Leflunomide is a pyrimidine synthesis inhibitor, primarily functioning by inhibiting dihydroorotate dehydrogenase (DHODH), and is recognized as a disease-modifying antirheumatic agent. This prodrug inhibits the proliferation of mononuclear and T-cells and acts as an inhibitor of several protein tyrosine kinases, with IC50 values ranging from 30 mM to 100 mM in in vitro assays. It also interferes with cell cycle progression and utilizes p53-dependent mechanisms to prevent the expansion of activated and autoimmune lymphocytes.
- Inhibits dihydroorotate dehydrogenase (DHODH)
- Acts as a disease-modifying antirheumatic agent
- Inhibits proliferation of mononuclear and T-cells
- Functions as an inhibitor of several protein tyrosine kinases
- Inhibits p59fyn and p56lck activity in tyrosine kinase assays
- Inhibits calcium mobilization in Jurkat cells
- Prevents expansion of activated and autoimmune lymphocytes