932
Views
22
CrossRef citations to date
0
Altmetric
Review

BRAF and MEK inhibition for the treatment of advanced BRAF mutant melanoma

, , &

Bibliography

  • Khattak M, Fisher R, Turajlic S, Larkin J. Targeted therapy and immunotherapy in advanced melanoma: an evolving paradigm. Ther Adv Med Oncol 2013;5:105-18
  • Chapman PB, Hauschild A, Robert C, et al. Improved survival with Vemurafenib in Melanoma with BRAF V600E Mutation. N Engl J Med 2011;364(26):2507-16
  • Hocker TL, Singh MK, Tsao H, et al. Melanoma genetics and therapeutic approaches in the 21st century: moving from the benchside to the bedside. J Invest Dermatol 2008;128:2575-95
  • McCubrey JA, Steelman LS, Chappell WH, et al. Roles of the RAF/MEK/ERK pathway in cell growth, malignant transformation and drug resistance. Biochim Biophys Acta 2007;1773(8):1263-84
  • Santarpia L, Lippman SM, El-Naggar AK, et al. Targeting the MAPK-RAS-RAF signalling pathway in cancer therapy. Expert Opin Ther Targets 2012;16:103-19
  • Spagnolo F, Ghiorzo P, Queirolo P, et al. Overcoming resistance to BRAF inhibition in BRAF-mutated metastatic melanoma. Oncotarget 2014;5:10206-21
  • Long GV, Menzies AM, Nagrial AM, et al. Prognostic and clinicopathologic associations of oncogenic BRAF in metastatic melanoma. J Clin Oncol 2011;29:1239-46
  • McArthur GA, Chapman PB, Robert C, et al. Safety and efficacy of vemurafenib in BRAF (V600E) and BRAF (V600K) mutation-positive melanoma (BRIM-3): extended follow-up of a phase 3 randomised open label study. Lancet Oncol 2014;15(3):323-32
  • Hauschild A, Grob JJ, Demidov LV, et al. Dabrafenib in BRAF- mutated metastatic melanoma: a multicentre, open-label, phase 3 randomised controlled trial. Lancet 2012;380(9839):358-65
  • Flaherty KT, Robert C, Hersey P, et al. Improved survival with MEK inhibition in BRAF-mutated melanoma. N Engl J Med 2012;367:107-14
  • Flaherty KT, Puzanov I, Kim KB, et al. Inhibition of mutated, activated BRAF in metastatic melanoma. N Engl J Med 2010;363(9):809-19
  • Das Thakur M, Salangasang F, Landman AS, et al. Modelling vemurafenib resistance in melanoma reveals a strategy to forestall drug resistance. Nature 2013;494:251-5
  • Corcoran RB, Settleman J, Engelman JA. Potential therapeutic strategies to overcome acquired resistance to BRAF or MEK inhibitors in BRAF mutant cancers. Oncotarget 2011;2:336-46
  • Flaherty KT, Infante JR, Daud A, et al. Combined BRAF and MEK Inhibition in Melanoma with BRAF V600 Mutations. N Engl J Med 2012;367(18):1694-703
  • Poulikakos PI, Persaud Y, Janakiraman M, et al. RAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF (V600E). Nature 2011;480:387-90
  • Paraiso KH, Fedorenko IV, Cantini LP, et al. Recovery of phosphor-ERK activity allows melanoma cells to escape from BRAF inhibitor therapy. Br J Cancer 2010;102:1724-30
  • McCubrey JA, Steelman LS, Chappell WH, et al. Roles of the RAF/MEK/ERK pathway in cell growth, malignant transformation and drug resistance. Biochim Biophys Acta 2007;1773(8):1263-84
  • Lito P, Rosen N, Solit DB. Tumour adaptation and resistance to RAF inhibitors. Nat Med 2013;19(11):1401-9
  • McCubrey JA, Steelman LS. Chappell, et al. Mutations and deregulation of Ras/Raf/MEK/ERK and P13K/PTEN/Akt/mTOR cascades. Oncotarget 2012;3:954-87
  • Davies H, Bignell GR, Cox C, et al. Mutations of the BRAF gene in human cancer. Nature 2002;417:949-54
  • Beeram M, Patnaik A, Rowinsky EK, et al. Raf: a strategic target for therapeutic development against cancer. J Clin Oncol 2005;23:6771-90
  • Ohren JF, Chen H, Pavlovsky A, et al. Structure of human MAP kinase kinase 1 (MEK1) and MEK2 describe novel noncompetetive kinase inbhibition. Nat Struct Mol Biol 2004;11:1192-7
  • Garnett MJ, Marais R. Guilty as charged: BRAF is a human oncogene. Cancer Cell 2004;6(4):313-19
  • Wan PT, Garnett MJ, Roe SM, et al. Mechanism of activation of the RAF-ERK signalling pathway by oncogenic mutations of B-RAF. Cell 2004;116:855-67
  • Sebolt-Leopold JS, Herrera R. Targeting the mitogen-activated protein kinase cascade to treat cancer. Nat Rev Can 2004;4:937-47
  • Bollag G, Tsai J, Zhang J, et al. Vemurafenib: the first drug approved for BRAF-mutant cancer. Nat Rev Drug Discov 2012;11:873-86
  • Bollag G, Hirth P, Tsai J, et al. Clinical efficacy of a RAF inhibitor needs broad target blockade in mutant-melanoma. Nature 2010;467:596-9
  • Yang H, Higgins B, Kolinsky K, et al. RG7204 (PLX4032), a selective BRAF V600E inhibitor, displays potent antitumor activity in preclinical melanoma models. Cancer Res 2010;70:5518
  • Hatzivassiliou G, Song K, Yen I, et al. Raf inhibitors prime wild type RAF to activate the MAPK pathway and enhance growth. Nature 2010;464:431-5
  • Girotti MR, Lopes F, Preece N, et al. Paradox-breaking RAF inhibitors that also target SRC are effective in drug resistant BRAF mutant melanoma. Cancer Cell 2015;27:85-96
  • Su F, Viros A, Milagre C, et al. RAS mutations in cutaneous squamous-cell carcinomas in patients treated with BRAF inhibitors. N Engl J Med 2012;366:207-15
  • Hauschild A, Grob JJ, Demidov LV, et al. An update on BREAK-3, a phase III, randomized trial: Dabrafenib (DAB) versus dacarbazine (DTIC) in patients with BRAF V600E-positive mutation metastatic melanoma (MM). J Clin Oncol 2013(Suppl l):abstract 9013
  • Nazarian R, Shi H, Wang Q, et al. Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation. Nature 2010;468:973-7
  • Maertens O, Johnson B, Hollstein P, et al. Elucidating distinct roles for NF1 in melanomagenesis. Cancer Discov 2013;3:338-49
  • Van Allen EM, Wagle N, Sucker A, et al. The genetic landscape of clinical resistance to RAF inhibition in metastatic melanoma. Cancer Discov 2014;4:94-109
  • Girotti M, Pedersen M, Sanchez-Laorden B, et al. Inhibiting EGF receptor or SRC family kinase signaling overcomes BRAF inhibitor resistance in melanoma. Cancer Discov 2013;3:158-67
  • Montagut C, Sharma SV, Shioda T, et al. Elevated CRAF as a potential mechanism of acquired resistance to BRAF inhibition in melanoma. Cancer Res 2008;68:4853-61
  • Wagle N, Emery C, Berger MF. Dissecting therapeutic resistance to RAF inhibition in melanoma by tumour genomic profiling. J Clin Oncol 2011;29:3085-96
  • Johannessen CM, Boehm JS, Kim SY. COT drives resistance to RAF inhibition through MAP kinase pathway reactivation. Nature 2010;468:968-72
  • Xing F, Persaud Y, Pratilas CA, et al. Concurrent loss of PTEN and RB1 tumor suppressors attenuates RAF dependence in melanomas harbouring (V600E)BRAF. 2012;31:446-57
  • Available from: http://www.accessdata.fda.gov/scripts/cder/drugsatfda/index.cfm?fuseaction=Search.DrugDetails
  • Available from: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_Public_assessment_report/human/002409/WC500124400.pdf
  • Tsai J, Lee JT, et al. Discovery of a selective inhibitor of oncogenic B-raf kinase with potent antimelanoma activity. Proc Natl Acad Sci USA 2008;105(8):3041-6
  • Sosman JA, Kim JB, Schuchter L, et al. Survival in BRAF V600-mutant advanced melanoma treated with vemurafenib. N Engl J Med 2012;366(8):707-14
  • Dummer R, Goldinger SM, Turtscbhi CP, et al. Vemurafenib in patients with BRAF(V600) mutation-positive melanoma with symptomatic brain metastases: final results of an open-label pilot study. Eur J Cancer 2014;50(3):611-12
  • Available from http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/202806s002lbl.pdf
  • Available from: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/002604/WC500149671.pdf
  • Falchook GS, Long GV, Kurzrock R, et al. Dabrafenib in patients with melanoma, untreated brain metastases and other solid tumours: a phase 1 dose escalation trial. Lancet 2012;379(9829):1893-901
  • Ascierto PA, Minor D, Ribas A, et al. Phase II trial (BREAK-2) of the BRAF Inhibitor Dabrafenib (GSK2118436) in patients with metastatic melanoma. J Clin Oncol 2013;31(26):3205-11
  • Long GV, Trefzer U, Davies MA, et al. Dabrafenib in patients with Val600Glu or Val600Lys BRAF-mutant melanoma metastatic to the brain (BREAK-MB): a multicentre, open-label, phase 2 trial. Lancet Oncol 2012;13:1087-95
  • Available from: http://www.accessdata.fda.gov/scripts/cder/drugsatfda/index.cfm?fuseaction=Search.DrugDetails
  • Falchook GS, Lewis KD, Infante JR, et al. Activity of the oral MEK inhibitor trametinib in patients with advanced melanoma: a phase 1 dose escalation trial. Lancet Oncol 2012;13(8):782-9
  • Kim KB, Kefford R, Pavlick AC, et al. Phase 2 study of the MEK1/MEK2 inhibitor trametinib in patients with metastatic BRAF-mutant cutaneous melanoma previously treated with or without a BRAF inhibitor. J Clin Oncol 2013;31(4):482-9
  • Akinleye A, Furgan M, Mukhi N, et al. MEK and the inhibitors: from bench to bedside. J Hematol Oncol 2013;6:27
  • Rosen L, LoRusso P, Wee Ma W, et al. A first-in-human phase 1 study to evaluate the MEK 1/2 inhibitor GDC-0973 administered daily in patients with advanced solid tumours. Cancer Research 2011;71(8 Suppl):abstract 4716
  • Available from: http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/202806s002lbl.pdf
  • Long GV, Stroyakovskiy D, Gogas H, et al. Combined BRAF and MEK inhibition versus BRAF inhibition alone in melanoma. N Engl J Med 2014;13:1877-88
  • Robert C, Karaszewska B, Schachter J, et al. Improved survival in melanoma with combined dabrafenib and trametinib. N Engl J Med 2014. [ Epub ahead of print]
  • Ribas A, Gonzalez R, Pavlick A, et al. Combination of vemurafenib and cobimetinib in patients with advanced BRAFV600 –mutated melanoma: a phase 1b study. Lancet Onc 2014;15:954-65
  • Larkin J, Ascierto PA, Dreno B, et al. Combined Vemurafenib and Cobimetinib in BRAF-Mutated Melanoma. N Engl J Med 2014; Epub ahead of print
  • Moriceau G, Hugo W, Hong A, et al. Tunable-combinatorial mechanisms of acquired resistance limit the efficacy of BRAF/MEK cotargeting but result in melanoma drug addiction. Cancer Cell 2015;27:1-17
  • Antonia SJ, Larkin J, Ascierto PA. Immuno-oncology Combinations: A Review of Clinical Experience and Future Prospects. Clin Cancer Res 2014;20:6258-68
  • Ribas A, Hodi FS, Callahan M, et al. Hepatotoxicity with combination of vemurafenib and ipilimumab. N Engl J Med 2013;368:1365-6

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.