Ripretinib

[5] Ripretinib is the first new drug specifically approved in the United States as a fourth-line treatment for advanced gastrointestinal stromal tumor (GIST).[4][6] Ripretinib can also cause serious side effects including skin cancer, hypertension (high blood pressure) and cardiac dysfunction manifested as ejection fraction decrease (when the muscle of the left ventricle of the heart is not pumping as well as normal).[4][7][8][6] The approval of ripretinib was based on the results of an international, multi-center, randomized, double-blind, placebo-controlled clinical trial (INVICTUS/NCT03353753) that enrolled 129 participants with advanced gastrointestinal stromal tumor (GIST) who had received prior treatment with imatinib, sunitinib, and regorafenib.[4][9] The trial compared participants who were randomized to receive ripretinib to participants who were randomized to receive placebo, to determine whether progression free survival (PFS) – the time from initial treatment in the clinical trial to growth of the cancer or death – was longer in the ripretinib group compared to the placebo group.[6] The major efficacy outcome measure was progression-free survival (PFS) based on assessment by blinded independent central review (BICR) using modified RECIST 1.1 in which lymph nodes and bone lesions were not target lesions and a progressively growing new tumor nodule within a pre-existing tumor mass must meet specific criteria to be considered unequivocal evidence of progression.
Drugs.comMedlinePlusLicense dataDailyMedPregnancycategoryRoutes ofadministrationBy mouthATC codeL01EX19Legal status ℞-only℞-onlyIUPAC nameCAS NumberDrugBankChemSpiderChEMBLCompTox DashboardFormulaMolar massSMILESmedicationgastrointestinal stromal tumorgastrointestinal tractalopeciamyalgiaindicatedimatinibsunitinibregorafenibFood and Drug Administrationpriority reviewfast trackbreakthrough therapyorphan drugInternational nonproprietary nameUnited States Adopted Namepublic domainEuropean Medicines AgencyClinicalTrials.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 IIIAvapritinibAxitinibMasitinibPazopanibSorafenibToceranibLestaurtinibGilteritinibCediranibFruquintinibLenvatinibNintedanibSemaxanibTivozanibAlectinibCeritinibCrizotinibEnsartinibLorlatinibEntrectinibFutibatinibInfigratinibLarotrectinibPemigatinibPralsetinibRepotrectinibSelpercatinibCabozantinibCapmatinibNon-receptorbcr-ablAsciminibBosutinibDasatinibNilotinibPonatinibRadotinibJanus 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