Epidermal growth factor receptor polymorphism development on pharmacodynamics of tyrosine kinase inhibitor

Abstract

Abstract: At present, epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor is extensively applicated in treatment of non small cell lung cancer(NSCLC). We review EGFR polymorphisms related to the pharmacodynamics of tyrosine kinase inhibitor(TKI), and the influence of pharmacodynamics of gefitinib, a typical drug of TKI. We conclude that the EGFR polymorphisms play an important role on the pharmacodynamics of TKI.

Key words: EGFR polymorphisms, NSCLC, Tyrosine kinase inhibitor, Gefitinib

CLC Number:

R968

WANG Li-ping, WANG Guo, ZHOU Hong-hao. Epidermal growth factor receptor polymorphism development on pharmacodynamics of tyrosine kinase inhibitor[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2010, 15(8): 938-944.

References

[1] 宋启斌,胡胜.EGFR与非小细胞肺癌[J].中国肿瘤,2007,16(17):910-914.
[2] Tokumo M, Toyooka S, Kiura K,et al.The relationship between epidermal growth factor receptor mutations and clinicopathologic features in non-small cell lung cancers[J]. Clin Cancer Res,2005 ,11(3):1167-1173.
[3] Soung YH , Lee JW , Kim SY,et al. Mutational analysis of EGFR and K-RAS genesin lung adenocarcinomas [J].Virchows Arch ,2005, 446(5): 483-488.
[4] Sasaki H, Endo K, Konishi A,et al.EGFR mutation status in Japanese lung cancer patients:genotyping analysis using light cycler [J]. Clin Cancer Res, 2005,11(8):2924-2930.
[5] Chou TY, Chiu CH, Li LH,et al. Mutation in the tyrosine kinase Domain of epidermal growth factor receptor is a predictive and prognostic factor for gefitinib treatment in patientswith non-small cell lung cancer[J]. Clin Cancer Res, 2005,11 (10):3750-3758.
[6] Sonobe M , Manabe T, Wada H,et al. Mutations in the epidermal growth factor receptor gene are linked to smoking-independent, lung adenocarcinoma[J]. Brit J Cancer,2005, 93(3): 355-363.
[7] 王敬萍,郑华,李宝兰,等. EGFR基因突变与肺癌EGFR-TKI获得性耐药的研究进展[J]. 实用临床医药杂志,2008,12(5):12-19.
[8] Pao W, Miller V, Zakowski M,et al. EGF receptor gene mutations are common in lung cancers from “never smokers” and are associated with sensitivity of tumors to gefitinib and erlotinib[J]. Proc Natl Acad Sci USA, 2005,101(36): 13306-13311.
[9] 李哲,袁守军. 表皮生长因子受体酪氨酸激酶抑制剂在肿瘤治疗中的应用[J].中国临床药理学与治疗学,2004, 9(4):361-364.
[10] Lynch TJ, Bell DW, Sordella R,et al. Activating mutations in the epidermal growth factor recep tor underlying responsiveness of non-small-cell lung cancer to gefitinib[J]. N Engl J Med,2004,350(21): 2129-2139.
[11] 吴健虹,谢秋玲,陈小佳, 等.表皮生长因子受体EGFR及其信号传导[J].生命科学,2006,18(2):116-127.
[12] Marchetti A, Martella C, Felicioni L,et al. EGFR mutations in non-small-cell lung cancer: analysis of a large series of cases and development of a rapid and sensitive method for diagnostic screening with potential implications on pharmacologic treatment[J]. J Clin Oncol, 2005,23(4):857-866.
[13] Tokumo M, Toyooka S, Kiura K,et al . The relationship between epidermal growth factor receptor mutations and clinicopathologic features in non-small cell lung cancers[J]. Clin Cancer Res,2005, 11(3):1167-1173.
[14] Han SW, Kim TY, Hwang PG,et al. Predictive and prognostic impact of epidermal growth factor receptor mutation in non-small-cell lung cancer patients treated with gefitinib[J]. Clin Cancer Res, 2005(23):2493-2502.
[15] Kim SK, Jeong JY, Kim YC,et al. Predictors of the response to gefitinib in refractory non-small cell lung cancer[J]. Clin Cancer Res,2005,23(11):2244-2251.
[16] Cappuzzo F , Hirsch FR , Rossi E,et al. Epidermal growth factor receptor gene and protein and gefi tinib sensitivity in non-small-cell lung cancer[J]. J Natl Cancer J Inst, 2005, 97(9):643-656.
[17] Cortes-Funes H, Gomez C, Rosell R,et al. Epidermal growth factor receptor activating mutations in Spanish gefitinib-treated non-small-cell lung cancer patients[J]. Ann Oncol, 2005,16(7):1081-1086.
[18] David AE, Bruce EJ, Lukas CA,et al. Mutations in the epidermal growth factor receptor and in kras are predictive and prognostic indicators in patients with non-small-cell lung cancer treated with chemotherapy alone and in combination with erlotinib[J]. Clin Cancer Res, 2005,23(25):5900-5910.
[19] Takano T, Ohe Y, Sakamoto H,et al. Epidermal growth factor receptor gene mutations and increased copy numbers predict gefitinib sensitivity in patients with recurrent non-small-cell lung cancer[J]. J Clin Oncol, 2005,23(28):6813-6816.
[20] Tsao MS, Sakurada A, Cutz JC,et al. Erlotinib in lung cancer-molecular and clinical predictors of outcome[J]. N Engl J Med,2005,353(2):133-146.
[21] Taron M, Ichinose Y, Rosell R,et al. Activating mutations in the tyrosine kinase domain of the epidermal growth factor receptorareassociatedwith improved survival in gefitinib-treated chemorefractory lung adenocarcinomas[J]. Clin Cancer Res,2005,11(16):5878-5886.
[22] Shigematsu H, Li L, Takao T,et al. Clinical and biological features associated with epidermal growth factor receptor gene mutations in lung cancers[J]. J Natl Cancer I, 2005, 97(5):339-347.
[23] Kosaka T, Yatabe Y, Endoh Y,et al. Mutations of the epidermal growth factor receptor gene in lung cancer:biological and clinical implications[J]. Cancer Res, 2004,64(24):8919-8923.
[24] Paez JG, Pasi AJ, Lee JC,et al. EGFR mutations in lung cancer:correlation with clinical response to gefitinib therapy[J]. Science, 2004,304(5676):1497-1450.
[25] Sreenath VS, Daphne WB, Settleman JH, et al. Epidermal growth factor receptor mutations in lung cancer[J].Nature, 2007,7(3):169-183.
[26] Blackledge G,Verbuch S.Gefitinib ('Iressa', ZD1839) and new epidermal growth factor receptor inhibitors[J]. Brit J Cancer, 2004, 90(3):566-572.
[27] Cappuzzo F, Finocchiaro G, Metro G,et al.Clinical experience with gefitinib: An update[J]. Hematology,2006 ,58(1):31-45.
[28] Krause DS,Richard A, Etten V, et al. Tyrosine kinases as targets for cancer therapy[J]. N Engl J Med,2005,353(2):172-187.
[29] Shawver LK, Slamon D, Ullrich A.Smart drugs:tyrosine kinase inhibitors in cancer therapy[J]. Cancer Cell, 2002,1(2):117-124.
[30] 何伍,凌霄. 小分子EGFR酪氨酸激酶抑制剂研究进展[J].中国药学杂志, 2007,42:1685-1693.
[31] Kantarjian HM, Talpaz M, Giles F, et al.New insights into the pathophysiology of chronic myeloid leukemia and imatinib resistance[J]. Ann Intern Med, 2006,145(2):913-923.
[32] Faivre S,Demetri G,Sargent M,et al.Molecular basis for sunitinib efficacy and future clinical development[J]. Nat R Drug Disov, 2007,6(9):734-745.
[33] Pytel D, Sliwinski T, Poplawski T,et al.Tyrosine kinase blockers: new hope for successful cancer therapy[J]. Anti Cancer Agents Med Chem, 2009,9(1): 66-76.
[34] Geyer CE, Forster J, Lindquist D,et al.Lapatinib plus Capecitabine for HER2-positive advanced breast cancer[J]. N Engl J Med,2006,355(26):2733-2743.
[35] Balak MN, Gong Y,Riely GJ ,et al. Novel D761Y and common secondary T790M mutations in epidermal growth factor receptor-mutant lung adenocarcinomas with acquired resistance to kinase inhibitors[J]. Clin Cancer Res, 2006, 12(21):6494-6501.
[36] Jiang H. Overview of gefitinib in non-small cell lung cancer: an asian perspective[J] , Jap J Clin Oncol,2009,39(3):137-150.
[37] Nadia GH, Bryant I,Miguel NR,et al.Oncogenic activity of epidermal growth factor receptor kinase mutant alleles is enhanced by the T790M drug resistance mutation[J]. Cancer Res, 2007,67(15):7319-7326.