Pharmacological background of EGFR targeting

Multi-Institutional Randomized Phase II Trial of Gefitinib for Previously Treated Patients With Advanced Non–Small-Cell Lung Cancer

2003 • 2,874 citations

The EGFR family and its ligands in human cancer

2001 • 1,554 citations

A novel approach in the treatment of cancer: targeting the epidermal growth factor receptor.

2001 • 988 citations

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.

2000 • 934 citations

A mutant epidermal growth factor receptor common in human glioma confers enhanced tumorigenicity.

1994 • 932 citations

ZD1839 (Iressa): an orally active inhibitor of epidermal growth factor signaling with potential for cancer therapy.

2002 • 910 citations

Improving the efficacy of antibody-based cancer therapies

2001 • 821 citations

Biological efficacy of a chimeric antibody to the epidermal growth factor receptor in a human tumor xenograft model.

1995 • 791 citations

Efficacy of cytotoxic agents against human tumor xenografts is markedly enhanced by coadministration of ZD1839 (Iressa), an inhibitor of EGFR tyrosine kinase.

2000 • 766 citations

Epidermal growth factor receptor blockade with C225 modulates proliferation, apoptosis, and radiosensitivity in squamous cell carcinomas of the head and neck.

1999 • 707 citations

The epidermal growth factor receptor family as a central element for cellular signal transduction and diversification.

2001 • 670 citations

Inhibition of growth factor production and angiogenesis in human cancer cells by ZD1839 (Iressa), a selective epidermal growth factor receptor tyrosine kinase inhibitor.

2001 • 642 citations

Frequent expression of a mutant epidermal growth factor receptor in multiple human tumors.

1995 • 633 citations

Identical splicing of aberrant epidermal growth factor receptor transcripts from amplified rearranged genes in human glioblastomas.

1990 • 593 citations

The Enhanced Tumorigenic Activity of a Mutant Epidermal Growth Factor Receptor Common in Human Cancers Is Mediated by Threshold Levels of Constitutive Tyrosine Phosphorylation and Unattenuated Signaling

1997 • 591 citations

Modulation of radiation response after epidermal growth factor receptor blockade in squamous cell carcinomas: inhibition of damage repair, cell cycle kinetics, and tumor angiogenesis.

2000 • 549 citations

Acquired resistance to the antitumor effect of epidermal growth factor receptor-blocking antibodies in vivo: a role for altered tumor angiogenesis.

2001 • 545 citations

Insulin-like growth factor receptor I mediates resistance to anti-epidermal growth factor receptor therapy in primary human glioblastoma cells through continued activation of phosphoinositide 3-kinase signaling.

2002 • 508 citations

Monoclonal antibodies against EGFRvIII are tumor specific and react with breast and lung carcinomas and malignant gliomas.

1995 • 465 citations

Loss of PTEN/MMAC1/TEP in EGF receptor-expressing tumor cells counteracts the antitumor action of EGFR tyrosine kinase inhibitors

2003 • 457 citations

Antitumor effect of anti-epidermal growth factor receptor monoclonal antibodies plus cis-diamminedichloroplatinum on well established A431 cell xenografts.

1993 • 430 citations

Antitumor Effects of Doxorubicin in Combination With Anti-epidermal Growth Factor Receptor Monoclonal Antibodies

1993 • 422 citations

Epidermal growth factor receptor blockade with C225 plus gemcitabine results in regression of human pancreatic carcinoma growing orthotopically in nude mice by antiangiogenic mechanisms.

2000 • 416 citations

Targeting the epidermal growth factor receptor for cancer therapy.

2002 • 412 citations

A common mutant epidermal growth factor receptor confers enhanced tumorigenicity on human glioblastoma cells by increasing proliferation and reducing apoptosis.

1996 • 407 citations

The epidermal growth factor receptor: from mutant oncogene in nonhuman cancers to therapeutic target in human neoplasia.

2001 • 393 citations

Antiangiogenic and antitumor activity of anti-epidermal growth factor receptor C225 monoclonal antibody in combination with vascular endothelial growth factor antisense oligonucleotide in human GEO colon cancer cells.

2000 • 376 citations

Enhanced antitumor activity of anti-epidermal growth factor receptor monoclonal antibody IMC-C225 in combination with irinotecan (CPT-11) against human colorectal tumor xenografts.

2002 • 351 citations

Antitumor activity of sequential treatment with topotecan and anti-epidermal growth factor receptor monoclonal antibody C225.

1999 • 335 citations

Cell surface localization and density of the tumor-associated variant of the epidermal growth factor receptor, EGFRvIII.

1997 • 327 citations

Antibody-induced epidermal growth factor receptor dimerization mediates inhibition of autocrine proliferation of A431 squamous carcinoma cells.

1994 • 281 citations

Modulation of radiation response and tumor-induced angiogenesis after epidermal growth factor receptor inhibition by ZD1839 (Iressa).

2002 • 261 citations

Receptor tyrosine kinases as targets for anticancer drugs

2002 • 251 citations

Enhancement of antitumor activity of ionizing radiation by combined treatment with the selective epidermal growth factor receptor-tyrosine kinase inhibitor ZD1839 (Iressa).

2002 • 245 citations

The Biologic Effects of C225, A Chimeric Monoclonal Antibody to the EGFR, on Human Prostate Carcinoma

1996 • 243 citations

Drug-induced ubiquitylation and degradation of ErbB receptor tyrosine kinases: implications for cancer therapy

2002 • 232 citations

Physical Interaction between Epidermal Growth Factor Receptor and DNA-dependent Protein Kinase in Mammalian Cells

1998 • 229 citations

Enhanced apoptosis with combination C225/radiation treatment serves as the impetus for clinical investigation in head and neck cancers.

2000 • 220 citations

PD153035, a tyrosine kinase inhibitor, prevents epidermal growth factor receptor activation and inhibits growth of cancer cells in a receptor number-dependent manner.

1997 • 205 citations

Growth suppression of intracranial xenografted glioblastomas overexpressing mutant epidermal growth factor receptors by systemic administration of monoclonal antibody (mAb) 806, a novel monoclonal antibody directed to the receptor.

2001 • 204 citations

Transformational and altered signal transduction by a naturally occurring mutant EGF receptor.

1996 • 195 citations

ZD1839 (‘Iressa’), a specific oral epidermal growth factor receptor-tyrosine kinase inhibitor, potentiates radiotherapy in a human colorectal cancer xenograft model

2002 • 175 citations

Tyrosine Kinase Inhibitors Targeted to the Epidermal Growth Factor Receptor Subfamily

2000 • 170 citations

Brain tumors in mice are susceptible to blockade of epidermal growth factor receptor (EGFR) with the oral, specific, EGFR-tyrosine kinase inhibitor ZD1839 (iressa).

2002 • 168 citations

Epidermal growth factor receptor blockade by antibody IMC-C225 inhibits growth of a human pancreatic carcinoma xenograft in nude mice

2000 • 160 citations

Influence of epidermal growth factor receptor (EGFR), p53 and intrinsic MAP kinase pathway status of tumour cells on the antiproliferative effect of ZD1839 (‘Iressa’)

2002 • 157 citations

Combination of a selective cyclooxygenase-2 inhibitor with epidermal growth factor receptor tyrosine kinase inhibitor ZD1839 and protein kinase A antisense causes cooperative antitumor and antiangiogenic effect.

2003 • 148 citations

True

2000 • 128 citations

Antitumor activity of combined treatment of human cancer cells with ionizing radiation and anti-epidermal growth factor receptor monoclonal antibody C225 plus type I protein kinase A antisense oligonucleotide.

2000 • 126 citations

Sequence-dependent effects of ZD1839 (‘Iressa’) in combination with cytotoxic treatment in human head and neck cancer

2002 • 114 citations

Fibroblast growth factor and insulin-like growth factor differentially modulate the apoptosis and G1 arrest induced by anti-epidermal growth factor receptor monoclonal antibody

2001 • 104 citations

Reciprocal changes in p27(Kip1) and p21(Cip1) in growth inhibition mediated by blockade or overstimulation of epidermal growth factor receptors.

1997 • 94 citations

Blockade of the epidermal growth factor receptor signaling inhibits angiogenesis leading to regression of human renal cell carcinoma growing orthotopically in nude mice.

2002 • 93 citations

Targeting the epidermal growth factor receptor: a clinical reality.

2001 • 84 citations

High levels of HER-2 expression alter the ability of epidermal growth factor receptor (EGFR) family tyrosine kinase inhibitors to inhibit EGFR phosphorylation in vivo.

2001 • 75 citations

Safety experience with IMC-C225, an anti-epidermal growth factor receptor antibody

2002 • 75 citations

IMC-C225, an anti-epidermal growth factor receptor monoclonal antibody for treatment of head and neck cancer

2002 • 70 citations

Safety experience with IMC-C225, an anti-epidermal growth factor receptor antibody

2002 • 70 citations

IMC-C225, an anti-epidermal growth factor receptor monoclonal antibody for treatment of head and neck cancer

2002 • 64 citations

Anti-Epidermal Growth Factor Receptor Monoclonal Antibody 225 Upregulates p27<sup>KIP1</sup> and p15<sup>INK4B</sup> and Induces G1 Arrest in Oral Squamous Carcinoma Cell Lines

2002 • 61 citations

Evidence for epidermal growth factor receptor-enhanced chemosensitivity in combinations of cisplatin and the new irreversible tyrosine kinase inhibitor CI-1033

2001 • 55 citations

Oral administration of a novel taxane, an antisense oligonucleotide targeting protein kinase A, and the epidermal growth factor receptor inhibitor Iressa causes cooperative antitumor and antiangiogenic activity.

2001 • 50 citations

ZD1839 (IRESSA™): a selective EGFR-TK inhibitor

2002 • 44 citations

The monoclonal antibody 225 activates caspase-8 and induces apoptosis through a tumor necrosis factor receptor family-independent pathway

2001 • 42 citations

Irreversible inhibitors of the erbB family of protein tyrosine kinases

2002 • 36 citations

An update on epidermal growth factor receptor inhibitors

2002 • 28 citations

Synergistic growth inhibition and induction of apoptosis by a novel mixed backbone antisense oligonucleotide targeting CRIPTO in combination with C225 anti-EGFR monoclonal antibody and 8-Cl-cAMP in human GEO colon cancer cells.

1999 • 25 citations

Anti‐epidermal growth factor receptor‐antibody therapy for treatment of breast cancer

2002 • 16 citations