Ibrutinib

Ibrutinib, sold under the brand name Imbruvica among others, is a small molecule drug that inhibits B-cell proliferation and survival by irreversibly binding the protein Bruton's tyrosine kinase (BTK).[5][6][7][10][11][12][13][14] Very common (>10% frequency) adverse effects include pneumonia, upper respiratory tract infection, sinusitis, skin infection, low neutrophil count, low platelet counts, headache, bleeding, bruising, diarrhea, vomiting, inflammation of mouth and lips, nausea, constipation, rash, joint pain, muscle spasms, musculoskeletal pain, fever, and edema.[5] Common (1–10% frequency) adverse effects include sepsis, urinary tract infection, non-melanoma skin cancer (basal-cell carcinoma, squamous cell carcinoma), low leukocyte count, low lymphocyte count, interstitial lung disease, tumor lysis syndrome,[15] high uric acid levels, dizziness, blurred vision, atrial fibrillation, subdural hematoma, nosebleeds, small bruises from broken blood vessels, high blood pressure, hives, and skin redness or blushing.Preclinical studies have shown that ibrutinib effectively inhibits malignant B-cell proliferation and survival in vivo as well as cell migration and substrate adhesion in vitro.[7] In early clinical studies, the activity of ibrutinib has been described to include a rapid reduction in lymphadenopathy accompanied by a transient lymphocytosis, suggesting that the drug might have direct effects on cell homing or migration to factors in tissue microenvironments.Ibrutinib has also been reported to reduce chronic lymphocytic leukemia cell chemotaxis towards the chemokines CXCL12 and CXCL13, and inhibit cellular adhesion following stimulation at the B-cell receptor (BCR).[34] In August 2018, ibrutinib in combination with rituximab was approved in the United States for the treatment of adults with Waldenström's macroglobulinemia (WM), a rare and incurable type of non-Hodgkin's lymphoma (NHL).
Drugs.comMedlinePlusLicense dataDailyMedPregnancycategoryRoutes ofadministrationBy mouthATC codeL01EL01Legal status ℞-only℞-onlyPharmacokineticProtein bindingMetabolismCYP2D6Elimination half-lifeExcretionIUPAC nameCAS NumberIUPHAR/BPSDrugBankChemSpiderChEMBLPDB ligandCompTox DashboardECHA InfoCardFormulaMolar massSMILESsmall moleculeirreversibly bindingBruton's tyrosine kinaseB-cell receptormantle cell lymphomachronic lymphocytic leukemiaWaldenström's macroglobulinemiaWorld Health Organization's List of Essential Medicinesindicatedpneumoniaupper respiratory tract infectionsinusitislow neutrophil countlow platelet countsinflammation of mouth and lipsjoint painsepsisurinary tract infectionbasal-cell carcinomasquamous cell carcinomalow leukocyte countlow lymphocyte countinterstitial lung diseasetumor lysis syndromehigh uric acid levelsdizzinessatrial fibrillationsubdural hematomasmall bruises from broken blood vesselshigh blood pressuregrapefruit juiceacrylamidelymphadenopathylymphocytosisERK1/2NF-κBTNF-αfibronectinchemotaxischemokinesCXCL12CXCL13rituximabofatumumabapoptosisCelera Genomicstool compoundcovalently binds its targetPharmacyclicsJohnson & JohnsonAbbVieFood and Drug Administrationgraft-versus-host diseaseobinutuzumabJanssen PharmaceuticaMedicareInflation Reduction ActEuropean Medicines AgencyWorld Health Organizationpublic domainThe Wall Street JournalThe Washington PostNational Cancer InstituteTargeted cancer therapyantineoplastic agentsmonoclonal antibodiesReceptor tyrosine kinaseHER1/EGFRCetuximabPanitumumabHER2/neuPertuzumabTrastuzumab+hyaluronidaseTrastuzumab emtansineTrastuzumab deruxtecanZanidatamabCatumaxomabEdrecolomabVEGF-ABevacizumabLeukemialymphomalymphoidGlofitamabElranatamabMosunetuzumabIbritumomabTositumomabBrentuximabAlemtuzumabmyeloidGemtuzumab ozogamicinAmivantamabAtezolizumabAvelumabAxatilimabBelantamab mafodotinBermekimabBlinatumomabCemiplimabCosibelimabDaratumumabDinutuximab betaDostarlimabDurvalumabElotuzumabEnfortumab vedotinEpcoritamabInotuzumab ozogamicinIpilimumabIsatuximabLoncastuximab tesirineMirvetuximab soravtansineMogamulizumabMoxetumomab pasudotoxNaxitamabNecitumumabNivolumab+relatlimabOlaratumabOportuzumab monatoxPembrolizumabPolatuzumab vedotinRamucirumabRetifanlimabSacituzumab govitecanSerplulimabSugemalimabTafasitamabTalquetamabTarlatamabTeclistamabTislelizumabTisotumab vedotinToripalimabTremelimumabZenocutuzumabZolbetuximabTyrosine kinase inhibitorsAfatinibAumolertinibBrigatinibDacomitinibErlotinibGefitinibIcotinibLazertinibMobocertinibOlmutinibOsimertinibRociletinibVandetanibLapatinibNeratinibTucatinibDabrafenibEncorafenibTovorafenibVemurafenibRTK class IIIAvapritinibAxitinibMasitinibPazopanibRipretinibSorafenibSunitinibToceranibLestaurtinibGilteritinibCediranibFruquintinibLenvatinibNintedanibRegorafenibSemaxanibTivozanibAlectinibCeritinibCrizotinibEnsartinibLorlatinibEntrectinibFutibatinibInfigratinibLarotrectinibPemigatinibPralsetinibRepotrectinibSelpercatinibCabozantinibCapmatinibNon-receptorbcr-ablAsciminibBosutinibDasatinibImatinibNilotinibPonatinibRadotinibJanus kinaseBaricitinibFedratinibFilgotinibMomelotinibPacritinibRuxolitinibBinimetinibCobimetinibSelumetinibTrametinibBruton'sAcalabrutinibOrelabrutinibPirtobrutinibZanubrutinibfusion proteinAfliberceptproapoptoticprohibitinAdipotideexotoxinDenileukin diftitoxmTOR inhibitorsEverolimusRidaforolimusSirolimusTemsirolimushedgehogGlasdegibSonidegibVismodegibCDK inhibitorsAbemaciclibDalpiciclibPalbociclibRibociclibTrilaciclibAdagrasibSotorasibPi3K inhibitorsAlpelisibCopanlisibDuvelisibIdelalisibInavolisibParsaclisibRevumenibFibroblast growth factor receptorErdafitinibMidostaurinOdronextamabPexidartinibQuizartinibTebentafuspTepotinibTunlametinibVenetoclax