Leflunomide

This page contains recent news articles, when available, and an overview of Leflunomide but does not offer medical advice. You should contact your physician with regard to any health issues or concerns.

Overview:

Leflunomide (when available)

Pharmacology and use:
Leflunomide is a pyrimidine synthesis inhibitor indicated in adults for the treatment of active rheumatoid arthritis (RA). RA is an auto-immune disease characterized by high T-cell activity. T cells have two pathways to synthesize pyrimidines: the salvage pathways and the de novo synthesis. At rest, T lymphocytes meet their metabolic requirements by the salvage pathway. Activated lymphocytes need to expand their pyrimidine pool 7 - to 8 -fold, while the purine pool is expanded only 2- to 3-fold. To meet the need for more pyrimidines, activated T cells use the de novo pathway for pyrimidine synthesis. Therefore, activated T cells, which are dependent on de novo pyrimidine synthesis, will be more affected by leflunomide’s inhibition of dihydroorotate dehydrogenase than other cell types that use the salvage pathway of pyrimidine synthesis. For the treatment of active rheumatoid arthritis (RA)

Mechanism Of Action:
Leflunomide is an isoxazole immunomodulatory agent which inhibits dihydroorotate dehydrogenase (an enzyme involved in de novo pyrimidine synthesis) and has antiproliferative activity. Specifically Leflunomide blocks the de novo synthesis of pyrimidines, thus preventing the proliferation of activated T cells. Several in vivo and in vitro experimental models have demonstrated an anti-inflammatory effect. Following oral administration, leflunomide is metabolized to an active metabolite A77 1726 which is responsible for essentially all of its activity in vivo

News Articles on Leflunomide

Health Chat  -  20 Apr 2009
Since then other drugs with variable immune normalising properties have been discovered - sulfasalazine, methotrexate and leflunomide are the most useful. Mmegi Online

New and emerging therapies  -  ‎Mar 8, 2009‎
...mycophenolate mofetil, chlorambucil, cyclosporine, TNF-alpha inhibitors, leflunomide or rituximab. Other therapies include interferon and ribavarin, Modern Medicine

What's the evidence for leflunomide?  -  Jan 21, 2009
...[3] All three studies[5] [1] [2] found that people taking leflunomide had fewer swollen and tender joints than those taking a placebo (a pretend treatment). guardian.co.uk,

Leflunomide effective as co-therapy in RA  -  Jan 15, 2009
NEW YORK (Reuters Health) - The immune-modulating drug leflunomide is effective as co-therapy with drugs that block the inflammation-producing protein TNF Reuters India,

Drugs for psoriasis  -  Jan 21, 2009
...[32] Treatment with leflunomide is still experimental. We need more research to know how well it works and how safe it is for people with psoriasis. guardian.co.uk,

What treatments work for rheumatoid arthritis?  -  Jan 21, 2009
Leflunomide: The brand name for this drug is Arava. More... Penicillamine: The brand name for this drug is Distamine. More... Antimalarials: These drugs are guardian.co.uk,

TNF-α抑制剂�?��?�应用甲氨喋呤或leflunomide的疗效比较  -  Jan 14, 2009
...医学空间（MEDcyber.com）1月15日消�?�—近期�?�表在《Annals of the Rheumatic Diseases》上的一篇文章指出leflunomide 医学空间,

'레플루노마�?�드' 류마티스성관절염 치료 효과�?  -  Jan 15, 2009
...레플루노마�?�드(leflunomide)�?�는 체내 면역력�?� 조절하는 약물�?� 류마티스성관절염�?� 앓는 사람�?서 염�?�?� 유발하는 단백질�?� 종양괴사�?��?를 차단하는 약물과 병행 Medical Today,

Arthritis Research Shows Better Management More Important Than New ...  -  Dec 1, 2008
...in terms of disease activity, disability and radiological progression in the period after the Spanish launch of Leflunomide and the TNF antagonists. Science Daily (press release)

Medicare drug plan can be misleading  -  Dec 16, 2008
...cost of Arava at $532.48 minus the cost of the generic equivalent Leflunomide at $35.51), bringing the actual cost of the drug to $534.17 per month. Times-Standard,

Induction therapies for proliferative lupus nephritis  -  Dec 9, 2008
Leflunomide has also been reported to be useful in the management of resistant LN. 16 Although none of these agents should be the first line for induction The Virtual Medical Centre,

한림제약(회장 김재윤)�?� 류마티스관절염�?� 징후 �? �?�?완화�? ...  -  Dec 22, 2008
...�?�장단위를 30T, 100T로 �?산하여 조제�?� 편리성�?� �?�모했다. 아레�?� 정�?� isoxazole유�?�체로 주요 작용기전�?� Pyrimidine synthesis inhibitor로 면역세�?� �?�? �? 메디파나뉴스,

Combination Cidofovir Plus Leflunomide Clears or Reduces Serum BK ...  -  Oct 28, 2008
By Maggie Schwarz WASHINGTON, DC -- October 28, 2008 -- Combination cidofovir plus leflunomide either cleared or significantly reduced serum BK viral load DG News

First-Ever Clinical Guidelines for Psoriatic Arthritis Released  -  Oct 29, 2008
Available evidence supports first-line treatment with sulfasalazine, leflunomide, methotrexate, and cyclosporine, Christopher T. Ritchlin, MD, MedPage Today,

Guidelines Issued for Management of Psoriatic Arthritis  -  Oct 28, 2008
Available evidence supports use of the following DMARDs as first-line therapy: sulfasalazine, leflunomide, methotrexate, and cyclosporine. Medscape (registration)

Ciclofosfamide incrementa rischio di neoplasie ematologiche in AR  -  Nov 6, 2008
...azatioprina, leflunomide, ciclofosfamide, ciclosporina, sali di oro, minociclina, penicillamina e anti-TNF-alfa) e dall’assenza di diagnosi di neoplasie Pillole.org,

岂止是表�?�问题牛皮癣关节炎  -  Oct 30, 2008
...则需�?更加强效的调节型抗风湿�?�，例如methotrexate (抗肿瘤类)�?sulfasalazine (抗风湿类)�? cyclosporine (抗孢霉素/抗风湿)和leflunomide �?�洋商报,

Polyomavirus-Associated Nephropathy Presenting Late After ...  -  Oct 17, 2008
Immunosuppression was modified by downward titration of cyclosporine and conversion of mycophenolate mofetil to leflunomide. Medscape (subscription)

Clinical Trials Update: Sept. 30, 2008  -  Sep 30, 2008
...have had an inadequate response to treatment with at least on anti-TNF agent, and are currently taking leflunomide or methotrexate, you may qualify for Washington Post,

Managing Rheumatoid Arthritis Patients With Concomitant ...  -  Sep 29, 2008
Moreover, in this patient group (with baseline concomitant hypertension), the use of leflunomide should be closely monitored (eg, weekly evaluation of blood Medscape (subscription)

I farmaci di fondo nell'artrite reumatoide: una revisione sistematica  -  Sep 28, 2008
La farmacoterapia dei pazienti con artrite reumatoide comprende l’utilizzo di DMARD sintetici (idrossiclorochina, leflunomide, metotrexato, e sulfasalazina) Pillole.org,

Treating Rheumatoid Arthritis: New Guidelines Developed For Physicians  -  Aug 24, 2008
Methotrexate or leflunomide therapy is recommended for most RA patients. Anti-TNF agents etanercept, infliximab, or adalimumab along with methotrexate can Science Daily (press release)

New Treatment Guidelines for Rheumatoid Arthritis  -  Aug 26, 2008
Leflunomide or methotrexate therapy for most RA patients. In new RA cases or those where symptoms are becoming more severe, an anti-TNF agent can be MedHeadlines,

Daily News: College Issues RA Treatment Recommendations  -  Aug 27, 2008
The college recommends leflunomide or methotrexate as monotherapy for patients with disease of any duration or degree of activity; hydroxychloroquine or Nurse.com,

New-age Medication for Rheumatoid Arthritis  -  Aug 25, 2008
Leflunomide gives respite from symptoms and stops the disease from spreading in the system. It de-activates an important enzyme that functions to activate Corsavoo.com,

Disseminated cutaneous herpes simplex virus-1 in a patient with ...  -  Aug 26, 2008
Case presentationOur patient presented with an inflammatory arthritis which failed to respond to both methotrexate and leflunomide, and sulphasalazine 7thSpace Interactive (press release),

Nuove linee guida per l’artrite reumatoide  -  Sep 4, 2008
...riassunte in quattro punti chiave: per la maggior parte dei pazienti con artrite reumatoide è raccomandata la terapia con metotressato o leflunomide; Corriere della Sera,

Terapias biológicas  -  Aug 25, 2008
...como el metotrexate o leflunomide, o en quienes, por las características iniciales de su enfermedad implican que tendrá un curso más severo o agresivo, La Prensa (Panamá),

Stockwire.com: (OTCBB:SOBM) Sinobiomed, Inc. just released some ...  -  Aug 21, 2008
...viral infections, and other conditions; Leflunomide, a drug for the treatment of rheumatoid arthritis; and Recombinant Acidic Fibroblast Growth Factor, Trading Markets (press release),

Farmaci anti-TNF: gravi reazioni avverse cutanee  -  Sep 3, 2008
Il 71% ha riportato di aver assunto in modo concomitante 1 o più farmaci ( Sulfalasalazina, Mercaptopurina, Leflunomide ). XagenaSalute,

New guidelines for treating rheumatoid arthritis  -  Jul 24, 2008
Methotrexate or leflunomide therapy is recommended for most RA patients. Anti-TNF agents etanercept, infliximab, or adalimumab along with methotrexate can HULIQ (press release),

Biologics and Combinations Top Arthritis Recommendations  -  Jul 24, 2008
The guidelines panel recommended leflunomide (Arava) or methotrexate monotherapy as initial treatment for virtually all patients, regardless of disease MedPage Today,

Assolti i farmaci: non aumentano le infezioni  -  Aug 3, 2008
...rischio di infezioni connesso all'uso di due farmaci che spesso fanno parte della terapia anti-artrite reumatoide, il metotressato e la leflunomide. Corriere della Sera,

Keerzijden van knappe middelen  -  Jul 31, 2008
Als kinderreumatoloog mag ik leflunomide wel off-label voorschrijven, maar het is voor de patiënten en de ouders beter als het netjes is geregistreerd. Medisch Contact,

Quali terapie funzionano meglio nell'artrite reumatoide?  -  Aug 4, 2008
La ricerca non ha evidenziato differenze di efficacia fra i DMARDs sintetici (methotrexato, leflunomide, sulfasalazina) e farmaci biologici anti-tumor Pillole.org,

Arthritis pain medications and their effects  -  May 13, 2008
...they don't protect the joints; "disease-modifying agents," however, such as methotrexate, leflunomide, adalimumab, etanercept or infliximab, Newsday,

Arthritis drugs may curb cardiovascular mishaps  -  Apr 2, 2008
However, after adjustment, the researchers found that prolonged exposure to certain anti-arthritis agents -- namely, methotrexate, leflunomide, Reuters India,

Local man receives best Christmas present ever — a new kidney  -  Apr 6, 2008
The transplant team recommended I stop taking CellCept, an anti-rejection medication, and start taking Leflunomide, an anti-inflammatory medication. Republican & Herald,

RA drugs cut cardiovascular events  -  Mar 8, 2008
Universidad de Las Palmas researchers claim these drugs include methotrexate, sulfasalazine, glucocorticoids, leflunomide and TNF-alpha blockers. PRESS TV,

Analysis confirms antirheumatic potential to ease CV risks  -  Mar 6, 2008
...“As assessed by this study, the risk was lower with the prolonged use of methotrexate, sulfasalazine, glucocorticoids, leflunomide and TNF-alpha blockers. Pharma Times (subscription),

Rheumatoid Arthritis Drugs May Lower Heart Attack, Stroke Risk  -  Mar 6, 2008
Those drugs include common RA medications such as methotrexate, sulfasalazine, glucocorticoids, leflunomide and biological agents such as TNF-alpha blockers U.S. News & World Report,

Arthritis Medications Reduce Risk Of Heart Attacks And Strokes ...  -  Mar 7, 2008
..."As assessed by this study, the risk was lower with the prolonged use of methotrexate, sulfasalazine, glucocorticoids, leflunomide and TNF-± blockers. Science Daily (press release)

Cytomegalovirus Infection in Paediatric Haemopoietic Stem Cell ...  -  Feb 26, 2008
30 Newer agents eg Leflunomide, an immunosuppressant used in autoimmune disorders and treatment of solid organ rejection has been noted to have anti CMV Irish Medical Journal,

Comparative Effectiveness of Treatments for Rheumatoid Arthritis  -  Jan 14, 2008
Currently available DMARDs fall into 2 broad categories: synthetic DMARDs, including sulfasalazine, hydroxychloroquine, methotrexate, and leflunomide, Annals of Internal Medicine

Combining Medications Often Best Strategy to Battle Rheumatoid ...  -  Dec 17, 2007
No meaningful clinical differences can be found between methotrexate and either leflunomide or sulfasalazine. • Combining the synthetic DMARDs methotrexate Newswise (press release)

Paper of the Day - No one RA treatment better than the other  -  Nov 23, 2007
They found no clinically significant difference among the conventional DMARDs studied - methotrexate, leflunomide or sulfasalazine – or among the biologic Pulse,

Drug Combos Effective Against Rheumatoid Arthritis  -  Nov 26, 2007
There was no difference in effectiveness between the synthetic DMARDs methotrexate, leflunomide and sulfasalazine. And combining methotrexate and Washington Post,

Little difference among rheumatoid arthritis drugs  -  Nov 20, 2007
The therapies included corticosteroids, synthetic disease modifying anti-rheumatic drugs, or dmards, such as hydroxychloroquine, leflunomide, Tehran Times,

Rheumatoid arthritis drugs: all the same?  -  Dec 4, 2007
The treatment option include agents known as disease modifying drugs, such as leflunomide, methotrexate and sulfasalazine and biological modifying drugs, IIT Tech News,

Risk of Diabetes in Patients With Rheumatoid Arthritis Taking ...  -  Nov 27, 2007
...receiving contractual reimbursement as site principal investigator for an Aventis-sponsored clinical trial of leflunomide in rheumatoid arthritis, Journal of American Medical Association (subscription),

ACR: Tocilizumab Shows Strong Results in Pivotal RA Trials  -  Nov 12, 2007
Patients in TOWARD had previously received such agents as methotrexate, leflunomide, sulfasalazine, and azathioprine with suboptimal results. MedPage Today,

Arthritis can be improved with exercise  -  Nov 5, 2007
...sulfasalazine and leflunomide; and biological agents such as infliximab, adalimumab and etanercept). The goal of arthritis treatment is to reduce pain, News-Leader.com,

My Doctor Has Diagnosed Me With Ankylosing Spondylitis... I Want ...  -  Nov 1, 2007
Traditional disease-modifying antirheumatic drugs (dmards), such as methotrexate, leflunomide (Arava), and sulfasalazine (Azulfidine), are not useful for PR-USA.net (press release),

Some arthritis drugs may protect the heart  -  Sep 27, 2007
...event such as heart attack, heart disease and stroke, compared with those treated with methotrexate, leflunomide, sulfasalazine and glucocorticoids. Reuters

Wal-Mart Announces Improvements to 2008 Health Benefits Package  -  Sep 18, 2007
Some examples of associate savings include: -- Leflunomide, the generic version of Arava, a drug used to reduce inflammation and swelling from rheumatoid CNNMoney.com

What Are The Pitfalls Of Current Treatment For Rheumatoid Arthritis  -  Sep 29, 2007
Other DMARDS such as Plaquenil (hydroxychloroquine) and sulfasalazine (Azulfidine), and leflunomide (Arava) are also used. Over time (less than 3 months), PR-GB.com (press release),

Chelsea Therapeutics: The Wall Street Analyst Forum Presentation ...  -  Sep 20, 2007
Our hope here is to have a compound that is more suited for patients here then Arava or leflunomide with a much shorter half-life, and that's what we are Seeking Alpha,

Report Highlights Impact of Recent Entries and New Mechanisms on ...  -  Aug 16, 2007
Orencia (abatacept; Bristol-Myers Squibb); MabThera (rituximab; Roche/Biogen/Genentech); methotrexate (generic); Arava (leflunomide; Sanofi-Aventis); PharmaLive.com (press release),

August 2007 PBS Listings, Australia  -  Aug 3, 2007
Medical News Today (press release),The listing for leflunomide, which is marketed as ARABLOC® and ARAVA®, is being extended to enable it to be used for the treatment of psoriatic arthritis.

Aspirin as lesions contained without sig balance.  -  Jul 8, 2007
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A new mechanism for respiratory syncytial virus-induced 2 ...  -  Jul 31, 2007
AJP-Lung Physiology (subscription)...[ISI][Medline] Davis IC, Lazarowski ER, Hickman-Davis JM, Fortenberry JA, Chen FP, Zhao X, Sorscher E, Graves LM, Sullender WM, Matalon S. Leflunomide

My Doctor Has Diagnosed Me With Ankylosing Spondylitis... I Want ...  -  Jul 20, 2007
PR-GB.com (press release),Traditional disease-modifying antirheumatic drugs (DMARDs), such as methotrexate, leflunomide (Arava), and sulfasalazine (Azulfidine), are not useful for

Antimalarial Drug May Reduce Diabetes Risk in RA Patients  -  Jul 10, 2007
MedPage Today,Dr.Wasko has received contractual reimbursement as site principal investigator for an Aventis-sponsored clinical trial of leflunomide in rheumatoid

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Early Rheumatoid Arthritis Disease Control Needs Improvement ...  -  Jun 18, 2007
DG NewsThe first DMARD chosen was often methotrexate (48%) and sulfasalazine, but also oral steroids (6%), hydroxychloroquine (5%), leflunomide (2%).

Treatment with Belimumab showed improvement in symptoms in 46 ...  -  Jun 14, 2007
EurekAlert (press release),SLE treatment regimes); 50% of these subjects were also taking an immunosuppressive drug (eg, methotrexate, azathioprine, mycophenolate, leflunomide).

Sinobiomed Wins Patent Approval For Viper Venom As Anti-Bleeding Agent  -  Jun 5, 2007
Seeking Alpha,...a recombinant human interferon for hepatitis B, hepatitis C, viral infections and other conditions, and Leflunomide, a rheumatoid arthritis drug.

Research and Markets: Examine the M&A Activity of the Generics ...  -  May 18, 2007
Genetic Engineering News (press release),Court orders Apotex to halt sales of clopidogrel Recent product approvals Diltiazem hydrochloride Clopidogrel Zonisamide Ofloxacin otic Leflunomide tablets

French Guidelines for Pretreatment Screening Inadequate to ...  -  Apr 10, 2007
DG NewsAnalysis of their concomitant immunosuppressive therapies showed use of methotrexate in 19 patients, leflunomide in 2, azathiprine in 1 and salazopine in 5;

Brand Names/Synonyms:
Leflunomide is also known by the following brand names and/or synonymsArava; Leflunomide; Leflunomide [Usan:Inn]; Leflunomidum [Inn-Latin]; Lefunomide; [Inn-Spanish]

Drug Category:
Leflunomide is categorized under the following by the FDA: Immunosuppressive Agents; Antivirals; Antiparasitics; Antineoplastic Agents; Anti-inflammatory Agents; Adjuvants; Unclassified Therapeutic Agents (92:00.00);

Dosage Forms:
TABLET

Absorption:
Well absorbed, peak plasma concentrations appear 6-12 hours after dosing

Interactions:
Interactions for Leflunomide:

Cholestyramine and Charcoal
Administration of cholestyramine or activated charcoal in patients (n=13) and volunteers (n=96) resulted in a rapid and significant decrease in plasma M1 (the active metabolite of leflunomide) concentration .

Hepatotoxic Drugs
Increased side effects may occur when leflunomide is given concomitantly with hepatotoxic substances. This is also to be considered when leflunomide treatment is followed by such drugs without a drug elimination procedure. In a small (n=30) combination study of ARAVA with methotrexate, a 2- to 3-fold elevation in liver enzymes was seen in 5 of 30 patients. All elevations resolved, 2 with continuation of both drugs and 3 after discontinuation of leflunomide. A >3-fold increase was seen in another 5 patients. All of these also resolved, 2 with continuation of both drugs and 3 after discontinuation of leflunomide. Three patients met "ACR criteria" for liver biopsy (1: Roegnik Grade I, 2: Roegnik Grade IIIa). No pharmacokinetic interaction was identified.

NSAIDs
In in vitro studies, M1 was shown to cause increases ranging from 13 - 50% in the free fraction of diclofenac and ibuprofen at concentrations in the clinical range. The clinical significance of this finding is unknown; however, there was extensive concomitant use of NSAIDs in clinical studies and no differential effect was observed.

Tolbutamide
In in vitro studies, M1 was shown to cause increases ranging from 13 - 50% in the free fraction of tolbutamide at concentrations in the clinical range. The clinical significance of this finding is unknown.

Rifampin
Following concomitant administration of a single dose of ARAVA to subjects receiving multiple doses of rifampin, M1 peak levels were increased (~40%) over those seen when ARAVA was given alone. Because of the potential for ARAVA levels to continue to increase with multiple dosing, caution should be used if patients are to be receiving both ARAVA and rifampin.

Warfarin
Increased INR (International Normalized Ratio) when ARAVA and warfarin were co-administered has been rarely reported.

Chemical IUPAC Name:
5-methyl-N-[4-(trifluoromethyl)phenyl]-oxazole-4-carboxamide

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