Targeting EGFR in Lung Cancer: Current Standards and Developments

Díaz-Serrano, Asunción; Gella, Pablo; Jiménez, Elisabeth; Zugazagoitia, Jon; Paz-Ares Rodríguez, Luis

doi:10.1007/s40265-018-0916-4

Cited by 109Lung Cancer Treatments and MutationsHER2/EGFR in Cancer ResearchLung Cancer Diagnosis and Treatment

Targeting EGFR in Lung Cancer: Current Standards and Developments

Díaz-Serrano, Asunción, Gella, Pablo, Jiménez, Elisabeth, Zugazagoitia, Jon, Paz-Ares Rodríguez, Luis·2018·Drugs

DOI 10.1007/s40265-018-0916-4

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Abstract

Lung cancer is the second most common malignant tumor and the leading cause of cancer death. Epidermal growth factor receptor (EGFR)-mutant non-small cell lung cancer (NSCLC) is a distinct subtype of lung cancer comprising approximately 15-40% of non-squamous tumors. The development of first- and second-generation EGFR tyrosine kinase inhibitors (TKIs) has been a significant step forward in the treatment of patients with EGFR-mutant tumors, and over the last few years has been the therapy of choice in the initial management of patients with activating mutations in EGFR, with some differences in efficacy and toxicity profile. Up to 50% of patients treated with first- and second-generation TKIs develop an EGFR exon 20 T790M mutation at the time of progression. In this context, osimertinib has shown a great benefit in terms of progression-free survival (PFS) in the second-line setting, including central nervous system metastasis control. The FLAURA trial, which compared osimertinib to first-generation inhibitors as first-line therapy, showed a clear PFS advantage for osimertinib and a trend towards an increased overall survival (OS) assessed by investigator review. Although T790M mutation is the most common mechanism of resistance to first- and second-generation EGFR TKIs, other EGFR-dependent and -independent mechanisms have been described, such as HER2 and MET amplifications or BRAF and MEK mutations. Some mechanisms of resistance to osimertinib and other third-generation TKIs have also been described. Several fourth-generation TKIs, targeted drug combinations and immunotherapy strategies are under investigation to overcome resistance to EGFR TKIs in order to improve EGFR-mutant NSCLC patient outcomes.

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Anti-EGFR antibodies cetuximab and panitumumab are approved for treatment of RAS/RAF wild type CRC, while EGFR tyrosine kinase inhibitors are approved for treatment of EGFR mutant lung cancer.
“The anti-EGFR antibodies cetuximab and panitumumab are approved for the treatment of RAS/RAF wild type CRC(34, 35), while EGFR tyrosine kinase inhibitors (TKI) are approved for the treatment of EGFR mutant lung cancer(36).”
From EGFR Blockade Reverts Resistance to KRASG12C Inhibition in Colorectal Cancer. (2020) · cites this paper as [36]
Cetuximab sensitizes the KRAS (G12C) CRC cells to AMG510, and the combination restores secondary resistance to anti-EGFR antibodies.
“Cetuximab sensitizes the KRAS (G12C) CRC cells to AMG510, and the combination restores secondary resistance to anti-EGFR antibodies.”
From Targeting KRAS mutant cancers: from druggable therapy to drug resistance (2022) · cites this paper as [104]

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Rociletinib in EGFR-Mutated Non–Small-Cell Lung Cancer
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Is There a Common Etiology for the Rising Incidence of and Decreasing Survival with Adenocarcinoma of the Lung?
Janssen-Heijnen, M. L. G., Coebergh, J. W. W., Klinkhamer, P. J. J. M., Schipper, R. M., Splinter, T. A. W., & Mooi, A. W. J. (2001) · Epidemiology · doi:10.1097/00001648-200103000-00020 · Cited by 57 · see citing works
Dacomitinib versus erlotinib in patients with EGFR-mutated advanced nonsmall-cell lung cancer (NSCLC): pooled subset analyses from two randomized trials
Ramalingam, S. S., O'Byrne, K. J., Boyer, M. J., Mok, T. S. K., Janne, P. A., Zhang, H., Liang, J. J., Taylor, I. W., Sbar, E. I., & Paz-Ares, L. (2016) · Annals of Oncology · doi:10.1093/annonc/mdv593 · Cited by 57 · see citing works
Polymorphisms of CYP2D6 Gene and Gefitinib-Induced Hepatotoxicity
Takimoto, T., Kijima, T., Otani, Y., Nonen, S., Namba, Y., Mori, M., Yokota, S., Minami, S., Komuta, K., Uchida, J., et al. (2013) · Clinical Lung Cancer · doi:10.1016/j.cllc.2013.03.003 · Cited by 56 · see citing works
Potential prognostic biomarker CD73 regulates epidermal growth factor receptor expression in human breast cancer
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Optimal management of EGFR -mutant non-small cell lung cancer with disease progression on first-line tyrosine kinase inhibitor therapy
Liao, B.-C., Lin, C., Lee, J., & Yang, J. C. (2017) · Lung Cancer · doi:10.1016/j.lungcan.2017.05.009 · Cited by 48 · see citing works
Anti-CD73 immunotherapy: A viable way to reprogram the tumor microenvironment
Antonioli, L., Blandizzi, C., Malavasi, F., Ferrari, D., & Haskó, G. (2016) · OncoImmunology · doi:10.1080/2162402x.2016.1216292 · Cited by 47 · see citing works
Carcinomatous meningitis from non-small-cell lung cancer responding to gefitinib
Sakai, M., Ishikawa, S., Ito, H., Ozawa, Y., Yamamoto, T., Onizuka, M., & Sakakibara, Y. (2006) · International Journal of Clinical Oncology · doi:10.1007/s10147-005-0558-x · Cited by 46 · see citing works
BI 1482694 (HM61713), an EGFR mutant-specific inhibitor, in T790M+ NSCLC: Efficacy and safety at the RP2D.
Park, K., Lee, J.-S., Lee, K. H., Kim, J.-H., Cho, B. C., Min, Y. J., Choi, Y., Han, J., Kim, B.-S., Kim, J.-S., et al. (2016) · Journal of Clinical Oncology · doi:10.1200/jco.2016.34.15_suppl.9055 · Cited by 43 · see citing works
PD-1 Axis Inhibitors in EGFR- and ALK-Driven Lung Cancer: Lost Cause?
Gettinger, S. N., & Politi, K. A. (2016) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-16-1401 · Cited by 40 · see citing works
Complete clearance of plasma EGFR mutations as a predictor of outcome on osimertinib in the AURA trial.
Thress, K. S., Markovets, A. A., Barrett, J. C., Chmielecki, J., Goldberg, S. B., Shepherd, F. A., Vowler, S. L., & Oxnard, G. R. (2017) · Journal of Clinical Oncology · doi:10.1200/jco.2017.35.15_suppl.9018 · Cited by 40 · see citing works
EGFR Mutation Status and First-Line Treatment in Patients with Stage III/IV Non–Small Cell Lung Cancer in Germany: An Observational Study
Schuette, W., Schirmacher, P., Eberhardt, W., Fischer, J. R., von der Schulenburg, J. M. G., Mezger, J., Schumann, C., Serke, M. H., Zaun, S., Dietel, M., et al. (2015) · Cancer Epidemiology Biomarkers & Prevention · doi:10.1158/1055-9965.epi-14-1149 · Cited by 38 · see citing works
Osimertinib vs standard of care (SoC) EGFR-TKI as first-line therapy in patients (pts) with EGFRm advanced NSCLC: FLAURA
Ramalingam, S., Reungwetwattana, T., Chewaskulyong, B., Dechaphunkul, A., Lee, K. H., Imamura, F., Nogami, N., Ohe, Y., Cheng, Y., Cho, B. C., et al. (2017) · Annals of Oncology · doi:10.1093/annonc/mdx440.050 · Cited by 36 · see citing works
Lower gefitinib dose led to earlier resistance acquisition before emergence of T790M mutation in epidermal growth factor receptor‐mutated lung cancer model
Hayakawa, H., Ichihara, E., Ohashi, K., Ninomiya, T., Yasugi, M., Takata, S., Sakai, K., Matsumoto, K., Takigawa, N., Tanimoto, M., et al. (2013) · Cancer Science · doi:10.1111/cas.12284 · Cited by 34 · see citing works
Dacomitinib versus gefitinib for the first-line treatment of advanced EGFR mutation positive non-small cell lung cancer (ARCHER 1050): A randomized, open-label phase III trial.
Mok, T. S. K., Cheng, Y., Zhou, X., Lee, K. H., Nakagawa, K., Niho, S., Tsuji, F., Rosell, R., Jaime, J. C., Migliorino, M. R., et al. (2017) · Journal of Clinical Oncology · doi:10.1200/jco.2017.35.18_suppl.lba9007 · Cited by 33 · see citing works
Toxicity profile of epidermal growth factor receptor tyrosine kinase inhibitors in patients with epidermal growth factor receptor gene mutation-positive lung cancer
Takeda, M., & Nakagawa, K. (2016) · Molecular and Clinical Oncology · doi:10.3892/mco.2016.1099 · Cited by 29 · see citing works
EGFR mutations in circulating tumour DNA
Rosell, R., Molina‐Vila, M. Á., & Serrano, M. J. (2012) · The Lancet Oncology · doi:10.1016/s1470-2045(12)70369-8 · Cited by 28 · see citing works
Second-line Treatment of Non-Small Cell Lung Cancer: Focus on the Clinical Development of Dacomitinib
Zugazagoitia, J., Díaz, A., Jiménez, E., Nuñez, J. A., Iglesias, L., Ponce-Aix, S., & Paz-Ares, L. G. (2017) · Frontiers in Medicine · doi:10.3389/fmed.2017.00036 · Cited by 12 · see citing works
Self-citation
P1.04-001 Osimertinib with Ramucirumab or Necitumumab in Advanced T790M-positive EGFR-Mutant NSCLC: Preliminary Ph1 Study Results
Yu, H. A., Planchard, D., Yang, J. C.-H., Lee, K. H., Garrido, P., Park, K., Kim, J. H., Lee, D., He, S., Wolff, K., et al. (2017) · Journal of Thoracic Oncology · doi:10.1016/j.jtho.2017.09.860 · Cited by 8 · see citing works
Dacomitinib versus gefitinib for the first-line treatment of advanced EGFR mutation positive non-small cell lung cancer (ARCHER 1050): A randomized, open-label phase III trial.
Mok, T. S. K., Cheng, Y., Zhou, X., Lee, K. H., Nakagawa, K., Niho, S., Tsuji, F., Rosell, R., Jaime, J. C., Migliorino, M. R., et al. (2017) · Journal of Clinical Oncology · doi:10.1200/jco.2017.35.15_suppl.lba9007 · Cited by 7 · see citing works
Abstract 4112: Overgrowth of competing resistance mechanisms, such as an acquired KRAS mutation, underlies a poor prognosis subtype of acquired resistance to osimertinib in T790M-positive NSCLC
Oxnard, G. R., Hu, Y., Tracy, P. D., Feeney, N. B., Paweletz, C. P., Thress, K. S., & Janne, P. A. (2017) · Cancer Research · doi:10.1158/1538-7445.am2017-4112 · Cited by 4 · see citing works

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Sorted by citations

Non‐small cell lung cancer in China
Chen, P., Liu, Y., Wen, Y., & Zhou, C. (2022) · 癌症：英文版 · doi:10.1002/cac2.12359 · Cited by 673 · see citing works
Adverse effects of tyrosine kinase inhibitors in cancer therapy: pathophysiology, mechanisms and clinical management
Sunder, S. S., Sharma, U. C., & Pokharel, S. (2023) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-023-01469-6 · Cited by 543 · see citing works
“The AURA3 Randomized Phase III Study (Osimertinib vs PlatinumPemetrexed) and the FLAURA trial (osimertinib vs first-generation EGFR-TKI) in EGFR-Mutated Advanced non-small cell lung cancers (NSCLC) reported the frequency of LVD at 5% and 10%, respectively.(43) Paradoxically, a larger population study with a 2-year fol…”
BackgroundInfluential
EGFR Blockade Reverts Resistance to KRASG12C Inhibition in Colorectal Cancer.
Amodio, V., Yaeger, R., Arcella, P., Cancelliere, C., Lamba, S., Lorenzato, A., Arena, S., Montone, M., Mussolin, B., Bian, Y., et al. (2020) · Cancer Discovery · doi:10.1158/2159-8290.cd-20-0187 · Cited by 504 · see citing works
“The anti-EGFR antibodies cetuximab and panitumumab are approved for the treatment of RAS/RAF wild type CRC(34, 35), while EGFR tyrosine kinase inhibitors (TKI) are approved for the treatment of EGFR mutant lung cancer(36).”
Background
Receptor Tyrosine Kinase-Targeted Cancer Therapy
Yamaoka, T., Kusumoto, S., Ando, K., Ohba, M., & Ohmori, T. (2018) · International Journal of Molecular Sciences · doi:10.3390/ijms19113491 · Cited by 297 · see citing works
“Several EGFR TKIs are currently available for cancer treatment [85].”
Background
Therapeutic advances of targeting receptor tyrosine kinases in cancer
Tomuleasa, C., Tigu, A.-B., Munteanu, R. A., Moldovan, C. S., Kegyes, D., Onaciu, A., Gulei, D., Ghiaur, G., Einsele, H., & Croce, C. M. (2024) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-024-01899-w · Cited by 279 · see citing works
Targeting KRAS mutant cancers: from druggable therapy to drug resistance
Zhu, C., Guan, X., Zhang, X., Luan, X., Song, Z., Cheng, X., Zhang, W., & Qin, J.-J. (2022) · Molecular Cancer · doi:10.1186/s12943-022-01629-2 · Cited by 231 · see citing works
Intrinsic Resistance to EGFR-Tyrosine Kinase Inhibitors in EGFR-Mutant Non-Small Cell Lung Cancer: Differences and Similarities with Acquired Resistance
Santoni‐Rugiu, E., Melchior, L. C., Urbanska, E. M., Jakobsen, J. N., de Stricker, K., Grauslund, M., & Sørensen, J. B. (2019) · Cancers · doi:10.3390/cancers11070923 · Cited by 195 · see citing works
“The investigation of new TKIs of fourth generation, such as mutant-selective allosteric inhibitors capable of simultaneously inhibiting sensitizing EGFR-mutations, T790M, and C797S (and similar resistant mutations), as well as targeted drug combinations capable of overcoming resistance to the currently used EGFR-TKIs…”
Background
Current Landscape of Therapeutic Resistance in Lung Cancer and Promising Strategies to Overcome Resistance
Ashrafi, A., Akter, Z., Modareszadeh, P., Modareszadeh, P., Berisha, E., Alemi, P. S., Castro, M. D. C. C., Deese, A. R., & Li, Z. (2022) · Cancers · doi:10.3390/cancers14194562 · Cited by 193 · see citing works
Acquired resistance mechanisms to osimertinib: The constant battle
Zalaquett, Z., Hachem, M. C. R., Kassis, Y., Hachem, S., Eid, R., Kourié, H. R., & Planchard, D. (2023) · Cancer Treatment Reviews · doi:10.1016/j.ctrv.2023.102557 · Cited by 97 · see citing works
CAR‐T cell therapy for lung cancer: Potential and perspective
Chen, L., Chen, F., Li, J., Pu, Y., Yang, C., Wang, Y., Lei, Y., & Huang, Y. (2022) · Thoracic Cancer · doi:10.1111/1759-7714.14375 · Cited by 77 · see citing works
Therapeutics Targeting Mutant KRAS
Thein, K. Z., Biter, A. B., & Hong, D. S. (2020) · Annual Review of Medicine · doi:10.1146/annurev-med-080819-033145 · Cited by 75 · see citing works
Advances in targeting EGFR allosteric site as anti-NSCLC therapy to overcome the drug resistance
Maity, S., Pai, K. S. R., & Nayak, Y. (2020) · Pharmacological Reports · doi:10.1007/s43440-020-00131-0 · Cited by 74 · see citing works
Current Approaches in NSCLC Targeting K-RAS and EGFR
Aran, V., & Omerović, J. (2019) · International Journal of Molecular Sciences · doi:10.3390/ijms20225701 · Cited by 74 · see citing works
Synthetic Approaches to New Drugs Approved During 2016
Flick, A. C., Ding, H. X., Leverett, C. A., Fink, S. J., & O’Donnell, C. J. (2018) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.8b00260 · Cited by 70 · see citing works
Efficacy, Safety, and Challenges of CAR T-Cells in the Treatment of Solid Tumors
Chen, Q., Lu, L., & Ma, W. (2022) · Cancers · doi:10.3390/cancers14235983 · Cited by 71 · see citing works
“EGFR is also a target of immunotherapy [90,91].”
Background
Beyond HER2: Targeting the ErbB receptor family in breast cancer
Drago, J. Z., Ferraro, E., Abuhadra, N. K., & Modi, S. (2022) · Cancer Treatment Reviews · doi:10.1016/j.ctrv.2022.102436 · Cited by 65 · see citing works
Synthetic Approaches to New Drugs Approved during 2018
Flick, A. C., Leverett, C. A., Ding, H. X., McInturff, E. L., Fink, S. J., Helal, C. J., DeForest, J. C., Morse, P., Mahapatra, S., & O’Donnell, C. J. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c00345 · Cited by 66 · see citing works
Toxicity profile of epidermal growth factor receptor tyrosine kinase inhibitors for patients with lung cancer: A systematic review and network meta-analysis
Zhao, Y., Cheng, B., Chen, Z., Li, J., Liang, H., Chen, Y., Zhu, F., Li, C., Xu, K., Xiong, S., et al. (2021) · Critical Reviews in Oncology/Hematology · doi:10.1016/j.critrevonc.2021.103305 · Cited by 62 · see citing works
MicroRNAs as Potential Targets for Therapeutic Intervention With Metastasis of Non-small Cell Lung Cancer
Weidle, U. H., Birzele, F., & Nopora, A. (2019) · Cancer Genomics & Proteomics · doi:10.21873/cgp.20116 · Cited by 52 · see citing works
CT and clinical characteristics that predict risk of EGFR mutation in non-small cell lung cancer: a systematic review and meta-analysis
Zhang, H., Cai, W., Wang, Y., Liao, M., & Tian, S. (2019) · International Journal of Clinical Oncology · doi:10.1007/s10147-019-01403-3 · Cited by 52 · see citing works
Precision medicine for gastrointestinal cancer: Recent progress and future perspective
Matsuoka, T., & Yashiro, M. (2019) · World Journal of Gastrointestinal Oncology · doi:10.4251/wjgo.v12.i1.1 · Cited by 47 · see citing works
Anticancer potential of some imidazole and fused imidazole derivatives: exploring the mechanism via epidermal growth factor receptor (EGFR) inhibition
Kalra, S., Joshi, G., Kumar, M., Arora, S., Kaur, H., Singh, S., Munshi, A., & Kumar, R. (2020) · RSC Medicinal Chemistry · doi:10.1039/d0md00146e · Cited by 42 · see citing works
Pulmonary delivery of osimertinib liposomes for non-small cell lung cancer treatment: formulation development and in vitro evaluation
Sawant, S. S., Patil, S. M., Shukla, S. K., Kulkarni, N. S., Gupta, V., & Kunda, N. K. (2021) · Drug Delivery and Translational Research · doi:10.1007/s13346-021-01088-0 · Cited by 42 · see citing works
Design, Synthesis, biological Evaluation, and molecular docking studies of novel Pyrazolo[3,4-d]Pyrimidine derivative scaffolds as potent EGFR inhibitors and cell apoptosis inducers
Sherbiny, F. F., Bayoumi, A. H., El-morsy, A., Sobhy, M., & Hagras, M. (2021) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2021.105325 · Cited by 38 · see citing works
Social and Biological Determinants in Lung Cancer Disparity
Brock, B. A., Mir, H., Flenaugh, E. L., Oprea‐Ilies, G., Singh, R., & Singh, S. (2024) · Cancers · doi:10.3390/cancers16030612 · Cited by 38 · see citing works
Metformin and tenovin‐6 synergistically induces apoptosis through LKB1‐independent SIRT1 down‐regulation in non‐small cell lung cancer cells
Lee, B. B., Kim, Y., Kim, D., Cho, E. Y., Han, J., Kim, H. K., Shim, Y. M., & Kim, D. (2019) · Journal of Cellular and Molecular Medicine · doi:10.1111/jcmm.14194 · Cited by 38 · see citing works
The Genetic Analysis and Clinical Therapy in Lung Cancer: Current Advances and Future Directions
Rina, A., Maffeo, D., Minnai, F., Esposito, M., Palmieri, M., Serio, V. B., Rosati, D., Mari, F., Frullanti, E., & Colombo, F. (2024) · Cancers · doi:10.3390/cancers16162882 · Cited by 41 · see citing works
“…target antigen choice, that needs to be highly specific, expressed and stable [299] such as, for lung cancers, the epidermal growth factor receptor (EGFR) [300], mucin 1, cell surface associated (MUC1) [301], the receptor tyrosine kinase like orphan receptor 1 (ROR1) [302], mesothelin (MSLN) [303].”
Background
A Self-Assembly ICG Nanoparticle Potentiating Targeted Photothermal and Photodynamic Therapy in NSCLC
Hu, X., Li, J., Chen, Y., Long, Q., Bai, Y., Li, R., Wang, K., Jiang, M., Chen, C., Mao, J., et al. (2022) · ACS Biomaterials Science & Engineering · doi:10.1021/acsbiomaterials.2c00620 · Cited by 36 · see citing works
MET inhibitor, capmatinib overcomes osimertinib resistance via suppression of MET/Akt/snail signaling in non-small cell lung cancer and decreased generation of cancer-associated fibroblasts
Zhu, K., Lv, Z., Xiong, J., Zheng, H., Zhang, S., Jin, H., Yu, L., Li, Z., Zhang, J., Li, C., et al. (2021) · Aging · doi:10.18632/aging.202547 · Cited by 33 · see citing works
“The recently developed osimertinib, the third generation of EGFR targeted inhibitor, has shown survival benefits in patients with acquired resistance against both gefitinib and afatinib [15].”
Computational identification of natural product inhibitors against EGFR double mutant (T790M/L858R) by integrating ADMET, machine learning, molecular docking and a dynamics approach
Agarwal, S. M., Nandekar, P. P., & Saini, R. P. (2022) · RSC Advances · doi:10.1039/d2ra00373b · Cited by 35 · see citing works
Identification of small proline‐rich protein 1B ( SPRR1B ) as a prognostically predictive biomarker for lung adenocarcinoma by integrative bioinformatic analysis
Zhang, Z., Shi, R., Xu, S., Li, Y., Zhang, H., Liu, M., Zhu, G., Chen, C., Pan, Z., Liu, H., et al. (2021) · Thoracic Cancer · doi:10.1111/1759-7714.13836 · Cited by 30 · see citing works
Gossypol overcomes EGFR-TKIs resistance in non-small cell lung cancer cells by targeting YAP/TAZ and EGFRL858R/T790M
Xu, J., Zhu, G., Cao, D., Pan, H., & Li, Y.-W. (2019) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2019.108860 · Cited by 28 · see citing works
Integrated bioinformatics analysis identifies ALDH18A1 as a prognostic hub gene in glutamine metabolism in lung adenocarcinoma
Ren, H., Ge, D.-F., Yang, Z., Cheng, Z.-T., Zhao, S.-X., & Zhang, B. (2025) · Discover Oncology · doi:10.1007/s12672-024-01698-3 · Cited by 27 · see citing works
KCa channel blockers increase effectiveness of the EGF receptor TK inhibitor erlotinib in non-small cell lung cancer cells (A549)
Glaser, F., Hundehege, P., Bulk, E., Todesca, L. M., Schimmelpfennig, S., Naß, E., Budde, T., Meuth, S. G., & Schwab, A. (2021) · Scientific Reports · doi:10.1038/s41598-021-97406-0 · Cited by 26 · see citing works
Androgen receptor promotes oral squamous cell carcinoma cell migration by increasing EGFR phosphorylation
Liu, X., Qing, S., Che, K., Li, L., & Liao, X. (2019) · OncoTargets and Therapy · doi:10.2147/ott.s200718 · Cited by 24 · see citing works
Dietary Antioxidants and Lung Cancer Risk in Smokers and Non-Smokers
Alsharairi, N. A. (2022) · Healthcare · doi:10.3390/healthcare10122501 · Cited by 24 · see citing works
Discovery, Development, Inventions, and Patent Trends on Mobocertinib Succinate: The First-in-Class Oral Treatment for NSCLC with EGFR Exon 20 Insertions
Imran, M., Khan, S. A., Alshammari, M. K., Alreshidi, M. A., Alreshidi, A. A., Alghonaim, R. S., Alanazi, F. A., Alshehri, S., Ghoneim, M. M., & Shakeel, F. (2021) · Biomedicines · doi:10.3390/biomedicines9121938 · Cited by 23 · see citing works
“The overexpression of EGFR is implicated in the pathogenesis of human cancers, including NSCLC [8].”
Background
Epidermal Growth Factor Receptor-Targeted Neoantigen Peptide Vaccination for the Treatment of Non-Small Cell Lung Cancer and Glioblastoma
Li, F., Wu, H., Du, X., Sun, Y., Rausseo, B. N., Talukder, A. H., Katailiha, A. S., Elzohary, L., Wang, Y., Wang, Z., et al. (2023) · Vaccines · doi:10.3390/vaccines11091460 · Cited by 23 · see citing works
Heterogeneity of glutamine metabolism in acquired-EGFR-TKI-resistant lung cancer
Kim, S., Jeon, J. S., Choi, Y. J., Baek, G. H., Kim, S. K., & Kang, K. W. (2022) · Life Sciences · doi:10.1016/j.lfs.2021.120274 · Cited by 22 · see citing works
Targeting KRASG12C in Non-Small-Cell Lung Cancer: Current Standards and Developments
Torres-Jiménez, J., Espinar, J. B., Bote, H., Berjaga, M. Z., Esteban-Villarrubia, J., Fraile, J. Z., & Paz-Ares, L. G. (2024) · Drugs · doi:10.1007/s40265-024-02030-7 · Cited by 22 · see citing works
“Mutations in the tyrosine kinase domain of EGFR were the first targetable mutations discovered, and targeted therapy with EGFR tyrosine kinase inhibitors (TKIs) led to improved outcomes and quality of life [7] .”
Unravelling the Triad of Lung Cancer, Drug Resistance, and Metabolic Pathways
Mohanty, P., Pande, B., Acharya, R. K., Bhaskar, L. V., & Verma, H. K. (2024) · Diseases · doi:10.3390/diseases12050093 · Cited by 20 · see citing works
“Recently, a new class of medications has emerged that can target the formerly “un-druggable” KRAS mutation [52,53].”
Background
Stable Isotope Tracing Analysis in Cancer Research: Advancements and Challenges in Identifying Dysregulated Cancer Metabolism and Treatment Strategies
Hilovsky, D. L., Hartsell, J., Young, J. D., & Liu, X. (2024) · Metabolites · doi:10.3390/metabo14060318 · Cited by 20 · see citing works
“Mechanisms of resistance to targeted therapy: Epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs), which target early-stage lung cancer with EGFR mutations, have been among the most successful targeted cancer therapies [175–177].”
Background
Safety assessment of KRAS (G12C) inhibitors based on the FDA Adverse Event Reporting System (FAERS) database: A real-world pharmacovigilance study
Chen, M., Huang, Y., Jiang, S., & Ke, C. (2024) · Lung Cancer · doi:10.1016/j.lungcan.2024.107966 · Cited by 20 · see citing works
Inhibition of epidermal growth factor receptor suppresses parathyroid hormone‐related protein expression in tumours and ameliorates cancer‐associated cachexia
Weber, B. Z. C., Agca, S., Domaniku, A., Bilgiç, Ş. N., Arabacı, D. H., & Kır, S. (2022) · Journal of Cachexia Sarcopenia and Muscle · doi:10.1002/jcsm.12985 · Cited by 20 · see citing works
Discovery of a Novel Potent EGFR Inhibitor Against EGFR Activating Mutations and On-Target Resistance in NSCLC
Lee, E. J., Oh, S. Y., Lee, Y. W., Kim, J. Y., Kim, M.-J., Kim, T. H., Lee, J. B., Hong, M. H., Lim, S. M., Baum, A., et al. (2024) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-23-2951 · Cited by 20 · see citing works
Patients with non‑small cell lung cancer with the exon 21 L858R mutation: From distinct mechanisms to epidermal growth factor receptor tyrosine kinase inhibitor treatments (Review)
Liu, J., Wang, S., Yuan, H., Li, J., & Xing, P. (2024) · Oncology Letters · doi:10.3892/ol.2024.14855 · Cited by 18 · see citing works
Two Faces of Glutaminase GLS2 in Carcinogenesis
Buczkowska, J., & Szeliga, M. (2023) · Cancers · doi:10.3390/cancers15235566 · Cited by 19 · see citing works
“It is worth mentioning that EGFR-tyrosine kinase inhibitors (EGFR-TKI) prolong progression-free survival in NSCLC patients, but many patients eventually develop disease progression due to TKI-acquired resistance [71].”
Background
DEK promotes the proliferation and invasion of lung cancers and indicates poor prognosis in lung adenocarcinomas
Yang, M., Bai, L., Lei, L., Zheng, Y., Wang, Z., Li, Z., Liu, C., Huang, W., & Xu, H. (2020) · Oncology Reports · doi:10.3892/or.2020.7488 · Cited by 17 · see citing works
“Previous studies have documented the expression of DEK in NSCLC (18,20,25), which indicated that DEK expression was correlated with the progression of NSCLCs.”
BackgroundInfluential
Cancer Therapy-Related Cardiac Dysfunction: A Review of Current Trends in Epidemiology, Diagnosis, and Treatment
Theofilis, P., Vlachakis, P. K., Oikonomou, E. K., Drakopoulou, M., Karakasis, P., Apostolos, A., Pamporis, K., Tsioufis, K. P., & Tousoulis, D. (2024) · Biomedicines · doi:10.3390/biomedicines12122914 · Cited by 16 · see citing works
“QTc prolongation occurs in 0.1% of VEGF-inhibitor cases but is higher with third-generation EGFR TKIs such as osimertinib [30,31].”
Influential
CAR-T Cells Targeting HLA-G as Potent Therapeutic Strategy for EGFR Mutated and Overexpressed Oral Cancer
Lin, Y., Hua, C., Lu, H.-M., Huang, S., Chen, Y., Tsai, M., Lin, F., Canoll, P., Chiu, S., Huang, W., et al. (2022) · iScience · doi:10.1016/j.isci.2023.106089 · Cited by 15 · see citing works
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Authors: Díaz-Serrano, A., Gella, P., Jiménez, E., Zugazagoitia, J., & Paz-Ares Rodríguez, L.
Affiliations: Research Institute Hospital 12 de Octubre (ES)
Yale Cancer Center (US)
ORCID: Díaz-Serrano, Asunción
Venue: Drugs
Publisher: Springer Science and Business Media LLC
Published: 2018-06
Volume: 78
Issue: 9
Pages: 893-911
ISSN: 0012-6667 (ISSN-L)
1179-1950
DOI: 10.1007/s40265-018-0916-4
OpenAlex: W2809285875
Semantic Scholar: 3bfe42a82922c9b186444aa869784e8c1be89711
Cited by: 108
References: 153
Citations by year: 2026: 9 · 2025: 12 · 2024: 19 · 2023: 9 · 2022: 17 · 2021: 12 · 2020: 10 · 2019: 15 · 2018: 4 · 2017: 1
FWCI: 1.82
Type: journal article
Language: en
Open access: closed
Licence: www.springer.com/tdm (tdm)
Locations: Drugs (publishedVersion)
PubMed (publishedVersion)
BURJC Digital (King Juan Carlos University) (submittedVersion)
Hispana (submittedVersion)
Funders: Consejería de Educación, Juventud y Deporte, Comunidad de Madrid (ES) and European Social Fund (PEJD16/2016/BMD-2715)
Instituto de Salud Carlos III (CM15/00196)
Sistema Nacional de Salud
Universidad Complutense de Madrid
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 › Pulmonary and Respiratory Medicine › Lung Cancer Diagnosis and Treatment
Keywords: EGFR-mutant non-small cell lung cancer, EGFR tyrosine kinase inhibitors, osimertinib, T790M mutation, acquired drug resistance, MET amplification, HER2 amplification, immunotherapy, FLAURA trial, central nervous system metastasis
MeSH terms: Acrylamides, Aniline Compounds, Antineoplastic Agents, Carcinoma, Non-Small-Cell Lung, Humans, Indoles, Lung Neoplasms, Piperazines, Pyrimidines, Disease Progression, Disease-Free Survival, Drug Resistance, Neoplasm, Protein Kinase Inhibitors, Molecular Targeted Therapy, ErbB Receptors

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Targeting EGFR in Lung Cancer: Current Standards and Developments

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