Leflunomide

The isoxazole derĂ­vate leflunomide (Arava) is a pyrimidine synthesis inhibitor that is rapidly converted to its active form malononitrilamide (A-771726). The active metabolite functions as an inhibitor of pyrimidine synthesis and thereby suppresses T-lymphocyte proliferation and the production of autoantibodies by B lymphocytes. Preliminary reports suggest that leflunomide may also be effective in the management of LE (Petera et al. 2000, Remer et al. 2001). According to two studies on treatment with leflunomide, the lupus activity scores (European Consensus Lupus Activity Measurement [ECLAM] or SLE Disease Activity Index [SLEDAI]) decreased, and in some patients the concomitant use of steroids could be reduced. Leflunomide was well tolerated, and no severe side effects have been observed. Currently leflunomide may be considered as a valuable additive therapy for severe (organ-threatening) cases of SLE (Petri 2001). However, the ultimate role of leflunomide in the treatment of the different forms of LE remains to be evaluated in further studies.

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