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Drug Profile

Erlotinib (Tarceva®): a promising drug targeting epidermal growth factor receptor tyrosine kinase

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Pages 269-279 | Published online: 10 Jan 2014

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Shubham Srivastava, Bhanwar Singh Choudhary, Pakhuri Mehta, Sukanya, Manish Sharma & Ruchi Malik. (2019) Molecular dynamics insights for PI3K-δ inhibition & structure guided identification of novel PI3K-δ inhibitors. Journal of Biomolecular Structure and Dynamics 37:9, pages 2404-2414.
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Corey A Carter, Ronan J Kelly & Giuseppe Giaccone. (2009) Small-molecule inhibitors of the human epidermal receptor family. Expert Opinion on Investigational Drugs 18:12, pages 1829-1842.
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Tina Cascone, Erika Martinelli, Maria Pia Morelli, Floriana Morgillo, Teresa Troiani & Fortunato Ciardiello. (2007) Epidermal growth factor receptor inhibitors in non-small-cell lung cancer. Expert Opinion on Drug Discovery 2:3, pages 335-348.
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Fortunato Ciardiello, Ferdinando De Vita, Michele Orditura, Sabino De Placido & Giampaolo Tortora. (2003) Epidermal growth factor receptor tyrosine kinase inhibitors in late stage clinical trials. Expert Opinion on Emerging Drugs 8:2, pages 501-514.
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Xiang Zhai, Richard A. Ward, Peter Doig & Argyrides Argyrou. (2020) Insight into the Therapeutic Selectivity of the Irreversible EGFR Tyrosine Kinase Inhibitor Osimertinib through Enzyme Kinetic Studies. Biochemistry 59:14, pages 1428-1441.
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C Yan, N Pattabiraman, J Goecks, P Lam, A Nayak, Y Pan, J Torcivia-Rodriguez, A Voskanian, Q Wan & R Mazumder. (2016) Impact of germline and somatic missense variations on drug binding sites. The Pharmacogenomics Journal 17:2, pages 128-136.
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Diego Prada-Gracia, Sara Huerta-Yépez & Liliana M. Moreno-Vargas. (2016) Application of computational methods for anticancer drug discovery, design, and optimization. Boletín Médico del Hospital Infantil de México 73:6, pages 411-423.
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Mohamed E.M. Saeed, Marion Meyer, Ahmed Hussein & Thomas Efferth. (2016) Cytotoxicity of South-African medicinal plants towards sensitive and multidrug-resistant cancer cells. Journal of Ethnopharmacology 186, pages 209-223.
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Xuequn Ren, Wanli Ma, Hong Lu, Lei Yuan, Lei An, Xicai Wang, Guanchang Cheng & Shuguang Zuo. (2015) Modification of cytokine-induced killer cells with chimeric antigen receptors (CARs) enhances antitumor immunity to epidermal growth factor receptor (EGFR)-positive malignancies. Cancer Immunology, Immunotherapy 64:12, pages 1517-1529.
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Feng Li, Yanmei Zhang, DanYe Qiu & Jingwu Kang. (2015) Screening of epidermal growth factor receptor inhibitors in natural products by capillary electrophoresis combined with high performance liquid chromatography–tandem mass spectrometry. Journal of Chromatography A 1400, pages 117-123.
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Ning Ding, Wei Zhang, Hua Ling Xiao, Peng Wang & Ying Xia Li. (2012) Synthesis and biological evaluation of a series of novel salicylanilides as inhibitors of EGFR protein tyrosine kinases. Chinese Chemical Letters 23:5, pages 529-532.
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Andrean L. Simons, Kevin P. Orcutt, Joshua M. Madsen, Peter M. Scarbrough & Douglas R. Spitz. 2012. Oxidative Stress in Cancer Biology and Therapy. Oxidative Stress in Cancer Biology and Therapy 21 46 .
Ruchi Saxena & Anila Dwivedi. (2012) ErbB family receptor inhibitors as therapeutic agents in breast cancer: Current status and future clinical perspective. Medicinal Research Reviews 32:1, pages 166-215.
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Jean Boucher, Linnea Olson & Bilal Piperdi. (2011) Preemptive Management of Dermatologic Toxicities Associated With Epidermal Growth Factor Receptor Inhibitors. Clinical Journal of Oncology Nursing 15:5, pages 501-508.
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Hanqing Li, Mengyao Li, Zaiquan Li, Liang Li, Shanshan Bi, Chenhui Deng, Rui Chen, Tianyan Zhou & Wei Lu. (2011) New Synthetic Route of Two Active Isomeric Metabolites of Erlotinib and Their Bioactivity Studies against Several Tumor Cell Lines. Chinese Journal of Chemistry 29:8, pages 1709-1714.
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Keith M. Giles, Andrew Barker, Priscilla M. Zhang, Michael R. Epis & Peter J. Leedman. 2011. MicroRNA and Cancer. MicroRNA and Cancer 147 163 .
Matthew L. H. ChuZhaolei LangLeonard M. G. Chavas, João NeresOlga S. Fedorova, Lydia TaberneroMike CherryDavid H. WilliamsKenneth T. DouglasPatrick A. Eyers. (2010) Biophysical and X-ray Crystallographic Analysis of Mps1 Kinase Inhibitor Complexes , . Biochemistry 49:8, pages 1689-1701.
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Noboru Yamamoto, Atsushi Horiike, Yasuhito Fujisaka, Haruyasu Murakami, Tatsu Shimoyama, Yasuhide Yamada & Tomohide Tamura. (2007) Phase I dose-finding and pharmacokinetic study of the oral epidermal growth factor receptor tyrosine kinase inhibitor Ro50-8231 (erlotinib) in Japanese patients with solid tumors. Cancer Chemotherapy and Pharmacology 61:3, pages 489-496.
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Paolo Zucali. 2007. Targeted Therapies in Oncology. Targeted Therapies in Oncology 19 44 .
Sharad S. Singhal, Yogesh C. Awasthi & Sanjay Awasthi. (2006) Regression of Melanoma in a Murine Model by RLIP76 Depletion. Cancer Research 66:4, pages 2354-2360.
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Janine Smith. (2005) Erlotinib: Small-molecule targeted therapy in the treatmentof non-small-cell lung cancer. Clinical Therapeutics 27:10, pages 1513-1534.
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Giuseppe Giaccone. (2005) Targeting HER1/EGFR in cancer therapy: experience with erlotinib. Future Oncology 1:4, pages 449-460.
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Thomas Friess, Werner Scheuer & Max Hasmann. (2005) Combination Treatment with Erlotinib and Pertuzumab against Human Tumor Xenografts Is Superior to Monotherapy. Clinical Cancer Research 11:14, pages 5300-5309.
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Fortunato Ciardiello. (2005) Epidermal growth factor receptor inhibitors in cancer treatment. Future Oncology 1:2, pages 221-234.
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Fortunato Ciardiello & Ferdinando De Vita. 2005. Advances in Targeted Cancer Therapy. Advances in Targeted Cancer Therapy 93 115 .
Ray Hinerman, Weiyi Gao, Hassan H Ramadan, Cynthia Cunningham & Peilin Zhang. (2004) Erlotinib (Tarceva ® ) inhibits oral cavity carcinoma and synergizes with cisplatin and ionizing radiation in vitro . Therapy 1:1, pages 67-74.
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Ray Hinerman, Weiyi Gao, Hassan H Ramadan, Cynthia Cunningham & Peilin Zhang. (2004) Erlotinib (TarcevaR) inhibits oral cavity carcinoma and synergizes with cisplatin and ionizing radiation in vitro. Therapy 1:1, pages 67-74.
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Joan Albanell Mestres, Montserrat Muñoz Mateo & Pedro Gascón. (2004) ErbB tyrosine kinase receptor inhibitors in breast cancer treatmentInhibidores del receptor ErbB de tirosina quinase en el tratamiento del cáncer de mama. Revista de Oncología 6:1, pages 12-21.
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Maarten L. Janmaat & Giuseppe Giaccone. (2003) Small-Molecule Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors. The Oncologist 8:6, pages 576-586.
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