The MEK inhibitor trametinib for the treatment of advanced melanoma

Bibliography

• Korn EL, Liu PY, Lee SJ, et al. Meta-analysis of phase II cooperative group trials in metastatic stage IV melanoma to determine progression-free and overall survival benchmarks for future phase II trials. J Clin Oncol 2008;26(4):527-34
   PubMed Web of Science ®Google Scholar
• Davies H, Bignell GR, Cox C, et al. Mutations of the BRAF gene in human cancer. Nature 2002;417(6892):949-54
   PubMed Web of Science ®Google Scholar
• Lovly CM, Dahlman KB, Fohn LE, et al. Routine multiplex mutational profiling of melanomas enables enrollment in genotype-driven therapeutic trials. PLoS One 2012;7(4):e35309
   PubMed Web of Science ®Google Scholar
• Curtin JA, Fridlyand J, Kageshita T, et al. Distinct sets of genetic alterations in melanoma. N Engl J Med 2005;353(20):2135-47
   PubMed Web of Science ®Google Scholar
• Fedorenko IV, Gibney GT, Smalley KS. NRAS mutant melanoma: biological behavior and future strategies for therapeutic management. Oncogene 2013;32(25):3009-18
   PubMed Web of Science ®Google Scholar
• Curtin JA, Busam K, Pinkel D, et al. Somatic activation of KIT in distinct subtypes of melanoma. J Clin Oncol 2006;24(26):4340-6
   PubMed Web of Science ®Google Scholar
• Carvajal RD, Antonescu CR, Wolchok JD, et al. KIT as a therapeutic target in metastatic melanoma. JAMA 2011;305(22):2327-34
   PubMed Web of Science ®Google Scholar
• Van Raamsdonk CD, Bezrookove V, Green G, et al. Frequent somatic mutations of GNAQ in uveal melanoma and blue naevi. Nature 2009;457(7229):599-602
   PubMed Web of Science ®Google Scholar
• Van Raamsdonk CD, Griewank KG, Crosby MB, et al. Mutations in GNA11 in uveal melanoma. N Engl J Med 2010;363(23):2191-9
   PubMed Web of Science ®Google Scholar
• 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
   PubMed Web of Science ®Google Scholar
• 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
   PubMed Web of Science ®Google Scholar
• Flaherty KT, Robert C, Hersey P, et al. Improved survival with MEK inhibition in BRAF-mutated melanoma. N Engl J Med 2012;367(2):107-14
   PubMed Web of Science ®Google Scholar
• 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
   PubMed Web of Science ®Google Scholar
• Long GV, Stroyakovsky DL, Gogas H, et al. COMBI-d: a randomized, double-blinded, Phase III study comparing the combination of dabrafenib and trametinib to dabrafenib and trametinib placebo as first-line therapy in patients (pts) with unresectable or metastatic BRAFV600E/Kmutation-positive cutaneous melanoma. J Clin Oncol 2014;32(15 Suppl):9011
   Google Scholar
• Johnson DB, Flaherty KT, Weber JS, et al. Combined BRAF (Dabrafenib) and MEK inhibition (trametinib) in patients with brafv600-mutant melanoma progressing on single-agent braf inhibitor. J. Clin Oncol; In press
   Google Scholar
• Hodis E, Watson IR, Kryukov GV, et al. A landscape of driver mutations in melanoma. Cell 2012;150(2):251-63
   PubMed Web of Science ®Google Scholar
• Hutchinson KE, Lipson D, Stephens PJ, et al. BRAF fusions define a distinct molecular subset of melanomas with potential sensitivity to MEK inhibition. Clin Cancer Res 2013;19(24):6696-702
   PubMed Web of Science ®Google Scholar
• Nissan MH, Pratilas CA, Jones AM, et al. Loss of NF1 in cutaneous melanoma is associated with ras activation and mek dependence. Cancer Res 2014;74(8):2340-50
   PubMed Web of Science ®Google Scholar
• Sosman JA, Kittaneh M, Lolkema MPJ, et al. A phase 1b/2 study of LEE011 in combination with binimetinib (MEK162) in patients with NRAS-mutant melanoma: early encouraging clinical activity. J Clin Oncol 2014;32(15 Suppl):9009
   Web of Science ®Google Scholar
• US FDA. Mekinist (trametinib) tablets: prescribing information. 2013. Available from: www.accessdata.fda.gov/drugsatfda_docs/label/2013/204114s000lbl.pdf
   Google Scholar
• Kassir N, Mouksassi M, Cox DS, et al. Population pharmacokinetics (PK) of trametinib (GSK1120212), a MEK inhibitor, in subjects with cancer [abstract PII-48]. Clin Pharmacol Ther 2013;93:1 S69
   Google Scholar
• Infante JR, Patnaik A, Jones SF, et al. A phase IB study of the MEK inhibitor GSK1120212 combined with everolimus in patients with solid tumors: interim results [abstract B128]. Mol Cancer Ther 2011;10:11 Suppl
   Google Scholar
• Infante JR, Fecher LA, Falchook GS, et al. Safety, pharmacokinetic, pharmacodynamic, and efficacy data for the oral MEK inhibitor trametinib: a phase 1 dose-escalation trial. Lancet Oncol 2012;13(8):773-81
   PubMed Web of Science ®Google Scholar
• US FDA. Dabrafenib and trametinib: approved drugs. Available from: www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm381451.htm [Accessed 29 March 2014]
   Google Scholar
• US FDA. Tafinlar (dabrafenib) capsules: prescribing information. 2013. Available from: www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf [Accessed 29 March 2014]
   Google Scholar
• Yoshida T, Kakegawa J, Yamaguchi T, et al. Identification and characterization of a novel chemotype MEK inhibitor able to alter the phosphorylation state of MEK1/2. Oncotarget 2012;3(12):1533-45
   PubMedGoogle Scholar
• Gilmartin AG, Bleam MR, Groy A, et al. GSK1120212 (JTP-74057) is an inhibitor of MEK activity and activation with favorable pharmacokinetic properties for sustained in vivo pathway inhibition. Clin Cancer Res 2011;17(5):989-1000
   PubMed Web of Science ®Google Scholar
• Koch K. Fourteenth international conference of the inflammation research association, October 15-19; Cambridge, MD, USA. Arthritis Rheum 2006;54:abstract SA40
   Google Scholar
• Hoeflich KP, Merchant M, Orr C, et al. Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition. Cancer Res 2012;72(1):210-19
   PubMed Web of Science ®Google Scholar
• Stones CJ, Kim JE, Joseph WR, et al. Comparison of responses of human melanoma cell lines to MEK and BRAF inhibitors. Front Genet 2013;4:66
   PubMedGoogle Scholar
• 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
   PubMed Web of Science ®Google Scholar
• Borthakur G, Foran J, Kadia T, et al. GSK1120212, a MEK1/MEK2 inhibitor demonstrates acceptable tolerability and preliminary activity in a dose rising trial in subjects with AML and other hematologic malignancies. Blood 2010;1116:3231
   Google Scholar
• Kim KB, Kefford R, Pavlick AC, et al. Phase II 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
   PubMed Web of Science ®Google Scholar
• 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(7326):973-7
   PubMed Web of Science ®Google Scholar
• Poulikakos PI, Persaud Y, Janakiraman M, et al. RAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF(V600E). Nature 2011;480(7377):387-90
   PubMed Web of Science ®Google Scholar
• Wagle N, Berger MF, Davis MJ, et al. High-throughput detection of actionable genomic alterations in clinical tumor samples by targeted, massively parallel sequencing. Cancer Discov 2012;2(1):82-93
   PubMed Web of Science ®Google Scholar
• Shi H, Moriceau G, Kong X, et al. Melanoma whole-exome sequencing identifies (V600E)B-RAF amplification-mediated acquired B-RAF inhibitor resistance. Nat Commun 2012;3:724
   PubMed Web of Science ®Google Scholar
• Shi H, Hugo W, Kong X, et al. Acquired resistance and clonal evolution in melanoma during braf inhibitor therapy. Cancer Discov 2014;4(1):80-93
   PubMed Web of Science ®Google Scholar
• 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(1):94-109
   PubMed Web of Science ®Google Scholar
• Johannessen CM, Boehm JS, Kim SY, et al. COT drives resistance to RAF inhibition through MAP kinase pathway reactivation. Nature 2010;468(7326):968-72
   PubMed Web of Science ®Google Scholar
• Emery CM, Vijayendran KG, Zipser MC, et al. MEK1 mutations confer resistance to MEK and B-RAF inhibition. Proc Natl Acad Sci USA 2009;106(48):20411-16
   PubMed Web of Science ®Google Scholar
• Shi H, Moriceau G, Kong X, et al. Preexisting MEK1 exon 3 mutations in V600E/KBRAF melanomas do not confer resistance to BRAF inhibitors. Cancer Discov 2012;2(5):414-24
   PubMed Web of Science ®Google Scholar
• 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(3):207-15
   PubMed Web of Science ®Google Scholar
• Callahan MK, Rampal R, Harding JJ, et al. Progression of RAS-mutant leukemia during RAF inhibitor treatment. N Engl J Med 2012;367:2316-21
   PubMed Web of Science ®Google Scholar
• Larkin J, Del Vecchio M, Ascierto PA, et al. Vemurafenib in patients with BRAF mutated metastatic melanoma: an open-label, multicentre, safety study. Lancet Oncol 2014;15(4):436-44
   PubMed Web of Science ®Google Scholar
• Dahlman KB, Xia J, Hutchinson K, et al. BRAF L597 mutations in melanoma are associated with sensitivity to MEK inhibitors. Cancer Discov 2012;2(9):791-7
   PubMed Web of Science ®Google Scholar
• Carvajal RD, Sosman JA, Quevedo JF, et al. Effect of selumetinib vs chemotherapy on progression-free survival in uveal melanoma: a randomized clinical trial. JAMA 2014;311(23):2397-405
   PubMed Web of Science ®Google Scholar
• Kirkwood JM, Bastholt L, Robert C, et al. Phase II, open-label, randomized trial of the MEK1/2 inhibitor selumetinib as monotherapy versus temozolomide in patients with advanced melanoma. Clin Cancer Res 2012;18(2):555-67
   PubMed Web of Science ®Google Scholar
• Ribas A, Gonzalez R, Pavlick A, et al. Combination of vemurafenib and cobimetinib in patients with advanced BRAF(V600)-mutated melanoma: a phase 1b study. Lancet Oncol 2014;15(9):954-65
   PubMed Web of Science ®Google Scholar
• Ascierto PA, Schadendorf D, Berking C, et al. MEK162 for patients with advanced melanoma harbouring NRAS or Val600 BRAF mutations: a non-randomised, open-label phase 2 study. Lancet Oncol 2013;14(3):249-56
   PubMed Web of Science ®Google Scholar
• Zimmer L, Barlesi F, Martinez-Garcia M, et al. Phase I expansion and pharmacodynamic study of the oral MEK inhibitor RO4987655 (CH4987655) in selected patients with advanced cancer with RAS-RAF mutations. Clin Cancer Res 2014;20(16):4251-61
   PubMed Web of Science ®Google Scholar
• Hatzivassiliou G, Haling JR, Chen H, et al. Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers. Nature 2013;501(7466):232-6
   PubMed Web of Science ®Google Scholar
• Ishii N, Harada N, Joseph EW, et al. Enhanced inhibition of ERK signaling by a novel allosteric MEK inhibitor, CH5126766, that suppresses feedback reactivation of RAF activity. Cancer Res 2013;73(13):4050-60
   PubMed Web of Science ®Google Scholar
• Topalian SL, Sznol M, McDermott DF, et al. Survival, durable tumor remission, and long-term safety in patients with advanced melanoma receiving nivolumab. J Clin Oncol 2014;32(10):1020-30
   PubMed Web of Science ®Google Scholar
• Topalian SL, Hodi FS, Brahmer JR, et al. Safety, activity, and immune correlates of anti-PD-1 antibody in cancer. N Engl J Med 2012;366(26):2443-54
   PubMed Web of Science ®Google Scholar
• Hamid O, Robert C, Daud A, et al. Safety and tumor responses with lambrolizumab (Anti-PD-1) in melanoma. N Engl J Med 2013;369(2):134-44
   PubMed Web of Science ®Google Scholar
• Robert C, Ribas A, Wolchok JD, et al. Anti-programmed-death-receptor-1 treatment with pembrolizumab in ipilimumab-refractory advanced melanoma: a randomised dose-comparison cohort of a phase 1 trial. Lancet 2014, pii: S0140-6736(14)60958-2. doi: 10.1016/S0140-6736(14)60958-2
   Google Scholar
• Puzanov I, Callahan MK, Linette GP, et al. Phase 1 study of the BRAF inhibitor dabrafenib (D) with or without the MEK inhibitor trametinib (T) in combination with ipilimumab (Ipi) for V600E/K mutation–positive unresectable or metastatic melanoma (MM). J Clin Oncol 2014;32(15 Suppl):2511
   Google Scholar
• Boni A, Cogdill AP, Dang P, et al. Selective BRAFV600E inhibition enhances T-cell recognition of melanoma without affecting lymphocyte function. Cancer Res 2010;70(13):5213-19
   PubMed Web of Science ®Google Scholar
• Tompers Frederick D, Piris A, Cogdill AP, et al. BRAF inhibition is associated with enhanced melanoma antigen expression and a more favorable tumor microenvironment in patients with metastatic melanoma. Clin Cancer Res 2013;19(5):1225-31
   PubMed Web of Science ®Google Scholar
• Berthon C, Driss V, Liu J, et al. In acute myeloid leukemia, B7-H1 (PD-L1) protection of blasts from cytotoxic T cells is induced by TLR ligands and interferon-gamma and can be reversed using MEK inhibitors. Cancer Immunol Immunother 2010;59(12):1839-49
   PubMed Web of Science ®Google Scholar
• Hu-Lieskovan S, Robert L, Homet Moreno B, et al. Combining targeted therapy with immunotherapy in BRAF-mutant melanoma: promise and challenges. J Clin Oncol 2014;32(21):2248-54
   PubMed Web of Science ®Google Scholar