: 140-199, 210-229   ICD10: C00-C75, C7A, C7B, D10-D36, D3A]
Drug(s)CetuximabApprovedColorectal Cancer[17][14][19]
LapatinibApprovedBreast cancer[20][21]
PanitumumabApprovedColorectal Cancer[22]
Tyverb/TykerbApprovedRefractory breast cancer[23]
DWP-401LaunchedDiabetic foot ulcers[24]
ErlotinibLaunchedNon-small cell lung cancer[25]
HEGFLaunchedDiabetic foot ulcers[24]
BIBW 2992Phase IIINon-small cell lung cancer[27]
DE-766Phase IIIGastric cancer
DE-766Phase IIINon small cell lung cancer
ErlotinibPhase IIIPancreatic cancer[25][28]
Erlotinib+BevacizumabPhase IIINSCLC[28][29]
GefitinibPhase IIIHead & neck cancer[30][31]
HKI-272Phase IIIBreast Cancer[30]
NecitumumabPhase IIISquamous non-small cell lung cancer
Pazopanib + Tyverb/TykerbPhase IIIInflammatory breast cancer[23]
RindopepimutPhase IIIFront-line glioblastoma
TykerbPhase IIIRefractory metastatic breast cancer, RCC[30]
Tyverb/TykerbPhase IIIGastric cancer[23]
VandetanibPhase IIISolid tumours, NSCLC[30][31]
TykerbPhase II completedBladder, head & neck, NSCLC, brain cancer[30]
XL647Phase II completedCarcinoma, Non-Small-Cell Lung[32]
Bevacizumab+ErlotinibPhase IINSCLC[28]
ErlotinibPhase IIColon, glioma, breast, RCC ovarian, head & neck cancer[25][28]
GefitinibPhase IIUrethral, bladder, ovarian, prostate, breast cancer[30][31]
HKI-272Phase IIAdvanced Malignant Solid Tumors; Breast Cancer[30]
MEHD7945APhase IIColorectal cancer
MEHD7945APhase IIHead and neck cancer
PF-299804Phase IICancer[33][34]
PanitumumabPhase IILocally advanced head and neck cancer[22][35][36]
RG7160Phase IISecond-line metastatic colorectal
RG7160Phase IISolid tumors
RG7597Phase IIHead and neck cancer
RG7597Phase IIMetastatic epithelial tumors
RindopepimutPhase IIRecurrent glioblastoma
Tyverb/TykerbPhase IIHead & neck squamous cell carcinoma[23]
VandetanibPhase IIBreast, thyroid tumours, multiple myeloma, brain, head & neck cancer[30][31]
CO-1686Phase I/IISecond-line NSCLC
XL647Phase I completedCancer[32]
S-222611Phase IbMalignant tumor[37]
ABT-806Phase ISolid Tumors
AMG 595Phase IGlioblastoma
Anti-HER3/EGFR DAFPhase IMetastatic epithelial tumors[38]
DE-766Phase IEsophageal cancer
MEHD7945APhase IMetastatic epithelial tumors
MM-151Phase ISolid Tumors
AZD4769Discontinued in Phase ISolid tumours[31]
BMS-599626Suspended in Phase IVarious cancers[30]
CI-1033Discontinued in Phase IICancer, NSCLC; cancer, colorectal; cancer, head and neck; cancer, thyroid; cancer, breast; cancer, mesothelioma; cancer, sarcoma, general; cancer, melanoma[30]
TAK165Suspended in Phase IVarious cancers[30]
BioChemical ClassTransferases transferring phosphorus-containing groups    
EC NumberEC
PathwayAdherens junction
Bladder cancer
Calcium signaling pathway
Colorectal cancer
Cytokine-cytokine receptor interaction
Endometrial cancer
Epithelial cell signaling in Helicobacter pylori
ErbB signaling pathway
Focal adhesion
Gap junction
GnRH signaling pathway
MAPK signaling pathway
Non-small cell lung cancer
Pancreatic cancer
Pathways in cancer
Prostate cancer
Regulation of actin cytoskeleton
UniProt IDP00533
PDB Structure1DNQ; 1DNR; 1IVO; 1M14; 1M17; 1MOX; 1NQL; 1XKK; 1YY9; 1Z9I; 2EB2; 2EB3; 2EXP; 2EXQ; 2GS2; 2GS6; 2GS7; 2ITN; 2ITO; 2ITP; 2ITQ; 2ITT; 2ITU; 2ITV; 2ITW; 2ITX; 2ITY; 2ITZ; 2J5E; 2J5F; 2J6M; 2JIT; 2JIU; 2JIV; 2KS1; 2M20; 2RF9; 2RFD; 2RFE; 2RGP; 3B2U; 3B2V; 3BEL; 3BUO; 3C09; 3G5V; 3G5Y; 3GOP; 3GT8; 3IKA; 3LZB; 3NJP; 3OB2; 3OP0; 3P0Y; 3PFV; 3POZ; 3QWQ; 3UG1; 3UG2; 3VJN; 3VJO; 3VRP; 3VRR; 3W2O; 3W2P; 3W2Q; 3W2R; 3W2S; 3W32; 3W33; 4G5J; 4G5P; 4HJO; 4I1Z; 4I20; 4I21; 4I22; 4I23; 4I24.    
FunctionReceptor for egf, but also for other members of the egf family, as tgf-alpha, amphiregulin, betacellulin, heparin-binding egf-like growth factor, gp30 and vaccinia virus growth factor. Is involved in the control of cell growth and differentiation.    
Related US Patent6,551,989
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
BIBW 2992[27]
Lapatinib ditosylate[48]
PD-0166326,   PD-166326[50]
Pazopanib + Tyverb/Tykerb[23]
cochliobolic acid[58]
Anti-HER3/EGFR DAF[38]
EMD 55900[18]
ICR 62[18]
MultitargetAnti-HER3/EGFR DAF[38]
BIBW 2992[27]
Pazopanib + Tyverb/Tykerb[23]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
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Ref 3Allelic length of a CA dinucleotide repeat in the egfr gene correlates with the frequency of amplifications of this sequence--first results of an inter-ethnic breast cancer study. J Pathol. 2004 May;203(1):545-50. To Reference
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Ref 6Identification of surrogate markers for determining drug activity using proteomics. Biochem Soc Trans. 2003 Dec;31(Pt 6):1488-90. To Reference
Ref 7Epidermal growth factor receptor expression and measurement in solid tumors. Semin Oncol. 2002 Oct;29(5 Suppl 14):45-54. To Reference
Ref 8Time and dose-dependent radiosensitization of the glioblastoma multiforme U251 cells by the EGF receptor tyrosine kinase inhibitor ZD1839 ('Iressa'). Cancer Lett. 2003 Dec 8;202(1):43-51. To Reference
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Ref 10Epidermal growth factor receptor as a therapeutic target in head and neck cancer. Semin Radiat Oncol. 2002 Jul;12(3 Suppl 2):11-20. To Reference
Ref 11Expression of epidermal growth-factor receptor in lymphangiomatosis: a new therapeutic target? Lancet Oncol. 2004 Jun;5(6):353. To Reference
Ref 12Targeting epidermal growth factor receptor in lung cancer. Curr Oncol Rep. 2002 Jul;4(4):317-24. To Reference
Ref 13'Targeting' the epidermal growth factor receptor tyrosine kinase with gefitinib (Iressa) in non-small cell lung cancer (NSCLC). Semin Cancer Biol. 2004 Feb;14(1):33-40. To Reference
Ref 14Epidermal growth factor receptor-targeted therapy for pancreatic cancer. Semin Oncol. 2002 Oct;29(5 Suppl 14):31-7. To Reference
Ref 15The epidermal growth factor receptor-tyrosine kinase: a promising therapeutic target in solid tumors. Semin Oncol. 2003 Feb;30(1 Suppl 1):3-11. To Reference
Ref 16Epidermal growth factor receptor: a promising target in solid tumours. Cancer Treat Rev. 2004 Feb;30(1):1-17. To Reference
Ref 17Molecular inhibition of angiogenesis and metastatic potential in human squamous cell carcinomas after epidermal growth factor receptor blockade. Mol Cancer Ther. 2002 May;1(7):507-14. To Reference
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Ref 27Boehringer Ingelheim. Product Development Pipeline. June 2 2009. To Reference
Ref 28Roche. Product Development Pipeline. July 29 2009. To Reference
Ref 29Gefitinib-sensitizing EGFR mutations in lung cancer activate anti-apoptotic pathways. Science. 2004 Aug 20;305(5687):1163-7. Epub 2004 Jul 29. To Reference
Ref 30A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22. To Reference
Ref 31AstraZeneca. Product Development Pipeline. January 29 2009. To Reference
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Ref 36Drug Insight: panitumumab, a human EGFR-targeted monoclonal antibody with promising clinical activity in colorectal cancer. Nat Clin Pract Oncol. 2008 Jul;5(7):415-25. Epub 2008 May 27. To Reference
Ref 372011 Pipeline of Shionogi. To Reference
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Ref 39Eur J Med Chem. 2008 Jul;43(7):1478-88. Epub 2007 Sep 29.Syntheses of 4-(indole-3-yl)quinazolines: a new class of epidermal growth factor receptor tyrosine kinase inhibitors. To Reference
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Ref 41J Med Chem. 2006 Nov 2;49(22):6465-88.N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor. To Reference
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Ref 52J Med Chem. 1996 Apr 26;39(9):1823-35.Tyrosine kinase inhibitors. 10. Isomeric 4-[(3-bromophenyl)amino]pyrido[d]-pyrimidines are potent ATP binding site inhibitors of the tyrosine kinase function of the epidermal growth factor receptor. To Reference
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Ref 58J Nat Prod. 1997 Jan;60(1):6-8.Cochliobolic acid, a novel metabolite produced by Cochliobolus lunatus, inhibits binding of TGF-alpha to the EGF receptor in a SPA assay. To Reference


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