PF00299804, an Irreversible Pan-ERBB Inhibitor, Is Effective in Lung Cancer Models with EGFR and ERBB2 Mutations that Are Resistant to Gefitinib

Engelman, Jeffrey A.; Zejnullahu, Kreshnik; Gale, Christopher-Michael; Lifshits, Eugene; Gonzales, Andrea J.; Shimamura, Takeshi; Zhao, Feng; Vincent, Patrick W.; Naumov, George N.; Bradner, James E.; Althaus, Irene W.; Gandhi, Leena; Shapiro, Geoffrey I.; Nelson, James M.; Heymach, John V.; Meyerson, Matthew; Wong, Kwok-Kin; Jänne, Pasi A.

doi:10.1158/0008-5472.can-07-1885

Cited by 730Lung Cancer Treatments and MutationsHER2/EGFR in Cancer ResearchLung Cancer Research Studies

PF00299804, an Irreversible Pan-ERBB Inhibitor, Is Effective in Lung Cancer Models with EGFR and ERBB2 Mutations that Are Resistant to Gefitinib

Engelman, Jeffrey A., Zejnullahu, Kreshnik, Gale, Christopher-Michael, Lifshits, Eugene, Gonzales, Andrea J., Shimamura, Takeshi, Zhao, Feng, Vincent, Patrick W. +10 more·2007·Cancer Research

DOI 10.1158/0008-5472.can-07-1885

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Abstract

Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors gefitinib and erlotinib are effective treatments for a subset of non–small cell lung cancers. In particular, cancers with specific EGFR-activating mutations seem to be the most sensitive to these agents. However, despite their initial response, such cancers almost invariably develop resistance. In 50% of such cancers, a secondary EGFR mutation, T790M, has been identified that renders gefitinib and erlotinib ineffective inhibitors of EGFR kinase activity. Thus, there is a clinical need to develop novel EGFR inhibitors that can effectively inactivate T790M-containing EGFR proteins. In this study, we evaluate the effectiveness of a novel compound, PF00299804, an irreversible pan-ERBB inhibitor. The results from these studies show that PF00299804 is a potent inhibitor of EGFR-activating mutations as well as the EGFR T790M resistance mutation both in vitro and in vivo. Additionally, PF00299804 is a highly effective inhibitor of both the wild-type ERBB2 and the gefitinib-resistant oncogenic ERBB2 mutation identified in lung cancers. These preclinical evaluations support further clinical development of PF00299804 for cancers with mutations and/or amplifications of ERBB family members. [Cancer Res 2007;67(24):11924–32]

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Dacomitinib is an irreversible second-generation EGFR TKI originally developed by Pfizer and co-developed by SFJ Pharmaceuticals in 2012, and was approved by the FDA in 2018 for metastatic NSCLC with exon 19 deletion and exon 21 replacement.
“Dacomitinib (VizimproTM, PF-299804) (46), also an irreversible second-generation EGFR TKI originally developed by Pfizer and co-developed by SFJ Pharmaceuticals in 2012, was approved by the FDA in 2018 for the treatment of metastatic NSCLC with exon 19 deletion and exon 21 replacement.125–128”
From Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials (2023) · cites this paper as [128]
Uncontrolled activation of MET is oncogenic and facilitates the invasive and metastatic behaviour of EGFR-TKI resistant cells.
“Uncontrolled activation of MET is oncogenic and facilitates the invasive and metastatic behaviour of EGFR-TKI resistant cells.44”
From Mechanisms of resistance to EGFR-targeted drugs: lung cancer (2016) · cites this paper as [44]
MET overactivation in most EGFR-TKI acquired resistant tumours occurs via increased transcription and expression of MET protein while MET gene amplification is detected in 22% of cases.
“MET overactivation in most EGFR-TKI acquired resistant tumours occurs via increased transcription and expression of MET protein while MET gene amplification is detected in 22% of cases.”
From Mechanisms of resistance to EGFR-targeted drugs: lung cancer (2016) · cites this paper as [44]
Amplification of the MET oncogene accounts for 5-20% of acquired resistance causes.
“In particular, amplification of the MET oncogene, described for the first time in 2007,44 accounts for 5–20% of acquired resistance causes.”
From Mechanisms of resistance to EGFR-targeted drugs: lung cancer (2016) · cites this paper as [44]
Second-generation irreversible TKIs afatinib and dacomitinib are effective in untreated EGFR-mutant lung cancer.
“Second-generation irreversible EGFR TKIs such as afatinib (24) and dacomitinib (25) are effective in untreated EGFR mutant lung cancer (26, 27).”
From AZD9291, an Irreversible EGFR TKI, Overcomes T790M-Mediated Resistance to EGFR Inhibitors in Lung Cancer (2014) · cites this paper as [25]

Activating Mutations in the Epidermal Growth Factor Receptor Underlying Responsiveness of Non–Small-Cell Lung Cancer to Gefitinib
Lynch, T. J., Bell, D. W., Sordella, R., Gurubhagavatula, S., Okimoto, R. A., Brannigan, B. W., Harris, P. L., Haserlat, S. M., Supko, J. G., Haluska, F. G., et al. (2004) · New England Journal of Medicine · doi:10.1056/nejmoa040938 · Cited by 11,486 · see citing works
EGFR Mutations in Lung Cancer: Correlation with Clinical Response to Gefitinib Therapy
Paez, J. G., Jänne, P. A., Lee, J. C., Tracy, S., Greulich, H., Gabriel, S., Herman, P., Kaye, F. J., Lindeman, N., Boggon, T. J., et al. (2004) · Science · doi:10.1126/science.1099314 · Cited by 9,368 · see citing works
Self-citation
Erlotinib in Previously Treated Non–Small-Cell Lung Cancer
Shepherd, F. A., Rodrigues Pereira, J., Ciuleanu, T., Tan, E. H., Hirsh, V., Thongprasert, S., Campos, D., Maoleekoonpiroj, S., Smylie, M., Martins, R., et al. (2005) · New England Journal of Medicine · doi:10.1056/nejmoa050753 · Cited by 5,419 · see citing works
MET Amplification Leads to Gefitinib Resistance in Lung Cancer by Activating ERBB3 Signaling
Engelman, J. A., Zejnullahu, K., Mitsudomi, T., Song, Y., Hyland, C., Park, J. O., Lindeman, N., Gale, C.-M., Zhao, X., Christensen, J., et al. (2007) · Science · doi:10.1126/science.1141478 · Cited by 4,496 · see citing works
Self-citation
EGF receptor gene mutations are common in lung cancers from “never smokers” and are associated with sensitivity of tumors to gefitinib and erlotinib
Pao, W., Miller, V., Zakowski, M., Doherty, J., Politi, K., Sarkaria, I., Singh, B., Heelan, R., Rusch, V., Fulton, L., et al. (2004) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0405220101 · Cited by 4,338 · see citing works
EGFR Mutation and Resistance of Non–Small-Cell Lung Cancer to Gefitinib
Kobayashi, S., Boggon, T. J., Dayaram, T., Jänne, P. A., Kocher, O., Meyerson, M., Johnson, B. E., Eck, M. J., Tenen, D. G., & Halmos, B. (2005) · New England Journal of Medicine · doi:10.1056/nejmoa044238 · Cited by 3,964 · see citing works
Self-citation
Acquired Resistance of Lung Adenocarcinomas to Gefitinib or Erlotinib Is Associated with a Second Mutation in the EGFR Kinase Domain
Pao, W., Miller, V. A., Politi, K. A., Riely, G. J., Somwar, R., Zakowski, M. F., Kris, M. G., & Varmus, H. (2005) · PLoS Medicine · doi:10.1371/journal.pmed.0020073 · Cited by 3,527 · see citing works
Multi-Institutional Randomized Phase II Trial of Gefitinib for Previously Treated Patients With Advanced Non–Small-Cell Lung Cancer
Fukuoka, M., Yano, S., Giaccone, G., Tamura, T., Nakagawa, K., Douillard, J., Nishiwaki, Y., Vansteenkiste, J., Kudoh, S., Rischin, D., et al. (2003) · Journal of Clinical Oncology · doi:10.1200/jco.2003.10.038 · Cited by 2,871 · see citing works
Efficacy of Gefitinib, an Inhibitor of the Epidermal Growth Factor Receptor Tyrosine Kinase, in Symptomatic Patients With Non–Small Cell Lung Cancer: A Randomized Trial
Kris, M. G., Natale, R. B., Herbst, R. S., Lynch, Jr., Prager, D., Belani, C. P., Schiller, J. H., Kelly, K., Spiridonidis, H., Sandler, A., et al. (2003) · JAMA · doi:10.1001/jama.290.16.2149 · Cited by 2,517 · see citing works
Epidermal Growth Factor Receptor Gene and Protein and Gefitinib Sensitivity in Non–Small-Cell Lung Cancer
Cappuzzo, F., Hirsch, F. R., Rossi, E., Bartolini, S., Ceresoli, G. L., Bemis, L., Haney, J., Witta, S. E., Danenberg, K. D., Domenichini, I., et al. (2005) · JNCI Journal of the National Cancer Institute · doi:10.1093/jnci/dji112 · Cited by 1,538 · see citing works
KRAS Mutations and Primary Resistance of Lung Adenocarcinomas to Gefitinib or Erlotinib
Pao, W. J., Wang, T. Y., Riely, G. J., Miller, V. A., Pan, Q., Ladanyi, M., Zakowski, M. F., Heelan, R. T., Kris, M. G., & VARMUS, H. E. (2005) · PLoS Medicine · doi:10.1371/journal.pmed.0020017 · Cited by 1,517 · see citing works
The specificities of protein kinase inhibitors: an update
BAIN, J., McLAUCHLAN, H., ELLIOTT, M., & COHEN, P. (2003) · Biochemical Journal · doi:10.1042/bj20021535 · Cited by 1,369 · see citing works
Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts
Fry, D. W., Harvey, P. J., Keller, P. R., Elliott, W. L., Meade, M., Trachet, E., Albassam, M., Zheng, X., Leopold, W. R., Pryer, N. K., et al. (2004) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.1427.3.11 · Cited by 1,236 · see citing works
Determinants of Tumor Response and Survival With Erlotinib in Patients With Non—Small-Cell Lung Cancer
Perez-Soler, R., Chachoua, A., Hammond, L. A., Rowinsky, E. K., Huberman, M. S., Karp, D. D., Rigas, J. R., Clark, G. M., Santabarbara, P., & Bonomi, P. (2004) · Journal of Clinical Oncology · doi:10.1200/jco.2004.11.057 · Cited by 1,067 · see citing works
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. M., Lynch, T. J., et al. (2005) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0502860102 · Cited by 950 · see citing works
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
Mitsudomi, T., Kosaka, T., Endoh, H., Horio, Y., Hida, T., Mori, S., Hatooka, S., Shinoda, M., Takahashi, T., & Yatabe, Y. (2005) · Journal of Clinical Oncology · doi:10.1200/jco.2005.00.992 · Cited by 938 · see citing works
Novel D761Y and Common Secondary T790M Mutations in Epidermal Growth Factor Receptor–Mutant Lung Adenocarcinomas with Acquired Resistance to Kinase Inhibitors
Balak, M. N., Gong, Y., Riely, G. J., Somwar, R., Li, A. R., Zakowski, M. F., Chiang, A. C., Yang, G., Ouerfelli, O., Kris, M. G., et al. (2006) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-06-1570 · Cited by 822 · see citing works
Intragenic ERBB2 kinase mutations in tumours
Stephens, P., Hunter, C., Bignell, G., Edkins, S., Davies, H., Teague, J., Stevens, C., O'Meara, S., Smith, R., Parker, A., et al. (2004) · Nature · doi:10.1038/431525b · Cited by 802 · see citing works
Efficacy of cytotoxic agents against human tumor xenografts is markedly enhanced by coadministration of ZD1839 (Iressa), an inhibitor of EGFR tyrosine kinase.
Sirotnak, F. M., Zakowski, M. F., Miller, V. A., Scher, H. I., & Kris, M. G. (2000) · PubMed · Cited by 761 · see citing works
Predictive and Prognostic Impact of Epidermal Growth Factor Receptor Mutation in Non–Small-Cell Lung Cancer Patients Treated With Gefitinib
Han, S., Kim, T., Hwang, P. G., Jeong, S., Kim, J., Choi, I. S., Oh, D., Kim, J. H., Kim, D., Chung, D. H., et al. (2005) · Journal of Clinical Oncology · doi:10.1200/jco.2005.01.388 · Cited by 757 · see citing works
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. J., Ceppa, D. P., Li, A. R., Rizvi, N. A., Venkatraman, E. S., Zakowski, M. F., Kris, M. G., Ladanyi, M., & Miller, V. A. (2006) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-05-1846 · Cited by 730 · see citing works
Epidermal Growth Factor Receptor Gene Mutations and Increased Copy Numbers Predict Gefitinib Sensitivity in Patients With Recurrent Non–Small-Cell Lung Cancer
Takano, T., Ohe, Y., Sakamoto, H., Tsuta, K., Matsuno, Y., Tateishi, U., Yamamoto, S., Nokihara, H., Yamamoto, N., Sekine, I., et al. (2005) · Journal of Clinical Oncology · doi:10.1200/jco.2005.01.0793 · Cited by 691 · see citing works
Oncogenic Transformation by Inhibitor-Sensitive and -Resistant EGFR Mutants
Greulich, H., Chen, T.-H., Feng, W., Jänne, P. A., Alvarez, J. V., Zappaterra, M., Bulmer, S. E., Frank, D. A., Hahn, W. C., Sellers, W. R., et al. (2005) · PLoS Medicine · doi:10.1371/journal.pmed.0020313 · Cited by 677 · see citing works
Self-citation
Prevention of Organ Allograft Rejection by a Specific Janus Kinase 3 Inhibitor
Changelian, P. S., Flanagan, M. E., Ball, D. J., Kent, C. R., Magnuson, K. S., Martin, W. H., Rizzuti, B. J., Sawyer, P. S., Perry, B. D., Brissette, W. H., et al. (2003) · Science · doi:10.1126/science.1087061 · Cited by 666 · see citing works
Analysis of Epidermal Growth Factor Receptor Gene Mutation in Patients with Non–Small Cell Lung Cancer and Acquired Resistance to Gefitinib
Kosaka, T., Yatabe, Y., Endoh, H., Yoshida, K., Hida, T., Tsuboi, M., Tada, H., Kuwano, H., & Mitsudomi, T. (2006) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-06-0714 · Cited by 595 · see citing works
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
Jackman, D. M., Yeap, B. Y., Sequist, L. V., Lindeman, N., Holmes, A. J., Joshi, V. A., Bell, D. W., Huberman, M. S., Halmos, B., Rabin, M. S., et al. (2006) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-06-0462 · Cited by 584 · see citing works
Self-citation
Pharmacodynamic Studies of the Epidermal Growth Factor Receptor Inhibitor ZD1839 in Skin From Cancer Patients: Histopathologic and Molecular Consequences of Receptor Inhibition
Albanell, J., Rojo, F., Averbuch, S., Feyereislova, A., Mascaro, J. M., Herbst, R. S., LoRusso, P. M., Rischin, D., Sauleda, S., Gee, J., et al. (2002) · Journal of Clinical Oncology · doi:10.1200/jco.20.1.110 · Cited by 529 · see citing works
Prospective phase II study of gefitinib for chemotherapy-naive patients with advanced non-small-cell lung cancer with epidermal growth factor receptor gene mutations
Inoue, A., Suzuki, T., Fukuhara, T., Maemondo, M., Kimura, Y., Morikawa, N., Watanabe, H., Saijo, Y., & Nukiwa, T. (2006) · Journal of Clinical Oncology · doi:10.1200/jco.2005.05.4692 · Cited by 509 · see citing works
ErbB-3 mediates phosphoinositide 3-kinase activity in gefitinib-sensitive non-small cell lung cancer cell lines
Engelman, J. A., Janne, P. A., Mermel, C. H., Pearlberg, J., Mukohara, T., Fleet, C., Cichowski, K. M., Johnson, B. E., & Cantley, L. C. (2005) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0409773102 · Cited by 494 · see citing works
Self-citation
HER2 kinase domain mutation results in constitutive phosphorylation and activation of HER2 and EGFR and resistance to EGFR tyrosine kinase inhibitors
Wang, S. E., Narasanna, A., Pérez-Torres, M., Xiang, B., Wu, F. Y., Yang, S., Carpenter, G. F., Gazdar, A. F., Muthuswamy, S. K., & Arteaga, C. L. (2006) · Cancer Cell · doi:10.1016/j.ccr.2006.05.023 · Cited by 474 · see citing works
Allelic dilution obscures detection of a biologically significant resistance mutation in EGFR-amplified lung cancer
Engelman, J. A., Mukohara, T., Zejnullahu, K., Lifshits, E., Borras, A. M., Gale, C.-M., Naumov, G. N., Yeap, B. Y., Jarrell, E., Sun, J., et al. (2006) · Journal of Clinical Investigation · doi:10.1172/jci28656 · Cited by 457 · see citing works
Self-citation
Loss of PTEN/MMAC1/TEP in EGF receptor-expressing tumor cells counteracts the antitumor action of EGFR tyrosine kinase inhibitors
Bianco, R., Shin, I., Ritter, C. A., Yakes, F. M., Basso, A., Rosen, N. X., Tsurutani, J., Dennis, P. A., Mills, G. B., & Arteaga, C. L. (2003) · Oncogene · doi:10.1038/sj.onc.1206388 · Cited by 449 · see citing works
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. (2006) · Cancer Research · doi:10.1158/0008-5472.can-06-0453 · Cited by 445 · see citing works
Aberrant Epidermal Growth Factor Receptor Signaling and Enhanced Sensitivity to EGFR Inhibitors in Lung Cancer
Amann, J. M., Kalyankrishna, S., Massion, P. P., Ohm, J. E., Girard, L., Shigematsu, H., Peyton, M., Juroske, D. M., Huang, Y., Salmon, J. S., et al. (2005) · Cancer Research · doi:10.1158/0008-5472.226.65.1 · Cited by 432 · see citing works
Epidermal Growth Factor Receptor Mutations in Non–Small-Cell Lung Cancer: Implications for Treatment and Tumor Biology
Janne, P. A., Engelman, J. A., & Johnson, B. E. (2005) · Journal of Clinical Oncology · doi:10.1200/jco.2005.09.985 · Cited by 405 · see citing works
Self-citation
IncreasedHER2Gene Copy Number Is Associated With Response to Gefitinib Therapy in Epidermal Growth Factor Receptor–Positive Non–Small-Cell Lung Cancer Patients
Cappuzzo, F., Varella-Garcia, M., Shigematsu, H., Domenichini, I., Bartolini, S., Ceresoli, G. L., Rossi, E., Ludovini, V., Gregorc, V., Toschi, L., et al. (2005) · Journal of Clinical Oncology · doi:10.1200/jco.2005.09.111 · Cited by 369 · see citing works
Gefitinib Induces Apoptosis in the EGFRL858R Non–Small-Cell Lung Cancer Cell Line H3255
Tracy, S. I., Mukohara, T., Hansen, M., Meyerson, M. M., Johnson, B. E., & Janne, P. A. (2004) · Cancer Research · doi:10.1158/0008-5472.can-04-1905 · Cited by 368 · see citing works
Self-citation
Homozygous Deletions and Chromosome Amplifications in Human Lung Carcinomas Revealed by Single Nucleotide Polymorphism Array Analysis
Zhao, X., Weir, B. A., LaFramboise, T., Lin, M. G., Beroukhim, R., Garraway, L. A., Beheshti, J., Lee, J. C., Naoki, K., Richards, W. G., et al. (2005) · Cancer Research · doi:10.1158/0008-5472.can-04-4603 · Cited by 333 · see citing works
Self-citation
Differential Effects of Gefitinib and Cetuximab on Non–small-cell Lung Cancers Bearing Epidermal Growth Factor Receptor Mutations
Mukohara, T., Engelman, J. A., Hanna, N. H., Yeap, B. Y., Kobayashi, S. S., Lindeman, N. I., Halmos, B., Pearlberg, J., Tsuchihashi, Z., Cantley, L. C., et al. (2005) · JNCI Journal of the National Cancer Institute · doi:10.1093/jnci/dji238 · Cited by 313 · see citing works
Self-citation
Human mammary epithelial cell transformation through the activation of phosphatidylinositol 3-kinase
Zhao, J. J., Gjoerup, O. V., Subramanian, R. R., Cheng, Y., Chen, W., Roberts, T. M., & Hahn, W. C. (2003) · Cancer Cell · doi:10.1016/s1535-6108(03)00088-6 · Cited by 280 · see citing works
Pharmacodynamic Studies of the Epidermal Growth Factor Receptor Inhibitor ZD1839 in Skin From Cancer Patients: Histopathologic and Molecular Consequences of Receptor Inhibition
Albanell, J., Rojo, F., Averbuch, S., et al. (2002) · Journal of Clinical Oncology · doi:10.1200/jco.2002.20.1.110 · Cited by 257 · see citing works
Bronchial and Peripheral Murine Lung Carcinomas Induced by T790M-L858R Mutant EGFR Respond to HKI-272 and Rapamycin Combination Therapy
Li, D., Shimamura, T., Ji, H., Chen, L., Haringsma, H. J., McNamara, K. L., Liang, M., Perera, S. A., Zaghlul, S., Borgman, C. L., et al. (2007) · Cancer Cell · doi:10.1016/j.ccr.2007.06.005 · Cited by 242 · see citing works
Self-citation
Micronutrient Sprinkles to Control Childhood Anaemia
Zlotkin, S. H., Schauer, C. S., Christofides, A., Sharieff, W., Tondeur, M. C., & Hyder, S. M. Z. (2005) · PLoS Medicine · doi:10.1371/journal.pmed.0020001 · Cited by 225 · see citing works
Prospective Study of Gefitinib in Epidermal Growth Factor Receptor Fluorescence In Situ Hybridization–Positive/Phospho-Akt–Positive or Never Smoker Patients With Advanced Non–Small-Cell Lung Cancer: The ONCOBELL Trial
Cappuzzo, F., Ligorio, C., Janne, P. A., Toschi, L., Rossi, E., Trisolini, R., Paioli, D., Tisch, A. H., Magrini, E., Finocchiaro, G., et al. (2007) · Journal of Clinical Oncology · doi:10.1200/jco.2006.09.4300 · Cited by 210 · see citing works
Self-citation
Epidermal Growth Factor–Independent Transformation of Ba/F3 Cells with Cancer-Derived Epidermal Growth Factor Receptor Mutants Induces Gefitinib-Sensitive Cell Cycle Progression
Jiang, J., Greulich, H. E., Janne, P. A., Sellers, W. R., Meyerson, M. M., & Griffin, J. D. (2005) · Cancer Research · doi:10.1158/0008-5472.can-05-1829 · Cited by 188 · see citing works
Self-citation
A prospective phase II trial of erlotinib in advanced non-small cell lung cancer (NSCLC) patients (p) with mutations in the tyrosine kinase (TK) domain of the epidermal growth factor receptor (EGFR)
Paz-Ares, L. G., Sanchez, J. M., Garcia-Velasco, A., Massutí, B., López-Vivanco, G., Provencio, M., Montés, A. F., Isla, D., Amador, M. L., & Rosell, R. (2006) · Journal of Clinical Oncology · doi:10.1200/jco.2006.24.18_suppl.7020 · Cited by 164 · see citing works
Momentous sprint at the 2156 Olympics?
Tatem, A. J., Guerra, C. A., Atkinson, P. M., & Hay, S. I. (2004) · Nature · doi:10.1038/431525a · Cited by 140 · see citing works
Non–Small-Cell Lung Cancer and Ba/F3 Transformed Cells Harboring the ERBB2 G776insV_G/C Mutation Are Sensitive to the Dual-Specific Epidermal Growth Factor Receptor and ERBB2 Inhibitor HKI-272
Shimamura, T., Ji, H., Minami, Y., Thomas, R. K., Lowell, A. M., Shah, K., Greulich, H. E., Glatt, K. A., Meyerson, M. M., Shapiro, G. I., et al. (2006) · Cancer Research · doi:10.1158/0008-5472.can-06-0971 · Cited by 135 · see citing works
Self-citation
Antitumor Activity of the Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase Inhibitor Gefitinib (ZD1839, Iressa) in Non–Small Cell Lung Cancer Cell Lines Correlates with Gene Copy Number and EGFR Mutations but not EGFR Protein Levels
Helfrich, B. A., Raben, D., Varella‐Garcia, M., Gustafson, D., Chan, D. C. F., Bemis, L., Coldren, C. D., Barón, A. E., Zeng, C., Franklin, W. A., et al. (2006) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-06-0760 · Cited by 126 · see citing works
Allele-dependent variation in the relative cellular potency of distinct EGFR inhibitors
Yuza, Y., Glatt, K. A., Jiang, J., Greulich, H., Minami, Y., Woo, M. S., Shimamura, T., Shapiro, G. I., Lee, J. C., Ji, H., et al. (2007) · Cancer Biology & Therapy · doi:10.4161/cbt.6.5.4003 · Cited by 88 · see citing works
Self-citation
EGFR exon 20 insertion mutation in Japanese lung cancer
Sasaki, H., Endo, K., Takada, M., Kawahara, M., Kitahara, N., Tanaka, H., Okumura, M., Matsumura, A., Iuchi, K., Kawaguchi, T., et al. (2007) · Lung Cancer · doi:10.1016/j.lungcan.2007.06.024 · Cited by 84 · see citing works
Transformation-specific interaction of the bovine papillomavirus E5 oncoprotein with the platelet-derived growth factor receptor transmembrane domain and the epidermal growth factor receptor cytoplasmic domain
Cohen, B. D., Goldstein, D. J., Rutledge, L., Vass, W. C., Lowy, D. R., Schlegel, R., & Schiller, J. T. (1993) · Journal of Virology · doi:10.1128/jvi.67.9.5303-5311.1993 · Cited by 82 · see citing works
Tyrosine Kinase Inhibitors. 19. 6-Alkynamides of 4-Anilinoquinazolines and 4-Anilinopyrido[3,4-d]pyrimidines as Irreversible Inhibitors of the erbB Family of Tyrosine Kinase Receptors
Klutchko, S. R., Zhou, H., Winters, R. T., Tran, T. P., Bridges, A. J., Althaus, I. W., Amato, D. M., Elliott, W. L., Ellis, P. A., Meade, M. A., et al. (2006) · Journal of Medicinal Chemistry · doi:10.1021/jm050936o · Cited by 81 · see citing works
Self-citation
Sensitivity of Non-Small-Cell Lung Cancer Cell Lines Established from Patients Treated with Prolonged Infusions of Paclitaxel
藤下, 隆., Loda, M. F., Turner, R. E., Gentler, M., Kashii, T., Breathnach, O. S., & Johnson, B. E. (2003) · Oncology · doi:10.1159/000070299 · Cited by 19 · see citing works
Activity of anti-erbB-2 recombinant toxin OLX-209 on lung cancer cell lines in the absence of erbB-2 gene amplification
Kasprzyk, P. G. (1996) · Lung Cancer · doi:10.1016/0169-5002(96)84186-9 · Cited by 16 · see citing works
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Schellens, J. H. M., Britten, C. D., Camidge, D. R., Boss, D. S., Wong, S., Diab, S., Guo, F., Maguire, R. P., Letrent, S. P., & Eckhardt, S. (2007) · Journal of Clinical Oncology · doi:10.1200/jco.2007.25.18_suppl.3599 · Cited by 13 · see citing works

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Bouyain, S., Longo, P. A., Li, S., Ferguson, K. M., & Leahy, D. J. (2005) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0507591102 · Cited by 191 · see citing works
ERBB3/HER3 and ERBB2/HER2 Duet in Mammary Development and Breast Cancer
Stern, D. F. (2008) · Journal of Mammary Gland Biology and Neoplasia · doi:10.1007/s10911-008-9083-7 · Cited by 150 · see citing works
Epidermal Growth Factor Mutant with Wild-Type Affinity for Both ErbB1 and ErbB3
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Abstract 3864: Biological basis of pan-ErbB receptor targeting for malignant melanoma treatment
Ng, Y., Stabile, L. P., Torres, S. M., et al. (2012) · Cancer Research · doi:10.1158/1538-7445.am2012-3864 · Cited by 5 · see citing works
Flotillin depletion affects ErbB protein levels in different human breast cancer cells
Asp, N., Pust, S., & Sandvig, K. (2014) · Biochimica et Biophysica Acta (BBA) - Molecular Cell Research · doi:10.1016/j.bbamcr.2014.04.013 · Cited by 25 · see citing works

Authors: Engelman, J. A., Zejnullahu, K., Gale, C.-M., Lifshits, E., Gonzales, A. J., Shimamura, T., Zhao, F., Vincent, P. W., Naumov, G. N., Bradner, J. E., Althaus, I. W., Gandhi, L., Shapiro, G. I., Nelson, J. M., Heymach, J. V., Meyerson, M., Wong, K.-K., & Jänne, P. A.
Affiliations: Beth Israel Deaconess Medical Center (US)
Dana-Farber Cancer Institute (US)
6Department of Surgery and Vascular Biology Program, Children's Hospital;
Pfizer (United States) (US)
Brigham and Women's Hospital (US)
The University of Texas MD Anderson Cancer Center (US)
Broad Institute (US)
4Lowe Center for Thoracic Oncology and
ORCID: Engelman, Jeffrey A.
Gonzales, Andrea J.
Shimamura, Takeshi
Zhao, Feng
Bradner, James E.
Gandhi, Leena
Shapiro, Geoffrey I.
Nelson, James M.
Heymach, John V.
Meyerson, Matthew
Wong, Kwok-Kin
Venue: Cancer Research
Publisher: American Association for Cancer Research (AACR)
Published: 2007-12-15
Volume: 67
Issue: 24
Pages: 11924-11932
ISSN: 0008-5472 (ISSN-L)
1538-7445
DOI: 10.1158/0008-5472.can-07-1885
OpenAlex: W2110841878
Cited by: 730
References: 56
Citations by year: 2026: 15 · 2025: 23 · 2024: 26 · 2023: 33 · 2022: 34 · 2021: 37 · 2020: 36 · 2019: 44 · 2018: 34 · 2017: 40 · 2016: 45 · 2015: 56 · 2014: 65 · 2013: 63 · 2012: 65
FWCI: 18.43
Type: journal article
Language: en
Open access: closed
Locations: Cancer Research (publishedVersion)
PubMed (publishedVersion)
Funders: National Cancer Institute (R01CA114465, K08CA120060)
Topics: Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Lung Cancer Treatments and Mutations
Health Sciences › Medicine › Oncology › HER2/EGFR in Cancer Research
Health Sciences › Medicine › Oncology › Lung Cancer Research Studies
Keywords: EGFR tyrosine kinase inhibitors, gefitinib resistance, T790M mutation, ERBB2 mutations, non-small cell lung cancer, EGFR activating mutations, EGFR amplification, ErbB family
MeSH terms: Gefitinib, Animals, Antineoplastic Agents, Cell Division, Cloning, Molecular, Humans, Lung Neoplasms, Mice, Nude, Quinazolines, Oncogene Proteins v-erbB, Cell Line, Tumor, Adaptor Proteins, Signal Transducing, Mice, Quinazolinones, ErbB Receptors

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PF00299804, an Irreversible Pan-ERBB Inhibitor, Is Effective in Lung Cancer Models with EGFR and ERBB2 Mutations that Are Resistant to Gefitinib

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