References
- Janne PA, Yang JC, Kim DW, et al. AZD9291 in EGFR inhibitor-resistant non-small-cell lung cancer. N Engl J Med. 2015;372:1689–1699.
- Mok TS, Wu Y-L, Ahn M-J, et al. Osimertinib or platinum-pemetrexed in EGFR T790M-positive lung cancer. N Engl J Med. 2017;376:629–640.
- Soria J-C, Ohe Y, Vansteenkiste J, et al. Osimertinib in untreated EGFR-mutated advanced non-small-cell lung cancer. N Engl J Med. 2018;378:113–125.
- Reungwetwattana T, Nakagawa K, Cho BC, 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. 2018;36:3290-3297.
- Yun J, Hong MH, Kim S-Y, et al. YH25448, an irreversible EGFR-TKI with potent intracranial activity in EGFR mutant non-small-cell lung cancer. Clin Cancer Res. 2019 [cited 2019 Apr 11]. DOI:10.1158/1078-0432.CCR-18-2906
- Cheng H, Nair SK, Murray BW. Recent progress on third generation covalent EGFR inhibitors. Bioorg Med Chem Lett. 2016;26:1861–1868.
- Jia Y, Juarez J, Li J, et al. EGF816 exerts anticancer effects in non-small cell lung cancer by irreversibly and selectively targeting primary and acquired activating mutations in the EGF receptor. Cancer Res. 2016;76:1591–1602.
- Johnson M, Karlix J, Burris H, et al. OA02.05 CK-101 (RX518), a third generation mutant-selective inhibitor of EGFR in NSCLC: results of an ongoing phase I/II trial. J Thorac Oncol. 2018;13:S323.
- Planken S, Behenna DC, Nair SK, et al. 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. J Med Chem. 2017;60:3002–3019.
- Sequist LV, Soria J-C, Goldman JW, et al. Rociletinib in EGFR-mutated non–small-cell lung cancer. N Engl J Med. 2015;372:1700–1709.
- Dhingra K. Rociletinib: has the TIGER lost a few of its stripes? Ann Oncol. 2016;27:1161–1164.
- Park K, Lee J-S, Lee KH, et al. BI 1482694 (HM61713), an EGFR mutant-specific inhibitor, in T790M+ NSCLC: efficacy and safety at the RP2D. J Clin Oncol. 2016;34:9055.
- Park K, Jänne PA, Yu C-J, et al. 412OA global phase II study of olmutinib (HM61713) in patients with T790M-positive NSCLC after failure of first-line EGFR-TKI. Ann Oncol. 2017;28:mdx671.001. Available from: https://academic.oup.com/annonc/article/28/suppl_10/mdx671.001/4652695
- Tan DS, Kim SW, Sequist LV, et al. LBA61Phase II results for single-agent nazartinib (EGF816) in adult patients (pts) with treatment-naive EGFR-mutant non-small cell lung cancer (NSCLC). Ann Oncol. 2018;29:mdy424.073-mdy424.073.
- Planchard D, Boyer MJ, Lee J-S, et al. Postprogression outcomes for osimertinib versus standard-of-care EGFR-TKI in patients with previously untreated EGFR-mutated advanced non-small cell lung cancer. Clin Cancer Res. 2019.
- Thress KS, Paweletz CP, Felip E, et al. Acquired EGFR C797S mutation mediates resistance to AZD9291 in non-small cell lung cancer harboring EGFR T790M. Nat Med. 2015;21:560–562.
- Ramalingam SS, Cheng Y, Zhou C, et al. LBA50Mechanisms of acquired resistance to first-line osimertinib: preliminary data from the phase III FLAURA study. Ann Oncol. 2018;29:mdy424.063. Available from: https://academic.oup.com/annonc/article/29/suppl_8/mdy424.063/5142018
- Lin -C-C, Shih J-Y, Yu C-J, et al. Outcomes in patients with non-small-cell lung cancer and acquired Thr790Met mutation treated with osimertinib: a genomic study. Lancet Respir Med. 2018;6:107–116.
- Yang Z, Yang N, Ou Q, et al. Investigating novel resistance mechanisms to third-generation EGFR tyrosine kinase inhibitor osimertinib in non-small cell lung cancer patients. Clin Cancer Res. 2018;24:3097–3107.
- Blakely CM, Watkins TBK, Wu W, et al. Evolution and clinical impact of co-occurring genetic alterations in advanced-stage EGFR-mutant lung cancers. Nat Genet. 2017;49:1693–1704.
- Chabon JJ, Simmons AD, Lovejoy AF, et al. Circulating tumour DNA profiling reveals heterogeneity of EGFR inhibitor resistance mechanisms in lung cancer patients. Nat Commun. 2016;7:11815.
- Helman E, Nguyen M, Karlovich CA, et al. Cell-free DNA next-generation sequencing prediction of response and resistance to third-generation EGFR inhibitor. Clin Lung Cancer. 2018;19:518–530.e7.
- Tan DS-W, Kim D-W, Leighl NB, et al. Genomic profiling of resistant tumor samples following progression on EGF816, a third generation, mutant-selective EGFR tyrosine kinase inhibitor (TKI), in advanced non-small cell lung cancer (NSCLC). J Clin Oncol. 2017;35:11506.
- Oxnard GR, Hu Y, Mileham KF, et al. Assessment of resistance mechanisms and clinical implications in patients with EGFR T790M-positive lung cancer and acquired resistance to osimertinib. JAMA Oncol. 2018;4:1527–1534.
- Piotrowska Z, Isozaki H, Lennerz JK, et al. Landscape of acquired resistance to osimertinib in EGFR-mutant NSCLC and clinical validation of combined EGFR and RET inhibition with osimertinib and BLU-667 for acquired RET fusion. Cancer Discov. 2018;8:1529–1539.
- Lai GGY, Lim TH, Lim J, et al. Clonal MET amplification as a determinant of tyrosine kinase inhibitor resistance in epidermal growth factor receptor-mutant non-small-cell lung cancer. J Clin Oncol. 2019;JCO1800177.
- Offin M, Rizvi H, Tenet M, et al. Tumor mutation burden and efficacy of EGFR-tyrosine kinase inhibitors in patients with EGFR-mutant lung cancers. Clin Cancer Res. 2019;25:1063-1069.
- Kannan S, Tan DS-W, Verma CS. Effects of single nucleotide polymorphisms on the binding of Afatinib to EGFR: a potential patient stratification factor revealed by modeling studies. J Chem Inf Model. 2019;59:309–315.
- Cross DAE, Ashton SE, Ghiorghiu S, et al. AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014;4:1046–1061.
- Nahar R, Zhai W, Zhang T, et al. Elucidating the genomic architecture of Asian EGFR-mutant lung adenocarcinoma through multi-region exome sequencing. Nat Commun. 2018;9:216.
- Niederst MJ, Engelman JA. Bypass mechanisms of resistance to receptor tyrosine kinase inhibition in lung cancer. Sci Signal. 2013;6:re6–re6.
- Wilson TR, Fridlyand J, Yan Y, et al. Widespread potential for growth-factor-driven resistance to anticancer kinase inhibitors. Nature. 2012;487:505–509.
- Sequist LV, Piotrowska Z, Niederst MJ, et al. Osimertinib responses after disease progression in patients who had been receiving rociletinib. JAMA Oncol. 2016;2:541–543.
- Arbour KC, Sequist LV, Piotrowska Z, et al. Response to osimertinib following treatment with EGF816 in patients with T790M EGFR mutant NSLCLC. J Clin Oncol. 2017;35:e20673–e20673.
- Thress KS, Jacobs V, Angell HK, et al. Modulation of biomarker expression by osimertinib: results of the paired tumor biopsy cohorts of the AURA phase I trial. J Thorac Oncol. 2017;12:1588–1594.
- Ahn MJ, Yang J, Yu H, et al. 136O: Osimertinib combined with durvalumab in EGFR-mutant non-small cell lung cancer: results from the TATTON phase Ib trial. J Thorac Oncol. 2016;11:S115.