Leflunomide

Leflunomide is a novel isoxazole derivative with immunosuppressant and anti-inflammatory properties. It has been most extensively evaluated in patients with rheumatoid arthritis and may be categorised as a disease-modifying antirheumatic drug (DMARD). The drug appears to have a unique mechanism of action involving inhibition of de novo pyrimidine synthesis in immune cells. In animal models of arthritis, lefunomide demonstrated a number of beneficial effects including reduced inflammation and joint stiffness. In patients with rheumatoid arthritis, lefunomide 10 or 25 mg/day for 24 weeks significantly improved various outcome measures such as patient global assessment and swollen joint scores compared with placebo. Efficacy seems to be similar to that of established DMARDs. Relative to established DMARDs, lefunomide appears to have a are gastrointestinal.