leflunomide / Generic mfg. 
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  • ||||||||||  leflunomide / Generic mfg.
    [VIRTUAL] STP938, a Novel, Potent and Selective Inhibitor of CTP Synthase 1 (CTPS1) Is a Targeted Therapy Specifically Blocking De Novo Nucleotide Synthesis in Lymphomas and Leukemias (Poster Hall (Virtual Meeting)) -  Nov 5, 2020 - Abstract #ASH2020ASH_952;    
    The pyrimidine synthesis pathway has been proposed as a metabolic sensitivity for cancer and over the past few decades several inhibitors of enzymes involved in the pathway have been evaluated in clinical trials (e.g. avicin, CPEC, PALA, leflunomide) primarily in solid tumors with limited efficacy and unacceptable toxicity...This disruption of de novo nucleotide synthesis by CTPS1 inhibition selectively induces apoptosis in lymphocyte cells but not in other cell types that are able to rely upon CTPS2 for their CTP synthesis. Orally bioavailable small molecule inhibitors of CTPS1 exert an anti-tumor effect in vivo in murine xenograft models and thus inhibition of CTPS1 represents a novel targeted approach to treat hematological malignancies.
  • ||||||||||  Enbrel (etanercept) / Pfizer, Amgen
    Enrollment closed, Enrollment change:  CareRA2020: COBRA-Slim With or Without Fast Access to TNF Blockade for Remission Induction in Early RA (clinicaltrials.gov) -  Nov 4, 2020   
    P4,  N=284, Active, not recruiting, 
    Orally bioavailable small molecule inhibitors of CTPS1 exert an anti-tumor effect in vivo in murine xenograft models and thus inhibition of CTPS1 represents a novel targeted approach to treat hematological malignancies. Recruiting --> Active, not recruiting | N=442 --> 284
  • ||||||||||  leflunomide / Generic mfg.
    Enrollment open, Trial initiation date:  Leflunomide for the Treatment of Relapsed or Refractory CD30+ Lymphoproliferative Disorders (clinicaltrials.gov) -  Oct 29, 2020   
    P2,  N=12, Recruiting, 
    A large-sample randomized double-blind controlled study with a long follow-up period is needed to verify the efficacy of LEF combined with prednisone. Not yet recruiting --> Recruiting | Initiation date: Jul 2020 --> Nov 2020
  • ||||||||||  leflunomide / Generic mfg.
    Trial completion date, Trial primary completion date:  Leflunomide in Mild COVID-19 Patients (clinicaltrials.gov) -  Oct 28, 2020   
    P1,  N=20, Recruiting, 
    Not yet recruiting --> Recruiting | Initiation date: Jul 2020 --> Nov 2020 Trial completion date: Sep 2020 --> Feb 2021 | Trial primary completion date: Sep 2020 --> Feb 2021
  • ||||||||||  Actemra IV (tocilizumab) / Roche, JW Pharma
    Review, Journal:  Managing rheumatoid arthritis during COVID-19. (Pubmed Central) -  Oct 27, 2020   
    • Initiation of high-dose steroids, DMARDs, and biologics, if the clinical situation demands so, can be done. • Maintenance biologic therapy for stable patients should be individualized by the treating physician.
  • ||||||||||  Otezla (apremilast) / Amgen
    Clinical, Reimbursement, Journal, Medicare:  Treatment of Medicare Patients with Moderate-to-Severe Psoriasis who Cannot Afford Biologics or Apremilast. (Pubmed Central) -  Oct 25, 2020   
    Specifically, alternative treatment options to biologics and small-molecule inhibitors are discussed and include topical therapies, phototherapy, methotrexate, acitretin, and cyclosporine and for psoriatic arthritis include corticosteroids and leflunomide. The specific risks and benefits of these therapies in the elderly population are provided, allowing providers to make patient-specific decisions about optimal regimens.
  • ||||||||||  hydroxychloroquine / Generic mfg., acyclovir / Generic mfg., leflunomide / Generic mfg.
    [VIRTUAL] SYMPTOMATIC PULMONARY AND INTRACRANIAL NODULES IN A PATIENT WITH LONGSTANDING, UNCONTROLLED RHEUMATOID ARTHRITIS () -  Oct 12, 2020 - Abstract #CHEST2020CHEST_2359;    
    Rheumatologically, the patient had RA flares multiple times per month despite maximal doses of hydroxychloroquine, leflunomide, and methrotrexate (MTX)...Repeat imaging showed multiple new bilateral pulmonary nodules up to 2.3 cm with stable intracranial nodules despite empiric acyclovir... This report highlights the need to consider RA as a potentially reversible cause when considering unexplained systemic findings, as well as the need for more research into treatment of extraarticular manifestations of RA.
  • ||||||||||  leflunomide / Generic mfg.
    [VIRTUAL] CLINICAL AND LABORATORY CHARACTERISTICS OF LEFLUNOMIDE-INDUCED LIVER INJURY IN INDIA AND THE USA () -  Oct 11, 2020 - Abstract #AASLD2020AASLD_1186;    
    Leflunomide-induced liver injury is predominantly hepatocellular and, in the Indian cohort, is more common in women where it was frequently accompanied by severe skin injury and was associated with high mortality. The differences in skin involvement, immunoallergic features and outcomes among patients from India vs. the US suggest that genetic or environmental factors may be important in the pathogenesis of leflunomide-induced liver injury.
  • ||||||||||  Actemra IV (tocilizumab) / Roche, JW Pharma
    [VIRTUAL] Efficacy and Safety of Tocilizumab in Patients with Giant Cell Arteritis and Visual Impairment () -  Oct 8, 2020 - Abstract #ACRARHP2020ACR_ARHP_2629;    
    4/19 patients presented with visual disturbances on oral prednisone and 2/19 patients were on csDMARDs (leflunomide, MTX) for polymyalgia. Inhibition of IL-6 with TCZ represents a valuable treatment option to prevent deterioration of visual complications in GCA patients with initial visual impairment.
  • ||||||||||  cyclophosphamide intravenous / Generic mfg.
    [VIRTUAL] Use of Contraceptive Methods in Mexican Women with Rheumatic Diseases () -  Oct 8, 2020 - Abstract #ACRARHP2020ACR_ARHP_2488;    
    Only 70% of the women with rheumatic diseases received a contraceptive counseling and despite this 42% continued using an ineffective method. It is necessary to promote the counseling and use of contraception and provide a multidisciplinary support among this high-risk population.
  • ||||||||||  Remicade (infliximab) / Mitsubishi Tanabe, J&J, Humira (adalimumab) / Eisai, AbbVie, Cimzia (certolizumab pegol) / Astellas, UCB, Eli Lilly
    [VIRTUAL] Treatment with Certolizumab Pegol in Refractory Uveitis Secondary to Inmune-Mediated Inflammatory Diseases. Multicenter Study of 39 Patients () -  Oct 8, 2020 - Abstract #ACRARHP2020ACR_ARHP_1882;    
    Background/Purpose: Infliximab and adalimumab therapy has significantly improved the prognosis of patients with non-infectious refractory uveitis...Previous CZP, patients received: oral prednisone (n=18) methylprednisolone bolus (1), methotrexate (22), azathioprine (10), cyclosporine (4), leflunomide (2), mycophenolate mofetil (2) and cyclophosphamide (1)... CZP seems to be effective and safe in patients with refractory uveitis due to IMID.
  • ||||||||||  leflunomide / Generic mfg.
    [VIRTUAL] Leflunomide: A Safe and Effective Alternative in Systemic Lupus Erythematosus () -  Oct 8, 2020 - Abstract #ACRARHP2020ACR_ARHP_1480;    
    Hydroxychloroquine administration may be a protective factor against fatty liver. Treatment with LEF in SLE seems to be an effective and safe option, particularly for joint symptoms, with significant improvement observed in PGA, SLEDAI and ESR, as well as a 48.6% of joint remission after its onset.
  • ||||||||||  Remicade (infliximab) / Mitsubishi Tanabe, J&J, Humira (adalimumab) / Eisai, AbbVie
    [VIRTUAL] Initial Pharmaceutical Management in a National Cohort of Elderly-Onset Rheumatoid Arthritis Patients () -  Oct 8, 2020 - Abstract #ACRARHP2020ACR_ARHP_1435;    
    In a national of elderly-onset RA patients, hydroxychloroquine instead of methotrexate was the preferred initial cDMARD, which could lead to inadequate control of disease. Further, with increasing age, the doses of cDMARDs prescribed reduced which could further contribute to reduced control of early disease.
  • ||||||||||  [VIRTUAL] Is Sex-adjusted Treatment in Early-PsA Justified? () -  Oct 8, 2020 - Abstract #ACRARHP2020ACR_ARHP_927;    
    Initial treatment strategies were similar in both sexes. However, over time women received methotrexate for a shorter period, were more often switched to other csDMARDs and started later with bDMARDs.
  • ||||||||||  Benlysta (belimumab) / GSK
    [VIRTUAL] Management of Rheumatic Diseases During COVID-19: A National Veterans Affairs Survey of Rheumatologists () -  Oct 8, 2020 - Abstract #ACRARHP2020ACR_ARHP_620;    
    A majority would hold methotrexate or leflunomide (66%) and glucocorticoids of 20 mg/day or higher (52%) for 2 weeks or less (Figure 3); and would hold non-TNF biologics (76%), anti TNF-biologics (85%), Janus-kinase inhibitors (78%), anti IL-17/23 biologics (82%), belimumab (77%)immunosuppressive drugs such as azathioprine (64%), for 3-8 weeks (Figure 3)... A better understanding of COVID-19 rheumatic disease healthcare issues using a health-system approach can inform improve the care of Veterans with rheumatic disease and their providers.
  • ||||||||||  chloroquine phosphate / Generic mfg., hydroxychloroquine / Generic mfg., cyclophosphamide intravenous / Generic mfg.
    [VIRTUAL] Hydroxychloroquine and Chloroquine and Hospitalizations for Viral Infection in the Pre-COVID-19 Era () -  Oct 8, 2020 - Abstract #ACRARHP2020ACR_ARHP_577;    
    Our models included demographic variables (age, sex), setting in which viral infection was initially identified (ER or other), underlying condition (RA or SLE), comorbidities, and use of other medications (modeled in the same way as the main exposure): methotrexate (MTX), mycophenolate (MMF), azathioprine, other DMARDs (cyclophosphamide, sulfasalazine, and leflunomide), corticosteroids, biologics, and NSAIDs. While we saw no clear effect of HCQ/CQ, comorbidity, ER presentation, older age, and MMF, azathioprine, and corticosteroids were all significantly associated with hospitalized viral infection in RA and SLE.
  • ||||||||||  teriflunomide / Generic mfg., leflunomide / Generic mfg.
    Journal:  Novel and potent inhibitors targeting DHODH are broad-spectrum antivirals against RNA viruses including newly-emerged coronavirus SARS-CoV-2. (Pubmed Central) -  Oct 7, 2020   
    Our results are the first to validate that DHODH is an attractive host target through high antiviral efficacy in vivo and low virus replication in DHODH knock-out cells. This work demonstrates that both S312/S416 and old drugs (Leflunomide/Teriflunomide) with dual actions of antiviral and immuno-regulation may have clinical potentials to cure SARS-CoV-2 or other RNA viruses circulating worldwide, no matter such viruses are mutated or not.
  • ||||||||||  Clinical, Journal:  Effect of Moxibustion on the Serum Levels of MMP-1, MMP-3, and VEGF in Patients with Rheumatoid Arthritis. (Pubmed Central) -  Oct 7, 2020   
    Above all, the contents of IL-1β, TNF-α, MMP-1, MMP-3, and VEGF in the treatment group decreased more significantly than those in the control group (P < 0.05). The improvement effect of moxibustion on the clinical symptoms of RA patients may be related to influence on the contents of IL-1β, TNF-α, MMP-1, MMP-3, and VEGF, and moxibustion may play a potential role in bone protection.
  • ||||||||||  leflunomide / Generic mfg.
    Trial completion date, Trial primary completion date:  Anti-rheumatic Drug Use and Risk of COVID-19 Infection in Rheumatoid Arthritis Patients (clinicaltrials.gov) -  Oct 5, 2020   
    P=N/A,  N=600, Enrolling by invitation, 
    The improvement effect of moxibustion on the clinical symptoms of RA patients may be related to influence on the contents of IL-1β, TNF-α, MMP-1, MMP-3, and VEGF, and moxibustion may play a potential role in bone protection. Trial completion date: Jul 2020 --> Dec 2020 | Trial primary completion date: Jun 2020 --> Dec 2020
  • ||||||||||  acyclovir / Generic mfg., leflunomide / Generic mfg.
    Journal:  Leflunomide increased the renal exposure of acyclovir by inhibiting OAT1/3 and MRP2. (Pubmed Central) -  Oct 3, 2020   
    Here we used a specific MRP inhibitor MK571 and probenecid (OAT1/3 and MRP2 inhibitor) to assess the effects of MRP2 and OAT1/3 on the pharmacokinetics and tissue distribution of acyclovir in rats...These results suggest that LEF/TER increased the kidney accumulation of acyclovir by inhibiting the efflux transporter MRP2, which increased its kidney/plasma ratio and renal injury risk. However, the inhibitory effects of LEF/TER on OAT1/3 reduced the tubular cells' uptake of acyclovir and increased the plasma concentration.
  • ||||||||||  Actemra IV (tocilizumab) / Roche, JW Pharma, Humira (adalimumab) / Eisai, AbbVie
    Preclinical, Journal:  The in vitro effect of antirheumatic drugs on platelet function. (Pubmed Central) -  Oct 2, 2020   
    Results indicate that teriflunomide, prednisolone, and tocilizumab inhibit, and adalimumab increases platelet aggregation. The study suggests that the majority of antirheumatic drugs mainly reduced cardiovascular risk through indirect effects (e.g., reducing inflammation).
  • ||||||||||  Xeljanz (tofacitinib) / Pfizer, Marche Polytechnic University
    Journal:  Oral disease-modifying antirheumatic drugs and immunosuppressants with antiviral potential, including SARS-CoV-2 infection: a review. (Pubmed Central) -  Sep 23, 2020   
    In fact, there are other immunosuppressants known with antiviral activities, including cyclosporine A, hydroxyurea, minocycline, mycophenolic acid, mycophenolate mofetil, leflunomide, tofacitinib, and thalidomide...However, some disease-modifying antirheumatic drugs (DMARDs) with inherent antiviral activity would be a reasonable choice in the situation of concomitant viral infections and flare up of autoimmune diseases. This review covers DMARDs of treatment potential for SARS-CoV-2 in part I, and antiviral mechanisms plus trial evidence for viruses other than SARS-CoV-2 in part II.
  • ||||||||||  leflunomide / Generic mfg.
    Journal:  Mitochondrial fusion exploits a therapeutic vulnerability of pancreatic cancer. (Pubmed Central) -  Sep 19, 2020   
    We found that the chief tumor suppressive mechanism of mitochondrial fusion was enhanced mitophagy, which proportionally reduced mitochondrial mass and ATP production. These data suggest that mitochondrial fusion is a specific and druggable regulator of pancreatic cancer growth that could be rapidly translated to the clinic.