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New RAF kinase inhibitors in cancer therapy

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  • Santarpia L, Lippman SM, El-Naggar AK. Targeting the MAPK-RAS-RAF signaling pathway in cancer therapy. Expert Opin Ther Targets 2012;16(1):103-19
  • Chang L, Karin M. Mammalian MAP kinase signalling cascades. Nature 2001;410(6824):37-40
  • 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
  • Davies H, Bignell GR, Cox C, et al. Mutations of the BRAF gene in human cancer. Nature 2002;417(6892):949-54
  • Flaherty KT, Hodi FS, Fisher DE. From genes to drugs: targeted strategies for melanoma. Nat Rev Cancer 2012;12(5):349-61
  • 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;15:323-32
  • Turajlic S, Ali Z, Yousaf N, et al. Phase I/II RAF kinase inhibitors in cancer therapy. Expert Opin Investig Drugs 2013;22(6):739-49
  • Available from: http://www.fda.gov/drugs/informationondrugs/approveddrugs/ucm354478.htm
  • 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
  • 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
  • Santarpia L, Myers JN, Sherman SI, et al. Genetic alterations in the RAS/RAF/mitogen-activated protein kinase and phosphatidylinositol 3-kinase/Akt signaling pathways in the follicular variant of papillary thyroid carcinoma. Cancer 2010;116(12):2974-83
  • Jakob JA, Bassett RL, Ng CS, et al. NRAS mutation status is an independent prognostic factor in metastatic melanoma. Cancer 2012;118(16):4014-23
  • Cros J, Sbidian E, Hans S, et al. Expression and mutational status of treatment-relevant targets and key oncogenes in 123 malignant salivary gland tumours. Ann Oncol 2013;24(10):2624-9
  • Vasko V, Ferrand M, Di Cristofaro J, et al. Specific pattern of RAS oncogene mutations in follicular thyroid tumors. J Clin Endocrinol Metab 2003;88(6):2745-52
  • Volante M, Rapa I, Gandhi M, et al. RAS mutations are the predominant molecular alteration in poorly differentiated thyroid carcinomas and bear prognostic impact. J Clin Endocrinol Metab 2009;94(12):4735-41
  • Díez D, Sánchez-Jiménez F, Ranea JA. Evolutionary expansion of the Ras switch regulatory module in eukaryotes. Nucleic Acids Res 2011;39(13):5526-37
  • Roskoski R. RAF protein-serine/threonine kinases: structure and regulation. Biochem Biophys Res Commun 2010;399(3):313-17
  • Khattak M, Fisher R, et al. Targeted therapy and immunotherapy in advanced melanoma: an evolving paradigm. Ther Adv Med Oncol 2013;5(2):105-18
  • Long GV, Menzies AM, Nagrial AM, et al. Prognostic and clinicopathologic associations of oncogenic BRAF in metastatic melanoma. J Clin Oncol 2011;29(10):1239-46
  • 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
  • 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
  • Mason CS, Springer CJ, Cooper RG, et al. Serine and tyrosine phosphorylations cooperate in Raf-1, but not B-Raf activation. EMBO J 1999;18(8):2137-48
  • Chong H, Vikis HG, Guan KL. Mechanisms of regulating the Raf kinase family. Cell Signal 2003;15(5):463-9
  • Blasco RB, Francoz S, Santamaría D, et al. C-Raf, but not B-Raf, is essential for development of K-Ras oncogene-driven non-small cell lung carcinoma. Cancer Cell 2011;19(5):652-63
  • Karreth FA, Frese KK, DeNicola GM, et al. C-Raf is required for the initiation of lung cancer by K-Ras(G12D). Cancer Discov 2011;1(2):128-36
  • Dumaz N, Hayward R, Martin J, et al. In melanoma, RAS mutations are accompanied by switching signaling from BRAF to CRAF and disrupted cyclic AMP signaling. Cancer Res 2006;66(19):9483-91
  • Rebocho AP, Marais R. ARAF acts as a scaffold to stabilize BRAF:CRAF heterodimers. Oncogene 2013;32(26):3207-12
  • Crews CM, Alessandrini A, Erikson RL. The primary structure of MEK, a protein kinase that phosphorylates the ERK gene product. Science 1992;258(5081):478-80
  • Bennouna J, Lang I, Valladares-Ayerbes M, et al. A Phase II, open-label, randomised study to assess the efficacy and safety of the MEK1/2 inhibitor AZD6244 (ARRY-142886) versus capecitabine monotherapy in patients with colorectal cancer who have failed one or two prior chemotherapeutic regimens. Invest New Drugs 2011;29(5):1021-8
  • Bodoky G, Timcheva C, Spigel DR, et al. A phase II open-label randomized study to assess the efficacy and safety of selumetinib (AZD6244 [ARRY-142886]) versus capecitabine in patients with advanced or metastatic pancreatic cancer who have failed first-line gemcitabine therapy. Invest New Drugs 2012;30(3):1216-23
  • Hainsworth JD, Cebotaru CL, Kanarev V, et al. A phase II, open-label, randomized study to assess the efficacy and safety of AZD6244 (ARRY-142886) versus pemetrexed in patients with non-small cell lung cancer who have failed one or two prior chemotherapeutic regimens. J Thorac Oncol 2010;5(10):1630-6
  • Hayes DN, Lucas AS, Tanvetyanon T, et al. Phase II efficacy and pharmacogenomic study of Selumetinib (AZD6244; ARRY-142886) in iodine-131 refractory papillary thyroid carcinoma with or without follicular elements. Clin Cancer Res 2012;18(7):2056-65
  • O'Neil BH, Goff LW, Kauh JS, et al. Phase II study of the mitogen-activated protein kinase 1/2 inhibitor selumetinib in patients with advanced hepatocellular carcinoma. J Clin Oncol 2011;29(17):2350-6
  • 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
  • Martin-Liberal J, Lagares-Tena L, Larkin J. Prospects for MEK inhibitors for treating cancer. Expert Opin Drug Saf 2014;13(4):483-95
  • Meloche S, Pouysségur J. The ERK1/2 mitogen-activated protein kinase pathway as a master regulator of the G1- to S-phase transition. Oncogene 2007;26(22):3227-39
  • Mebratu Y, Tesfaigzi Y. How ERK1/2 activation controls cell proliferation and cell death: is subcellular localization the answer? Cell Cycle 2009;8(8):1168-75
  • Tsai J, Lee JT, Wang W, 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
  • 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
  • Sosman JA, Kim KB, 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, Rinderknecht J, Goldinger SM, et al. An open-label pilot study of vemurafenib in previously treated metastatic melanoma patients with brain metastases. J Clin Oncol 2011;29(Suppl):abstract 8548
  • Available from: http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm268241.htm
  • Available from: http://www.ema.europa.eu/ema/index.jsp?curl=pages/medicines/human/medicines/002409/human_med_001544.jsp&mid=WC0b01ac058001d124
  • King AJ, Arnone MR, Bleam MR, et al. Dabrafenib; preclinical characterization, increased efficacy when combined with trametinib, while BRAF/MEK tool combination reduced skin lesions. PLoS One 2013;8(7):e67583
  • 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(11):1087-95
  • 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;31(Suppl):9013
  • Latimer N, Abrams KR, Amonkar M, et al. Adjusting for treatment crossover in the BREAK-3 metastatic melanoma trial for dabrafenib: preliminary analysis. J Clin Oncol 2013;31(Suppl):9044
  • Available from: http://www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm354477.htm
  • Available from: http://www.ema.europa.eu/docs/en_GB/document_library/Press_release/2013/06/WC500144939.pdf
  • Stuart DD, Li N, Poon DJ, et al. Preclinical profile of LGX818: a potent and selective RAF kinase inhibitor. Cancer Res 2012;72(8 Suppl 1):3790
  • Dummer R, Robert C, Nyakas M, et al. Initial results from a phase I, open-label, dose escalation study of the oral BRAF inhibitor LGX818 in patients with BRAF V600 mutant advanced or metastatic melanoma. J Clin Oncol 2013;31(Suppl):9028
  • Huang T, Karsy M, Zhuge J, et al. B-Raf and the inhibitors: from bench to bedside. J Hematol Oncol 2013;6:30
  • Gilmartin AG, Bleam MR, 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
  • 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
  • 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 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
  • Available from: http://www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm381451.htm
  • Corcoran RB, Falchook GS, Infante JR, et al. Pharmacodynamic and efficacy analysis of the BRAF inhibitor dabrafenib (GSK436) in combination with the MEK inhibitor trametinib (GSK212) in patients with BRAFV600 mutant colorectal cancer (CRC). J Clin Oncol 2013;31(Suppl):abstract 3507
  • Wong H, Vernillet L, Peterson A, et al. Bridging the gap between preclinical and clinical studies using pharmacokinetic-pharmacodynamic modeling: an analysis of GDC-0973, a MEK inhibitor. Clin Cancer Res 2012;18(11):3090-9
  • 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
  • Choo EF, Ng CM, Berry L, et al. PK-PD modeling of combination efficacy effect from administration of the MEK inhibitor GDC-0973 and PI3K inhibitor GDC-0941 in A2058 xenografts. Cancer Chemother Pharmacol 2013;71(1):133-43
  • McArthur G, Gonzalez R, Pavlick A, et al. Vemurafenib (VEM) and MEK inhibitor, cobimetinib (GDC-0973), in advanced BRAFV600-mutated melanoma (BRIM7): dose-escalation and expansion results of a phase IB study [abstract:3703]. ESMO/ECCO/ESTRO Meeting; Amsterdam, The Netherlands; 2013
  • Kefford R, Miller WH, Shao-Weng Tan D, et al. Preliminary results from a phase Ib/II, open-label, dose-escalation study of the oral BRAF inhibitor LGX818 in combination with the oral MEK1/2 inhibitor MEK162 in BRAF V600-dependent advanced solid tumors. J Clin Oncol 2013;31(Suppl):9029
  • Jang S, Atkins MB. Which drug, and when, for patients with BRAF-mutant melanoma? Lancet Oncol 2013;14(2):e60-9
  • Dienstmann R, Tabernero J. BRAF as a target for cancer therapy. Anticancer Agents Med Chem 2011;11(3):285-95
  • Menzies AM, Long GV, Murali R. Dabrafenib and its potential for the treatment of metastatic melanoma. Drug Des Devel Ther 2012;6:391-405
  • Heidorn SJ, Milagre C, Whittaker S, et al. Kinase-dead BRAF and oncogenic RAS cooperate to drive tumor progression through CRAF. Cell 2010;140(2):209-21
  • Poulikakos PI, Zhang C, Bollag G, et al. RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF. Nature 2010;464(7287):427-30
  • Arnault JP, Mateus C, Escudier B, et al. Skin tumors induced by sorafenib; paradoxic RAS-RAF pathway activation and oncogenic mutations of HRAS, TP53, and TGFBR1. Clin Cancer Res 2012;18(1):263-72
  • 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
  • Gibney GT, Messina JL, Fedorenko IV, et al. Paradoxical oncogenesis--the long-term effects of BRAF inhibition in melanoma. Nat Rev Clin Oncol 2013;10(7):390-9
  • Flaherty KT, Puzanov I, Sosman J, et al. Phase I study of PLX4032: proof of concept for V600E BRAF mutation as a therapeutic target in human cancer. J Clin Oncol 2009;27:15s
  • Kopetz S, Desai J, Chan E, et al. PLX4032 in metastatic colorectal cancer patients with BRAF tumors. J Clin Oncol 2010;28:7s
  • Prahallad A, Sun C, Huang S, et al. Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR. Nature 2012;483(7387):100-3
  • Montero-Conde C, Ruiz-Llorente S, Dominguez JM, et al. Relief of feedback inhibition of HER3 transcription by RAF and MEK inhibitors attenuates their antitumor effects in BRAF-mutant thyroid carcinomas. Cancer Discov 2013;3(5):520-33
  • Pritchard AL, Hayward NK. Molecular pathways: mitogen-activated protein kinase pathway mutations and drug resistance. Clin Cancer Res 2013;19(9):2301-9
  • Lito P, Rosen N, Solit DB. Tumor adaptation and resistance to RAF inhibitors. Nat Med 2013;19(11):1401-9
  • 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
  • Maertens O, Johnson B, Hollstein P, et al. Elucidating distinct roles for NF1 in melanomagenesis. Cancer Discov 2013;3(3):338-49
  • Whittaker SR, Theurillat JP, Van Allen E, et al. A genome-scale RNA interference screen implicates NF1 loss in resistance to RAF inhibition. Cancer Discov 2013;3(3):350-62
  • 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
  • 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(12):4853-61
  • 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
  • Xing F, Persaud Y, Pratilas CA, et al. Concurrent loss of the PTEN and RB1 tumor suppressors attenuates RAF dependence in melanomas harboring (V600E)BRAF. Oncogene 2012;31(4):446-57
  • Eisen T, Ahmad T, Flaherty KT, et al. Sorafenib in advanced melanoma: a phase II randomised discontinuation trial analysis. Br J Cancer 2006;95(5):581-6
  • Hauschild A, Agarwala SS, Trefzer U, et al. Results of a phase III, randomized, placebo-controlled study of sorafenib in combination with carboplatin and paclitaxel as second-line treatment in patients with unresectable stage III or stage IV melanoma. J Clin Oncol 2009;27(17):2823-30

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