Abemaciclib
Abemaciclib, sold under the brand name Verzenio among others, is a medication for the treatment of advanced or metastatic breast cancers.[4] It was designated as a breakthrough therapy for breast cancer by the US Food and Drug Administration (FDA) in October 2015.[8] These enzymes are responsible for phosphorylating and thus deactivating the retinoblastoma protein, which plays a role in cell cycle progression from the G1 (first gap) to the S (synthesis) phase.The substance is mainly metabolized by the liver enzyme CYP3A4 to N-desethylabemaciclib (M2), and to a lesser extent to hydroxy derivatives (M18, M20) and another oxidative metabolite (M1).[13] Abemaciclib was approved by the FDA in September 2017 either in combination with fulvestrant or as a monotherapy for women with HR+, HER2- advanced or metastatic breast cancer that had progressed while receiving endocrine therapy.
Drugs.comLicense dataDailyMedRoutes ofadministrationBy mouthATC codeL01EF03Legal status ℞-only℞-onlyPharmacokineticBioavailabilityProtein bindingElimination half-lifeExcretionIUPAC nameCAS NumberDrugBankChemSpiderChEMBLPDB ligandCompTox DashboardECHA InfoCardFormulaMolar massSMILESmedicationbreast cancersdevelopedEli LillyCDK inhibitorbreakthrough therapyFood and Drug Administrationhuman epidermal growth factor receptor 2fulvestrantplaceboprogression-free survivalnausealeukopenianeutropeniaanemiathrombocytopeniafatigueCYP3A4ketoconazoleblood plasmarifampicinpalbociclibribociclibcyclin-dependent kinase 4cyclin-dependent kinase 6phosphorylatingretinoblastoma proteincell cyclefirst gapsynthesisapoptosismetaboliteplasma proteinshydroxyoxidativePhase IIIhead and neck squamous cell carcinomabiliary tract carcinomabrain tumorsneurofibromatosisKaposi sarcomarenal cell carcinomaMantle Cell lymphomaSuzuki couplingBuchwald–Hartwig aminationreductive aminationLeuckart reactionHealth CanadaLee EYchemotherapeutic agentsantineoplastic agentsM phasemicrotubuleVinca alkaloidsVinblastineVincristineVindesineVinflunineVinorelbineTaxanesCabazitaxelDocetaxelLarotaxelOrtataxelPaclitaxelTesetaxelEpothilonesIxabepiloneDNA replicationantimetabolitesS phaseFolic acidDihydrofolate reductase inhibitorAminopterinMethotrexatePemetrexedPralatrexateThymidylate synthase inhibitorRaltitrexedPurineAdenosine deaminase inhibitorPentostatinHalogenatedribonucleotide reductase inhibitorsCladribineClofarabineFludarabineNelarabineRabacfosadineThiopurineMercaptopurineTioguaninePyrimidineCapecitabineCarmofurDoxifluridineFloxuridineFluorouracilTegafur+gimeracil/oteracil