Mechanisms of resistance to EGFR tyrosine kinase inhibitors gefitinib/erlotinib and to ALK inhibitor crizotinib

被引：53

作者：

Tartarone, Alfredo ^{[1
]}

Lazzari, Chiara ^{[4
]}

Lerose, Rosa ^{[2
]}

Conteduca, Vincenza ^{[1
]}

Improta, Giuseppina ^{[3
]}

Zupa, Angela ^{[3
]}

Bulotta, Alessandra ^{[4
]}

Aieta, Michele ^{[1
]}

Gregorc, Vanesa ^{[4
]}

机构：

[1] IRCCS, Ctr Riferimento Oncol Basilicata, Div Med Oncol, I-85028 Rionero In Vulture, PZ, Italy

[2] IRCCS, Ctr Riferimento Oncol Basilicata, Hosp Pharm, I-85028 Rionero In Vulture, PZ, Italy

[3] IRCCS, Ctr Riferimento Oncol Basilicata, Lab Clin Res, I-85028 Rionero In Vulture, PZ, Italy

[4] Ist Sci San Raffaele, Dept Oncol, I-20132 Milan, Italy

来源：

LUNG CANCER | 2013年 / 81卷 / 03期

关键词：

Non small cell lung cancer; Epidermal growth factor receptor; ALK translocation; Primary and acquired resistance to EGFR-TKIs; Resistance to crizotinib; Targeted therapy; CELL LUNG-CANCER; GROWTH-FACTOR RECEPTOR; PHASE-III TRIAL; ACQUIRED-RESISTANCE; NUCLEAR TRANSLOCATION; GEFITINIB RESISTANCE; TARGETED THERAPY; ERLOTINIB; MUTATIONS; CHEMOTHERAPY;

D O I：

10.1016/j.lungcan.2013.05.020

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

摘要：

The discovery of several molecular alterations that underlie non-small cell lung cancer (NSCLC) pathogenesis has led to the development of targeted therapies. In particular, gefitinib and erlotinib have become the standard of care in patients harboring epidermal growth factor receptor mutations, while crizotinib showed an impressive efficacy in patients with ALK-positive NSCLC. Nevertheless, the occurrence of clinical resistance limits the long term results of these novel agents. The identification of the molecular mechanisms responsible for acquired resistance to targeted therapy is crucial in order to pursue the creation of rational strategies to overcome resistance. In the current review, we will focus on the acquired resistance mechanisms to EGFR-TKIs and crizotinib and the therapeutic strategies currently under study to overcome resistance. (C) 2013 Elsevier Ireland Ltd. All rights reserved.

引用

页码：328 / 336

页数：9

共 107 条

[1]

[Anonymous], FREQ ASK QUEST BREAK

[2]

[Anonymous], J CLIN ONCOL S

[3] Rebiopsy of Lung Cancer Patients with Acquired Resistance to EGFR Inhibitors and Enhanced Detection of the T790M Mutation Using a Locked Nucleic Acid-Based Assay [J].

Arcila, Maria E. ;

Oxnard, Geoffrey R. ;

Nafa, Khedoudja ;

Riely, Gregory J. ;

Solomon, Stephen B. ;

Zakowski, Maureen F. ;

Kris, Mark G. ;

Pao, William ;

Miller, Vincent A. ;

Ladanyi, Marc .

CLINICAL CANCER RESEARCH, 2011, 17 (05) :1169-1180

[4]

Atagi S, 2011, J THORAC ONCOL, V6, pS360

[5] FAS and NF-κB signalling modulate dependence of lung cancers on mutant EGFR [J].

Bivona, Trever G. ;

Hieronymus, Haley ;

Parker, Joel ;

Chang, Kenneth ;

Taron, Miquel ;

Rosell, Rafael ;

Moonsamy, Philicia ;

Dahlman, Kimberly ;

Miller, Vincent A. ;

Costa, Carlota ;

Hannon, Gregory ;

Sawyers, Charles L. .

NATURE, 2011, 471 (7339) :523-526

[6] Activity and safety of crizotinib in patients with ALK-positive non-small-cell lung cancer: updated results from a phase 1 study [J].

Camidge, D. Ross ;

Bang, Yung-Jue ;

Kwak, Eunice L. ;

Iafrate, A. John ;

Varella-Garcia, Marileila ;

Fox, Stephen B. ;

Riely, Gregory J. ;

Solomon, Benjamin ;

Ou, Sai-Hong I. ;

Kim, Dong-Wan ;

Salgia, Ravi ;

Fidias, Panagiotis ;

Engelman, Jeffrey A. ;

Gandhi, Leena ;

Jaenne, Pasi A. ;

Costa, Daniel B. ;

Shapiro, Geoffrey I. ;

LoRusso, Patricia ;

Ruffner, Katherine ;

Stephenson, Patricia ;

Tang, Yiyun ;

Wilner, Keith ;

Clark, Jeffrey W. ;

Shaw, Alice T. .

LANCET ONCOLOGY, 2012, 13 (10) :1011-1019

[7]

Camidge DR, 2011, J THORAC ONCOL, V3, P411

[8] Kinetic analysis of epidermal growth factor receptor somatic mutant proteins shows increased sensitivity to the epidermal growth factor receptor tyrosine kinase inhibitor, erlotinib [J].

Carey, Kendall D. ;

Garton, Andrew J. ;

Romero, Maria S. ;

Kahler, Jennifer ;

Thomson, Stuart ;

Ross, Sarajane ;

Park, Frances ;

Haley, John D. ;

Gibson, Neil ;

Sliwkowski, Mark X. .

CANCER RESEARCH, 2006, 66 (16) :8163-8171

[9] Disease Flare after Tyrosine Kinase Inhibitor Discontinuation in Patients with EGFR-Mutant Lung Cancer and Acquired Resistance to Erlotinib or Gefitinib: Implications for Clinical Trial Design [J].

Chaft, Jamie E. ;

Oxnard, Geoffrey R. ;

Sima, Camelia S. ;

Kris, Mark G. ;

Miller, Vincent A. ;

Riely, Gregory J. .

CLINICAL CANCER RESEARCH, 2011, 17 (19) :6298-6303

[10] Mechanisms of acquired resistance to tyrosine kinase inhibitors [J].

Chen, Yi-fan ;

Fu, Li-wu .

ACTA PHARMACEUTICA SINICA B, 2011, 1 (04) :197-207

← 1 2 3 4 5 6 7 8 9 10 →