II. Indications: Rheumatoid Arthritis

  1. First line DMARD instead or Methotrexate
  2. Combination with Methotrexate

III. Mechanism

  1. Pyrimidine inhibitor
  2. T-Cell activation and proliferation inhibitor
  3. Similar to Methotrexate in effects
  4. Onset of action in 1-2 months

IV. Efficacy

  1. Comparable to Methotrexate
  2. Used with Methotrexate for maximal effect

V. Adverse effects

  1. Nausea (may limit use)
  2. Alopecia
  3. Liver injury occurs in 1 in 200 patients
    1. Increased Liver transaminases (e.g. AST, SGOT)
  4. Lung injury (observe for new onset cough)

VI. Monitoring

  1. Labs:
    1. Aspartate Transaminase (SGOT, AST)
    2. Complete Blood Count with Platelet Count
  2. History
    1. Ask about new onset cough
  3. Timing
    1. Check monthly for 6 months
    2. Check every 6-8 weeks

VII. Dose

  1. Loading dose: 100 mg PO qd for 3 days
  2. Maintenance: 10 mg PO qd (or 20 mg PO qod)
  3. Inadequate relief at lower dose: 20 mg PO qd

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Cost: Medications

leflunomide (on 8/17/2016 at Medicaid.Gov Survey of pharmacy drug pricing)
LEFLUNOMIDE 10 MG TABLET Generic $4.28 each
LEFLUNOMIDE 20 MG TABLET Generic $4.49 each

Ontology: leflunomide (C0063041)

Definition (NCI) A derivative of isoxazole used for its immunosuppressive and anti-inflammatory properties. As a prodrug, leflunomide is converted to an active metabolite, A77 1726, which blocks dihydroorotate dehydrogenase, a key enzyme of de novo pyrimidine synthesis, thereby preventing the expansion of activated T lymphocytes. This agent also inhibits various protein tyrosine kinases, such as protein kinase C (PKC), thereby inhibiting cell proliferation. (NCI04)
Definition (NCI_NCI-GLOSS) An anticancer drug that works by inhibiting a cancer cell growth factor.
Definition (PDQ) A derivative of isoxazole used for its immunosuppressive and anti-inflammatory properties. As a prodrug, leflunomide is converted to an active metabolite, A77 1726, which blocks dihydroorotate dehydrogenase, a key enzyme of de novo pyrimidine synthesis, thereby preventing the expansion of activated T lymphocytes. This agent also inhibits various protein tyrosine kinases, such as protein kinase C (PKC), thereby inhibiting cell proliferation. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=42253&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=42253&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C1128" NCI Thesaurus)
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C045463
SnomedCT 109143003, 386981009
LNC LP34970-1, MTHU017708
English 4-Isoxazolecarboxamide, 5-methyl-N-(4-(trifluoromethyl)phenyl)-, leflunomide, N-(4-trifluoromethyphenyl)-5-methylisoxazole-4-carboxamide, 4-Isoxazolecarboxamide, 5-Methyl-N-(4-(trifluoromethyl)phenyl)-, leflunomide (medication), LEFLUNOMIDE, leflunomide [Chemical/Ingredient], Leflunomide (product), Leflunomide (substance), Leflunomide
Spanish leflunomida (producto), leflunomida (sustancia), leflunomida

Ontology: Arava (C0718644)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C045463
English arava, Hoechst Brand of Leflunomide, Aventis Behring Brand of Leflunomide, Aventis Brand of Leflunomide, Aventis Pharma Brand of Leflunomide, Arava