Vemurafenib

Melanoma cells without these mutations are not inhibited by vemurafenib; the drug paradoxically stimulates normal BRAF and may promote tumor growth in such cases.[5][6] Three mechanisms of resistance to vemurafenib (covering 40% of cases) have been discovered: At the maximum tolerated dose (MTD) of 960 mg twice a day 31% of patients get skin lesions that may need surgical removal.[25] In February 2012, the European Commission approved vemurafenib as a monotherapy for the treatment of adults with BRAF V600E mutation positive unresectable or metastatic melanoma, the most aggressive form of skin cancer.[26] In November 2017, the US Food and Drug Administration (FDA) approved vemurafenib for the treatment of people with Erdheim–Chester disease (ECD), a rare type of histiocytic neoplasm.[30] In a phase II clinical trial, Memorial Sloan Kettering is testing Vemurafenib, plus Obinutuzumab, in patients with previously untreated classical hairy cell leukemia.
Drugs.comMedlinePlusLicense dataPregnancycategoryRoutes ofadministrationBy mouthATC codeL01XE15Legal status ℞-only℞-onlyIUPAC nameCAS NumberIUPHAR/BPSDrugBankChemSpiderChEMBLPDB ligandCompTox DashboardECHA InfoCardFormulaMolar massSMILESN-terminusC-terminusmelanomaBiological targetMechanism of actionprotein kinase inhibitorLIGPLOTmedicationB-Raf enzymePlexxikonprogrammed cell deathB-Raf/MEK stepB-Raf/MEK/ERK pathwayamino acidvalineglutamic acidlysinePDGFRBoncogeneStromal cellhepatocyte growth factorarthralgiaphase I clinical studycolorectal cancerdacarbazinecobimetinibMEK-inhibitorFood and Drug Administrationdabrafenibtrametinibfragment-based lead discoveryEuropean Commissionmutationmetastatic melanomaErdheim–Chester diseaseliver toxicityHairy cell leukemiaBibcodeThe New York TimesClinicalTrials.govNational Center for Biotechnology InformationTargeted cancer therapyantineoplastic agentsmonoclonal antibodiesReceptor tyrosine kinaseHER1/EGFRCetuximabPanitumumabHER2/neuPertuzumabTrastuzumab+hyaluronidaseTrastuzumab emtansineTrastuzumab deruxtecanZanidatamabCatumaxomabEdrecolomabVEGF-ABevacizumabLeukemialymphomalymphoidGlofitamabElranatamabMosunetuzumabIbritumomabObinutuzumabOfatumumabRituximabTositumomabBrentuximabAlemtuzumabmyeloidGemtuzumab ozogamicinAmivantamabAtezolizumabAvelumabAxatilimabBelantamab mafodotinBermekimabBlinatumomabCemiplimabCosibelimabDaratumumabDinutuximab betaDostarlimabDurvalumabElotuzumabEnfortumab vedotinEpcoritamabInotuzumab ozogamicinIpilimumabIsatuximabLoncastuximab tesirineMirvetuximab soravtansineMogamulizumabMoxetumomab pasudotoxNaxitamabNecitumumabNivolumab+relatlimabOlaratumabOportuzumab monatoxPembrolizumabPolatuzumab vedotinRamucirumabRetifanlimabSacituzumab govitecanSerplulimabSugemalimabTafasitamabTalquetamabTarlatamabTeclistamabTislelizumabTisotumab vedotinToripalimabTremelimumabZenocutuzumabZolbetuximabTyrosine kinase inhibitorsAfatinibAumolertinibBrigatinibDacomitinibErlotinibGefitinibIcotinibLazertinibMobocertinibOlmutinibOsimertinibRociletinibVandetanibLapatinibNeratinibTucatinibEncorafenibTovorafenibRTK class IIIAvapritinibAxitinibMasitinibPazopanibRipretinibSorafenibSunitinibToceranibLestaurtinibGilteritinibCediranibFruquintinibLenvatinibNintedanibRegorafenibSemaxanibTivozanibAlectinibCeritinibCrizotinibEnsartinibLorlatinibEntrectinibFutibatinibInfigratinibLarotrectinibPemigatinibPralsetinibRepotrectinibSelpercatinibCabozantinibCapmatinibNon-receptorbcr-ablAsciminibBosutinibDasatinibImatinibNilotinibPonatinibRadotinibJanus kinaseBaricitinibFedratinibFilgotinibMomelotinibPacritinibRuxolitinibBinimetinibSelumetinibBruton'sAcalabrutinibIbrutinibOrelabrutinibPirtobrutinibZanubrutinibfusion proteinAfliberceptproapoptoticprohibitinAdipotideexotoxinDenileukin diftitoxmTOR inhibitorsEverolimusRidaforolimusSirolimusTemsirolimushedgehogGlasdegibSonidegibVismodegibCDK inhibitorsAbemaciclibDalpiciclibPalbociclibRibociclibTrilaciclibAdagrasibSotorasibPi3K inhibitorsAlpelisibCopanlisibDuvelisibIdelalisibInavolisibParsaclisibRevumenibFibroblast growth factor receptorErdafitinibMidostaurinOdronextamabPexidartinibQuizartinibTebentafuspTepotinibTunlametinibVenetoclaxGrowth factor receptormodulatorsAngiopoietinAngiopoietin 1Angiopoietin 4Angiopoietin 2RebastinibEvinacumabNesvacumabAxokineEGF (ErbB)EGF(ErbB1/HER1)AmphiregulinBetacellulinEGF (urogastrone)EpigenEpiregulinHeparin-binding EGF-like growth factor (HB-EGF)MuroderminNepiderminTransforming growth factor alpha (TGFα)CanertinibGrandininDepatuxizumab mafodotinFutuximabImgatuzumabMatuzumabNimotuzumabZalutumumabErbB2/HER2ErtumaxomabMubritinibErbB3/HER3Neuregulins (heregulins)6 (neuroglycan C)DuligotumabPatritumabSeribantumabErbB4/HER42 (bFGF)10 (KGF2)TraferminPaliferminSpriferminBurosumabFGF15/19HGF (c-Met)FosgonimetonDihexa (PNB-0408)ForetinibTivantinibVolitinibEmibetuzumabFiclatuzumabFlanvotumabOnartuzumabRilotumumabTelisotuzumab vedotindes(1-3)IGF-1Insulin-like growth factor-1 (somatomedin C)IGF-1 LR3Insulin-like growth factor-2 (somatomedin A)InsulinMecaserminMecasermin rinfabateLinsitinibCixutumumabDalotuzumabFigitumumabGanitumabRobatumumabTeprotumumabDusigitumabTrofinetideLNGF (p75NTR)BNN-20BNN-27CenegerminDHEA-SDexamethasoneTestosteroneFasinumabFrunevetmabFulranumabTanezumabBecaplerminPlatelet-derived growth factorCrenolanibMotesanibTovetumabRET (GFL)GFRα1Glial cell line-derived neurotrophic factor (GDNF)GFRα2Neurturin (NRTN)GFRα3Artemin (ARTN)GFRα4Persephin (PSPN)SCF (c-Kit)AncestimStem cell factorAmitriptylineTavilermide4'-DMA-7,8-DHF7,8-DHF7,8,3'-THFDeoxygeduninDeprenylDiosmetinLM22A-4N-AcetylserotoninNorwogonin (5,7,8-THF)ANA-12Cyclotraxin BGossypetin (3,5,7,8,3',4'-HHF)Placental growth factor (PGF)D (FIGF)PegaptanibAlacizumab pegolIcrucumabRanibizumabAdrenomedullinColony-stimulating factorsConnective tissue growth factor (CTGF)EphrinsErythropoietinGlucose-6-phosphate isomerase (GPI; PGI, PHI, AMF)Glia maturation factor (GMF)Hepatoma-derived growth factor (HDGF)InterleukinsT-cell growth factorsLeukemia inhibitory factor (LIF)Macrophage-stimulating protein (MSP; HLP, HGFLP)Midkine (NEGF2)Migration-stimulating factor (MSF; PRG4)OncomodulinPituitary adenylate cyclase-activating peptide (PACAP)PleiotrophinRenalaseThrombopoietinWnt signaling proteinsCerebrolysin