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Chemical Compound Review

Erlotinib     N-(3-ethynylphenyl)-6,7- bis(2...

Synonyms: Erlotinin, erlotinib;, CHEMBL553, Erlotinib Base, OSI-744, ...
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Disease relevance of Tarceva


High impact information on Tarceva


Chemical compound and disease context of Tarceva


Biological context of Tarceva


Anatomical context of Tarceva


Associations of Tarceva with other chemical compounds


Gene context of Tarceva


Analytical, diagnostic and therapeutic context of Tarceva


  1. Lung adenocarcinomas induced in mice by mutant EGF receptors found in human lung cancers respond to a tyrosine kinase inhibitor or to down-regulation of the receptors. Politi, K., Zakowski, M.F., Fan, P.D., Schonfeld, E.A., Pao, W., Varmus, H.E. Genes Dev. (2006) [Pubmed]
  2. Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases. Carter, T.A., Wodicka, L.M., Shah, N.P., Velasco, A.M., Fabian, M.A., Treiber, D.K., Milanov, Z.V., Atteridge, C.E., Biggs, W.H., Edeen, P.T., Floyd, M., Ford, J.M., Grotzfeld, R.M., Herrgard, S., Insko, D.E., Mehta, S.A., Patel, H.K., Pao, W., Sawyers, C.L., Varmus, H., Zarrinkar, P.P., Lockhart, D.J. Proc. Natl. Acad. Sci. U.S.A. (2005) [Pubmed]
  3. Phase I/II trial evaluating the anti-vascular endothelial growth factor monoclonal antibody bevacizumab in combination with the HER-1/epidermal growth factor receptor tyrosine kinase inhibitor erlotinib for patients with recurrent non-small-cell lung cancer. Herbst, R.S., Johnson, D.H., Mininberg, E., Carbone, D.P., Henderson, T., Kim, E.S., Blumenschein, G., Lee, J.J., Liu, D.D., Truong, M.T., Hong, W.K., Tran, H., Tsao, A., Xie, D., Ramies, D.A., Mass, R., Seshagiri, S., Eberhard, D.A., Kelley, S.K., Sandler, A. J. Clin. Oncol. (2005) [Pubmed]
  4. Modern treatment of lung cancer: case 2. Response to erlotinib after failure of gefitinib in a patient with advanced non-small-cell lung carcinoma. Garfield, D.H. J. Clin. Oncol. (2005) [Pubmed]
  5. Treatment of metastatic renal cell carcinoma with a combination of bevacizumab and erlotinib. Hainsworth, J.D., Sosman, J.A., Spigel, D.R., Edwards, D.L., Baughman, C., Greco, A. J. Clin. Oncol. (2005) [Pubmed]
  6. Erlotinib exhibits antineoplastic off-target effects in AML and MDS: a preclinical study. Boehrer, S., Adès, L., Braun, T., Galluzzi, L., Grosjean, J., Fabre, C., Le Roux, G., Gardin, C., Martin, A., de Botton, S., Fenaux, P., Kroemer, G. Blood (2008) [Pubmed]
  7. Are there any ethnic differences in molecular predictors of erlotinib efficacy in advanced non-small cell lung cancer? Ahn, M.J., Park, B.B., Ahn, J.S., Kim, S.W., Kim, H.T., Lee, J.S., Kang, J.H., Cho, J.Y., Song, H.S., Park, S.H., Sohn, C.H., Shin, S.W., Choi, J.H., Ki, C.S., Park, C.K., Holmes, A.J., Jänne, P.A., Park, K. Clin. Cancer Res. (2008) [Pubmed]
  8. Phase I and pharmacokinetic studies of erlotinib administered concurrently with radiotherapy for children, adolescents, and young adults with high-grade glioma. Broniscer, A., Baker, S.J., Stewart, C.F., Merchant, T.E., Laningham, F.H., Schaiquevich, P., Kocak, M., Morris, E.B., Endersby, R., Ellison, D.W., Gajjar, A. Clin. Cancer Res. (2009) [Pubmed]
  9. Erlotinib and bevacizumab have synergistic activity against melanoma. Schicher, N., Paulitschke, V., Swoboda, A., Kunstfeld, R., Loewe, R., Pilarski, P., Pehamberger, H., Hoeller, C. Clin. Cancer Res. (2009) [Pubmed]
  10. Epidermal growth factor receptor variant III mutations in lung tumorigenesis and sensitivity to tyrosine kinase inhibitors. Ji, H., Zhao, X., Yuza, Y., Shimamura, T., Li, D., Protopopov, A., Jung, B.L., McNamara, K., Xia, H., Glatt, K.A., Thomas, R.K., Sasaki, H., Horner, J.W., Eck, M., Mitchell, A., Sun, Y., Al-Hashem, R., Bronson, R.T., Rabindran, S.K., Discafani, C.M., Maher, E., Shapiro, G.I., Meyerson, M., Wong, K.K. Proc. Natl. Acad. Sci. U.S.A. (2006) [Pubmed]
  11. Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib. Kwak, E.L., Sordella, R., Bell, D.W., Godin-Heymann, N., Okimoto, R.A., Brannigan, B.W., Harris, P.L., Driscoll, D.R., Fidias, P., Lynch, T.J., Rabindran, S.K., McGinnis, J.P., Wissner, A., Sharma, S.V., Isselbacher, K.J., Settleman, J., Haber, D.A. Proc. Natl. Acad. Sci. U.S.A. (2005) [Pubmed]
  12. C-fos assessment as a marker of anti-epidermal growth factor receptor effect. Jimeno, A., Kulesza, P., Kincaid, E., Bouaroud, N., Chan, A., Forastiere, A., Brahmer, J., Clark, D.P., Hidalgo, M. Cancer Res. (2006) [Pubmed]
  13. TRIBUTE: a phase III trial of erlotinib hydrochloride (OSI-774) combined with carboplatin and paclitaxel chemotherapy in advanced non-small-cell lung cancer. Herbst, R.S., Prager, D., Hermann, R., Fehrenbacher, L., Johnson, B.E., Sandler, A., Kris, M.G., Tran, H.T., Klein, P., Li, X., Ramies, D., Johnson, D.H., Miller, V.A. J. Clin. Oncol. (2005) [Pubmed]
  14. A phase I trial to determine the optimal biological dose of celecoxib when combined with erlotinib in advanced non-small cell lung cancer. Reckamp, K.L., Krysan, K., Morrow, J.D., Milne, G.L., Newman, R.A., Tucker, C., Elashoff, R.M., Dubinett, S.M., Figlin, R.A. Clin. Cancer Res. (2006) [Pubmed]
  15. Novel combinations based on epidermal growth factor receptor inhibition. Adjei, A.A. Clin. Cancer Res. (2006) [Pubmed]
  16. Strategies to enhance epidermal growth factor inhibition: targeting the mevalonate pathway. Dimitroulakos, J., Lorimer, I.A., Goss, G. Clin. Cancer Res. (2006) [Pubmed]
  17. Heterodimerization of Insulin-like Growth Factor Receptor/Epidermal Growth Factor Receptor and Induction of Survivin Expression Counteract the Antitumor Action of Erlotinib. Morgillo, F., Woo, J.K., Kim, E.S., Hong, W.K., Lee, H.Y. Cancer Res. (2006) [Pubmed]
  18. Kinetic analysis of epidermal growth factor receptor somatic mutant proteins shows increased sensitivity to the epidermal growth factor receptor tyrosine kinase inhibitor, erlotinib. Carey, K.D., Garton, A.J., Romero, M.S., Kahler, J., Thomson, S., Ross, S., Park, F., Haley, J.D., Gibson, N., Sliwkowski, M.X. Cancer Res. (2006) [Pubmed]
  19. Mechanisms of enhanced radiation response following epidermal growth factor receptor signaling inhibition by erlotinib (Tarceva). Chinnaiyan, P., Huang, S., Vallabhaneni, G., Armstrong, E., Varambally, S., Tomlins, S.A., Chinnaiyan, A.M., Harari, P.M. Cancer Res. (2005) [Pubmed]
  20. Epidermal growth factor receptor dynamics influences response to epidermal growth factor receptor targeted agents. Jimeno, A., Rubio-Viqueira, B., Amador, M.L., Oppenheimer, D., Bouraoud, N., Kulesza, P., Sebastiani, V., Maitra, A., Hidalgo, M. Cancer Res. (2005) [Pubmed]
  21. Cross-talk between G protein-coupled receptor and epidermal growth factor receptor signaling pathways contributes to growth and invasion of head and neck squamous cell carcinoma. Thomas, S.M., Bhola, N.E., Zhang, Q., Contrucci, S.C., Wentzel, A.L., Freilino, M.L., Gooding, W.E., Siegfried, J.M., Chan, D.C., Grandis, J.R. Cancer Res. (2006) [Pubmed]
  22. Dual-agent molecular targeting of the epidermal growth factor receptor (EGFR): combining anti-EGFR antibody with tyrosine kinase inhibitor. Huang, S., Armstrong, E.A., Benavente, S., Chinnaiyan, P., Harari, P.M. Cancer Res. (2004) [Pubmed]
  23. Erlotinib Effectively Inhibits JAK2V617F Activity and Polycythemia Vera Cell Growth. Li, Z., Xu, M., Xing, S., Ho, W.T., Ishii, T., Li, Q., Fu, X., Zhao, Z.J. J. Biol. Chem. (2007) [Pubmed]
  24. Novel targeted approaches to treating biliary tract cancer: the dual epidermal growth factor receptor and ErbB-2 tyrosine kinase inhibitor NVP-AEE788 is more efficient than the epidermal growth factor receptor inhibitors gefitinib and erlotinib. Wiedmann, M., Feisthammel, J., Blüthner, T., Tannapfel, A., Kamenz, T., Kluge, A., Mössner, J., Caca, K. Anticancer Drugs (2006) [Pubmed]
  25. Determinants of tumor response and survival with erlotinib in patients with non--small-cell lung cancer. Pérez-Soler, R., Chachoua, A., Hammond, L.A., Rowinsky, E.K., Huberman, M., Karp, D., Rigas, J., Clark, G.M., Santabárbara, P., Bonomi, P. J. Clin. Oncol. (2004) [Pubmed]
  26. Phase I, pharmacokinetic, and biological study of erlotinib in combination with Paclitaxel and Carboplatin in patients with advanced solid tumors. Patnaik, A., Wood, D., Tolcher, A.W., Hamilton, M., Kreisberg, J.I., Hammond, L.A., Schwartz, G., Beeram, M., Hidalgo, M., Mita, M.M., Wolf, J., Nadler, P., Rowinsky, E.K. Clin. Cancer Res. (2006) [Pubmed]
  27. Enhanced sensitivity to the HER1/epidermal growth factor receptor tyrosine kinase inhibitor erlotinib hydrochloride in chemotherapy-resistant tumor cell lines. Dai, Q., Ling, Y.H., Lia, M., Zou, Y.Y., Kroog, G., Iwata, K.K., Perez-Soler, R. Clin. Cancer Res. (2005) [Pubmed]
  28. High affinity targets of protein kinase inhibitors have similar residues at the positions energetically important for binding. Sheinerman, F.B., Giraud, E., Laoui, A. J. Mol. Biol. (2005) [Pubmed]
  29. Pilot study of neoadjuvant treatment with erlotinib in nonmetastatic head and neck squamous cell carcinoma. Thomas, F., Rochaix, P., Benlyazid, A., Sarini, J., Rives, M., Lefebvre, J.L., Allal, B.C., Courbon, F., Chatelut, E., Delord, J.P. Clin. Cancer Res. (2007) [Pubmed]
  30. Schedule-dependent cytotoxic synergism of pemetrexed and erlotinib in human non-small cell lung cancer cells. Li, T., Ling, Y.H., Goldman, I.D., Perez-Soler, R. Clin. Cancer Res. (2007) [Pubmed]
  31. The potential predictive value of cyclooxygenase-2 expression and increased risk of gastrointestinal hemorrhage in advanced non-small cell lung cancer patients treated with erlotinib and celecoxib. Fidler, M.J., Argiris, A., Patel, J.D., Johnson, D.H., Sandler, A., Villaflor, V.M., Coon, J., Buckingham, L., Kaiser, K., Basu, S., Bonomi, P. Clin. Cancer Res. (2008) [Pubmed]
  32. A Phase I Trial of Erlotinib and Concurrent Chemoradiotherapy for Stage III and IV (M0) Squamous Cell Carcinoma of the Head and Neck. Gilbert, J., Rudek, M.A., Higgins, M.J., Zhao, M., Bienvenu, S., Tsottles, N., Wahl, R., Forastiere, A., Gillison, M. Clin. Cancer Res. (2012) [Pubmed]
  33. A phase I, pharmacokinetic, and pharmacodynamic study of panobinostat, an HDAC inhibitor, combined with erlotinib in patients with advanced aerodigestive tract tumors. Gray, J.E., Haura, E., Chiappori, A., Tanvetyanon, T., Williams, C.C., Pinder-Schenck, M., Kish, J.A., Kreahling, J., Lush, R., Neuger, A., Tetteh, L., Akar, A., Zhao, X., Schell, M.J., Bepler, G., Altiok, S. Clin. Cancer Res. (2014) [Pubmed]
  34. Erlotinib, erlotinib-sulindac versus placebo: a randomized, double-blind, placebo-controlled window trial in operable head and neck cancer. Gross, N.D., Bauman, J.E., Gooding, W.E., Denq, W., Thomas, S.M., Wang, L., Chiosea, S., Hood, B.L., Flint, M.S., Sun, M., Conrads, T.P., Ferris, R.L., Johnson, J.T., Kim, S., Argiris, A., Wirth, L., Nikiforova, M.N., Siegfried, J.M., Grandis, J.R. Clin. Cancer Res. (2014) [Pubmed]
  35. 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. Eberhard, D.A., Johnson, B.E., Amler, L.C., Goddard, A.D., Heldens, S.L., Herbst, R.S., Ince, W.L., Jänne, P.A., Januario, T., Johnson, D.H., Klein, P., Miller, V.A., Ostland, M.A., Ramies, D.A., Sebisanovic, D., Stinson, J.A., Zhang, Y.R., Seshagiri, S., Hillan, K.J. J. Clin. Oncol. (2005) [Pubmed]
  36. Molecular determinants of the response of glioblastomas to EGFR kinase inhibitors. Mellinghoff, I.K., Wang, M.Y., Vivanco, I., Haas-Kogan, D.A., Zhu, S., Dia, E.Q., Lu, K.V., Yoshimoto, K., Huang, J.H., Chute, D.J., Riggs, B.L., Horvath, S., Liau, L.M., Cavenee, W.K., Rao, P.N., Beroukhim, R., Peck, T.C., Lee, J.C., Sellers, W.R., Stokoe, D., Prados, M., Cloughesy, T.F., Sawyers, C.L., Mischel, P.S. N. Engl. J. Med. (2005) [Pubmed]
  37. Epidermal growth factor receptor, protein kinase B/Akt, and glioma response to erlotinib. Haas-Kogan, D.A., Prados, M.D., Tihan, T., Eberhard, D.A., Jelluma, N., Arvold, N.D., Baumber, R., Lamborn, K.R., Kapadia, A., Malec, M., Berger, M.S., Stokoe, D. J. Natl. Cancer Inst. (2005) [Pubmed]
  38. Signaling interactions of rapamycin combined with erlotinib in cervical carcinoma xenografts. Birle, D.C., Hedley, D.W. Mol. Cancer Ther. (2006) [Pubmed]
  39. Acquired resistance to erlotinib in A-431 epidermoid cancer cells requires down-regulation of MMAC1/PTEN and up-regulation of phosphorylated Akt. Yamasaki, F., Johansen, M.J., Zhang, D., Krishnamurthy, S., Felix, E., Bartholomeusz, C., Aguilar, R.J., Kurisu, K., Mills, G.B., Hortobagyi, G.N., Ueno, N.T. Cancer Res. (2007) [Pubmed]
  40. Role of ATP-binding cassette and solute carrier transporters in erlotinib CNS penetration and intracellular accumulation. Elmeliegy, M.A., Carcaboso, A.M., Tagen, M., Bai, F., Stewart, C.F. Clin. Cancer Res. (2011) [Pubmed]
  41. Phase I/II Trial of Cetuximab and Erlotinib in Patients with Lung Adenocarcinoma and Acquired Resistance to Erlotinib. Janjigian, Y.Y., Azzoli, C.G., Krug, L.M., Pereira, L.K., Rizvi, N.A., Pietanza, M.C., Kris, M.G., Ginsberg, M.S., Pao, W., Miller, V.A., Riely, G.J. Clin. Cancer Res. (2011) [Pubmed]
  42. c-Src activation mediates erlotinib resistance in head and neck cancer by stimulating c-Met. Stabile, L.P., He, G., Lui, V.W., Thomas, S., Henry, C., Gubish, C.T., Joyce, S., Quesnelle, K.M., Siegfried, J.M., Grandis, J.R. Clin. Cancer Res. (2013) [Pubmed]
  43. Clinical course of patients with non-small cell lung cancer and epidermal growth factor receptor exon 19 and exon 21 mutations treated with gefitinib or erlotinib. Riely, G.J., Pao, W., Pham, D., Li, A.R., Rizvi, N., Venkatraman, E.S., Zakowski, M.F., Kris, M.G., Ladanyi, M., Miller, V.A. Clin. Cancer Res. (2006) [Pubmed]
  44. Approval summary for erlotinib for treatment of patients with locally advanced or metastatic non-small cell lung cancer after failure of at least one prior chemotherapy regimen. Johnson, J.R., Cohen, M., Sridhara, R., Chen, Y.F., Williams, G.M., Duan, J., Gobburu, J., Booth, B., Benson, K., Leighton, J., Hsieh, L.S., Chidambaram, N., Zimmerman, P., Pazdur, R. Clin. Cancer Res. (2005) [Pubmed]
  45. Combination treatment with erlotinib and pertuzumab against human tumor xenografts is superior to monotherapy. Friess, T., Scheuer, W., Hasmann, M. Clin. Cancer Res. (2005) [Pubmed]
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