Filgotinib

[3][6][7] Filgotinib is indicated for the treatment of moderate to severe active rheumatoid arthritis in adults who have responded inadequately to, or who are intolerant to one or more disease‑modifying anti‑rheumatic drugs (DMARDs).[medical citation needed] Nonetheless it is thought that JAK2 inhibition might lead to anemia and thrombopenia by interference with erythropoietin and thrombopoietin and granulocyte-macrophage colony-stimulating factor.[citation needed] It was shown in Phase I studies that the pharmacokinetics of filgotinib metabolism is independent of hepatic CYP450 enzymatic degradation.[15] In November 2011 Galapagos released the results of their Phase II study (identification: NCT01384422, Eudract: 2010-022953-40) in which 36 rheumatoid arthritis patients were treated who showed a suboptimal clinical response to methotrexate treatment.As a result of this study, the company stated that "GLPG0634 shows one of the highest initial response rates ever reported for rheumatoid arthritis treatments".[19][20] Galapagos announced that the drug met key efficacy endpoints, showed ACR70 responses up to 39%, and maintained its safety profile.[28] Due to concerns over testicular toxicity in males, the MANTA study is examining the safety of the drug in the context of treating ulcerative colitis.[29][full citation needed] Despite these concerns, the FDA allowed a 200-mg daily dose for males in the Phase III FINCH trials.
Routes ofadministrationBy mouthDrug classJanus kinase inhibitorATC codeL04AF04Legal statusPharmacokineticElimination half-lifeIUPAC nameCAS NumberIUPHAR/BPSDrugBankChemSpiderChEMBLPDB ligandCompTox DashboardFormulaMolar massSMILESrheumatoid arthritisBelgianGalapagos NVindicatedmethotrexateupadacitinibtofacitinibbaricitinibproinflammatorycytokinesanemiathrombopeniaerythropoietinthrombopoietingranulocyte-macrophage colony-stimulating factorNew Drug Applicationpriority reviewFood and Drug AdministrationCommittee for Medicinal Products for Human UseEuropean Medicines AgencyPhase IIb programpharmacokineticsCYP450carboxylesterasesACR20 scoredouble blindplacebo-controlledadalimumabDMARDsGilead SciencesClinicalTrials.govImmunosuppressive drugsImmunosuppressantsAntimetabolitespurine synthesis inhibitorsAzathioprineMycophenolic aciddihydroorotate 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