In Vitro and In Vivo characterization of irreversible mutant-selective EGFR inhibitors that are wild-type sparing

Molecular Cancer Therapeutics

Volumn 13, Issue 6, 2014, Pages 1468-1479

  Sjin, Robert Tjin Tham ^a   Lee, Kwangho ^a   Walter, Annette O ^b   Dubrovskiy, Aleksandr ^a   Sheets, Michael ^a   St Martin, Thia ^a   Labenski, Matthew T ^a   Zhu, Zhendong ^a   Tester, Richland ^a   Karp, Russell ^a   Medikonda, Aravind ^a   Chaturvedi, Prasoon ^a   Ren, Yixuan ^a   Haringsma, Henry ^b   Etter, Jeff ^b   Raponi, Mitch ^b   Simmons, Andrew D ^b   Harding, Thomas C ^b   Niu, Deqiang ^a   Nacht, Mariana ^a   Westlin, William F ^a   Petter, Russell C ^a   Allen, Andrew ^b   Singh, Juswinder ^a   more..

^a Celgene Avilomics Research   (United States)

^b Clovis Oncology Inc   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2,4 DIAMINOPYRIMIDINE DERIVATIVE; AFATINIB; CO 1686; EPIDERMAL GROWTH FACTOR RECEPTOR; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; ERLOTINIB; GEFITINIB; UNCLASSIFIED DRUG; WZ 4002; 2,4-DIAMINOPYRIDINE; 4 AMINOPYRIDINE; EGFR PROTEIN, HUMAN;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTINEOPLASTIC ACTIVITY; ARTICLE; CANCER RECURRENCE; CONTROLLED STUDY; DRUG RECEPTOR BINDING; FEMALE; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; LUNG SMALL CELL CANCER; MOUSE; NONHUMAN; PHARMACODYNAMICS; PRIORITY JOURNAL; RECEPTOR AFFINITY; WILD TYPE; ANALOGS AND DERIVATIVES; ANIMAL; ANTAGONISTS AND INHIBITORS; CARCINOMA, NON-SMALL-CELL LUNG; CELL PROLIFERATION; CLINICAL TRIAL (TOPIC); DRUG EFFECTS; DRUG RESISTANCE; DRUG SCREENING; GENETICS; METABOLISM; MUTATION; NEOPLASM RECURRENCE, LOCAL; PATHOLOGY; TUMOR CELL LINE;

4-AMINOPYRIDINE; ANIMALS; CARCINOMA, NON-SMALL-CELL LUNG; CELL LINE, TUMOR; CELL PROLIFERATION; CLINICAL TRIALS AS TOPIC; DRUG RESISTANCE, NEOPLASM; HUMANS; IN VITRO TECHNIQUES; MICE; MUTATION; NEOPLASM RECURRENCE, LOCAL; RECEPTOR, EPIDERMAL GROWTH FACTOR; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 84902668773     PISSN: 15357163     EISSN: 15388514     Source Type: Journal    
DOI: 10.1158/1535-7163.MCT-13-0966     Document Type: Article

References (37)

1. Sequist LV, Waltman BA, Dias-Santagata D, Digumarthy S, Turke AB, Fidias P, et al. Genotypic and histological evolution of lung cancers acquiring resistance to EGFR inhibitors. Sci Transl Med 2011;3: 75ra26.
2. Robinson KW, Sandler AB. EGFR tyrosine kinase inhibitors: difference in efficacy and resistance. Curr Oncol Rep 2013;15:396-404.
3. Siegel R, Naishadham D, Jemal A. Cancer statistics, 2013. CA Cancer J Clin 2013;63:11-30.
4. American Cancer Society. Cancer Facts & Figures 2013. American Cancer Society 2013.
5. Rosell R, Moran T, Queralt C, Porta R, Cardenal F, Camps C, et al. Screening for epidermal growth factor receptor mutations in lung cancer. N Engl J Med 2009;361:958-67.
6. Tabara K, Kanda R, Sonoda K, Kubo T, Murakami Y, Kawahara A, et al. Loss of activating EGFR mutant gene contributes to acquired resistance to EGFR tyrosine kinase inhibitors in lung cancer cells. PLoS ONE 2012;7:e41017.
7. Ohashi K, Maruvka YE, Michor F, Pao W. Epidermal growth factor receptor tyrosine kinase inhibitor-resistant disease. J Clin Oncol 2013; 31:1070-80.
8. Chen X, Zhu Q, Zhu L, Pei D, Liu Y, Yin Y, et al. Clinical perspective of afatinib in non-small cell lung cancer. Lung Cancer 2013;81: 155 -61.
9. Fukuoka M, Wu YL, Thongprasert S, Sunpaweravong P, Leong SS, Sriuranpong V, et al. Biomarker analyses and final overall survival results from a phase III, randomized, open-label, first-line study of gefitinib versus carboplatin/paclitaxel in clinically selected patients with advanced non-small-cell lung cancer in Asia (IPASS). J Clin Oncol 2011;29:2866-74.
10. Rosell R, Carcereny E, Gervais R, Vergnenegre A, Massuti B, Felip E, et al. Erlotinib versus standard chemotherapy as first-line treatment for European patients with advanced EGFR mutation-positive non-smallcell lung cancer (EURTAC): a multicentre, open-label, randomised phase 3 trial. Lancet Oncol 2012;13:239-46.
11. Yu HA, Arcila ME, Rekhtman N, Sima CS, Zakowski MF, Pao W, et al. Analysis of tumor specimens at the time of acquired resistance to EGFR-TKI therapy in 155 patients with EGFR-mutant lung cancers. Clin Cancer Res 2013;19:2240-7.
12. Yun CH, Mengwasser KE, Toms AV, Woo MS, Greulich H, Wong KK, et al. The T790M mutation in EGFR kinase causes drug resistance by increasing the af finity for ATP. Proc Natl Acad Sci U S A 2008;105: 2070-5. (Pubitemid 351439466)
13. Herbst RS, LoRusso PM, Purdom M, Ward D. Dermatologic side effects associated with gefitinib therapy: clinical experience and management. Clin Lung Cancer 2003;4:366-9. (Pubitemid 36798559)
14. Engelman JA, Zejnullahu K, Gale CM, Lifshits E, Gonzales AJ, Shimamura T, et al. PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefitinib. Cancer Res 2007;67:11924-32.
15. Kwak EL, Sordella R, Bell DW, Godin-Heymann N, Okimoto RA, Brannigan BW, et al. Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib. Proc Natl Acad Sci U S A 2005;102:7665-70.
16. Li D, Ambrogio L, Shimamura T, Kubo S, Takahashi M, Chirieac LR, et al. BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models. Oncogene 2008;27: 4702-11.
17. Miller VA, Hirsh V, Cadranel J, Chen YM, Park K, Kim SW, et al. Afatinib versus placebo for patients with advanced, metastatic non-small-cell lung cancer after failure of erlotinib, gefitinib, or both, and one or two lines of chemotherapy (LUX-Lung 1): a phase 2b/3 randomised trial. Lancet Oncol 2012;13:528 -38.
18. Heuckmann JM, Rauh D, Thomas RK. Epidermal growth factor receptor (EGFR) signaling and covalent EGFR inhibition in lung cancer. J Clin Oncol 2012;30:3417-20.
19. Ramalingam SS, Blackhall F, Krzakowski M, Barrios CH, Park K, Bover I, et al. Randomized phase II study of dacomitinib (PF-00299804), an irreversible pan-human epidermal growth factor receptor inhibitor, versus erlotinib in patients with advanced non-small-cell lung cancer. J Clin Oncol 2012;30:3337-44.
20. Sequist LV, Besse B, Lynch TJ, Miller VA, Wong KK, Gitlitz B, et al. Neratinib, an irreversible pan-ErbB receptor tyrosine kinase inhibitor: results of a phase II trial in patients with advanced non-small-cell lung cancer. J Clin Oncol 2010;28:3076-83.
21. Lee K, Niu D, Petter RC, Baevsky M, Singh J. Heterocyclic compounds and uses thereof. US20120149687 A1 2010.
22. Zhou W, Ercan D, Chen L, Yun CH, Li D, Capelletti M, et al. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature 2009;462:1070-4.
23. Lee HJ, Schaefer G, Heffron TP, Shao L, Ye X, Sideris S, et al. Noncovalent wild-type-sparing inhibitors of EGFR T790M. Cancer Discov 2013;3:168-81.
24. Ward RA, Anderton M, Ashton S, Bethel P, Box M, Butterworth S, 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 2013;56: 7025-48.
25. Chong CR, Janne PA. The quest to overcome resistance to EGFR-targeted therapies in cancer. Nat Med 2013;19:1389-400.
26. Walter AO, Tjin Tham Sjin R, Haringsma HJ, Ohashi K, Sun J, Lee K, et al. Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC. Cancer Discov 2013;3:1404-15.
27. Yu J, Kane S, Wu J, Benedettini E, Li D, Reeves C, et al. Mutation-specific antibodies for the detection of EGFR mutations in non-smallcell lung cancer. Clin Cancer Res 2009;15:3023-8.
28. Singh J, Evans EK, Hagel M, Labenski MT, Dubrovskiy A, Nacht M, et al. Superiority of a novel EGFR targeted covalent inhibitor over its reversible counterpart in overcoming drug resistance. Med Chem Comm 2012;3:780-3.
29. Evans EK, Tester R, Aslanian S, Karp R, Sheets M, Labenski MT, et al. Inhibition of Btk with CC-292 provides early pharmacodynamic assessment of activity in mice and humans. J Pharmacol Exp Ther 2013;346:219-28.
30. Langer CJ. Epidermal growth factor receptor inhibition in mutation-positive non-small-cell lung cancer: is afatinib better or simply newer? J Clin Oncol 2013;31:3303-6.
31. Ramalingam S, Belani C. Systemic chemotherapy for advanced nonsmall cell lung cancer: recent advances and future directions. Oncologist 2008;13 Suppl 1:5-13.
32. McCoach CE, Kelly K. Treatment paradigms in advanced non-small-cell lung cancer. Clin Adv Hematol Oncol 2013;11:629-39.
33. Kim Y, Ko J, Cui Z, Abolhoda A, Ahn JS, Ou SH, et al. The EGFR T790M mutation in acquired resistance to an irreversible second-generation EGFR inhibitor. Mol Cancer Ther 2012;11:784-91.
34. ZhouW,Ercan D, Janne PA, Gray NS. Discovery of selective irreversible inhibitors for EGFR-T790M. Bioorg Med Chem Lett 2011;21:638-43.
35. Walter AO, Tjin Tham Sjin R, Haringsma H, Lin K, Dubrovskiy A, Lee KK, et al. CO-1686, a novel mutant-selective EGFR inhibitor, overcomes T790M-mediated resistance in non-small cell lung cancer (NSCLC). American Association of Cancer Research; 2012.
36. Soria JC, Sequist LV, Gadgeel S, Goldman J, Wakelee H, Varga A, et al. First-in-human evaluation of CO-1686, an irreversible, highly selective tyrosine kinase inhibitor of mutations of EGFR (activating and T790M). In Proceedings of the 15th World Conference on Lung Cancer; Sydney, Australia; 2013.
37. Sequist LV, Soria JC, Gadgeel SM, Wakelee H, Camidge DR, Varga A, et al.First-in-human evaluation of CO-1686, an irreversible, selective, and potent tyrosine kinase inhibitor of EGFR T790M. American Society of Clinical Oncology; 2013.