Leflunomide: An immunomodulatory agent for the treatment of rheumatoid arthritis

Formulary

Volumn 34, Issue 1, 1999, Pages 21-31

  Dunn, Erin C ^a   Small, Ralph E ^a  

^a VIRGINIA COMMONWEALTH UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIRHEUMATIC AGENT; AURANOFIN; AUROTHIOGLUCOSE; AUROTHIOMALATE; AZATHIOPRINE; CIMETIDINE; CYCLOPHOSPHAMIDE; CYCLOSPORIN; DICLOFENAC; ETANERCEPT; HYDROXYCHLOROQUINE; IBUPROFEN; LEFLUNOMIDE; METHOTREXATE; NONSTEROID ANTIINFLAMMATORY AGENT; ORAL CONTRACEPTIVE AGENT; PENICILLAMINE; SALAZOSULFAPYRIDINE; TERIFLUNOMIDE; TOLBUTAMIDE; UNCLASSIFIED DRUG; WARFARIN;

ALOPECIA; CELL PROLIFERATION; CLINICAL TRIAL; DIARRHEA; DISEASE COURSE; DRUG COST; DRUG FORMULARY; DRUG MECHANISM; HEADACHE; HUMAN; HUMAN CELL; HUMAN TISSUE; IMMUNOMODULATION; LIVER DISEASE; LIVER FUNCTION TEST; META ANALYSIS; NAUSEA; RASH; REVIEW; RHEUMATOID ARTHRITIS;

EID: 0033021526     PISSN: 1082801X     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (21)

1. American College of Rheumatology Ad Hoc Committee on Clinical Guidelines. Guidelines for the management of rheumatoid arthritis. Arth Rheum 1996; 39:713-22.
2. Firestein GS, Zvaifler NJ. How important are T cells in chronic rheumatoid synovitis? Arth Rheum 1990;33:768-73.
3. Panayi GS, Lanchbury JS, Kingsley GH. The importance of the T cell in initiating and maintaining the chronic synovitis of rheumatoid arthritis. Arth Rheum 1992;35: 729-35.
4. Chong ASF, Rezai K, Gebel HM, et al. Effects of leflunomide and other immunosuppressive agents on T cell proliferation in vitro. Transplantation 1996;61: 140-5.
5. Davis JP, Cain GA, Pitts WJ, et al. The immunosuppressive metabolite of leflunomide is a potent inhibitor of human dihydroorotate dehydrogenase. Biochemistry 1996;35:1270-3.
6. Fox RI. Mechanism of action of leflunomide in rheumatoid arthritis. J Rheumatol 1998;25(Suppl 53):S20-S25.
7. Kuo EA, Hambleton PT, Kay DP, et al. Synthesis, structure-activity relationships, and pharmacokinetic properties of dihydroorotate dehydrogenase inhibitors: 2-cyano-3-cyclopropyl-3-hydroxy-N-[3′-methyl-4′-(trifluoromethyl) phenyl]propenamide and related compounds. J Med Chem 1996;39:4608-21.
8. Rückemann K, Fairbanks LD, Carrey EA, et al. Leflunomide inhibits pyrimidine de novo synthesis in mitogen-stimulated T-lymphocytes from healthy humans. J Biol Chem 1998;273:21682-91.
9. Siemasko KF, Chong ASF, Williams JW, et al. Regulation of B cell function by the immunosuppressive agent leflunomide. Transplantation 1996;61:635-42.
10. Xu X, Williams JW, Gong H, et al. Two activities of the immunosuppressive metabolite of leflunomide, A77 1726. Biochem Pharmacol 1996;52:527-34.
11. Hamilton C, Vojnovic I, Bakhle YS, et al. The anti-inflammatory drug leflunomide inhibits in vitro and in vivo the activity of COX-2 more potently than the induction of COX-2 or iNOS [abstract]. Br J Pharmacol 1997;120(Suppl):49P.
12. Leflunomide (Arava) package insert. Kansas City, MO: Hoechst Marion Roussel, Inc; September 1998.
13. Mladenovic V, Domljan Z, Rozman B, et al. Safety and effectiveness of leflunomide in the treatment of patients with active rheumatoid arthritis. Arth Rheum 1995;38: 1595-603.
14. Data on file. Hoechst Marion Roussel, Inc. Kansas City, MO.
15. Weaver A, Caldwell J, Olsen N, et al. Treatment of active rheumatoid arthritis with leflunomide compared to placebo or methotrexate [abstract]. Arth Rheum 1998;41(Suppl):S131. Abstract 593.
16. Furst D, Cannon GW, Fox R, Strand V. Onset of effect and duration of response to leflunomide treatment of active rheumatoid arthritis compared to placebo or methotrexate [abstract]. Arth Rheum 1998;41(Suppl): S155. Abstract 734.
17. Moreland LW, Fleischmann RM, Strand V. Efficacy of leflunomide vs placebo vs methotrexate in early and late rheumatoid arthritis [abstract]. Arth Rheum 1998; 41(Suppl):S155. Abstract 733.
18. Schiff M, Kaine J, Sharp J, Strand V. X-ray analysis of 12 months' treatment of active rheumatoid arthritis with leflunomide compared to placebo or methotrexate [abstract]. Arth Rheum 1998;41(Suppl):S155. Abstract 736.
19. Tugwell P, Bomberdler C, Strand V, et al. Treatment of active rheumatoid arthritis with leflunomide improves functional activities and health-related quality of life [abstract]. Arth Rheum 1998;41(Suppl): S154. Abstract 732.
20. Smolen JS, Kalden JR, Rozman B, et al. A double-blind randomized phase III trial of leflunomide vs placebo vs sulfasalazine in rheumatoid arthritis [abstract]. Arth Rheum 1998;41(Suppl):S131. Abstract 594.
21. Scott DL, Shattenkirchner M, Smolen JS, et al. Efficacy of leflunomide vs placebo vs sulfasalazine in rheumatoid arthritis: Effect of disease duration [abstract]. Arth Rheum 1998;41(Suppl):S155. Abstract 735.