The advance of the third‑generation EGFR‑TKI in the treatment of non‑small cell lung cancer (Review)
- Authors:
- Zhinan Cheng
- Hongwei Cui
- Yaqi Wang
- Jin Yang
- Chunyang Lin
- Xiaoyu Shi
- Yuxiu Zou
- Jing Chen
- Xiaoqiong Jia
- Liqing Su
-
Affiliations: Department of Medical Oncology, Affiliated Cancer Hospital of Inner Mongolia Medical University, Hohhot, Inner Mongolia Autonomous Region 010000, P.R. China, Scientific Research Department, Peking University Cancer Hospital (Inner Mongolia Campus)/Affiliated Cancer Hospital of Inner Mongolia Medical University, Inner Mongolia Cancer Center, Hohhot, Inner Mongolia Autonomous Region 010000, P.R. China, Laboratory of Molecular Tumor Diagnosis, Peking University Cancer Hospital (Inner Mongolia Campus)/Affiliated Cancer Hospital of Inner Mongolia Medical University, Hohhot, Inner Mongolia Autonomous Region 010000, P.R. China, Children's Ultrasound Department, Cangzhou Central Hospital, Cangzhou, Hebei 061000, P.R. China, Department of Oncology, Bayan Nur Hospital, Bayan Nur, Inner Mongolia Autonomous Region 015000, P.R. China, Department of Medicine, Ordos Institute of Technology, Ordos, Inner Mongolia Autonomous Region 017000, P.R. China, Department of Medical Oncology, Peking University Cancer Hospital (Inner Mongolia Campus)/Affiliated Cancer Hospital of Inner Mongolia Medical University, Huimin, Hohhot, Inner Mongolia Autonomous Region 010000, P.R. China, Department of Respiratory Medicine, Affiliated Hospital of Inner Mongolia Medical University, Huimin, Hohhot, Inner Mongolia Autonomous Region 010000, P.R. China - Published online on: December 5, 2023 https://doi.org/10.3892/or.2023.8675
- Article Number: 16
-
Copyright: © Cheng et al. This is an open access article distributed under the terms of Creative Commons Attribution License.
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|
Sung H, Ferlay J, Siegel RL, Laversanne M, Soerjomataram I, Jemal A and Bray F: Global cancer statistics 2020: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 countries. CA Cancer J Clin. 71:209–249. 2021. View Article : Google Scholar : PubMed/NCBI | |
|
Siegel RL, Miller KD, Fuchs HE and Jemal A: Cancer statistics, 2022. CA Cancer J Clin. 72:7–33. 2022. View Article : Google Scholar : PubMed/NCBI | |
|
Xia C, Dong X, Li H, Cao M, Sun D, He S, Yang F, Yan X, Zhang S, Li N and Chen W: Cancer statistics in China and United States, 2022: Profiles, trends, and determinants. Chin Med J (Engl). 135:584–590. 2022. View Article : Google Scholar : PubMed/NCBI | |
|
Miller KD, Nogueira L, Mariotto AB, Rowland JH, Yabroff KR, Alfano CM, Jemal A, Kramer JL and Siegel RL: Cancer treatment and survivorship statistics, 2019. CA Cancer J Clin. 69:363–385. 2019. View Article : Google Scholar : PubMed/NCBI | |
|
Herbst RS, Morgensztern D and Boshoff C: The biology and management of non-small cell lung cancer. Nature. 553:446–454. 2018. View Article : Google Scholar : PubMed/NCBI | |
|
Sun C, Gao W, Liu J, Cheng H and Hao J: FGL1 regulates acquired resistance to Gefitinib by inhibiting apoptosis in non-small cell lung cancer. Respir Res. 21:2102020. View Article : Google Scholar : PubMed/NCBI | |
|
Leonetti A, Sharma S, Minari R, Perego P, Giovannetti E and Tiseo M: Resistance mechanisms to osimertinib in EGFR-mutated non-small cell lung cancer. Br J Cancer. 121:725–737. 2019. View Article : Google Scholar : PubMed/NCBI | |
|
Andrews Wright NM and Goss GD: Third-generation epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of non-small cell lung cancer. Transl Lung Cancer Res. 8 (Suppl 3):S247–S264. 2019. View Article : Google Scholar : PubMed/NCBI | |
|
Simeone JC, Nordstrom BL, Patel K and Klein AB: Treatment patterns and overall survival in metastatic non-small-cell lung cancer in a real-world, US setting. Future Oncol. 15:3491–3502. 2019. View Article : Google Scholar : PubMed/NCBI | |
|
Mok TS, Wu YL, Thongprasert S, Yang CH, Chu DT, Saijo N, Sunpaweravong P, Han B, Margono B, Ichinose Y, et al: Gefitinib or carboplatin-paclitaxel in pulmonary adenocarcinoma. N Engl J Med. 361:947–957. 2009. View Article : Google Scholar : PubMed/NCBI | |
|
Tran PN and Klempner SJ: Profile of rociletinib and its potential in the treatment of non-small-cell lung cancer. Lung Cancer (Auckl). 7:91–97. 2016.PubMed/NCBI | |
|
He J, Huang Z, Han L, Gong Y and Xie C: Mechanisms and management of 3rd-generation EGFR-TKI resistance in advanced non-small cell lung cancer (Review). Int J Oncol. 59:902021. View Article : Google Scholar : PubMed/NCBI | |
|
Tan CS, Kumarakulasinghe NB, Huang YQ, Ang YLE, Choo JR, Goh BC and Soo RA: Third generation EGFR TKIs: Current data and future directions. Mol Cancer. 17:292018. View Article : Google Scholar : PubMed/NCBI | |
|
Remon J, Steuer CE, Ramalingam SS and Felip E: Osimertinib and other third-generation EGFR TKI in EGFR-mutant NSCLC patients. Ann Oncol. 29 (Suppl_1):i20–i27. 2018. View Article : Google Scholar : PubMed/NCBI | |
|
Cooper AJ, Sequist LV and Lin JJ: Third-generation EGFR and ALK inhibitors: Mechanisms of resistance and management. Nat Rev Clin Oncol. 19:499–514. 2022. View Article : Google Scholar : PubMed/NCBI | |
|
Nagasaka M, Zhu VW, Lim SM, Greco M, Wu F and Ou SI: Beyond osimertinib: The development of third-generation EGFR tyrosine kinase inhibitors for advanced EGFR+ NSCLC. J Thorac Oncol. 16:740–763. 2021. View Article : Google Scholar : PubMed/NCBI | |
|
Yang JC, Reckamp KL, Kim YC, Novello S, Smit EF, Lee JS, Su WC, Akerley WL, Blakely CM, Groen HJM, et al: Efficacy and safety of rociletinib versus chemotherapy in patients with EGFR-Mutated NSCLC: The results of TIGER-3, a phase 3 randomized study. JTO Clin Res Rep. 2:1001142020.PubMed/NCBI | |
|
Kim ES: Olmutinib: First global approval. Drugs. 76:1153–1157. 2016. View Article : Google Scholar : PubMed/NCBI | |
|
H L, H X and H Y, . Research on the third-generation epidermal growth factor receptor tyrosine kinase inhibitor drugs and their patents. Chin J N Drugs. 31:1553–1559. 2022. | |
|
Kelly RJ, Shepherd FA, Krivoshik A, Jie F and Horn L: A phase III, randomized, open-label study of ASP8273 versus erlotinib or gefitinib in patients with advanced stage IIIB/IV non-small-cell lung cancer. Ann Oncol. 30:1127–1133. 2019. View Article : Google Scholar : PubMed/NCBI | |
|
Dhillon S: Lazertinib: First approval. Drugs. 81:1107–1113. 2021. View Article : Google Scholar : PubMed/NCBI | |
|
Deeks ED: Furmonertinib: First approval. Drugs. 81:1775–1780. 2021. View Article : Google Scholar : PubMed/NCBI | |
|
Koch AL, Vellanki PJ, Drezner N, Li X, Mishra-Kalyani PS, Shen YL, Xia H, Li Y, Liu J, Zirkelbach JF, et al: FDA approval summary: Osimertinib for adjuvant treatment of surgically resected non-small cell lung cancer, a collaborative project orbis review. Clin Cancer Res. 27:6638–6643. 2021. View Article : Google Scholar : PubMed/NCBI | |
|
Prenzel N, Fischer OM, Streit S, Hart S and Ullrich A: The epidermal growth factor receptor family as a central element for cellular signal transduction and diversification. Endocr Relat Cancer. 8:11–31. 2001. View Article : Google Scholar : PubMed/NCBI | |
|
Levantini E, Maroni G, Del Re M and Tenen DG: EGFR signaling pathway as therapeutic target in human cancers. Semin Cancer Biol. 85:253–275. 2022. View Article : Google Scholar : PubMed/NCBI | |
|
Ward RA, Anderton MJ, Ashton S, Bethel PA, Box M, Butterworth S, Colclough N, Chorley CG, Chuaqui C, Cross DA, et al: Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR). J Med Chem. 56:7025–7048. 2013. View Article : Google Scholar : PubMed/NCBI | |
|
Dong RF, Zhu ML, Liu MM, Xu YT, Yuan LL, Bian J, Xia YZ and Kong LY: EGFR mutation mediates resistance to EGFR tyrosine kinase inhibitors in NSCLC: From molecular mechanisms to clinical research. Pharmacol Res. 167:1055832021. View Article : Google Scholar : PubMed/NCBI | |
|
Wee P and Wang Z: Epidermal growth factor receptor cell proliferation signaling pathways. Cancers (Basel). 9:522017. View Article : Google Scholar : PubMed/NCBI | |
|
Huang L and Fu L: Mechanisms of resistance to EGFR tyrosine kinase inhibitors. Acta Pharm Sin B. 5:390–401. 2015. View Article : Google Scholar : PubMed/NCBI | |
|
Liu Q, Yu S, Zhao W, Qin S, Chu Q and Wu K: EGFR-TKIs resistance via EGFR-independent signaling pathways. Mol Cancer. 17:532018. View Article : Google Scholar : PubMed/NCBI | |
|
Soejima K, Yasuda H and Hirano T: Osimertinib for EGFR T790M mutation-positive non-small cell lung cancer. Expert Rev Clin Pharmacol. 10:31–38. 2017. View Article : Google Scholar : PubMed/NCBI | |
|
Sigismund S, Avanzato D and Lanzetti L: Emerging functions of the EGFR in cancer. Mol Oncol. 12:3–20. 2018. View Article : Google Scholar : PubMed/NCBI | |
|
Sabbah DA, Hajjo R and Sweidan K: Review on epidermal growth factor receptor (EGFR) structure, signaling pathways, interactions, and recent updates of EGFR inhibitors. Curr Top Med Chem. 20:815–834. 2020. View Article : Google Scholar : PubMed/NCBI | |
|
Yun CH, Mengwasser KE, Toms AV, Woo MS, Greulich H, Wong KK, Meyerson M and Eck MJ: The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP. Proc Natl Acad Sci USA. 105:2070–2075. 2008. View Article : Google Scholar : PubMed/NCBI | |
|
Cross DA, Ashton SE, Ghiorghiu S, Eberlein C, Nebhan CA, Spitzler PJ, Orme JP, Finlay MR, Ward RA, Mellor MJ, et al: AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 4:1046–1061. 2014. View Article : Google Scholar : PubMed/NCBI | |
|
Wu L, Ke L, Zhang Z, Yu J and Meng X: Development of EGFR TKIs and options to manage resistance of Third-generation EGFR TKI osimertinib: Conventional ways and immune checkpoint inhibitors. Front Oncol. 10:6027622020. View Article : Google Scholar : PubMed/NCBI | |
|
Lamb YN: Osimertinib: A review in previously untreated, EGFR Mutation-positive, advanced NSCLC. Target Oncol. 16:687–695. 2021. View Article : Google Scholar : PubMed/NCBI | |
|
Singh M and Jadhav HR: Targeting non-small cell lung cancer with small-molecule EGFR tyrosine kinase inhibitors. Drug Discov Today. 23:745–753. 2018. View Article : Google Scholar : PubMed/NCBI | |
|
Patel H, Pawara R, Ansari A and Surana S: Recent updates on Third generation EGFR inhibitors and emergence of Fourth generation EGFR inhibitors to combat C797S resistance. Eur J Med Chem. 142:32–47. 2017. View Article : Google Scholar : PubMed/NCBI | |
|
Zhou C, Wang M, Cheng Y, Li H, Wang J and Wu YL: AURA17 study of osimertinib in Asia-Pacific patients (pts) with EGFR T790M-positive advanced non-small cell lung cancer (NSCLC): Updated phase II results including overall survival (OS). Ann Oncol. 29:IX1572018. View Article : Google Scholar | |
|
Goss G, Tsai CM, Shepherd FA, Bazhenova L, Lee JS, Chang GC, Crino L, Satouchi M, Chu Q, Hida T, et al: Osimertinib for pretreated EGFR Thr790Met-positive advanced non-small-cell lung cancer (AURA2): A multicentre, open-label, single-arm, phase 2 study. Lancet Oncol. 17:1643–1652. 2016. View Article : Google Scholar : PubMed/NCBI | |
|
Papadimitrakopoulou VA, Mok TS, Han JY, Ahn MJ, Delmonte A, Ramalingam SS, Kim SW, Shepherd FA, Laskin J, He Y, et al: Osimertinib versus platinum-pemetrexed for patients with EGFR T790M advanced NSCLC and progression on a prior EGFR-tyrosine kinase inhibitor: AURA3 overall survival analysis. Ann Oncol. 31:1536–1544. 2020. View Article : Google Scholar : PubMed/NCBI | |
|
Cheng Y, He Y, Li W, Zhang HL, Zhou Q, Wang B, Liu C, Walding A, Saggese M, Huang X, et al: Osimertinib versus comparator EGFR TKI as First-line treatment for EGFR-mutated advanced NSCLC: FLAURA China, A randomized study. Target Oncol. 16:165–176. 2021. View Article : Google Scholar : PubMed/NCBI | |
|
Wu L, Zhong W, Li A, Qiu Z, Xie R, Shi H and Lu S: Successful treatment of EGFR T790M-mutant non-small cell lung cancer with almonertinib after osimertinib-induced interstitial lung disease: A case report and literature review. Ann Transl Med. 9:9502021. View Article : Google Scholar : PubMed/NCBI | |
|
Soria JC, Ohe Y, Vansteenkiste J, Reungwetwattana T, Chewaskulyong B, Lee KH, Dechaphunkul A, Imamura F, Nogami N, Kurata T, et al: Osimertinib in untreated EGFR-mutated advanced non-small-cell lung cancer. N Engl J Med. 378:113–125. 2018. View Article : Google Scholar : PubMed/NCBI | |
|
Leighl NB, Karaseva N, Nakagawa K, Cho BC, Gray JE, Hovey T, Walding A, Rydén A and Novello S: Patient-reported outcomes from FLAURA: Osimertinib versus erlotinib or gefitinib in patients with EGFR-mutated advanced non-small-cell lung cancer. Eur J Cancer. 125:49–57. 2020. View Article : Google Scholar : PubMed/NCBI | |
|
Reungwetwattana T, Nakagawa K, Cho BC, Cobo M, Cho EK, Bertolini A, Bohnet S, Zhou C, Lee KH, Nogami N, et al: CNS response to osimertinib versus standard epidermal growth factor receptor tyrosine kinase inhibitors in patients with untreated EGFR-mutated advanced non-small-cell lung cancer. J Clin Oncol: Jco2018783118. 2018.doi: 10.1200/JCO.2018.78.3118 (Epub ahead of print). View Article : Google Scholar : PubMed/NCBI | |
|
Lu S, Wang Q, Zhang G, Dong X, Yang CT, Song Y, Chang GC, Lu Y, Pan H, Chiu CH, et al: Efficacy of aumolertinib (HS-10296) in patients with advanced EGFR T790M+ NSCLC: updated post-national medical products administration approval results from the APOLLO registrational trial. J Thorac Oncol. 17:411–422. 2022. View Article : Google Scholar : PubMed/NCBI | |
|
Shirley M and Keam SJ: Aumolertinib: A review in non-small cell lung cancer. Drugs. 82:577–584. 2022. View Article : Google Scholar : PubMed/NCBI | |
|
Lu S, Dong X, Jian H, Chen J, Chen G, Sun Y, Ji Y, Wang Z, Shi J, Lu J, et al: AENEAS: A randomized phase III trial of aumolertinib versus gefitinib as First-line therapy for locally advanced or metastaticnon-small-cell lung cancer with EGFR exon 19 deletion or L858R mutations. J Clin Oncol. 40:3162–3171. 2022. View Article : Google Scholar : PubMed/NCBI | |
|
Benjamin DJ and Nagasaka M: Freeing the competition: Will aumolertinib (AENEAS) have a fighting chance against osimertinib (FLAURA)? J Clin Oncol. 41:742–744. 2023. View Article : Google Scholar : PubMed/NCBI | |
|
Shi Y, Hu X, Zhang S, Lv D, Wu L, Yu Q, Zhang Y, Liu L, Wang X, Cheng Y, et al: Efficacy, safety, and genetic analysis of furmonertinib (AST2818) in patients with EGFR T790M mutated non-small-cell lung cancer: A phase 2b, multicentre, single-arm, open-label study. Lancet Respir Med. 9:829–839. 2021. View Article : Google Scholar : PubMed/NCBI | |
|
Shi Y, Chen G, Wang X, Liu Y, Wu L, Hao Y, Liu C, Zhu S, Zhang X, Li Y, et al: Furmonertinib (AST2818) versus gefitinib as first-line therapy for Chinese patients with locally advanced or metastatic EGFR mutation-positive non-small-cell lung cancer (FURLONG): A multicentre, double-blind, randomised phase 3 study. Lancet Respir Med. 10:1019–1028. 2022. View Article : Google Scholar : PubMed/NCBI | |
|
Shi Y, Chen G, Wang X, Liu Y, Wu L, Hao Y, Liu C, Zhu S, Zhang X, Li Y, et al: Central Nervous system efficacy of furmonertinib (AST2818) versus gefitinib as first-line treatment for EGFR-mutated NSCLC: Results from the FURLONG study. J Thorac Oncol. 17:1297–1305. 2022. View Article : Google Scholar : PubMed/NCBI | |
|
Park K, Jӓnne PA, Kim DW, Han JY, Wu MF, Lee JS, Kang JH, Lee DH, Cho BC, Yu CJ, et al: Olmutinib in T790M-positive non-small cell lung cancer after failure of first-line epidermal growth factor receptor-tyrosine kinase inhibitor therapy: A global, phase 2 study. Cancer. 127:1407–1416. 2021. View Article : Google Scholar : PubMed/NCBI | |
|
Murtuza A, Bulbul A, Shen JP, Keshavarzian P, Woodward BD, Lopez-Diaz FJ, Lippman SM and Husain H: Novel Third-generation EGFR tyrosine kinase inhibitors and strategies to overcome therapeutic resistance in lung cancer. Cancer Res. 79:689–698. 2019. View Article : Google Scholar : PubMed/NCBI | |
|
Lee J, Hong MH and Cho BC: Lazertinib: On the Way to Its Throne. Yonsei Med J. 63:799–805. 2022. View Article : Google Scholar : PubMed/NCBI | |
|
Cho BC, Han JY, Kim SW, Lee KH, Cho EK, Lee YG, Kim DW, Kim JH, Lee GW, Lee JS, et al: A Phase 1/2 Study of Lazertinib 240 mg in patients with advanced EGFR T790M-positive NSCLC after previous EGFR tyrosine kinase inhibitors. J Thorac Oncol. 17:558–567. 2022. View Article : Google Scholar : PubMed/NCBI | |
|
Cho BC, Ahn MJ, Kang JH, Soo RA, Reungwetwattana T, Yang JC, Cicin I, Kim DW, Wu YL, Lu S, et al: Lazertinib versus gefitinib as First-line treatment in patients with EGFR-mutated advanced non-small-cell lung cancer: Results from LASER301. J Clin Oncol. 41:4208–4217. 2023. View Article : Google Scholar : PubMed/NCBI | |
|
Cho BC, Kim DW, Spira AI, Gomez JE, Haura EB, Kim SW, Sanborn RE, Cho EK, Lee KH, Minchom A, et al: Amivantamab plus lazertinib in osimertinib-relapsed EGFR-mutant advanced non-small cell lung cancer: A phase 1 trial. Nat Med. 14:023–02554. 2023. | |
|
Tan DSW, Kim SW, Ponce Aix S, Sequist LV, Smit EF, Yang JCH, Hida T, Toyozawa R, Felip E, Wolf J, et al: Nazartinib for treatment-naive EGFR-mutant non-small cell lung cancer: Results of a phase 2, single-arm, open-label study. Eur J Cancer. 172:276–286. 2022. View Article : Google Scholar : PubMed/NCBI | |
|
Zhou Q, Wu L, Hu P, An T, Zhou J, Zhang L, Liu XQ, Luo F, Zheng X, Cheng Y, et al: A Novel Third-generation EGFR Tyrosine kinase inhibitor abivertinib for EGFR T790M-mutant Non-small cell lung cancer: A multicenter phase I/II study. Clin Cancer Res. 28:1127–1135. 2022. View Article : Google Scholar : PubMed/NCBI | |
|
Wang F and Zhou Q: The challenges of Third-generation EGFR tyrosine kinase inhibitors in the therapy of advanced NSCLC. J Thorac Oncol. 17:481–486. 2022. View Article : Google Scholar : PubMed/NCBI | |
|
Azuma K, Nishio M, Hayashi H, Kiura K, Satouchi M, Sugawara S, Hida T, Iwamoto Y, Inoue A, Takeda K, et al: ASP8273 tolerability and antitumor activity in tyrosine kinase inhibitor-naïve Japanese patients with EGFR mutation-positive non-small-cell lung cancer. Cancer Sci. 109:2532–2538. 2018. View Article : Google Scholar : PubMed/NCBI | |
|
Cho BC, Goldberg SB, Kim DW, Socinski MA, Burns TF, Lwin Z, Pathan N, Ma WD, Masters JC, Cossons N, et al: A phase 1b/2 study of PF-06747775 as monotherapy or in combination with Palbociclib in patients with epidermal growth factor receptor mutant advanced non-small cell lung cancer. Expert Opin Investig Drugs. 31:747–757. 2022. View Article : Google Scholar : PubMed/NCBI | |
|
Shi Y, Li B, Wu L, Pan Y, Pan Z, Liu Y, Fan Y, Ji Y, Fang J, Shi Q, et al: Efficacy and safety of limertinib (ASK120067) in patients with locally advanced or metastatic EGFR Thr790Met-mutated NSCLC: A multicenter, single-arm, phase 2b study. J Thorac Oncol. 17:1205–1215. 2022. View Article : Google Scholar : PubMed/NCBI | |
|
Zhang T, Qu R, Chan S, Lai M, Tong L, Feng F, Chen H, Song T, Song P, Bai G, et al: Discovery of a novel third-generation EGFR inhibitor and identification of a potential combination strategy to overcome resistance. Mol Cancer. 19:902020. View Article : Google Scholar : PubMed/NCBI | |
|
Lu S, Zhang Y, Zhang G, Zhou J, Cang S, Cheng Y, Wu G, Cao P, Lv D, Jian H, et al: Efficacy and safety of befotertinib (D-0316) in patients with EGFR T790M-mutated NSCLC that had progressed after prior EGFR tyrosine kinase inhibitor therapy: A phase 2, multicenter, single-arm, open-label study. J Thorac Oncol. 17:1192–1204. 2022. View Article : Google Scholar : PubMed/NCBI | |
|
Han L, Zhang X, Wang Z, Zhang X, Zhao L, Fu W, Liang X, Zhang Z and Wang Y: SH-1028, An irreversible Third-generation EGFR TKI, overcomes T790M-mediated resistance in non-small cell lung cancer. Front Pharmacol. 12:6652532021. View Article : Google Scholar : PubMed/NCBI | |
|
Xiong A, Ren S, Liu H, Miao L, Wang L, Chen J, Li W, Li R, Wang X, Lu Z, et al: Efficacy and Safety of SH-1028 in patients with EGFR T790M-positive NSCLC: A multicenter, single-arm, open-label, phase 2 trial. J Thorac Oncol. 17:1216–1226. 2022. View Article : Google Scholar : PubMed/NCBI | |
|
Ito K, Nishio M, Kato M, Murakami H, Aoyagi Y, Ohe Y, Okayama T, Hashimoto A, Ohsawa H, Tanaka G, et al: TAS-121, A selective mutant EGFR inhibitor, shows activity against tumors expressing various EGFR mutations including T790M and uncommon mutations G719X. Mol Cancer Ther. 18:920–928. 2019. View Article : Google Scholar : PubMed/NCBI | |
|
Wu YL, Cheng Y, Zhou X, Lee KH, Nakagawa K, Niho S, Tsuji F, Linke R, Rosell R, Corral J, et al: Dacomitinib versus gefitinib as first-line treatment for patients with EGFR-mutation-positive non-small-cell lung cancer (ARCHER 1050): A randomised, open-label, phase 3 trial. Lancet Oncol. 18:1454–1466. 2017. View Article : Google Scholar : PubMed/NCBI | |
|
Park K, Tan EH, O'Byrne K, Zhang L, Boyer M, Mok T, Hirsh V, Yang JC, Lee KH, Lu S, et al: Afatinib versus gefitinib as first-line treatment of patients with EGFR mutation-positive non-small-cell lung cancer (LUX-Lung 7): A phase 2B, open-label, randomised controlled trial. Lancet Oncol. 17:577–589. 2016. View Article : Google Scholar : PubMed/NCBI | |
|
Lei T, Xu T, Zhang N, Zou X, Kong Z, Wei C and Wang Z: Anlotinib combined with osimertinib reverses acquired osimertinib resistance in NSCLC by targeting the c-MET/MYC/AXL axis. Pharmacol Res. 188:1066682023. View Article : Google Scholar : PubMed/NCBI | |
|
Jia Y, Yun CH, Park E, Ercan D, Manuia M, Juarez J, Xu C, Rhee K, Chen T, Zhang H, et al: Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors. Nature. 534:129–132. 2016. View Article : Google Scholar : PubMed/NCBI | |
|
Choi YJ, Kim DS, Hoon Sung Y, Kim DH, Im K, Lee H, Lee CW, Cho J, Min J, Woo DC, et al: The reversible fourth-generation EGFR tyrosine kinase inhibitor OBX02-011 overcomes C797S-mediated resistance in lung cancer. Cancer Res. Jun 14–2022.(Epub ahead of print). doi: 10.1158/0008-5472.CAN-22-0394. View Article : Google Scholar | |
|
Liu Y, Lai M, Li S, Wang Y, Feng F, Zhang T, Tong L, Zhang M, Chen H, Chen Y, et al: LS-106, a novel EGFR inhibitor targeting C797S, exhibits antitumor activities both in vitro and in vivo. Cancer Sci. 113:709–720. 2022. View Article : Google Scholar : PubMed/NCBI | |
|
Kashima K, Kawauchi H, Tanimura H, Tachibana Y, Chiba T, Torizawa T and Sakamoto H: CH7233163 overcomes osimertinib-resistant EGFR-Del19/T790M/C797S mutation. Mol Cancer Ther. 19:2288–2297. 2020. View Article : Google Scholar : PubMed/NCBI |
