Targeting EGFR L858R/T790M and EGFR L858R/T790M/C797S resistance mutations in NSCLC: Current developments in medicinal chemistry

Lu, Xiaoyun; Yu, Lei; Zhang, Zhang; Ren, Xiaomei; Smaill, Jeff B.; Ding, Ke

doi:10.1002/med.21488

Cited by 173Lung Cancer Treatments and MutationsHER2/EGFR in Cancer ResearchCancer Mechanisms and Therapy

Targeting EGFR L858R/T790M and EGFR L858R/T790M/C797S resistance mutations in NSCLC: Current developments in medicinal chemistry

Lu, Xiaoyun, Yu, Lei, Zhang, Zhang, Ren, Xiaomei, Smaill, Jeff B., Ding, Ke·2018·Medicinal Research Reviews

DOI 10.1002/med.21488

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Abstract

Both the first‐generation reversible epidermal growth factor receptor (EGFR) inhibitors gefitinib and erlotinib and the second‐generation covalent epidermal growth factor receptor tyrosine kinase inhibitor (EGFR‐TKI) afatinib have significantly improved the survival of non‐small‐cell lung cancer (NSCLC) patients with activating EGFR mutations. However, a secondary EGFR T790M mutation leads to the clinically acquired resistance to the first‐ and second‐generation EGFR‐TKIs drugs. A number of the third‐generation wild‐type sparing EGFR inhibitors, for example, WZ4002, CO1686, AZD9291, HM61713, EGF816, ASP8173, and PF0674775, have been developed, among which AZD9291 has been approved by US FDA for the treatment of NSCLC patients with EGFR T790M . More recently, a tertiary EGFR C797S mutation was reported as the dominant resistance mechanism to the third‐generation irreversible inhibitors. It is highly desirable to develop the fourth‐generation EGFR inhibitors. This review summarizes the mechanisms of acquired resistance and the latest medicinal chemistry advances on the third‐ and fourth‐generation EGFR inhibitors, with special attention being paid to the allosteric and reversible inhibitors combating the tertiary EGFR C797S mutation.

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Nazartinib demonstrates potent inhibitory effects on pEGFR levels in H3255, HCC827, and H1975 cell lines, leading to effective inhibition of cell proliferation.
“The drug demonstrates potent inhibitory effects on pEGFR levels in H3255, HCC827, and H1975 cell lines, leading to effective inhibition of cell proliferation.173–176”
From Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials (2023) · cites this paper as [176]

Global cancer statistics, 2012
Torre, L. A., Bray, F., Siegel, R. L., Ferlay, J., Lortet‐Tieulent, J., & Jemal, A. (2015) · CA A Cancer Journal for Clinicians · doi:10.3322/caac.21262 · Cited by 26,858 · see citing works
Cancer statistics, 2016
Siegel, R. L., Miller, K. D., & Jemal, A. (2016) · CA: A Cancer Journal for Clinicians · doi:10.3322/caac.21332 · Cited by 16,003 · see citing works
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
Gefitinib or Chemotherapy for Non–Small-Cell Lung Cancer with Mutated EGFR
Maemondo, M., Inoue, A., Kobayashi, K., Sugawara, S., Oizumi, S., Isobe, H., Gemma, A., Harada, M., Yoshizawa, H., Kinoshita, I., et al. (2010) · New England Journal of Medicine · doi:10.1056/nejmoa0909530 · Cited by 5,525 · see citing works
Erlotinib versus standard chemotherapy as first-line treatment for European patients with advanced EGFR mutation-positive non-small-cell lung cancer (EURTAC): a multicentre, open-label, randomised phase 3 trial
Rosell, R., Carcereny, E., Gervais, R., Vergnenegre, A., Massuti, B., Felip, E., Palmero, R., Garcia-Gomez, R., Pallares, C., Sanchez, J. M., et al. (2012) · The Lancet Oncology · doi:10.1016/s1470-2045(11)70393-x · Cited by 5,489 · 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
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
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
Genotypic and Histological Evolution of Lung Cancers Acquiring Resistance to EGFR Inhibitors
Sequist, L. V., Waltman, B. A., Dias-Santagata, D., Digumarthy, S., Turke, A. B., Fidias, P., Bergethon, K., Shaw, A. T., Gettinger, S., Cosper, A. K., et al. (2011) · Science Translational Medicine · doi:10.1126/scitranslmed.3002003 · Cited by 3,499 · see citing works
Osimertinib or Platinum–Pemetrexed in EGFR T790M–Positive Lung Cancer
Mok, T. S., Wu, Y.-L., Ahn, M.-J., Garassino, M. C., Kim, H. R., Ramalingam, S. S., Shepherd, F. A., He, Y., Akamatsu, H., Theelen, W. S. M. E., et al. (2017) · New England Journal of Medicine · doi:10.1056/nejmoa1612674 · Cited by 3,379 · see citing works
ERBB receptors and cancer: the complexity of targeted inhibitors
Hynes, N. E., & Lane, H. A. (2005) · Nature reviews. Cancer · doi:10.1038/nrc1609 · Cited by 3,313 · see citing works
Epidermal growth factor receptor mutations in lung cancer
Sharma, S. V., Bell, D. W., Settleman, J., & Haber, D. A. (2007) · Nature Reviews Cancer · doi:10.1038/nrc2088 · Cited by 3,170 · see citing works
AZD9291, an Irreversible EGFR TKI, Overcomes T790M-Mediated Resistance to EGFR Inhibitors in Lung Cancer
Cross, D. A. E., Ashton, S. E., Ghiorghiu, S., Eberlein, C., Nebhan, C. A., Spitzler, P. J., Orme, J. P., Finlay, M. R. V., Ward, R. A., Mellor, M. J., et al. (2014) · Cancer Discovery · doi:10.1158/2159-8290.cd-14-0337 · Cited by 2,246 · see citing works
The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP
Yun, C.-H., Mengwasser, K. E., Toms, A. V., Woo, M. S., Greulich, H., Wong, K.-K., Meyerson, M., & Eck, M. J. (2008) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0709662105 · Cited by 2,118 · see citing works
AZD9291 in EGFR Inhibitor–Resistant Non–Small-Cell Lung Cancer
Jänne, P. A., Yang, J. C.-H., Kim, D.-W., Planchard, D., Ohe, Y., Ramalingam, S. S., Ahn, M.-J., Kim, S.-W., Su, W.-C., Horn, L., et al. (2015) · New England Journal of Medicine · doi:10.1056/nejmoa1411817 · Cited by 2,116 · see citing works
Clinical Features and Outcome of Patients With Non–Small-Cell Lung Cancer Who Harbor EML4-ALK
Shaw, A. T., Yeap, B. Y., Mino-Kenudson, M. A., Digumarthy, S. R., Costa, D. B., Heist, R. S., Solomon, B., Stubbs, H., Admane, S., McDermott, U., et al. (2009) · Journal of Clinical Oncology · doi:10.1200/jco.2009.22.6993 · Cited by 1,873 · see citing works
MET amplification occurs with or without T790M mutations in EGFR mutant lung tumors with acquired resistance to gefitinib or erlotinib
Bean, J., Brennan, C., Shih, J.-Y., Riely, G., Viale, A., Wang, L., Chitale, D., Motoi, N., Szoke, J., Broderick, S., et al. (2007) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0710370104 · Cited by 1,598 · see citing works
Acquired EGFR C797S mutation mediates resistance to AZD9291 in non–small cell lung cancer harboring EGFR T790M
Thress, K. S., Paweletz, C. P., Felip, E., Cho, B. C., Stetson, D., Dougherty, B., Lai, Z., Markovets, A., Vivancos, A., Kuang, Y., et al. (2015) · Nature Medicine · doi:10.1038/nm.3854 · Cited by 1,589 · 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
BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models
Li, D., Ambrogio, L., Shimamura, T., Kubo, S., Takahashi, M., Chirieac, L. R., Padera, R. F., Shapiro, G. I., Baum, A., Himmelsbach, F., et al. (2008) · Oncogene · doi:10.1038/onc.2008.109 · Cited by 1,447 · see citing works
Small-cell lung cancer
van Meerbeeck, J. P., Fennell, D. A., & Ruysscher, D. D. (2011) · The Lancet · doi:10.1016/s0140-6736(11)60165-7 · Cited by 1,239 · see citing works
BRAF and RAS mutations in human lung cancer and melanoma.
Brose, M. S., Volpe, P., Feldman, M. D., Kumar, M. S., Rishi, I., Gerrero, R. M., Einhorn, E., Herlyn, M., Minna, J. D., Nicholson, A. G., et al. (2002) · PubMed · Cited by 1,053 · see citing works
Novel mutant-selective EGFR kinase inhibitors against EGFR T790M
Zhou, W., Ercan, D., Chen, L., Yun, C.-H., Li, D., Capelletti, M., Cortot, A. B., Chirieac, L., Iacob, R. E., Padera, R., et al. (2009) · Nature · doi:10.1038/nature08622 · Cited by 1,013 · see citing works
Protein kinase C and other diacylglycerol effectors in cancer
Griner, E. M., & Kazanietz, M. G. (2007) · Nature Reviews Cancer · doi:10.1038/nrc2110 · Cited by 978 · see citing works
Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors
Jia, Y., Yun, C., Park, E., Ercan, D., Manuia, M., Juarez, J., Xu, C., Rhee, K., Chen, T., Zhang, H., et al. (2016) · Nature · doi:10.1038/nature17960 · Cited by 933 · see citing works
Induction of apoptosis and cell cycle arrest by CP-358,774, an inhibitor of epidermal growth factor receptor tyrosine kinase.
Moyer, J. D., Barbacci, E. G., Iwata, K. K., Arnold, L., Boman, B., Cunningham, A., DiOrio, C., Doty, J., Morin, M. J., Moyer, M. P., et al. (1997) · PubMed · doi:10.7270/q2dr317m · Cited by 841 · 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 823 · see citing works
Assessment of somatic k-RAS mutations as a mechanism associated with resistance to EGFR-targeted agents: a systematic review and meta-analysis of studies in advanced non-small-cell lung cancer and metastatic colorectal cancer
Linardou, H., Dahabreh, I. J., Kanaloupiti, D., Siannis, F., Bafaloukos, D., Kosmidis, P., Papadimitriou, C. A., & Murray, S. (2008) · The Lancet Oncology · doi:10.1016/s1470-2045(08)70206-7 · Cited by 739 · see citing works
PF00299804, an Irreversible Pan-ERBB Inhibitor, Is Effective in Lung Cancer Models with EGFR and ERBB2 Mutations that Are Resistant to Gefitinib
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., et al. (2007) · Cancer Research · doi:10.1158/0008-5472.can-07-1885 · Cited by 730 · see citing works
Osimertinib for pretreated EGFR Thr790Met-positive advanced non-small-cell lung cancer (AURA2): a multicentre, open-label, single-arm, phase 2 study
Goss, G. D., Tsai, C., Shepherd, F. A., Bazhenova, L. A., Lee, J. S., Chang, G., Crinò, L., Satouchi, M., Chu, Q. S.-C., Hida, T., et al. (2016) · The Lancet Oncology · doi:10.1016/s1470-2045(16)30508-3 · Cited by 647 · see citing works
Hepatocyte growth factor induces gefitinib resistance of lung adenocarcinoma with epidermal growth factor receptor-activating mutations
Yano, S., Wang, W., Li, Q., Matsumoto, K., Sakurama, H., Nakamura, T., Ogino, H., Kakiuchi, S., Hanibuchi, M., Nishioka, Y., et al. (2008) · Cancer Research · doi:10.1158/0008-5472.can-08-1643 · Cited by 643 · see citing works
Antitumor Activity of HKI-272, an Orally Active, Irreversible Inhibitor of the HER-2 Tyrosine Kinase
Rabindran, S. K., Discafani, C. M., Rosfjord, E. C., Baxter, M., Floyd, M. B., Golas, J., Hallett, W. A., Johnson, B. D., Nilakantan, R., Overbeek, E., et al. (2004) · Cancer Research · doi:10.1158/0008-5472.can-03-2868 · Cited by 642 · see citing works
Discovery of a Potent and Selective EGFR Inhibitor (AZD9291) of Both Sensitizing and T790M Resistance Mutations That Spares the Wild Type Form of the Receptor
Finlay, M. R. V., Anderton, M., Ashton, S., Ballard, P., Bethel, P. A., Box, M. R., Bradbury, R. H., Brown, S. J., Butterworth, S., Campbell, A., et al. (2014) · Journal of Medicinal Chemistry · doi:10.1021/jm500973a · Cited by 636 · see citing works
Acquired Resistance to EGFR Tyrosine Kinase Inhibitors in EGFR-Mutant Lung Cancer: Distinct Natural History of Patients with Tumors Harboring the T790M Mutation
Oxnard, G. R., Arcila, M. E., Sima, C. S., Riely, G. J., Chmielecki, J., Kris, M. G., Pao, W., Ladanyi, M., & Miller, V. A. (2011) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-10-2692 · Cited by 627 · see citing works
Discovery of a Mutant-Selective Covalent Inhibitor of EGFR that Overcomes T790M-Mediated Resistance in NSCLC
Walter, A. O., Sjin, R. T. T., Haringsma, H. J., Ohashi, K., Sun, J., Lee, K., Dubrovskiy, A., Labenski, M., Zhu, Z., Wang, Z., et al. (2013) · Cancer Discovery · doi:10.1158/2159-8290.cd-13-0314 · Cited by 620 · 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
Rebiopsy of Lung Cancer Patients with Acquired Resistance to EGFR Inhibitors and Enhanced Detection of the T790M Mutation Using a Locked Nucleic Acid-Based Assay
Arcila, M. E., Oxnard, G. R., Nafa, K., Riely, G. J., Solomon, S. B., Zakowski, M. F., Kris, M. G., Pao, W., Miller, V. A., & Ladanyi, M. (2011) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-10-2277 · Cited by 574 · see citing works
Studies leading to the identification of ZD1839 (iressa™): an orally active, selective epidermal growth factor receptor tyrosine kinase inhibitor targeted to the treatment of cancer
Barker, A. J., Gibson, K. H., Grundy, W., Godfrey, A. A., Barlow, J. J., Healy, M. P., Woodburn, J. R., Ashton, S. E., Curry, B. J., Scarlett, L., et al. (2001) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/s0960-894x(01)00344-4 · Cited by 572 · see citing works
BIM Mediates EGFR Tyrosine Kinase Inhibitor-Induced Apoptosis in Lung Cancers with Oncogenic EGFR Mutations
Costa, D. B., Halmos, B., Kumar, A., Schumer, S., Huberman, M. S., Boggon, T. J., Tenen, D. G., & Kobayashi, S. S. (2007) · PLoS Medicine · doi:10.1371/journal.pmed.0040315 · Cited by 499 · see citing works
Heterogeneity Underlies the Emergence of EGFR T790 Wild-Type Clones Following Treatment of T790M-Positive Cancers with a Third-Generation EGFR Inhibitor
Piotrowska, Z., Niederst, M. J., Karlovich, C., Wakelee, H. A., Neal, J. W., Mino-Kenudson, M. A., Fulton, L. E., Hata, A. N., Lockerman, E. L., Kalsy, A., et al. (2015) · Cancer Discovery · doi:10.1158/2159-8290.cd-15-0399 · Cited by 459 · see citing works
Presence ofEpidermal Growth Factor ReceptorGene T790M Mutation as a Minor Clone in Non–Small Cell Lung Cancer
Inukai, M., Toyooka, S., Ito, S., Asano, H., Ichihara, S., Soh, J., Suehisa, H., Ouchida, M., Aoe, K., Aoe, M., et al. (2006) · Cancer Research · doi:10.1158/0008-5472.can-06-1951 · Cited by 450 · see citing works
Neratinib, an Irreversible Pan-ErbB Receptor Tyrosine Kinase Inhibitor: Results of a Phase II Trial in Patients With Advanced Non–Small-Cell Lung Cancer
Sequist, L. V. D., Besse, B., Lynch, T. J., Miller, V. A., Wong, K., Gitlitz, B. J., Eaton, K. D., Zacharchuk, C., Freyman, A., Powell, C., et al. (2010) · Journal of Clinical Oncology · doi:10.1200/jco.2009.27.9414 · Cited by 432 · see citing works
FAS and NF-κB signalling modulate dependence of lung cancers on mutant EGFR
Bivona, T. G., Hieronymus, H., Parker, J., Chang, K., Taron, M., Rosell, R., Moonsamy, P., Dahlman, K., Miller, V. A., Costa, C., et al. (2011) · Nature · doi:10.1038/nature09870 · Cited by 396 · see citing works
EGFR Mutations and Resistance to Irreversible Pyrimidine-Based EGFR Inhibitors
Ercan, D., Choi, H. G., Yun, C.-H., Capelletti, M., Xie, T., Eck, M. J., Gray, N. S., & Jänne, P. A. (2015) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-14-2789 · Cited by 368 · see citing works
New Strategies in Overcoming Acquired Resistance to Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors in Lung Cancer
Oxnard, G. R., Arcila, M. E., Chmielecki, J., Ladanyi, M., Miller, V. A., & Pao, W. J. (2011) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-10-2571 · Cited by 355 · see citing works
Osimertinib: First Global Approval
Greig, S. L. (2016) · Drugs · doi:10.1007/s40265-015-0533-4 · Cited by 334 · see citing works
EGFR-independent mechanisms of acquired resistance to AZD9291 in EGFR T790M-positive NSCLC patients
Planchard, D., Loriot, Y., André, F., Gobert, A., Auger, N., Lacroix, L., & Soria, J. (2015) · Annals of Oncology · doi:10.1093/annonc/mdv319 · Cited by 312 · see citing works
Evaluation of epidermal growth factor-related growth factors and receptors and of neoangiogenesis in completely resected stage I-IIIA non-small-cell lung cancer: amphiregulin and microvessel count are independent prognostic indicators of survival.
Fontanini, G., Laurentiis, M. D., Vignati, S., et al. (1998) · PubMed · Cited by 306 · see citing works
EAI045: The fourth-generation EGFR inhibitor overcoming T790M and C797S resistance
Wang, S., Song, Y., & Liu, D. (2016) · Cancer Letters · doi:10.1016/j.canlet.2016.11.008 · Cited by 302 · see citing works
Structure- and Reactivity-Based Development of Covalent Inhibitors of the Activating and Gatekeeper Mutant Forms of the Epidermal Growth Factor Receptor (EGFR)
Ward, R. A., Anderton, M. J., Ashton, S., Bethel, P. A., Box, M., Butterworth, S., Colclough, N., Chorley, C. G., Chuaqui, C., Cross, D. A. E., et al. (2013) · Journal of Medicinal Chemistry · doi:10.1021/jm400822z · Cited by 279 · see citing works
Epithelial to Mesenchymal Transition in an Epidermal Growth Factor Receptor-Mutant Lung Cancer Cell Line with Acquired Resistance to Erlotinib
Suda, K., Tomizawa, K., Fujii, M., Murakami, H., Osada, H., Maehara, Y., Yatabe, Y., Sekido, Y., & Mitsudomi, T. (2011) · Journal of Thoracic Oncology · doi:10.1097/jto.0b013e318216ee52 · Cited by 277 · see citing works
Acquired Resistance to Epidermal Growth Factor Receptor Kinase Inhibitors Associated with a Novel T854A Mutation in a Patient with EGFR-Mutant Lung Adenocarcinoma
Bean, J. M., Riely, G. J., Balak, M. N., Marks, J. L., Ladanyi, M., Miller, V. A., & Pao, W. J. (2008) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-08-0151 · Cited by 276 · see citing works
PIK3CA mutation status in Japanese lung cancer patients
Kawano, O., Sasaki, H., Endo, K., Suzuki, E., Haneda, H., Yukiue, H., Kobayashi, Y., Yano, M., & Fujii, Y. (2006) · Lung Cancer · doi:10.1016/j.lungcan.2006.07.006 · Cited by 274 · see citing works
An Alternative Inhibitor Overcomes Resistance Caused by a Mutation of the Epidermal Growth Factor Receptor
Kobayashi, S., Ji, H., Yuza, Y., Meyerson, M., Wong, K.-K., Tenen, D. G., & Halmos, B. (2005) · Cancer Research · doi:10.1158/0008-5472.can-05-1346 · Cited by 272 · see citing works
Synthesis and Structure−Activity Relationships of 6,7-Disubstituted 4-Anilinoquinoline-3-carbonitriles. The Design of an Orally Active, Irreversible Inhibitor of the Tyrosine Kinase Activity of the Epidermal Growth Factor Receptor (EGFR) and the Human Epidermal Growth Factor Receptor-2 (HER-2)
Wissner, A., Overbeek, E., Reich, M. F., Floyd, M. B., Johnson, B. D., Mamuya, N. N., Rosfjord, E. C., Discafani, C. M., Davis, R. E., Shi, X., et al. (2002) · Journal of Medicinal Chemistry · doi:10.1021/jm020241c · Cited by 270 · see citing works
Tyrosine Kinase Inhibitors. 17. Irreversible Inhibitors of the Epidermal Growth Factor Receptor: 4-(Phenylamino)quinazoline- and 4-(Phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides Bearing Additional Solubilizing Functions
Smaill, J. B., Rewcastle, G. W., Loo, J. A., Greis, K. D., Chan, O. H., Reyner, E. L., Lipka, E., Showalter, H. D. H., Vincent, P. W., Elliott, W. L., et al. (2000) · Journal of Medicinal Chemistry · doi:10.1021/jm990482t · Cited by 269 · see citing works
Self-citation
Molecular pathology of lung cancer: key to personalized medicine
Liang Cheng, C., Alexander, R. E., MacLennan, G. T., Cummings, O. W., Montironi, R., Antonio Lopez-beltran, B., Cramer, H. M., Davidson, D. D., & Zhang, S. (2012) · Modern Pathology · doi:10.1038/modpathol.2011.215 · Cited by 245 · see citing works
Antitumor activity and pharmacokinetic properties of PF-00299804, a second-generation irreversible pan-erbB receptor tyrosine kinase inhibitor
Gonzales, A. J., Hook, K. E., Althaus, I. W., Ellis, P. A., Trachet, E., Delaney, A. M., Harvey, P. J., Ellis, T. A., Amato, D. M., Nelson, J. M., et al. (2008) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-07-2232 · Cited by 226 · see citing works
Chemogenomic profiling provides insights into the limited activity of irreversible EGFR Inhibitors in tumor cells expressing the T790M EGFR resistance mutation.
Sos, M. L., Rode, H. B., Heynck, S., Peifer, M., Fischer, F., Klüter, S., Pawar, V. G., Reuter, C., Heuckmann, J. M., Weiss, J., et al. (2010) · Cancer Research · doi:10.1158/0008-5472.can-09-3106 · Cited by 220 · see citing works
Overview of molecular testing in non-small-cell lung cancer: mutational analysis, gene copy number, protein expression and other biomarkers of EGFR for the prediction of response to tyrosine kinase inhibitors
John, T., Liu, G., & Tsao, M. (2009) · Oncogene · doi:10.1038/onc.2009.197 · Cited by 206 · see citing works
Poor response to erlotinib in patients with tumors containing baseline EGFR T790M mutations found by routine clinical molecular testing
Yu, H. A., Arcila, M. E., Hellmann, M. D., Kris, M. G., Ladanyi, M., & Riely, G. J. (2014) · Annals of Oncology · doi:10.1093/annonc/mdt573 · Cited by 206 · see citing works
Clinical and molecular evidences of epithelial to mesenchymal transition in acquired resistance to EGFR-TKIs
Chung, J.-H., Rho, J. K., Xu, X., Lee, J. S., Yoon, H. I., Lee, C. T., Choi, Y. J., Kim, H.-R., Kim, C. H., & Lee, J. C. (2010) · Lung Cancer · doi:10.1016/j.lungcan.2010.11.011 · Cited by 186 · see citing works
Second-generation irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs): A better mousetrap? A review of the clinical evidence
Ou, S.-H. I. (2012) · Critical Reviews in Oncology/Hematology · doi:10.1016/j.critrevonc.2011.11.010 · Cited by 182 · see citing works
Structure-Based Approach for the Discovery of Pyrrolo[3,2-d]pyrimidine-Based EGFR T790M/L858R Mutant Inhibitors
Sogabe, S., Kawakita, Y., Igaki, S., Iwata, H., Miki, H., Cary, D. R., Takagi, T., Takagi, S., Ohta, Y., & Ishikawa, T. (2012) · ACS Medicinal Chemistry Letters · doi:10.1021/ml300327z · Cited by 175 · see citing works
Olmutinib: First Global Approval
Kim, E. S. (2016) · Drugs · doi:10.1007/s40265-016-0606-z · Cited by 170 · see citing works
Recent updates on third generation EGFR inhibitors and emergence of fourth generation EGFR inhibitors to combat C797S resistance
Patel, H., Pawara, R., Ansari, A., & Surana, S. (2017) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2017.05.027 · Cited by 170 · see citing works
Mutations of the epidermal growth factor receptor in non-small cell lung cancer – Search and destroy
Chan, S. K., Gullick, W. J., & Hill, M. E. (2005) · European Journal of Cancer · doi:10.1016/j.ejca.2005.07.031 · Cited by 165 · see citing works
Loss of PTEN expression by blocking nuclear translocation of EGR1 in gefitinib-resistant lung cancer cells harboring epidermal growth factor receptor-activating mutations
Yamamoto, C., Basaki, Y., Kawahara, A., Nakashima, K., Kage, M., Izumi, H., Kohno, K., Uramoto, H., Yasumoto, K., Kuwano, M., et al. (2010) · Cancer Research · doi:10.1158/0008-5472.can-10-0043 · Cited by 155 · see citing works
Phase I Study of EKB-569, an Irreversible Inhibitor of the Epidermal Growth Factor Receptor, in Patients With Advanced Solid Tumors
Erlichman, C., Hidalgo, M. M., Boni, J. P., Martins, P., Quinn, S., Zacharchuk, C., Amorusi, P., Adjei, A. A., & Rowinsky, E. K. (2006) · Journal of Clinical Oncology · doi:10.1200/jco.2005.01.8960 · Cited by 149 · see citing works
Better survival with EGFR exon 19 than exon 21 mutations in gefitinib-treated non-small cell lung cancer patients is due to differential inhibition of downstream signals
Zhu, J., Zhong, W., Zhang, G.-C., Li, R., Zhang, X., Guo, A., Zhang, Y.-F., An, S., Mok, T. S. K., & Wu, Y.-L. L. C. (2008) · Cancer Letters · doi:10.1016/j.canlet.2008.02.064 · Cited by 129 · see citing works
EGF816 Exerts Anticancer Effects in Non–Small Cell Lung Cancer by Irreversibly and Selectively Targeting Primary and Acquired Activating Mutations in the EGF Receptor
Jia, Y., Juarez, J., Li, J., Manuia, M., Niederst, M. J., Tompkins, C., Timple, N., Vaillancourt, M.-T., Pferdekamper, A. C., Lockerman, E. L., et al. (2016) · Cancer Research · doi:10.1158/0008-5472.can-15-2581 · Cited by 121 · see citing works
Multicenter, Randomized, Phase II Trial of CI-1033, an Irreversible Pan-ERBB Inhibitor, for Previously Treated Advanced Non–Small-Cell Lung Cancer
Janne, P. A., von Pawel, J., Cohen, R. B., Crinò, L., Butts, C. A., Olson, S. S., Eiseman, I. A., Chiappori, A., Yeap, B. Y., Lenehan, P. F., et al. (2007) · Journal of Clinical Oncology · doi:10.1200/jco.2007.11.1336 · Cited by 120 · see citing works
EGFR G796D mutation mediates resistance to osimertinib
Zheng, D., Hu, M., Bai, Y., Zhu, X., Lu, X., Wu, C., Wang, J., Liu, L., Wang, Z., Ni, J., et al. (2017) · Oncotarget · doi:10.18632/oncotarget.17913 · Cited by 111 · see citing works
Self-citation
Recent progress on third generation covalent EGFR inhibitors
Cheng, H., Nair, S. K., & Murray, B. W. (2016) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2016.02.067 · Cited by 110 · see citing works
Challenges and Perspectives on the Development of Small-Molecule EGFR Inhibitors against T790M-Mediated Resistance in Non-Small-Cell Lung Cancer
Song, Z., Yang, G., Wang, C., Huang, S., Shu, X. H., Liu, K., Zhou, Y., & Ma, X. (2016) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5b00840 · Cited by 109 · see citing works
Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site
Günther, M., Lategahn, J., Juchum, M., Döring, E., Keul, M., Engel, J., Tumbrink, H. L., Rauh, D., & Laufer, S. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.7b00316 · Cited by 108 · see citing works
Afatinib—new therapy option for EGFR-mutant lung cancer
Yu, H. A., & Pao, W. (2013) · Nature Reviews Clinical Oncology · doi:10.1038/nrclinonc.2013.154 · Cited by 105 · see citing works
Lung Cancer: EGFR Inhibitors with Low Nanomolar Activity against a Therapy‐Resistant L858R/T790M/C797S Mutant
Günther, M., Juchum, M., Kelter, G., Fiebig, H. H., & Laufer, S. (2016) · Angewandte Chemie International Edition · doi:10.1002/anie.201603736 · Cited by 102 · see citing works
Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants with Selectivity over Wild-Type EGFR
Planken, S., Behenna, D. C., Nair, S. K., Johnson, T. O., Nagata, A., Almaden, C., Bailey, S., Ballard, T. E., Bernier, L., Cheng, H., et al. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b01894 · Cited by 97 · see citing works
Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants
Cheng, H., Nair, S. K., Murray, B. W., Almaden, C., Bailey, S., Baxi, S. M., Behenna, D. C., Cho-Schultz, S., Dalvie, D., Dinh, D. M., et al. (2016) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5b01633 · Cited by 96 · see citing works
Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants for the Treatment of EGFR Mutant Non-Small-Cell Lung Cancers
Lelais, G., Epple, R., Marsilje, T. H., Long, Y. O., McNeill, M., Chen, B., Lu, W., Anumolu, J., Badiger, S., Bursulaya, B., et al. (2016) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5b01985 · Cited by 95 · see citing works
Noncovalent Wild-type–Sparing Inhibitors of EGFR T790M
Lee, H.-J., Schaefer, G., Heffron, T. P., Shao, L., Ye, X., Sideris, S., Malek, S., Chan, E., Merchant, M., La, H., et al. (2013) · Cancer Discovery · doi:10.1158/2159-8290.cd-12-0357 · Cited by 90 · see citing works
Strategies for overcoming resistance to EGFR family tyrosine kinase inhibitors
Giaccone, G., & Wang, Y. (2011) · Cancer Treatment Reviews · doi:10.1016/j.ctrv.2011.01.003 · Cited by 90 · see citing works
AC0010, an Irreversible EGFR Inhibitor Selectively Targeting Mutated EGFR and Overcoming T790M-Induced Resistance in Animal Models and Lung Cancer Patients
Xu, X., Mao, L., Xu, W., Tang, W., Zhang, X., Xi, B., Xu, R., Fang, X., Liu, J., Fang, C., et al. (2016) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-16-0281 · Cited by 87 · see citing works
Trisubstituted Imidazoles with a Rigidized Hinge Binding Motif Act As Single Digit nM Inhibitors of Clinically Relevant EGFR L858R/T790M and L858R/T790M/C797S Mutants: An Example of Target Hopping
Juchum, M., Günther, M., Döring, E., Sievers‐Engler, A., Lämmerhofer, M., & Laufer, S. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.7b00178 · Cited by 84 · see citing works
Discovery of EGF Receptor Inhibitors That Are Selective for the d746‐750/T790M/C797S Mutant through Structure‐Based de Novo Design
Park, H., Jung, H., Mah, S., & Hong, S. (2017) · Angewandte Chemie International Edition · doi:10.1002/anie.201703389 · Cited by 74 · see citing works
Discovery of Selective and Noncovalent Diaminopyrimidine-Based Inhibitors of Epidermal Growth Factor Receptor Containing the T790M Resistance Mutation
Hanan, E. J., Eigenbrot, C. W., Bryan, M. C., Burdick, D. J., Chan, B. K., Chen, Y., Dotson, J., Heald, R. A., Jackson, P. S., La, H., et al. (2014) · Journal of Medicinal Chemistry · doi:10.1021/jm501578n · Cited by 65 · see citing works
Insight into the Inhibition of Drug‐Resistant Mutants of the Receptor Tyrosine Kinase EGFR
Engel, J., Becker, C., Lategahn, J., Keul, M., Ketzer, J., Mühlenberg, T., Kollipara, L., Schultz‐Fademrecht, C., Zahedi, R. P., Bauer, S., et al. (2016) · Angewandte Chemie International Edition · doi:10.1002/anie.201605011 · Cited by 64 · see citing works
Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study
Heald, R. A., Bowman, K. K., Bryan, M. C., Burdick, D. J., Chan, B. K., Chan, E. W., Chen, Y., Clausen, S., Dominguez‐Fernandez, B., Eigenbrot, C. W., et al. (2015) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5b01412 · Cited by 63 · see citing works
Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family
Smaill, J. B., Gonzales, A. J., Spicer, J. A., Lee, H., Reed, J. E., Sexton, K., Althaus, I. W., Zhu, T., Black, S. L., Blaser, A., et al. (2016) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b00883 · Cited by 63 · see citing works
Self-citation
Overcoming resistance to targeted therapies in NSCLC: current approaches and clinical application
Maione, P., Sacco, P. C., Sgambato, A., Casaluce, F., Rossi, A., & Gridelli, C. (2015) · Therapeutic Advances in Medical Oncology · doi:10.1177/1758834015595048 · Cited by 58 · see citing works
Conversion from the “oncogene addiction” to “drug addiction” by intensive inhibition of the EGFR and MET in lung cancer with activating EGFR mutation
Suda, K., Tomizawa, K., Osada, H., Maehara, Y., Yatabe, Y., Sekido, Y., & Mitsudomi, T. (2011) · Lung Cancer · doi:10.1016/j.lungcan.2011.11.007 · Cited by 56 · see citing works
A structure-guided optimization of pyrido[2,3-d]pyrimidin-7-ones as selective inhibitors of EGFRL858R/T790M mutant with improved pharmacokinetic properties
Yu, L., Huang, M., Xu, T., Tong, L., Yan, X.-E., Zhang, Z., Xu, Y., Yun, C., Xie, H., Ding, K., et al. (2016) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2016.12.006 · Cited by 48 · see citing works
Self-citation
Abstract LB-100: Discovery of HM61713 as an orally available and mutant EGFR selective inhibitor
Lee, K., Cha, M. Y., Kim, M., Song, J. Y., Lee, J., Kim, Y. H., Lee, Y.-M., Suh, K. H., & Son, J. (2014) · Cancer Research · doi:10.1158/1538-7445.am2014-lb-100 · Cited by 43 · see citing works
Discovery of a Noncovalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor
Chan, B. K., Hanan, E. J., Bowman, K. K., Bryan, M. C., Burdick, D. J., Chan, E. W., Chen, Y., Clausen, S., Vega, T. D., Dotson, J., et al. (2016) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b00995 · Cited by 38 · see citing works
Pyrimido[4,5‐d]pyrimidin‐4(1H)‐one Derivatives as Selective Inhibitors of EGFR Threonine790 to Methionine790 (T790M) Mutants
Xu, T., Zhang, L., Xu, S., Yang, C., Luo, J., Ding, F., Lu, X., Liu, Y., Tu, Z., Li, S., et al. (2013) · Angewandte Chemie International Edition · doi:10.1002/anie.201302313 · Cited by 37 · see citing works
Self-citation
1300: Efficacy and safety of BI 1482694 (HM61713), an EGFR mutant-specific inhibitor, in T790M-positive NSCLC at the recommended phase II dose
Park, K., Lee, J.-S., Han, J. Y., Lee, K. H., Kim, J. H., Cho, E. K., Cho, J., Min, Y. J., Kim, J., & Kim, D.-W. (2016) · Journal of Thoracic Oncology · doi:10.1016/s1556-0864(16)30243-x · Cited by 37 · see citing works
Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR
Bryan, M. C., Burdick, D. J., Chan, B. K., Chen, Y., Clausen, S., Dotson, J., Eigenbrot, C. W., Elliott, R. L., Hanan, E. J., Heald, R. A., et al. (2015) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.5b00428 · Cited by 36 · see citing works
C5-substituted pyrido[2,3-d]pyrimidin-7-ones as highly specific kinase inhibitors targeting the clinical resistance-related EGFR T790M mutant
Xu, T., Peng, T., Ren, X., Zhang, L., Yu, L., Luo, J., Zhang, Z., Tu, Z., Tong, L., Huang, Z., et al. (2015) · MedChemComm · doi:10.1039/c5md00208g · Cited by 34 · see citing works
Self-citation
Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor
Engel, J., Smith, S. P., Lategahn, J., Tumbrink, H. L., Goebel, L., Becker, C., Hennes, E., Keul, M., Unger, A., Müller, H., et al. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.7b00515 · Cited by 32 · see citing works
Dacomitinib in lung cancer: a &ldquo;lost generation&rdquo; EGFR tyrosine-kinase inhibitor from a bygone era?
Ou, S.-H., & Soo, R. (2015) · Drug Design, Development and Therapy · doi:10.2147/dddt.s52787 · Cited by 28 · see citing works
Rociletinib, a third generation EGFR tyrosine kinase inhibitor: current data and future directions
Chuang, J. C., Salahudeen, A. A., & Wakelee, H. A. (2016) · Expert Opinion on Pharmacotherapy · doi:10.1517/14656566.2016.1162786 · Cited by 23 · see citing works
Abstract 1728: ASP8273, a novel mutant-selective irreversible EGFR inhibitor, inhibits growth of non-small cell lung cancer (NSCLC) cells with EGFR activating and T790M resistance mutations
Sakagami, H., Konagai, S., Yamamoto, H., Tanaka, H., Matsuya, T., Mori, M., Koshio, H., Yuri, M., Hirano, M., & Kuromitsu, S. (2014) · Cancer Research · doi:10.1158/1538-7445.am2014-1728 · Cited by 20 · see citing works
Development of an UPLC–MS/MS method for quantification of Avitinib (AC0010) and its five metabolites in human cerebrospinal fluid: Application to a study of the blood-brain barrier penetration rate of non-small cell lung cancer patients
Wang, W., Zheng, X. X., Wang, H., et al. (2017) · Journal of Pharmaceutical and Biomedical Analysis · doi:10.1016/j.jpba.2017.02.057 · Cited by 13 · see citing works
Abstract 2586: ASP8273 selectively inhibits mutant EGFR signal pathway and induces tumor shrinkage in EGFR mutated tumor models
Konagai, S., Sakagami, H., Yamamoto, H., et al. (2015) · Cancer Research · doi:10.1158/1538-7445.am2015-2586 · Cited by 9 · see citing works
An LC–MS/MS method for quantification of AC0010, a novel mutant-selective epidermal growth factor receptor (EGFR) inhibitor, and its metabolites in human plasma and the application to a pharmacokinetic study
Wang, L., Zheng, X. X., Wang, W., Hu, P., & Jiang, J. (2017) · Journal of Pharmaceutical and Biomedical Analysis · doi:10.1016/j.jpba.2017.03.051 · Cited by 5 · see citing works
Allosteric EGFR Inhibitors Overcome Resistance Mutations
(2016) · Cancer Discovery · doi:10.1158/2159-8290.cd-rw2016-104 · Cited by 4 · see citing works

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Authors: Lu, X., Yu, L., Zhang, Z., Ren, X., Smaill, J. B., & Ding, K.
Affiliations: Jinan University (CN)
Chinese Academy of Sciences (CN)
University of Auckland (NZ)
Corresponding author: Lu, Xiaoyun
Ding, Ke
ORCID: Lu, Xiaoyun
Yu, Lei
Zhang, Zhang
Ren, Xiaomei
Smaill, Jeff B.
Ding, Ke
Venue: Medicinal Research Reviews
Publisher: Wiley
Published: 2018-01-26
Volume: 38
Issue: 5
Pages: 1550-1581
ISSN: 0198-6325 (ISSN-L)
1098-1128
DOI: 10.1002/med.21488
OpenAlex: W2887271393
Cited by: 173
References: 108
Citations by year: 2026: 14 · 2025: 22 · 2024: 28 · 2023: 31 · 2022: 18 · 2021: 20 · 2020: 20 · 2019: 14 · 2018: 6
FWCI: 2.81
Type: journal article
Language: en
Open access: closed
Licence: onlinelibrary.wiley.com/termsAndConditions#vor (vor)
Locations: Medicinal Research Reviews (publishedVersion)
PubMed (publishedVersion)
Funders: National Natural Science Foundation of China (81673285, 81425021)
Jinan University
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 › Pathology and Forensic Medicine › Cancer Mechanisms and Therapy
Keywords: EGFR, non-small cell lung cancer, L858R mutation, T790M mutation, EGFR C797S, acquired drug resistance, third-generation EGFR tyrosine kinase inhibitors, fourth-generation EGFR inhibitors, allosteric inhibitors, reversible inhibitors, tyrosine kinase inhibitors, gefitinib, erlotinib, afatinib, osimertinib, WZ4002
MeSH terms: Carcinoma, Non-Small-Cell Lung, Chemistry, Pharmaceutical, Humans, Lung Neoplasms, Mutation, Drug Resistance, Neoplasm, Protein Kinase Inhibitors, ErbB Receptors

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Targeting EGFR L858R/T790M and EGFR L858R/T790M/C797S resistance mutations in NSCLC: Current developments in medicinal chemistry

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