Basic therapy of rheumatoid arthritis with leflunomide (review)


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Yu A Olyunin

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  1. Bartlett R. Я, Schleyerbach R. Immunopharmacological profile of a novel isoxazol derivative, HWA 486, with potential antirheumatic activity I. Disease modifying action on adjuvant arthritis of the rat. Int. J. Immunopharrnacol. 1985; 7 (1): 7- 18.
  2. Rozman B. Clinical pharmacokinetics of leflunomide. Clin. Pharmacokinet. 2002; 41 (6): 421-430.
  3. Bartlett R. R., Dimitrijevic M., Mattar T. et al. Leflunomide (HWA 486), a novel immunomodulating compound for the treatment of autoimmune disorders and reactions leading to transplantation rejection. Agents and Actions 1991; 32 (1-2): 10-21.
  4. Cao W. W., Kao P. N.. Chao A. C. et al. Mechanism of the antiproliferative action of leflunomide. A77 1726, the active metabolite of leflunomide, does not block T-cell receptormediates signal transduction but its antiproliferative effects are antagonized by pyrimidine nucleosides. J. Heart Lung Transplant. 1995; 14 (6, pt 1): 1016-1030.
  5. Cherwinski К M., Byars N., Ballaron S. J. et al. Leflunomide interferes with pyrimidine nucleotide biosynthesis. Inflamm. Res. 1995; 44: 317-322.
  6. Zielinski Т., Zeitter D., Milliner S., Bartlett R. R. Leflunomide, a reversible inhibitor of pyrimidine biosynthesis. Inflamm. Res. 1995; 44 (suppl. 2): 207-208.
  7. Fairbanks L. D., Bofll M., Ruckemann K., Simmonds H. A. Importance of ribonucleotide availability to proliferating T-lymphocytes from healthy humans. J. Biol. Chem. 1995; 270: 29682-29691.
  8. Fox R. I., Herrmann M. L., Frangou С G. et al. Mechanism of action for leflunomide in rheumatoid arthritis. Clin. Immunol. 1999; 93 (3): 198-208.
  9. Linke S. P., Clarkin К. С, Di Leonardo A. et al. A reversible, p53-dependent G0/G1 cell cycle arrest induced by ribonucleotide depletion in the absence of detectable DNA damage. Genes Dev. 1996; 10: 934-947.
  10. Linke S. P., Clarkin К. С, Wahl G. M. p53 mediates permanent arrest over multiple cell cycles in response to gammairradiation. Cancer Res. 1997; 57: 1171-1179.
  11. Wahl G. M., Linke S. P., Paulson T. C, Huang L.-C. Maintaining genetic stability through TP53 mediated checkpoint control. Cancer Surv. 1997; 29: 183-219.
  12. Xu X., Willians J. W., Gong H. et al. Two activities of the im munosuppressive metabolite of leflunomide, A771726. Inhibition of pyrimidine nucleotide synthesis and protein tyrosine phosphorylation. Biochem. Pharmacol. 1996; 52 (4): 527-534.
  13. Ruckemann K, Fairbanks L. D., Carrey E. A. et al. Leflunomide inhibits pyrimidine de novo synthesis in mitogen-stimulated T-lymphocytes from healthy humans. J. Biol. Chem. 1998; 273: 21682-21691.
  14. Nikcevich D. A., Finnegan A., Chong A. S. F. et al. Inhibition of interleukin 2 (IL-2)-stimulated tyrosine kinase activity by leflunomide. Agents and Actions 1994; 41: 279-282.
  15. Xu X., Williams J. W., Bremer E. G. et al. Inhibition of protein tyrosine phosphorylation in T cells by a novel immunosuppressive agent, leflunomide. J. Biol. Chem. 1995; 270: 12398- 12403.
  16. Breedveld F. C, Dayer J. M. Leflunomide: mode of action in the treatment of rheumatoid arthritis. Ann. Rheum. Dis. 2000; 59 (11): 84849.
  17. Elder R. Т., Xu X., Williams J. W. et al. The immunosuppressive metabolite of leflunomide, A77 1726, affects murine T cells through two biochemical mechanisms. J. Immunol. 1997; 159 (1): 22-27.
  18. Popovic S., Bartlett R. R. Disease modifying activity of HWA 486 on the development of SLE/1 mice. Agents and Actions 1986; 19: 313-313.
  19. Williams J. W., Xiao F., Foster P. et al. Leflunomide in experimental transplantation: control of rejection and alloantibody production, reversal of acute rejection, and interaction with cyclosporin. Transplantation 1994; 57: 1223-1223.
  20. Xiao F, Chong A. S.-F., Foster P. et al. Leflunomide controls rejection in hamster to rat cardiac xenografts. Transplantation 1994; 58: 828-828.
  21. Siemasko K. F., Chong A. S. F., Williams J. W. et al. Regulation of В cell function by the immunosuppressive agent leflunomide. Transplantation 1996; 61: 635-642.
  22. Siemasko K, Chong A. S., Jack H. M. et al. Inhibition of JAK3 and STAT6 tyrosine phosphorylation by the immunosuppressive drug leflunomide leads to a block in IgGl production. J. Immunol. 1998; 160 (4): 1581-1588.
  23. Manna S. K., Aggarwal В. В. Immunosuppressive leflunomide metabolite (A77 1726) bkappa В activation and gene expression. J. Immunol. 1999; 162 (4): 2095-2102.
  24. Manna S. K., Mukhopadhyay A., Aggarwal В. В. Leflunomide suppresses TNF-induced cellular responses: effects on NF-kappa B, activator protein-1, c-Jun N-terminal protein kinase, and apoptosis. J. Immunol. 2000; 165 (10): 5962-5969.
  25. Schorlemmer H. U., Kurrle R., Schleyerbach R., Bartlett R. R. Generation of 02-radicals in macrophages can be inhibited in vitro and in vivo by derivatives of leflunomide's primary metabolite. Inflamm. Res. 1999; 48 (suppl. 2): S117-S118.
  26. Elkayam O., Yaron I., Shirazi I. et al. Active leflunomide me tabolite inhibits interleukin lbeta, tumour necrosis factor alpha, nitric oxide, and metalloproteinase-3 production in activated human synovial tissue cultures. Ann. Rheum. Dis. 2003; 62 (5): 440-443.
  27. Burger D., Begue-Pastor N., Senavent S. et al. The active metabolite of leflunomide, A77 1726, inhibits the production of prostaglandin E(2), matrix metalloproteinase 1 and interleukin 6 in human fibroblast-like synoviocytes. Rheumatology 2003; 42 (1): 89-96.
  28. Kraan M. C, Reece R. J., Barg E. С et al. Modulation of inflammation and metalloproteinase expression in synovial tissue by leflunomide and methotrexate in patients with active rheumatoid arthritis. Findings in a prospective, randomized, doubleblind, paraleldesign clinical trial in thirty-nine patients at two centers. Arthr. and Rheum. 2000; 43 (8): 1820-1830.
  29. Hamilton L. C, Vojnovic I., Warner T. D. A77 1726, the active metabolite of leflunomide, directly inhibits the activity of cyclooxygenase-2 in vitro and in vivo in a substrate-sensitive manner. Br. J. Pharmacol. 1999; 127 (7): 1589-1596.
  30. Mladenovic V., Domljan Z., Rozman et al. Safety and effectiveness of leflunomide in the treatment of patients with active rheumatoid arthritis. Results of a randomized, placebocontrolled, phase II study. Arthr. and Rheum. 1995; 38 (11): 1595-1603.
  31. Smolen J. S., Kalden J. R., Scott D. L. et al. Efficacy and safety of leflunomide compared with placebo and sulphasalazine in active rheumatoid arthritis: a double-blind, randomized, multicentre trial. European Leflunomide Study Group. Lancet 1999; 353 (9149): 259-266.
  32. Smolen J. S., Emery P. Efficacy and safety of leflunomide in active rheumatoid arthritis. Rheumatology 2000; 39 (suppl 1): 48-56.
  33. Scott D. L., Strand V. The effects of disease-modifying antirheumatic drugs on the Health Assessment Questionnaire score. Lessons from the leflunomide clinical trials database. Rheumatology 2002; 41 (8): 899-909.
  34. Larsen A., Kvien T. K., Schattenkirchner M. et al. European Leflunomide Study Group. Slowing of disease progression in rheumatoid arthritis patients during long-term treatment with leflunomide or sulfasalazine. Scand. J. Rheumatol. 2001; 30 (3): 135-142.
  35. Strand V., Cohen S., Schiff M. et al. Treatment of active rheumatoid arthritis with leflunomide compared with placebo and methotrexate. Leflunomide Rheumatoid Arthritis Investigators Group. Arch. Intern. Med. 1999; 159 (21): 2542-2550.
  36. Strand V., Tugwell P., Bombardier С et al. Function and health-related quality of life: results from a randomized controlled trial of leflunomide versus methortexate or placebo in patients with active rheumatoid arthritis. Leflunomide,Rheumatoid Arthritis Investigators Group. Arthr. and Rheum. 1999; 42 (9): 1870-1878.
  37. Sharp J. Т., Strand V., Leung H. et al. Treatment with leflunomide slows radiographic progression of rheumatoid arthritis: results from three randomized controlled trials of leflunomide in patients with active rheumatoid arthritis. Leflunomide Rheumatoid Arthritis Investigators Group. Arthr. and Rheum. 2000; 43 (3): 495-505.
  38. Cohen S. В., Iqbal I. Leflunomide. Int. J. Clin. Pract. 2003: 57 (2): 115-120.
  39. Emery P., Breedveld F. C, Lemmel E. M. et al. A comparison of the efficacy and safety of leflunomide and methotrexate for the treatment of rheumatoid arthritis. Rheumatology 2000; 39 (6): 655-665.
  40. Griffith S. M., Fisher J., Clarke S. et al. Do patients with rheumatoid arthritis established on methotrexate and folic acid 5 mg daily need to continue folic acid supplements long term? Rheumatology 2000; 39 (10): 1102-1109.
  41. van Ede A. E., Laan R. F., Rood M. J. et al. Effect of folic or folinic acid supplementation on the toxicity and efficacy of methotrexate in rheumatoid arthritis: a forty-eight week, multicenter, randomized, double-blind, placebo-controlled study. Arthr. and Rheum. 2001; 44 (7): 1515-1524.
  42. Reece R. J., Kraan M. C, Radjenovic A. et al. Comparative assessment of leflunomide and methotrexate for the treatment of rheumatoid arthritis, by dynamic enhanced magnetic resonance imaging. Arthr. and Rheum. 2002; 46 (2): 366-372.
  43. Alldred A., Emery P. Leflunomide: a novel DMARD for the treatment of rheumatoid arthritis. Exp. Opin. Pharmacother. 2001; 2 (1): 125-137.
  44. Miceli-Richard C, Dougados M. Leflunomide for the treatment of rheumatoid arthritits. Exp. Opin. Pharmacother. 2003; 4 (6): 987-997.
  45. Weinbtatt M. E., Kremer J. M., Coblyn J. S. et al. Pharmacokinetics, safety, and efficacy of combination treatment with methotrexate and leflunomide in patients with active rheumatoid arthritis. Arthr. and Rheum. 1999; 42 (7): 1322-1328.
  46. Kremer J. M., Genovese M. C, Cannon G. W. Concomitant leflunomide therapy in patients with active rheumatoid arthritis despite stable doses of methotrexate. A randomized, doubleblind, placebocontrdlled trial. Ann. Intern. Med. 2002; 137 (9): 726-733.
  47. Dougados M., Combe В., van Riel P. Efficacy and safety of leflunomide in combination with sulfasalazine versus sulfasalazine in patients with rheumatoid arthritis: results from the RE- LIEF study. Ann. Rheum. Dis. 2002; 61 (suppl. 1): abstr. FR1071.
  48. Kalden J. R., Schattenkirchner M., Sorensen H. et al. The efficacy and safety of leflunomide in patients with active rheumatoid arthritis: A five-year followup study. Arthr. and Rheum. 2003; 48 (6): 1513-1520.

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