Resistance to BRAF-targeted therapy in melanoma

被引：293

作者：

Sullivan, Ryan J. ^{[1
]}

Flaherty, Keith T. ^{[1
]}

机构：

[1] Massachusetts Gen Hosp, Ctr Canc, Ctr Melanoma, Boston, MA 02114 USA

来源：

EUROPEAN JOURNAL OF CANCER | 2013年 / 49卷 / 06期

关键词：

Melanoma; BRAF inhibitor resistance; Molecular targeted therapy; RANDOMIZED DISCONTINUATION TRIAL; INHIBITOR AZD6244 ARRY-142886; CHRONIC MYELOID-LEUKEMIA; B-RAF; PHASE-II; MULTIKINASE INHIBITOR; METASTATIC MELANOMA; OPEN-LABEL; CYCLIN D1; WILD-TYPE;

D O I：

10.1016/j.ejca.2012.11.019

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 [肿瘤学];

摘要：

BRAF mutations are identified in 40-50% of patients with melanoma. Treatment of these patients with either of two BRAF inhibitors (vemurafenib, dabrafenib) or the MEK inhibitor trametinib is associated with improved clinical benefit (response rate, progression free survival, and overall survival) compared with treatment with chemotherapy in three phase III trials. Unfortunately, most patients, including those who experience initial, profound tumour regression, have evidence of disease progression within 6-8 months after commencing therapy with one of these agents. The mechanisms of resistance are varied and include activation of alternative signalling pathways as well as reactivating the MAP kinase pathway through alternative means. This review describes relevant aspects of MAP kinase pathway signalling, summarises the clinical data with BRAF and MEK inhibitors, presents the known resistance mechanisms to BRAF inhibitor therapy, and provides some strategies for how resistance may be overcome. (C) 2012 Elsevier Ltd. All rights reserved.

引用

页码：1297 / 1304

页数：8

共 64 条

[1]

Phase I pharmacokinetic and pharmacodynamic study of the oral, small-molecule mitogen-activated protein kinase kinase 1/2 inhibitor AZD6244 (ARRY-142886) in patients with advanced cancers [J].

Adjei, Alex A. ;

Cohen, Roger B. ;

Franklin, Wilbur ;

Morris, Clive ;

Wilson, David ;

Molina, Julian R. ;

Hanson, Lorelei J. ;

Gore, Lia ;

Chow, Laura ;

Leong, Stephen ;

Maloney, Lara ;

Gordon, Gilad ;

Simmons, Heidi ;

Marlow, Allison ;

Litwiler, Kevin ;

Brown, Suzy ;

Poch, Gregory ;

Kane, Katie ;

Haney, Jerry ;

Eckhardt, S. Gail .

JOURNAL OF CLINICAL ONCOLOGY, 2008, 26 (13) :2139-2146

[2]

Phase II Trial of Temozolomide and Sorafenib in Advanced Melanoma Patients with or without Brain Metastases [J].

Amaravadi, Ravi K. ;

Schuchter, Lynn M. ;

McDermott, David F. ;

Kramer, Amy ;

Giles, Lydia ;

Gramlich, Kristi ;

Carberry, Mary ;

Troxel, Andrea B. ;

Letrero, Richard ;

Nathanson, Katherine L. ;

Atkins, Michael B. ;

O'Dwyer, Peter J. ;

Flaherty, Keith T. .

CLINICAL CANCER RESEARCH, 2009, 15 (24) :7711-7718

[3]

[Anonymous], N ENGL J MED

[4]

Ascierto PA, 2012, J CLIN ONCOL

[5]

Reversing Melanoma Cross-Resistance to BRAF and MEK Inhibitors by Co-Targeting the AKT/mTOR Pathway [J].

Atefi, Mohammad ;

von Euw, Erika ;

Attar, Narsis ;

Ng, Charles ;

Chu, Connie ;

Guo, Deliang ;

Nazarian, Ramin ;

Chmielowski, Bartosz ;

Glaspy, John A. ;

Comin-Anduix, Begonya ;

Mischel, Paul S. ;

Lo, Roger S. ;

Ribas, Antoni .

PLOS ONE, 2011, 6 (12)

[6]

The First-in-Human Study of the Hydrogen Sulfate (Hyd-Sulfate) Capsule of the MEK1/2 Inhibitor AZD6244 (ARRY-142886): A Phase I Open-Label Multicenter Trial in Patients with Advanced Cancer [J].

Banerji, Udai ;

Camidge, D. Ross ;

Verheul, Henk M. W. ;

Agarwal, Roshan ;

Sarker, Debashis ;

Kaye, Stan B. ;

Desar, Ingrid M. E. ;

Timmer-Bonte, Johanna N. H. ;

Eckhardt, S. Gail ;

Lewis, Karl D. ;

Brown, Kathryn H. ;

Cantarini, Mireille V. ;

Morris, Clive ;

George, Sarah M. A. ;

Smith, Paul D. ;

van Herpen, Carla M. L. .

CLINICAL CANCER RESEARCH, 2010, 16 (05) :1613-1623

[7]

Raf: A strategic target for therapeutic development against cancer [J].

Beeram, M ;

Patnaik, A ;

Rowinsky, EK .

JOURNAL OF CLINICAL ONCOLOGY, 2005, 23 (27) :6771-6790

[8]

Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma [J].

Bollag, Gideon ;

Hirth, Peter ;

Tsai, James ;

Zhang, Jiazhong ;

Ibrahim, Prabha N. ;

Cho, Hanna ;

Spevak, Wayne ;

Zhang, Chao ;

Zhang, Ying ;

Habets, Gaston ;

Burton, ElizabethA. ;

Wong, Bernice ;

Tsang, Garson ;

West, Brian L. ;

Powell, Ben ;

Shellooe, Rafe ;

Marimuthu, Adhirai ;

Nguyen, Hoa ;

Zhang, Kam Y. J. ;

Artis, Dean R. ;

Schlessinger, Joseph ;

Su, Fei ;

Higgins, Brian ;

Iyer, Raman ;

D'Andrea, Kurt ;

Koehler, Astrid ;

Stumm, Michael ;

Lin, Paul S. ;

Lee, Richard J. ;

Grippo, Joseph ;

Puzanov, Igor ;

Kim, Kevin B. ;

Ribas, Antoni ;

McArthur, Grant A. ;

Sosman, Jeffrey A. ;

Chapman, Paul B. ;

Flaherty, Keith T. ;

Xu, Xiaowei ;

Nathanson, Katherine L. ;

Nolop, Keith .

NATURE, 2010, 467 (7315) :596-599

[9]

Selective BRAFV600E Inhibition Enhances T-Cell Recognition of Melanoma without Affecting Lymphocyte Function [J].

Boni, Andrea ;

Cogdill, Alexandria P. ;

Dang, Ping ;

Udayakumar, Durga ;

Njauw, Ching-Ni Jenny ;

Sloss, Callum M. ;

Ferrone, Cristina R. ;

Flaherty, Keith T. ;

Lawrence, Donald P. ;

Fisher, David E. ;

Tsao, Hensin ;

Wargo, Jennifer A. .

CANCER RESEARCH, 2010, 70 (13) :5213-5219

[10]

Improved Survival with Vemurafenib in Melanoma with BRAF V600E Mutation [J].

Chapman, Paul B. ;

Hauschild, Axel ;

Robert, Caroline ;

Haanen, John B. ;

Ascierto, Paolo ;

Larkin, James ;

Dummer, Reinhard ;

Garbe, Claus ;

Testori, Alessandro ;

Maio, Michele ;

Hogg, David ;

Lorigan, Paul ;

Lebbe, Celeste ;

Jouary, Thomas ;

Schadendorf, Dirk ;

Ribas, Antoni ;

O'Day, Steven J. ;

Sosman, Jeffrey A. ;

Kirkwood, John M. ;

Eggermont, Alexander M. M. ;

Dreno, Brigitte ;

Nolop, Keith ;

Li, Jiang ;

Nelson, Betty ;

Hou, Jeannie ;

Lee, Richard J. ;

Flaherty, Keith T. ;

McArthur, Grant A. .

NEW ENGLAND JOURNAL OF MEDICINE, 2011, 364 (26) :2507-2516

← 1 2 3 4 5 6 7 →