Ruxolitinib

Ruxolitinib (sold under the brand names Jakafi and Jakavi among others, and as Opzelura in cream form) is a medication used for the treatment of intermediate or high-risk myelofibrosis,[6] a type of myeloproliferative neoplasm that affects the bone marrow;[11][12] polycythemia vera, when there has been an inadequate response to or intolerance of hydroxyurea;[6][13] and steroid-refractory acute graft-versus-host disease.[6] In March 2012, the phase III Controlled Myelofibrosis Study with Oral JAK Inhibitor-I (COMFORT-I) and COMFORT-II trials showed significant benefits by reducing spleen size and relieving debilitating symptoms.[23][24][25][26] In November 2011, ruxolitinib was approved by the U.S. Food and Drug Administration (FDA)[15] for the treatment of intermediate or high-risk myelofibrosis based on results of the COMFORT-I and COMFORT-II Trials.[29] The indication was further expanded in the US in September 2021, for the treatment of chronic graft-versus-host disease (cGVHD) after failure of one or two lines of systemic therapy in people 12 years of age and older.[30] In September 2021, ruxolitinib cream (sold under the brand name Opzelura) was approved for medical use in the United States[31] for the treatment of mild to moderate atopic dermatitis (AD).
Drugs.comMedlinePlusLicense dataDailyMedPregnancycategoryRoutes ofadministrationBy mouthtopicalATC codeL01EJ01D11AH09Legal status ℞-onlyWARNINGPharmacokineticBioavailabilityProtein bindingMetabolismCYP3A4Elimination half-lifeExcretionIUPAC nameCAS NumberIUPHAR/BPSDrugBankChemSpiderChEMBLPDB ligandCompTox DashboardFormulaMolar massSMILESmedicationmyelofibrosismyeloproliferative neoplasmbone marrowpolycythemia verahydroxyureagraft-versus-host diseaseJanus kinase inhibitorIncyte CorpNovartisvitiligoindicatedsplenomegalyatopic dermatitisthrombocytopeniaanaemianeutropeniaurinary tract infectionskidneyrenal pelvisureterbladderurethrahypercholesterolaemialiver enzymeherpes zosteralanine transaminaseaspartate transaminasesignal transducers and activators of transcriptioncytokine receptorsgene expressionFood and Drug AdministrationCommittee for Medicinal Products for Human UseEuropean Medicines Agencyplaque psoriasisalopecia areatadiffuse large B-cell lymphomaperipheral T-cell lymphomaadipogenesisinsulin sensitivityHealth Canadapublic domainBibcodeWayback MachineClinicalTrials.govTargeted 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 inhibitorsAfatinibAumolertinibBrigatinibDacomitinibErlotinibGefitinibIcotinibLazertinibMobocertinibOlmutinibOsimertinibRociletinibVandetanibLapatinibNeratinibTucatinibDabrafenibEncorafenibTovorafenibVemurafenibRTK class IIIAvapritinibAxitinibMasitinibPazopanibRipretinibSorafenibSunitinibToceranibLestaurtinibGilteritinibCediranibFruquintinibLenvatinibNintedanibRegorafenibSemaxanibTivozanibAlectinibCeritinibCrizotinibEnsartinibLorlatinibEntrectinibFutibatinibInfigratinibLarotrectinibPemigatinibPralsetinibRepotrectinibSelpercatinibCabozantinibCapmatinibNon-receptorbcr-ablAsciminibBosutinibDasatinibImatinibNilotinibPonatinibRadotinibJanus kinaseBaricitinibFedratinibFilgotinibMomelotinibPacritinibBinimetinibCobimetinibSelumetinibTrametinibBruton'sAcalabrutinibIbrutinibOrelabrutinibPirtobrutinibZanubrutinibfusion proteinAfliberceptproapoptoticprohibitinAdipotideexotoxinDenileukin diftitoxmTOR inhibitorsEverolimusRidaforolimusSirolimusTemsirolimushedgehogGlasdegibSonidegibVismodegibCDK inhibitorsAbemaciclibDalpiciclibPalbociclibRibociclibTrilaciclibAdagrasibSotorasibPi3K inhibitorsAlpelisibCopanlisibDuvelisibIdelalisibInavolisibParsaclisibRevumenibFibroblast growth factor receptorErdafitinibMidostaurinOdronextamabPexidartinibQuizartinibTebentafuspTepotinibTunlametinibVenetoclaxCytokine receptormodulatorsChemokineErythropoietinDarbepoetin alfaEpoetin alfaEpoetin betaEpoetin thetaEpoetin zetaErythropoietin (EPO)Methoxy polyethylene glycol-epoetin beta (CERA/Mircera)PeginesatideG-CSF (CSF3)FilgrastimGranulocyte colony-stimulating factorLenograstimLipegfilgrastimPegfilgrastimGM-CSF (CSF2)Granulocyte macrophage colony-stimulating factorMolgramostimSargramostimMavrilimumabNamilumabOtilimabM-CSF (CSF1)Interleukin-34Macrophage colony-stimulating factorSCF (c-Kit)ThrombopoietinEltrombopagPromegapoietinRomiplostimThrombopoietin (THPO, MGDF)InterferonIFNAR (α/β, I)AlbinterferonInterferon alpha (interferon alfa, IFN-α)Interferon alfaIFNA10IFNA13IFNA14IFNA16IFNA17IFNA21Interferon alfa 2aInterferon alfa 2bInterferon alfacon-1Interferon alpha-n3Interferon beta (IFN-β)Interferon beta 1aInterferon beta 1bInterferon kappa (IFN-ε/κ/τ/ζ, IFNK)Interferon omega (IFN-ω, IFNW1)Peginterferon alfa-2aPeginterferon alfa-2bAnifrolumabFaralimomabRontalizumabSifalimumabIFNGR (γ, II)Interferon gamma (IFN-γ)Interferon gamma 1bEmapalumabFontolizumabIFNLR (λ, III)InterleukininhibitorsAbrocitinibDeuruxolitinibOclacitinibPeficitinibTofacitinib (tasocitinib)UpadacitinibAtiprimodCHZ868Cucurbitacin I (elatericin B, JSI-124)CYT387Decernotinib (VX-509)RitlecitinibDeucravacitinibCardiotrophin 1 (CT-1)FMS-like tyrosine kinase 3 ligand (FLT3L)Leukemia/leukocyte inhibitory factor (LIF)Oncostatin M (OSM)Thymic stromal lymphopoietin (TSLP)