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Leflunomide
drug data and news
Leflunomide drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Leflunomide | ||
| Brand Names/Synonyms | Arava; Leflunomide; Leflunomide [Usan:Inn]; Leflunomidum [Inn-Latin]; Lefunomide; [Inn-Spanish] | ||
| Indication | For the treatment of active rheumatoid arthritis (RA) | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | 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. | ||
| 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 | ||
| Leflunomide News (When available) |
Sanofi expects Acomplia launch in 06; profits up Feb 24, 2006 DTB recommends caution with new psoriatic arthritis drugs Jan 27, 2006 New Year, new drug for arthritis patients Dec 4, 2005 Actemra Monotherapy Significantly Slows Down Damage to Joints in ... Nov 16, 2005 Novel Actemra monotherapy in treating patients with early ... Nov 17, 2005 Earlier Use of Second-Line Agents in Juvenile Arthritis Associated ... Nov 18, 2005 Apotex Receives Final Approval for Leflunomide Tablets Sep 14, 2005 Barr Receives Approval for Leflunomide Tablets, 10 mg & 20 mg Sep 14, 2005 Teva receives FDA approval for leflunomide tablets Sep 14, 2005 Teva Announces Approval of Leflunomide Tablets Sep 14, 2005 Prasco Ships Leflunomide Tablets; Prasco Will Market the Adult ... Sep 14, 2005 (PRN) - Barr Receives Approval for Leflunomide Tablets, 10 mg & 20 ... Sep 14, 2005 Par Pharmaceutical Receives Approval to Market Generic Arava(TM) Sep 14, 2005 Teva wins US OK for arthritis drug Sep 14, 2005 Green light for Barr's generic arthritis drug Sep 15, 2005 Juvenile Idiopathic Arthritis Oct 4, 2005 Par Pharmaceutical Receives Approval to Market Generic Arava(TM) Sep 14, 2005 Sanofi-Aventis: Arava facing generic attack Sep 15, 2005 Adalimumab Plus Methotrexate Effective for Long Standing ... Sep 28, 2005 Par Unit Receives FDA Generic Arava OK Sep 14, 2005 New arthritis drug found effective Sep 14, 2005 Barr Pharma cleared for arthritis drug Sep 14, 2005 Market Report / Lipman overcomes rumored weak sales Sep 15, 2005 Wed: Banks boost TA 25 to new high Sep 14, 2005 (PRN) - Sears Holdings Corporation Announces $500 Million Share ... Sep 14, 2005 Treatment For Rare Liver Disease Increases Mortality Risk Aug 24, 2005 Long-standing rheumatoid arthritis - Adalimumab plus methotrexate ... Aug 15, 2005 Humira plus Methotrexate effective for long standing rheumatoid ... Aug 18, 2005 Prasco Laboratories and sanofi-aventis Sign a Distribution and ... Jul 25, 2005 Business briefs Jul 26, 2005 Tailoring Arthritis Therapy in the Wake of the NSAID Crisis Jun 22, 2005 Advisory Committee Conference Room Jun 23, 2005 | ||
| Dosage Forms | TABLET | ||
| Drug_Category | Immunosuppressive Agents; Antivirals; Antiparasitics; Antineoplastic Agents; Anti-inflammatory Agents; Adjuvants; Unclassified Therapeutic Agents (92:00.00); | ||
| Absorption | Well absorbed, peak plasma concentrations appear 6-12 hours after dosing | ||
| Interactions |
Interactions for Leflunomide: Cholestyramine and Charcoal Hepatotoxic Drugs NSAIDs Tolbutamide Rifampin Warfarin | ||
| Toxicity | LD50=100-250 mg/kg (acute oral toxicity) | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | 5-methyl-N-[4-(trifluoromethyl)phenyl]-oxazole-4-carboxamide | ||
| Chemical Formula | C12H9F3N2O2 | ||
| Molecular Weight | 270.207 g/mol | ||
| Smiles String | CC1=C(C=NO1)C(=O)NC2=CC=C(C=C2)C(F)(F)F | ||
| Melting Point | 165-166 °C | ||
| Water Solubility | 21 mg/L (poorly soluble) | ||
| State | Solid | ||
| LogP/Hphobicity | 2.659 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Primarily hepatic. Leflunomide is converted to its active form following oral intake | ||
| Half Life | 2 weeks | ||
| Protein Binding [%] | >99.3% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Leflunomide.html http://www.rxlist.com/cgi/generic3/leflunomide.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00205 | ||
| CAS Registry Number | 75706-12-6 | ||
| KEGG Compound ID | C07905 | ||
| PubChem ID | SID:191162 | ||
| PharmGKB ID | Not Available | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2261278 |
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