Vemurafenib: a new treatment for BRAF-V600 mutated advanced melanoma

References

• JemalABrayFCenterMMGlobal cancer statisticsCA Cancer J Clin201161699021296855
   PubMed Web of Science ®Google Scholar
• JemalASiegelRXuJCancer statistics, 2010CA Cancer J Clin20106027730020610543
   PubMed Web of Science ®Google Scholar
• World Health OrganizationCancer Available from: http://www.who.int/cancer/Accessed June 25, 2012
   Google Scholar
• Cancer Research UKCancer Statistics2011 Available at http://info.cancerresearchuk.org/cancerstats/
   Google Scholar
• BalchCMGershenwaldJESoongSJFinal version of 2009 AJCC melanoma staging and classificationJ Clin Oncol2009276199620619917835
   PubMed Web of Science ®Google Scholar
• KornELLiuPYLeeSJMeta-analysis of Phase II cooperative group trials in metastatic stage IV melanoma to determine progressionfree and overall survival benchmarks for future Phase II trialsJ Clin Oncol20082652753418235113
   PubMed Web of Science ®Google Scholar
• ChapmanPBEinhornLHMeyersMLPhase III multicenter randomized trial of the Dartmouth regimen versus dacarbazine in patients with metastatic melanomaJ Clin Oncol1999172745275110561349
   PubMed Web of Science ®Google Scholar
• MiddletonMRGrobJJAaronsonNRandomized Phase III study of temozolomide versus dacarbazine in the treatment of patients with advanced metastatic malignant melanomaJ Clin Oncol20001815816610623706
   PubMed Web of Science ®Google Scholar
• AvrilMFAamdalSGrobJJFotemustine compared with dacarbazine in patients with disseminated malignant melanoma: a Phase III studyJ Clin Oncol2004221111125
   Web of Science ®Google Scholar
• BedikianAYMillwardMPehambergerHBcl-2 antisense (oblimersen sodium) plus dacarbazine in patients with advanced melanoma: the Oblimersen Melanoma Study GroupJ Clin Oncol2006244738474516966688
   PubMed Web of Science ®Google Scholar
• AtkinsMBLotzeMTDutcherJPHigh-dose recombinant interleukin 2 therapy for patients with metastatic melanoma: analysis of 270 patients treated between 1985 and 1993J Clin Oncol1999172105211610561265
   PubMed Web of Science ®Google Scholar
• HodiFSO’DaySJMcDermottDFImproved survival with ipilimumab in patients with metastatic melanomaN Engl J Med201036371172320525992
   PubMed Web of Science ®Google Scholar
• ChapmanPBHauschildARobertCImproved survival with vemurafenib in melanoma with BRAF V600E mutationN Engl J Med20113642507251621639808
   PubMed Web of Science ®Google Scholar
• DaviesHBignellGRCoxCMutations of the BRAF gene in human cancerNature200241794995412068308
   PubMed Web of Science ®Google Scholar
• CurtinJAFridlyandJKageshitaTDistinct sets of genetic alterations in melanomaN Engl J Med20053532135214716291983
   PubMed Web of Science ®Google Scholar
• CurtinJABusamKPinkelDSomatic activation of KIT in distinct subtypes of melanomaJ Clin Oncol2006244340434616908931
   PubMed Web of Science ®Google Scholar
• BeadlingCJacobson-DunlopEHodiFSKIT gene mutations and copy number in melanoma subtypesClin Cancer Res2008146821682818980976
   PubMed Web of Science ®Google Scholar
• Van RaamsdonkCDGriewankKGCrosbyMBMutations in GNA11 in uveal melanomaN Engl J Med20103632191219921083380
   PubMed Web of Science ®Google Scholar
• RobinsonMJCobbMHMitogen-activated protein kinase pathwaysCurr Opin Cell Biol199791801869069255
   PubMed Web of Science ®Google Scholar
• WellbrockCKarasaridesMMaraisRThe RAF proteins take centre stageNat Rev Mol Cell Biol2004587588515520807
   PubMed Web of Science ®Google Scholar
• BallNJYohnJJMorelliJGRas mutations in human melanoma: a marker of malignant progressionJ Invest Dermatol19941022852908120410
   PubMed Web of Science ®Google Scholar
• van ‘t VeerLJBurgeringBMVersteegRN-ras mutations in human cutaneous melanoma from sun-exposed body sitesMol Cell Biol19899311431162674680
   PubMed Web of Science ®Google Scholar
• MalumbresMBarbacidMRAS oncogenes: the first 30 yearsNat Rev Cancer2003345946512778136
   PubMed Web of Science ®Google Scholar
• GarnettMJMaraisRGuilty as charged: B-RAF is a human oncogeneCancer Cell2004631331915488754
   PubMed Web of Science ®Google Scholar
• WanPTGarnettMJRoeSMMechanism of activation of the RAF-ERK signaling pathway by oncogenic mutations of B-RAFCell200411685586715035987
   PubMed Web of Science ®Google Scholar
• GarnettMJRanaSPatersonHWild-type and mutant B-RAF activate C-RAF through distinct mechanisms involving heterodimerizationMol Cell20052096396916364920
   PubMed Web of Science ®Google Scholar
• WellbrockCOgilvieLHedleyDV599EB-RAF is an oncogene in melanocytesCancer Res2004642338234215059882
   PubMed Web of Science ®Google Scholar
• KarasaridesMChiloechesAHaywardRB-RAF is a therapeutic target in melanomaOncogene2004236292629815208680
   PubMed Web of Science ®Google Scholar
• DhomenNReis-FilhoJSda Rocha DiasSOncogenic BRAF induces melanocyte senescence and melanoma in miceCancer Cell20091529430319345328
   PubMed Web of Science ®Google Scholar
• MichaloglouCVredeveldLCSoengasMSBRAF E600- associated senescence-like cell cycle arrest of human naeviNature200543672072416079850
   PubMed Web of Science ®Google Scholar
• PollockPMHarperULHansenKSHigh frequency of BRAF mutations in neviNat Genet200333192012447372
   PubMed Web of Science ®Google Scholar
• WilhelmSMCarterCTangLBAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesisCancer Res2004647099710915466206
   PubMed Web of Science ®Google Scholar
• EisenTAhmadTFlahertyKTSorafenib in advanced melanoma: a Phase II randomised discontinuation trial analysisBr J Cancer20069558158616880785
   PubMed Web of Science ®Google Scholar
• HauschildAAgarwalaSSTrefzerUResults 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 melanomaJ Clin Oncol2009272823283019349552
   PubMed Web of Science ®Google Scholar
• BollagGHirthPTsaiJClinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanomaNature201046759659920823850
   PubMed Web of Science ®Google Scholar
• TsaiJLeeJTWangWDiscovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activityProc Natl Acad Sci U S A20081053041304618287029
   PubMed Web of Science ®Google Scholar
• YangHHigginsBKolinskyKRG7204 (PLX4032), a selective BRAFV600E inhibitor, displays potent antitumor activity in preclinical melanoma modelsCancer Res2010705518552720551065
   PubMed Web of Science ®Google Scholar
• SalaEMologniLTruffaSBRAF silencing by short hairpin RNA or chemical blockade by PLX4032 leads to different responses in melanoma and thyroid carcinoma cellsMol Cancer Res2008675175918458053
   PubMed Web of Science ®Google Scholar
• JosephEWPratilasCAPoulikakosPIThe RAF inhibitor PLX4032 inhibits ERK signaling and tumor cell proliferation in a V600E BRAF-selective mannerProc Natl Acad Sci U S A2010107149031490820668238
   PubMed Web of Science ®Google Scholar
• HalabanRZhangWBacchiocchiAPLX4032, a selective BRAF(V600E) kinase inhibitor, activates the ERK pathway and enhances cell migration and proliferation of BRAF melanoma cellsPigment Cell Melanoma Res20102319020020149136
   PubMed Web of Science ®Google Scholar
• TapWDGongKWDer ingJPharmacodynami c characterization of the eff icacy signals due to selective BRAF inhibition with PLX4032 in malignant melanomaNeoplasia20101263764920689758
   PubMed Web of Science ®Google Scholar
• FlahertyKTPuzanovIKimKBInhibition of mutated, activated BRAF in metastatic melanomaN Engl J Med201036380981920818844
   PubMed Web of Science ®Google Scholar
• McArthurGHauschildARobertCVemurafenib improves overall survival compared to dacarbazine in advanced BRAFV600E-mutated melanoma: Updated survival results from a Phase III randomised, open-label, multicentre trialEur J Cancer20114714
   Web of Science ®Google Scholar
• McArthurGAPuzanovIAmaravadiRMarked, homogeneous, and early [18F]fluorodeoxyglucose-positron emission tomography responses to vemurafenib in BRAF-mutant advanced melanomaJ Clin Oncol2012301628163422454415
   PubMed Web of Science ®Google Scholar
• SosmanJAKimKBSchuchterLSurvival in BRAF V600- mutant advanced melanoma treated with vemurafenibN Engl J Med201236670771422356324
   PubMed Web of Science ®Google Scholar
• WhittakerSKirkRHaywardRGatekeeper mutations mediate resistance to BRAF-targeted therapiesSci Transl Med201023541
   Web of Science ®Google Scholar
• NazarianRShiHWangQMelanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulationNature201046897397721107323
   PubMed Web of Science ®Google Scholar
• VillanuevaJVulturALeeJTAcquired resistance to BRAF inhibitors mediated by a RAF kinase switch in melanoma can be overcome by cotargeting MEK and IGF-1R/PI3KCancer Cell20101868369521156289
   PubMed Web of Science ®Google Scholar
• PoulikakosPIPersaudYJanakiramanMRAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF(V600E)Nature201148038739022113612
   PubMed Web of Science ®Google Scholar
• McArthurGARibasAChapmanPBMolecular analyses from a Phase I trial of vemurafenib to study mechanism of action (MOA) and resistance in repeated biopsies from BRAF mutation-positive metastatic melanoma patientsJ Clin Oncol201129Abstr 8502
   Web of Science ®Google Scholar
• HeidornSJMilagreCWhittakerSKinase-dead BRAF and oncogenic RAS cooperate to drive tumor progression through CRAFCell201014020922120141835
   PubMed Web of Science ®Google Scholar
• PoulikakosPIZhangCBollagGRAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAFNature201046442743020179705
   PubMed Web of Science ®Google Scholar
• HatzivassiliouGSongKYenIRAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growthNature201046443143520130576
   PubMed Web of Science ®Google Scholar
• ShiHMoriceauGKongXMelanoma whole-exome sequencing identifies (V600E)B-RAF amplification-mediated acquired B-RAF inhibitor resistanceNat Commun2010372422395615
   PubMed Web of Science ®Google Scholar
• WagleNEmeryCBergerMFDissecting therapeutic resistance to RAF inhibition in melanoma by tumor genomic profilingJ Clin Oncol2011293085309621383288
   PubMed Web of Science ®Google Scholar
• JohannessenCMBoehmJSKimSYCOT drives resistance to RAF inhibition through MAP kinase pathway reactivationNature201046896897221107320
   PubMed Web of Science ®Google Scholar
• MontagutCSharmaSVShiodaTElevated CRAF as a potential mechanism of acquired resistance to BRAF inhibition in melanomaCancer Res2008684853486118559533
   PubMed Web of Science ®Google Scholar
• RochetNMKottschadeLAMarkovicSNVemurafenib for melanoma metastases to the brainN Engl J Med20113652439244122188003
   PubMed Web of Science ®Google Scholar
• DummerRRinderknechtJGoldingerSMAn open-label pilot study of vemurafenib in previously treated metastatic melanoma patients with brain metastasesJ Clin Oncol201129Abstr 8548
   Web of Science ®Google Scholar
• BafaloukosDGogasHThe treatment of brain metastases in melanoma patientsCancer Treat Rev20043051552015325032
   PubMed Web of Science ®Google Scholar
• FifeKMColmanMHStevensGNDeterminants of outcome in melanoma patients with cerebral metastasesJ Clin Oncol2004221293130015051777
   PubMed Web of Science ®Google Scholar
• AgarwalaSSKirkwoodJMGoreMTemozolomide for the treatment of brain metastases associated with metastatic melanoma: a Phase II studyJ Clin Oncol2004222101210715169796
   PubMed Web of Science ®Google Scholar
• LongGVMenziesAMNagrialAMPrognostic and clinicopathologic associations of oncogenic BRAF in metastatic melanomaJ Clin Oncol2011291239124621343559
   PubMed Web of Science ®Google Scholar
• RubinsteinJCSznolMPavlickACIncidence of the V600K mutation among melanoma patients with BRAF mutations, and potential therapeutic response to the specific BRAF inhibitor PLX4032J Transl Med201086720630094
   PubMed Web of Science ®Google Scholar
• SchmidtCChallenges ahead for companion diagnosticsJ Natl Cancer Inst2012104141522173588
   PubMedGoogle Scholar
• OberholzerPAKeeDDziunyczPRAS mutations are associated with the development of cutaneous squamous cell tumors in patients treated with RAF inhibitorsJ Clin Oncol20113031632122067401
   PubMed Web of Science ®Google Scholar
• SuFVirosAMilagreCRAS mutations in cutaneous squamous-cell carcinomas in patients treated with BRAF inhibitorsN Engl J Med201236620721522256804
   PubMed Web of Science ®Google Scholar
• ArnaultJPMateusCEscudierBSkin tumors induced by sorafenib; paradoxic RAS-RAF pathway activation and oncogenic mutations of HRAS, TP53, and TGFBR1Clin Cancer Res20111826327222096025
   PubMed Web of Science ®Google Scholar
• WeeraratnaATRAF around the edges – the paradox of BRAF inhibitorsN Engl J Med201236627127322256810
   PubMed Web of Science ®Google Scholar
• InfanteJRFalchookGSLawrenceDPPhase I/II study to assess safety, pharmacokinetics, and efficacy of the oral MEK 1/2 inhibitor GSK1120212 (GSK212) dosed in combination with the oral BRAF inhibitor GSK2118436 (GSK436)J Clin Oncol201129Abstr CRA 8503
   Google Scholar
• BoniACogdillAPDangPSelective BRAFV600E inhibition enhances T-cell recognition of melanoma without affecting lymphocyte functionCancer Res2010705213522920551059
   PubMed Web of Science ®Google Scholar
• HandoliasDHamiltonALSalemiRClinical responses observed with imatinib or sorafenib in melanoma patients expressing mutations in KITBr J Cancer20101021219122320372153
   PubMed Web of Science ®Google Scholar