Leflunomide is an isoxazole derivative with antiproliferative activity, primarily used to treat adult rheumatoid arthritis and lupus nephritis.
Basic Information
English Name: Leflunomide
Chemical Formula: C12H9F3N2O2
Molecular Weight: 270.207
CAS Registry Number: 75706-12-6
Pharmacological Action
Leflunomide inhibits dihydroorotate dehydrogenase activity through its active metabolite A77 1726, thereby blocking the de novo pyrimidine synthesis pathway and inhibiting T and B cell proliferation and antibody production. Additionally, it suppresses NF-κB activation, downregulates the expression of various inflammatory factors (such as IL-1, TNF, etc.), and inhibits metalloproteinase expression, delaying bone destruction.
Indications
Leflunomide is primarily used to treat the following conditions:
Adult Rheumatoid Arthritis: It exhibits disease-modifying activity.
Lupus Nephritis: As one of the therapeutic options.
Moreover, Leflunomide can also be used for the treatment of bullous pemphigoid, connective tissue diseases, Wegener's granulomatosis, severe psoriasis, and other diseases.
