Drug intelligence / Profile preview

leflunomide

Development stage
Approved
Lead developer
Sanofi
Modality
Small Molecules
Administration
Oral
01

Overview

Leflunomide is an immunosuppressive disease-modifying antirheumatic drug (DMARD) primarily used to treat moderate-to-severe rheumatoid arthritis and psoriatic arthritis. It works by inhibiting the mitochondrial enzyme dihydroorotate dehydrogenase (DHODH), which is essential for de novo pyrimidine synthesis required for DNA and RNA production in rapidly dividing cells such as activated lymphocytes. By blocking DHODH, leflunomide reduces the proliferation of these immune cells, thereby decreasing inflammation and slowing disease progression. Its active metabolite, teriflunomide, also inhibits several tyrosine kinases involved in cell signaling pathways related to immune activation[1][5][6][8]. Leflunomide does not cure rheumatoid arthritis but helps control symptoms and improve physical function.

Brand names
Arava
Other names
leflunomideA77 1726A-77 1726A 77 1726Arava
02

Targets

Tyrosine kinaseDHODH (Dihydroorotate dehydrogenase (quinone), mitochondrial)

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