Activating Mutations in the Epidermal Growth Factor Receptor Underlying Responsiveness of Non-Small-Cell Lung Cancer to Gefitinib

New England Journal of Medicine

Volumn 350, Issue 21, 2004, Pages 2129-2139

  Lynch, Thomas J ^a,b   Bell, Daphne W ^a,b   Sordella, Raffaella ^a   Gurubhagavatula, Sarada ^a,c   Okimoto, Ross A ^a   Brannigan, Brian W ^a   Harris, Patricia L ^a   Haserlat, Sara M ^a   Supko, Jeffrey G ^a,b   Haluska, Frank G ^a   Louis, David N ^a,b   Christiani, David C ^a,b,c   Settleman, Jeff ^a,b   Haber, Daniel A ^a,b,d  

^a HARVARD MEDICAL SCHOOL   (United States)

^b MASSACHUSETTS GENERAL HOSPITAL   (United States)

^c HARVARD SCHOOL OF PUBLIC HEALTH   (United States)

^d MASSACHUSETTS GENERAL HOSPITAL CANCER CENTER   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CARBOPLATIN; DOCETAXEL; EPIDERMAL GROWTH FACTOR RECEPTOR; GEFITINIB; GEMCITABINE; NAVELBINE; PROTEIN TYROSINE KINASE; PROTEIN TYROSINE KINASE INHIBITOR; ANTINEOPLASTIC AGENT; EPIDERMAL GROWTH FACTOR; QUINAZOLINE DERIVATIVE;

ADULT; AGED; AMINO ACID SUBSTITUTION; ARTICLE; CLINICAL ARTICLE; CORRELATION ANALYSIS; DIAGNOSTIC VALUE; DRUG MECHANISM; DRUG RESPONSE; EGFR GENE; ENZYME ACTIVITY; FEMALE; FRAMESHIFT MUTATION; GENE; GENE MUTATION; GENETIC SCREENING; HETEROZYGOSITY; HUMAN; HUMAN TISSUE; LUNG NON SMALL CELL CANCER; MALE; PRIORITY JOURNAL; PROTEIN DOMAIN; TREATMENT FAILURE; TREATMENT OUTCOME; ADENOCARCINOMA; AMINO ACID SEQUENCE; CHEMISTRY; DRUG ANTAGONISM; DRUG RESISTANCE; GENE DELETION; GENETICS; HETEROZYGOTE; LUNG TUMOR; METABOLISM; MIDDLE AGED; MOLECULAR GENETICS; MUTATION; NUCLEOTIDE SEQUENCE; PROTO ONCOGENE;

ADENOCARCINOMA; ADULT; AGED; AGED, 80 AND OVER; AMINO ACID SEQUENCE; ANTINEOPLASTIC AGENTS; BASE SEQUENCE; CARCINOMA, NON-SMALL-CELL LUNG; DNA MUTATIONAL ANALYSIS; DRUG RESISTANCE, NEOPLASM; EPIDERMAL GROWTH FACTOR; FEMALE; GENES, ERBB-1; HETEROZYGOTE; HUMANS; LUNG NEOPLASMS; MALE; MIDDLE AGED; MOLECULAR SEQUENCE DATA; MUTATION; PROTEIN-TYROSINE KINASES; QUINAZOLINES; RECEPTOR, EPIDERMAL GROWTH FACTOR; SEQUENCE DELETION;

EID: 2342471392     PISSN: 00284793     EISSN: None     Source Type: Journal    
DOI: 10.1056/NEJMoa040938     Document Type: Article

References (29)

1. Schiller JH, Harrington D, Belani CP, et al. Comparison of four chemotherapy regimens for advanced non-small-cell lung cancel. N Engl J Med 2002;346:92-8.
2. Druker BJ, Talpaz M, Resta DJ, et al. Efficacy and safety of a specific inhibitor of the BCR-ABL tyrosine kinase in chronic myeloid leukemia. N Engl J Med 2001;344:1031-7.
3. Wakeling AE, Guy SP, Woodburn JR, et al. ZD1839 (Iressa): an orally active inhibitor of epidermal growth factor signaling with potential for cancer therapy. Cancer Res 2002;62:5749-54.
4. Arteaga CL. ErbB-targeted therapeutic approaches in human cancer. Exp Cell Res 2003;284:122-30.
5. Jorissen RN, Walker F, Pouliot N, Garrett TP, Ward CW, Burgess AW. Epidermal growth factor receptor: mechanisms of activation and signaling. Exp Cell Res 2003;284:31-53.
6. Luetteke NC, Phillips HK, Qui TH, et al. The mouse waved-2 phenotype results from a point mutation in the EGF receptor tyrosine kinase. Genes Dev 1994;8:399-413.
7. Threadgill DW, Dlugosz AA, Hansen LA, et al. Targeted disruption of mouse EGF receptor: effect of genetic background on mutant phenotype. Science 1995;269:230-4.
8. Ranson M, Hammond LA, Ferry D, et al. ZD1839, a selective oral epidermal growth factor receptor-tyrosine kinase inhibitor, is well tolerated and active in patients with solid, malignant tumors: results of a phase I trial. J Clin Oncol 2002;20:2240-50.
9. Herbst RS, Maddox A-M, Rothenberg ML, et al. Selective oral epidermal growth factor receptor tyrosine kinase inhibitor ZD1839 is generally well-tolerated and has activity in non-small-cell lung cancer and other solid tumors: results of a phase I trial. J Clin Oncol 2002;20:3815-25.
10. Baselga J, Rischin D, Ranson M, et al. Phase I safety, pharmacokinetic, and pharmacodynamic trial of ZD1839, a selective oral epidermal growth factor receptor tyrosine kinase inhibitor, in patients with five selected solid tumor types. J Clin Oncol 2002;20: 4292-302.
11. Kris MG, Natale RB, Herbst RS, et al. Efficacy of gefitinib, an inhibitor of the epidermal growth factor receptor tyrosine kinase, in symptomatic patients with non-small cell lung cancer: a randomized trial. JAMA 2003;290:2149-58.
12. Fukuoka M, Yano S, Giaccone G, et al. Multi-institutional randomized phase II trial of gefitinib for previously treated patients with advanced non-small-cell lung cancer. J Clin Oncol 2003;21:2237-46.
13. Giaccone G, Herbst RS, Manegold C, et al. Gefitinib in combination with gemcitabine and cisplatin in advanced non-small-cell lung cancer: a phase III trial - INTACT 1. J Clin Oncol 2004;22:777-84.
14. Herbst RS, Giaccone G, Schiller JH, et al. Gefitinib in combination with paclitaxel and carboplatin in advanced non-small-cell lung cancer: a phase III trial - INTACT 2. J Clin Oncol 2004;22:785-94.
15. Frederick L, Wang X-Y, Eley G, James CD. Diversity and frequency of epidermal growth factor receptor mutations in human glioblastomas. Cancer Res 2000;60:1383-7.
16. Rich JN, Reardon DA, Peery T, et al. Phase II trial of gefitinib in recurrent glioblastoma. J Clin Oncol 2004;22:133-42.
17. Cohen MH, Williams GA, Sridhara R, et al. United States Food and Drug Administration drug approval summary: gefitinib (ZD1839: Iressa): tablets. Clin Cancer Res 2004;10:1212-8.
18. Therasse P, Arbuck SG, Eisenhauer EA, et al. New guidelines to evaluate the response to treatment in solid tumors. J Natl Cancer Inst 2000;92:205-16.
19. Fitch KR, McGowan KA, van Raamsdonk CD, et al. Genetics of dark skin in mice. Genes Dev 2003;17:214-28.
20. Nielsen UB, Cardone MH, Sinskey AJ, MacBeath G, Sorgez PK. Profiling receptor tyrosine kinase activation by using Ab microarrays. Proc Natl Acad Sci U S A 2003; 100:9330-5.
21. Albanell J, Rojo F, Averbuch S, et al. Pharmacodynamic studies of the epidermal growth factor receptor inhibitor ZD1839 in skin from cancer patients: histopathologic and molecular consequences of receptor inhibition. J Clin Oncol 2002;20:110-24.
22. Stamos J, Sliwkowski MX, Eigenbrot C. Structure of the epidermal growth factor receptor kinase domain alone and in complex with a 4-anilinoquinazoline inhibitor. J Biol Chem 2002;277:46265-72.
23. Daley GQ, Van Etten RA, Baltimore D. Induction of chronic myelogenous leukemia in mice by the P210bcr/abl gene of the Philadelphia chromosome. Science 1990; 247:824-30.
24. Pegram MD, Konecny G, Slamon DJ. The molecular and cellular biology of HER2/neu gene amplification/overexpression and the clinical development of herceptin (trastuzumab) therapy for breast cancer. Cancer Treat Res 2000;103:57-75.
25. Heinrich MC, Corless CL, Demetri GD, et al. Kinase mutations and imatinib response in patients with metastatic gastrointestinal stromal tumor. J Clin Oncol 2003;21:4342-9.
26. Davies H, Bignell GR, Cox C, et al. Mutations of the BRAF gene in human cancer. Nature 2002;417:949-54.
27. Bardelli A, Parsons DW, Silliman N, et al. Mutational analysis of the tyrosine kinome in colorectal cancers. Science 2003;300: 949.
28. Li B, Chang CM, Yuan M, McKenna WG, Shu HK. Resistance to small molecule inhibitors of epidermal growth factor receptor in malignant gliomas. Cancer Res 2003; 63:7443-50.
29. Paez JG, Jänne PA, Lee JC, et al. EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy. Science 10.1126/science.1099314 (2004).