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Review

MEK inhibitors and their potential in the treatment of advanced melanoma: the advantages of combination therapy

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Pages 43-52 | Published online: 21 Dec 2015

References

  • JhappanCNoonanFPMerlinoGUltraviolet radiation and cutaneous malignant melanomaOncogene200322203099311212789287
  • MaverakisEMiyamuraYBowenMPCorreaGOnoYGoodarziHLight, including ultravioletJ Autoimmun2010343J247J25720018479
  • PeyssonnauxCEychèneAThe Raf/MEK/ERK pathway: new concepts of activationBiol Cell2001931–2536211730323
  • DaviesHBignellGRCoxCMutations of the BRAF gene in human cancerNature2002417689294995412068308
  • KimGMcKeeAENingYMFDA Approval summary: vemu-rafenib for treatment of unresectable or metastatic melanoma with the BRAFV600E mutationClin Cancer Res201420194994500025096067
  • ChapmanPBHauschildARobertCBRIM-3 Study GroupImproved Survival with vemurafenib in melanoma with BRAF V600E mutationN Engl J Med2011364262507251621639808
  • SosmanJAKimKBSchuchterLSurvival in BRAF V600-mutant advanced melanoma treated with vemurafenibN Engl J Med2012366870771422356324
  • McArthurGAChapmanPBRobertCSafety 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 studyLancet Oncol201415332333224508103
  • RobertCThomasLBondarenkoIIpilimumab plus dacarba-zine for previously untreated metastatic melanomaN Engl J Med2011364262517252621639810
  • FDA Approval for Dabrafenib [webpage on the Internet]BethesdaNational Cancer Institute [updated January 16, 2014]. Available from: http://www.cancer.gov/about-cancer/treatment/drugs/fda-dabrafenibAccessed October 4, 2015
  • HauschildAGrobJJDemidovLVDabrafenib in BRAF-mutated metastatic melanoma: a multicentre, open-label, phase 3 randomised controlled trialLancet2012380983935836522735384
  • RizosHMenziesAMPupoGMBRAF inhibitor resistance mechanisms in metastatic melanoma: spectrum and clinical impactClin Cancer Res20142071965197724463458
  • SullivanRJFlahertyKMAP kinase signaling and inhibition in melanomaOncogene201332192373237922945644
  • AbelEVBasileKJKugelCH3rdMelanoma adapts to RAF/MEK inhibitors through FOXD3-mediated upregulation of ERBB3J Clin Invest201312352155216823543055
  • GirottiMRPedersenMSanchez-LaordenBInhibiting EGF receptor or SRC family kinase signaling overcomes BRAF inhibitor resistance in melanomaCancer Discov20133215816723242808
  • NazarianRShiHWangQMelanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulationNature2010468732697397721107323
  • YadavVZhangXLiuJReactivation of mitogen-activated protein kinase (MAPK) pathway by FGF receptor 3 (FGFR3)/Ras mediates resistance to vemurafenib in human B-RAF V600E mutant melanomaJ Biol Chem201228733280872809822730329
  • DoughertyMKMüllerJRittDARegulation of Raf-1 by direct feedback phosphorylationMol Cell200517221522415664191
  • DouvilleEDownwardJEGF induced SOS phosphorylation in PC12 cells involves P90 RSK-2Oncogene19971543733839242373
  • EblaghieMCLunnJSDickinsonRJNegative feedback regulation of FGF signaling levels by Pyst1/MKP3 in chick embryosCurr Biol200313121009101812814546
  • HanafusaHToriiSYasunagaTNishidaESprouty1 and Sprouty2 provide a control mechanism for the Ras/MAPK signalling pathwayNat Cell Biol200241185085812402043
  • LitoPPratilasCAJosephEWRelief of profound feedback inhibition of mitogenic signaling by RAF inhibitors attenuates their activity in BRAFV600E melanomasCancer Cell201222566868223153539
  • StraussmanRMorikawaTSheeKTumour micro-environment elicits innate resistance to RAF inhibitors through HGF secretionNature2012487740850050422763439
  • ParaisoKHFedorenkoIVCantiniLPRecovery of phospho-ERK activity allows melanoma cells to escape from BRAF inhibitor therapyBr J Cancer2010102121724173020531415
  • Sanchez-LaordenBVirosAGirottiMRBRAF inhibitors induce metastasis in RAS mutant or inhibitor-resistant melanoma cells by reactivating MEK and ERK signalingSci Signal20147318ra3024667377
  • OberholzerPAKeeDDziunyczPRAS mutations are associated with the development of cutaneous squamous cell tumors in patients treated with RAF inhibitorsJ Clin Oncol201230331632122067401
  • SuFVirosAMilagreCRAS mutations in cutaneous squamous-cell carcinomas in patients treated with BRAF inhibitorsN Engl J Med2012366320721522256804
  • TrunzerKPavlickACSchuchterLPharmacodynamic effects and mechanisms of resistance to vemurafenib in patients with metastatic melanomaJ Clin Oncol201331141767177423569304
  • HeidornSJMilagreCWhittakerSKinase-dead BRAF and oncogenic RAS cooperate to drive tumor progression through CRAFCell2010140220922120141835
  • EskandarpourMKiaiiSZhuCCastroJSakkoAJHanssonJSuppression of oncogenic NRAS by RNA interference induces apoptosis of human melanoma cellsInt J Cancer20051151657315688405
  • LiYBollagGClarkRSomatic mutations in the neurofibroma-tosis 1 gene in human tumorsCell19926922752811568247
  • WhittakerSRTheurillatJPVan AllenEA genome-scale RNA interference screen implicates NF1 loss in resistance to RAF inhibitionCancer Discov20133335036223288408
  • WanPTGarnettMJRoeSMMechanism of activation of the RAF-ERK signaling pathway by oncogenic mutations of B-RAFCell2004116685586715035987
  • NissanMHPratilasCAJonesAMLoss of NF1 in cutaneous melanoma is associated with RAS activation and MEK dependenceCancer Res20147482340235024576830
  • ShiHMoriceauGKongXMelanoma whole-exome sequencing identifies (V600E)B-RAF amplification-mediated acquired B-RAF inhibitor resistanceNat Commun2012372422395615
  • PoulikakosPIPersaudYJanakiramanMRAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF(V600E)Nature2011480737738739022113612
  • MontagutCSharmaSVShiodaTElevated CRAF as a potential mechanism of acquired resistance to BRAF inhibition in melanomaCancer Res200868124853486118559533
  • GibneyGTMessinaJLFedorenkoIVSondakVKSmalleyKSParadoxical oncogenesis – the long-term effects of BRAF inhibition in melanomaNat Rev Clin Oncol201310739039923712190
  • FreemanAKRittAAMorrisonDKEffects of Raf dimerization and its inhibition on normal and disease-associated Raf signalingMol Cell201349475175823352452
  • JohannessenCMBoehmJSKimSYCOT drives resistance to RAF inhibition through MAP kinase pathway reactivationNature2010468732696897221107320
  • MarusiakAAEdwardsZCHugoWMixed lineage kinases activate MEK independently of RAF to mediate resistance to RAF inhibitorsNat Commun20145390124849047
  • FrederickDTPirisACogdillAPBRAF inhibition is associated with enhanced melanoma antigen expression and a more favorable tumor microenvironment in patients with metastatic melanomaClin Cancer Res20131951225123123307859
  • KhaliliJSLiuSRodríguez-CruzTGOncogenic BRAF(V600E) promotes stromal cell-mediated immunosuppression via induction of interleukin-1 in melanomaClin Cancer Res201218195329534022850568
  • WilmottJSLongGVHowleJRSelective BRAF inhibitors induce marked T-cell infiltration into human metastatic melanomaClin Cancer Res20121851386139422156613
  • BoniACogdillAPDangPSelective BRAFV600E inhibition enhances T-cell recognition of melanoma without affecting lymphocyte functionCancer Res201070135213521920551059
  • HodiFSO’DaySJMcDermottDFImproved survival with ipilimumab in patients with metastatic melanomaN Engl J Med2010363871172320525992
  • FreemanGJLongAJIwaiYEngagement of the PD-1 immunoin-hibitory receptor by a novel B7 family member leads to negative regulation of lymphocyte activationJ Exp Med200019271027103411015443
  • JiangXZhouJGiobbie-HurderAWargoJHodiFSThe activation of MAPK in melanoma cells resistant to BRAF inhibition promotes PD-L1 expression that is reversible by MEK and PI3K inhibitionClin Cancer Res201319359860923095323
  • AtefiMAvramisELassenAEffects of MAPK and PI3K pathways on PD-L1 expression in melanomaClin Cancer Res201420133446345724812408
  • BerthonCDrissVLiuJIn 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 inhibitorsCancer Immunol Immunother201059121839184920814675
  • RiceKDAayNAnandNKNovel carboxamide-based allosteric MEK inhibitors: discovery and optimization efforts toward XL518 (GDC-0973)ACS Med Chem Lett20123541642124900486
  • HatzivassiliouGHalingJRChenHMechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancersNature2013501746623223623934108
  • SolitDBGarrawayLAPratilasCABRAF mutation predicts sensitivity to MEK inhibitionNature2006439707435836216273091
  • GilmartinAGBleamMRGroyAGSK1120212 (JTP-74057) is an inhibitor of MEK activity and activation with favorable pharmacoki-netic properties for sustained in vivo pathway inhibitionClin Cancer Res2011175989100021245089
  • FlahertyKTRobertCHerseyPETRIC Study GroupImproved survival with MEK inhibition in BRAF-mutated melanomaN Engl J Med2012367210711422663011
  • CatalanottiFSolitDBPulitzerMPPhase II trial of MEK inhibitor selumetinib (AZD6244, ARRY-142886) in patients with BRAFV600E/K-mutated melanomaClin Cancer Res20131982257226423444215
  • RosenLLoRussoPMaWWA first-in-human phase 1 study to evaluate the MEK1/2 inhibitor GDC-0973 administered daily in patients with advanced solid tumors [abstract]. In: Proceedings of the 102nd Annual Meeting of the American Association for Cancer Research; 2011 April 2–6; Orlando, FLPhiladelphiaAACRCancer Res2011718 Suppl Abstract 4716
  • LarkinJAsciertoPADrénoBCombined vemurafenib and cobimetinib in BRAF-mutated melanomaN Engl J Med2014371201867187625265494
  • LongGVStroyakovskiyDGogasHCombined BRAF and MEK inhibition versus BRAF inhibition alone in melanomaN Engl J Med2014371201877188825265492
  • RobertCKaraszewskaBSchachterJImproved overall survival in melanoma with combined dabrafenib and trametinibN Engl J Med20153721303925399551
  • FlahertyKTInfanteJRDaudACombined BRAF and MEK inhibition in melanoma with BRAF V600 mutationsN Engl J Med2012367181694170323020132
  • LongGVStroyakovskyDLGogasHCOMBI-d: a randomized, double-blinded, Phase III study comparing the combination of dab-rafenib and trametinib to dabrafenib and trametinib placebo as first-line therapy in patients (pts) with unresectable or metastatic BRAFV600E/K mutation-positive cutaneous melanomaJ Clin Oncol2014325s suppl; abstr 9011
  • SanlorenzoMChoudhryAVujicIComparative profile of cutaneous adverse events: BRAF/MEK inhibitor combination therapy versus BRAF monotherapy in melanomaJ Am Acad Dermatol201471611021109.e125440439
  • HatzivassiliouGSongKYenIRAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growthNature2010464728743143520130576
  • PoulikakosPIZhangCBollagGShokatKMRosenNRAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAFNature2010464728742743020179705
  • CurtiBDRapid evolution of combination therapy in melanomaN Engl J Med2014371201929193025390744
  • RibasAGonzalezRPavlickACombination of vemurafenib and cobimetinib in patients with advanced BRAF(V600)-mutated melanoma: a phase 1b studyLancet Oncol201415995496525037139
  • KimKBKeffordRPavlickACPhase II study of the MEK1/MEK2 inhibitor trametinib in patients with metastatic BRAF-mutant cutaneous melanoma previously treated with or without a BRAF inhibitorJ Clin Oncol201331448248923248257
  • GirottiMRLopesFPreeceNParadox-breaking RAF inhibitors that also target SRC are effective in drug-resistant BRAF mutant melanomaCancer Cell2015271859625500121
  • LeKBlomainESRodeckUAplinAESelective RAF inhibitor impairs ERK1/2 phosphorylation and growth in mutant NRAS, vemurafenib-resistant melanoma cellsPigment Cell Melanoma Res201326450951723490205
  • HaoMSongFDuXAdvances in targeted therapy for unre-sectable melanoma: new drugs and combinationsCancer Lett201535911825578781
  • NiezgodaANiezgodaPCzajkowskiRNovel approaches to treatment of advanced melanoma: a review on targeted therapy and immuno-therapyBiomed Res Int2015201585138726171394
  • ChengHTeraiMKageyamaKParacrine effect of NRG1 and HGF drives resistance to MEK inhibitors in metastatic uveal melanomaCancer Res201575132737274825952648
  • SunCWangLHuangSReversible and adaptive resistance to BRAF(V600E) inhibition in melanomaNature2014508749411812224670642
  • VillanuevaJVulturALeeJTAcquired resistance to BRAF inhibitors mediated by a RAF kinase switch in melanoma can be overcome by cotargeting MEK and IGF-1R/PI3KCancer Cell201018668369521156289
  • NathansonKLMartinAMWubbenhorstBTumor genetic analyses of patients with metastatic melanoma treated with the BRAF inhibitor dabrafenib (GSK2118436)Clin Cancer Res201319174868487823833299
  • SmalleyKSLioniMDalla PalmaMIncreased cyclin D1 expression can mediate BRAF inhibitor resistance in BRAF V600E-mutated melanomasMol Cancer Ther2008792876288318790768
  • WagleNEmeryCBergerMFDissecting therapeutic resistance to RAF inhibition in melanoma by tumor genomic profilingJ Clin Oncol201129223085309621383288
  • EmeryCMVijayendranKGZipserMCMEK1 mutations confer resistance to MEK and B-RAF inhibitionProc Natl Acad Sci U S A200910648204112041619915144
  • HatzivassiliouGLiuBO’BrienCERK inhibition overcomes acquired resistance to MEK inhibitorsMol Cancer Ther20121151143115422402123
  • JaiswalBSJanakiramanVKljavinNMCombined targeting of BRAF and CRAF or BRAF and PI3K effector pathways is required for efficacy in NRAS mutant tumorsPLoS One200945e571719492075
  • HoeflichKPMerchantMOrrCIntermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibitionCancer Res201272121021922084396
  • SpagnoloFGhiorzoPOrgianoLBRAF-mutant melanoma: treatment approaches, resistance mechanisms, and diagnostic strategiesOnco Targets Ther2015815716825653539
  • RosenbergSARestifoNPYangJCMorganRADudleyMEAdoptive cell transfer: a clinical path to effective cancer immunotherapyNat Rev Cancer20088429930818354418
  • JohnsonLAMorganRADudleyMEGene therapy with human and mouse T-cell receptors mediates cancer regression and targets normal tissues expressing cognate antigenBlood2009114353554619451549
  • Hu-LieskovanSRobertLHomet MorenoBRibasACombining targeted therapy with immunotherapy in BRAF-mutant melanoma: promise and challengesJ Clin Oncol201432212248225424958825
  • MenziesAMLongGVSystemic treatment for BRAF-mutant melanoma: where do we go next?Lancet Oncol2014159e371e38125079100
  • RibasAHodiFSCallahanMKontoCWolchokJHepatotoxicity with combination of vemurafenib and ipilimumabN Engl J Med2013368141365136623550685
  • McDermottDLebbéCHodiFSDurable benefit and the potential for long-term survival with immunotherapy in advanced melanomaCancer Treat Rev20144091056106425060490
  • PorterDLLevineBLKalosMBaggAJuneCHChimeric antigen receptor-modified T cells in chronic lymphoid leukemiaN Engl J Med2011365872573321830940
  • MaverakisECorneliusLABowenGMMetastatic melanoma – a review of current and future treatment optionsActa Derm Venereol201595551652425520039
  • ShiVYTranKPatelF100% complete response rate in patients with cutaneous metastatic melanoma treated with intralesional interleukin (IL)-2, imiquimod, and topical retinoid cominbation therapy: results of a case seriesJ Am Acad Dermatol201573464565426259990