Olmutinib

It acts by covalently bonding to a cysteine residue near the kinase domain of epidermal growth factor receptor (EGFR).[2] In the US, it was given a breakthrough therapy designation in non-small cell lung cancer (NSCLC) in December 2015, and In South Korea, the drug was approved in May 2016 for the second-line treatment of NSCLC with the T790M mutation of EGFR.[2] Resistance to olmutinib has been reported; a person's cancer started progressing after they developed a C797S mutation in EGFR.[4] In November 2015 Hanmi granted an exclusive license to sell olmutinib in China to the Chinese company ZAI Labs.[5] On September 30, 2016, Korean regulatory authorities issued a safety alert about olmutinib in which it described two cases of toxic epidermal necrolysis, one of which was fatal, and a case of Stevens–Johnson syndrome; Boeheringer announced the termination its deal with Hanmi the same day, citing that the decision came after a review of "all available clinical data" on the drug, and also referring to competing drugs.
Routes ofadministrationBy mouthATC codeL01EB06Legal statusIUPAC nameCAS NumberChemSpiderCompTox DashboardFormulaMolar massSMILESepidermal growth factor receptorbreakthrough therapynon-small cell lung cancerHanmi PharmaceuticalBoehringer Ingelheimtoxic epidermal necrolysisStevens–Johnson syndromeTargeted 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 inhibitorsAfatinibAumolertinibBrigatinibDacomitinibErlotinibGefitinibIcotinibLazertinibMobocertinibOsimertinibRociletinibVandetanibLapatinibNeratinibTucatinibDabrafenibEncorafenibTovorafenibVemurafenibRTK class IIIAvapritinibAxitinibMasitinibPazopanibRipretinibSorafenibSunitinibToceranibLestaurtinibGilteritinibCediranibFruquintinibLenvatinibNintedanibRegorafenibSemaxanibTivozanibAlectinibCeritinibCrizotinibEnsartinibLorlatinibEntrectinibFutibatinibInfigratinibLarotrectinibPemigatinibPralsetinibRepotrectinibSelpercatinibCabozantinibCapmatinibNon-receptorbcr-ablAsciminibBosutinibDasatinibImatinibNilotinibPonatinibRadotinibJanus 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 proteinsCerebrolysinantineoplasticimmunomodulatory