References
- MarriottJJO’ConnorPWEmerging therapies in relapsing-remitting multiple sclerosisRev Recent Clin Trials2010517918820500147
- OsiriMSheaBRobinsonVLeflunomide for treating rheumatoid arthritisCochrane Database Syst Rev20031CD00204712535423
- BartlettRRSchleyerbachRImmunopharmacological profile of a novel isoxazol derivative, HWA 486, with potential antirheumatic activity – I. Disease modifying action on adjuvant arthritis of the ratInt J Immunopharmacol198577183873420
- KornTMagnusTToykaKJungSModulation of effector cell functions in experimental autoimmune encephalomyelitis by leflunomide – mechanisms independent of pyrimidine depletionJ Leukoc Biol20047695096015328336
- PosevitzVTeriflunomide selectively suppresses antigen induced T cell expansion in a TCR avidity dependent fashionPaper presented at the 28th Congress of the European Committee for Treatment and Research in Multiple Sclerosis (ECTRIMS)October 10–13, 2012Lyon, France
- BruneauJMYeaCMSpinella-JaegleSPurification of human dihydro-orotate dehydrogenase and its inhibition by A77 1726, the active metabolite of leflunomideBiochem J19983362993039820804
- CherwinskiHMCohnRGCheungPThe immunosuppressant leflunomide inhibits lymphocyte proliferation by inhibiting pyrimidine biosynthesisJ Pharmacol Exp Ther1995275104310497473131
- FoxRIHerrmannMLFrangouCGMechanism of action for leflunomide in rheumatoid arthritisClin Immunol19999319820810600330
- RuckemannKFairbanksLDCarreyEALeflunomide inhibits pyrimidine de novo synthesis in mitogen-stimulated T-lymphocytes from healthy humansJ Biol Chem199827321682216919705303
- HerrmannMLSchleyerbachRKirschbaumBJLeflunomide: an immunomodulatory drug for the treatment of rheumatoid arthritis and other autoimmune diseasesImmunopharmacology20004727328910878294
- FairbanksLDBofillMRuckemannKSimmondsHAImportance of ribonucleotide availability to proliferating T-lymphocytes from healthy humans. Disproportionate expansion of pyrimidine pools and contrasting effects of de novo synthesis inhibitorsJ Biol Chem199527029682296898530356
- ElderRTXuXWilliamsJWGongHFinneganAChongASThe immunosuppressive metabolite of leflunomide, A77 1726, affects murine T cells through two biochemical mechanismsJ Immunol199715922279200434
- KornTToykaKHartungHPJungSSuppression of experimental autoimmune neuritis by leflunomideBrain20011241791180211522581
- SiemaskoKChongASJackHMGongHWilliamsJWFinneganAInhibition of JAK3 and STAT6 tyrosine phosphorylation by the immunosuppressive drug leflunomide leads to a block in IgG1 productionJ Immunol1998160158115889469413
- XuXWilliamsJWBremerEGFinneganAChongASInhibition of protein tyrosine phosphorylation in T cells by a novel immunosuppressive agent, leflunomideJ Biol Chem199527012398124037759480
- HoskinDWTaylorRMMakrigiannisAPJamesHLeeTDDose-dependent enhancing and inhibitory effects of A77 1726 (leflunomide) on cytotoxic T lymphocyte inductionInt J Immunopharmacol1998205055139818794
- MannaSKAggarwalBBImmunosuppressive leflunomide metabolite (A77 1726) blocks TNF-dependent nuclear factor-kappa B activation and gene expressionJ Immunol1999162209521029973483
- González-AlvaroIOrtizAMDomínguez-JiménezCAragón-BodiADíaz SánchezBSánchez-MadridFInhibition of tumour necrosis factor and IL-17 production by leflunomide involves the JAK/STAT pathwayAnn Rheum Dis2009681644165018957484
- MattarTKochharKBartlettRBremerEGFinneganAInhibition of the epidermal growth factor receptor tyrosine kinase activity by leflunomideFEBS Lett19933341611648224241
- MannaSKMukhopadhyayAAggarwalBBLeflunomide suppresses TNF-induced cellular responses: effects on NF-kappa B, activator protein-1, c-Jun N-terminal protein kinase, and apoptosisJ Immunol20001655962596911067959
- HamiltonLCVojnovicIWarnerTDA771726, the active metabolite of leflunomide, directly inhibits the activity of cyclo-oxygenase-2 in vitro and in vivo in a substrate-sensitive mannerBr J Pharmacol19991271589159610455314
- JankovicVSamardzicTStosic-GrujicicSPopadicDTrajkovicVCell-specific inhibition of inducible nitric oxide synthase activation by leflunomideCell Immunol2000199738010698616
- ZeydaMPoglitschMGeyereggerRDisruption of the interaction of T cells with antigen-presenting cells by the active leflunomide metabolite teriflunomide: involvement of impaired integrin activation and immunologic synapse formationArthritis Rheum2005522730273916142756
- Layseca-EspinosaEPedraza-AlvaGMontielJLT cell aggregation induced through CD43: intracellular signals and inhibition by the immunomodulatory drug leflunomideJ Leukoc Biol2003741083109312972508
- DimitrovaPSkapenkoAHerrmannMLSchleyerbachRKaldenJRSchulze-KoopsHRestriction of de novo pyrimidine biosynthesis inhibits Th1 cell activation and promotes Th2 cell differentiationJ Immunol20021693392339912218161
- DeageVBurgerDDayerJMExposure of T lymphocytes to leflunomide but not to dexamethasone favors the production by monocytic cells of interleukin-1 receptor antagonist and the tissue-inhibitor of metalloproteinases-1 over that of interleukin-1beta and metalloproteinasesEur Cytokine Netw199896636689889411
- CutoloMSulliAGhiorzoPPizzorniCCraviottoCVillaggioBAnti-inflammatory effects of leflunomide on cultured synovial macrophages from patients with rheumatoid arthritisAnn Rheumatic Dis200362297302
- KraanMCde KosterBMElferinkJGPostWJBreedveldFCTakPPInhibition of neutrophil migration soon after initiation of treatment with leflunomide or methotrexate in patients with rheumatoid arthritis: findings in a prospective, randomized, double-blind clinical trial in fifteen patientsArthritis Rheum2000431488149510902750
- KraanMCReeceRJBargECModulation of inflammation and metalloproteinase expression in synovial tissue by leflunomide and methotrexate in patients with active rheumatoid arthritis. Findings in a prospective, randomized, double-blind, parallel-design clinical trial in thirty-nine patients at two centersArthritis Rheum2000431820183010943872
- FuentealbaRAMarasaJDiamondMIPiwnica-WormsDWeihlCCAn aggregation sensing reporter identifies leflunomide and teriflunomide as polyglutamine aggregate inhibitorsHum Mol Genet20122166468022052286
- SanofiTeriflunomide [data on file]Paris, FranceSanofi2012
- LimsakunTMenguy-VacheronFMazarinCPharmacokinetics of oral teriflunomide, a novel oral disease-modifying agent under investigation for the treatment of multiple sclerosisPrograms and abstracts of the 62nd American Academy of Neurology Annual MeetingApril 10–17, 2010Toronto, ON, Canada
- TallantyreEEvangelouNConstantinescuCSSpotlight on teriflunomideInt MS J200815626818782502
- StorchMKStefferlABrehmUAutoimmunity to myelin oligodendrocyte glycoprotein in rats mimics the spectrum of multiple sclerosis pathologyBrain Pathol199886816949804377
- WeissertRWallströmEStorchMKMHC haplotype-dependent regulation of MOG-induced EAE in ratsJ Clin Invest1998102126512739739061
- KornTMitsdoerfferMKuchrooVKImmunological basis for the development of tissue inflammation and organ-specific autoimmunity in animal models of multiple sclerosisResults Probl Cell Differ201051437419513635
- MerrillJEHanakSPuSFTeriflunomide reduces behavioral, electrophysiological, and histopathological deficits in the Dark Agouti rat model of experimental autoimmune encephalomyelitisJ Neurol20092568910319169851
- StyrenSBarbierASelkDWettsteinJGBeneficial effects of teriflunomide in experimental allergic encephalomyelitisPaper presented at Society for Neuroscience Annual MeetingOctober 23–27, 2004San Diego, CA, USA
- O’ConnorPWLiDFreedmanMSA phase II study of the safety and efficacy of teriflunomide in multiple sclerosis with relapsesNeurology20066689490016567708
- ConfavreuxCLiDKFreedmanMSLong-term follow-up of a phase 2 study of oral teriflunomide in relapsing multiple sclerosis: safety and efficacy results up to 8.5 yearsMult Scler2012181278128922307384
- FreedmanMSWolinskyJSWamilBTeriflunomide added to interferon-beta in relapsing multiple sclerosis: a randomized phase II trialNeurology2012781877188522622860
- FreedmanMSWJFranginGAOral teriflunomide or placebo added to glatiramer acetate for 6 months in patients with relapsing multiple sclerosis: safety and efficacy resultsPrograms and abstracts of the 62nd American Academy of Neurology Annual MeetingApril 10–17, 2010Toronto, ON, Canada
- SanofiEfficacy and safety of teriflunomide in patients with relapsing multiple sclerosis and treated with interferon-beta (TERACLES)2012 Available from: http://clinicaltrials.gov/ct2/show/NCT01252355?term=teriflunomide&rank=3Accessed October 30, 2012
- SanofiLong term safety of teriflunomide when added to interferon-beta or glatiramer acetate in patients with multiple sclerosis2012 Available from: http://clinicaltrials.gov/ct2/show/NCT00811395?term=teriflunomide&rank=4Accessed October 30, 2012
- Bar-OrAFreedmanMSKremenchutzkyFEffect of teriflunomide on immune responses to seasonal influenza vaccination in patients with relapsing multiple sclerosis: results from the TERIVA studyPaper presented at the 28th Congress of the European Committee for Treatment and Research in Multiple Sclerosis (ECTRIMS)October 10–13, 2012Lyon, France
- O’ConnorPWolinskyJSConfavreuxCRandomized trial of oral teriflunomide for relapsing multiple sclerosisN Engl J Med20113651293130321991951
- SanofiLong term safety and efficacy study of teriflunomide 7 mg or 14 mg in patients with relapsing-remitting multiple sclerosis2012 Available from: http://clinicaltrials.gov/ct2/show/NCT00803049?term=teriflunomide&rank=13Accessed October 30, 2012
- KapposLComiGConfavreuxCThe efficacy and safety of teriflunomide in patients with relapsing MS: results from TOWER, a phase III, placebo-controlled studyPaper presented at the 28th Congress of the European Committee for Treatment and Research in Multiple Sclerosis (ECTRIMS)October 10–13, 2012Lyon, France
- VermerschPCzlonkowskaAGrimaldiLMEA multicenter, randomized, parallel-group, rater-blinded study comparing the effectiveness and safety of teriflunomide and subcutaneous interferon beta-1a in patients with relapsing multiple sclerosisPaper presented at the 28th Congress of the European Committee for Treatment and Research in Multiple Sclerosis (ECTRIMS)October 10–13, 2012Lyon, France
- SanofiPhase III study with teriflunomide versus placebo in patients with first clinical symptom of multiple sclerosis (TOPIC)2012 Available from: http://clinicaltrials.gov/ct2/show/NCT00622700?term=TOPIC&rank=1Accessed October 30, 2012
- BrentRLTeratogen update: reproductive risks of leflunomide (Arava); a pyrimidine synthesis inhibitor: counseling women taking leflunomide before or during pregnancy and men taking leflunomide who are contemplating fathering a childTeratology20016310611211241434
- FukushimaRKanamoriSHirashibaMTeratogenicity study of the dihydroorotate-dehydrogenase inhibitor and protein tyrosine kinase inhibitor Leflunomide in miceReprod Toxicol20072431031617604599
- ChambersCDJohnsonDLRobinsonLKBirth outcomes in women who have taken leflunomide during pregnancyArthritis Rheum2010621494150320131283
- CassinaMJohnsonDLRobinsonLKPregnancy outcome in women exposed to leflunomide before or during pregnancyArthritis Rheum2012642085209422307734
- KieseierBBenamorMBenzerdjebHStüveOPregnancy outcomes from the teriflunomide clinical development programme: retrospective analysis of the teriflunomide clinical trial databasePaper presented at the 28th Congress of the European Committee for Treatment and Research in Multiple Sclerosis (ECTRIMS)October 10–13, 2012Lyon, France
- WhiteDHLynskeyNVJonesPBLeflunomide use in New Zealand. A national prospective post-marketing studyIntern Medicine J20093995102
- WarnatzKPeterHHSchumacherMInfectious CNS disease as a differential diagnosis in systemic rheumatic diseases: three case reports and a review of the literatureAnn Rheumatic Dis2003625057
- RahmlowMShusterEADominikJLeflunomide-associated progressive multifocal leukoencephalopathyArch Neurol2008651538153919001176
- GoldRWolinskyJSPathophysiology of multiple sclerosis and the place of teriflunomideActa Neurol Scand2011124758420880295