Bosutinib

Bosutinib, sold under the brand name Bosulif, is a small molecule BCR-ABL and src tyrosine kinase inhibitor used for the treatment of chronic myelogenous leukemia.[citation needed] It is an ATP-competitive Bcr-Abl tyrosine-kinase inhibitor with an additional inhibitory effect on Src family kinases (including Src, Lyn and Hck).Bosutinib received US FDA and EU European Medicines Agency approval in September 2012, and March 2013, respectively for the treatment of adults with Philadelphia chromosome-positive (Ph+) chronic myelogenous leukemia (CML) with resistance, or intolerance to prior therapy.[3] Hence P-gp and CYP3A4 inhibitors may increase plasma levels of bosutinib.[3] Likewise CYP3A4 inducers may reduce plasma concentrations of bosutinib.
WEE1 kinase domain in complex with bosutinib.
License dataDailyMedRoutes ofadministrationBy mouthATC codeL01EA04Legal status℞-onlyPharmacokineticProtein bindingMetabolismCYP3A4Elimination half-lifeExcretionIUPAC nameCAS NumberIUPHAR/BPSDrugBankChemSpiderChEMBLCompTox DashboardECHA InfoCardFormulaMolar massSMILESBCR-ABLtyrosine kinase inhibitorchronic myelogenous leukemiaPfizerBcr-Abl tyrosine-kinase inhibitorSrc family kinasesplatelet derived growth factorvascular endothelial growth factorEuropean Medicines AgencyPhiladelphia chromosomeP-glycoproteinDiscovery and development of Bcr-Abl tyrosine kinase inhibitorsTargeted 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-receptorAsciminibDasatinibImatinibNilotinibPonatinibRadotinibJanus kinaseBaricitinibFedratinibFilgotinibMomelotinibPacritinibRuxolitinibBinimetinibCobimetinibSelumetinibTrametinibBruton'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)FosgonimetonHepatocyte growth factorDihexa (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