Drug intelligence / Profile preview

leflunomide + methotrexate + prednisone

Development stage
Unknown
Lead developer
Sanofi
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

This is a combination therapy consisting of three drugs—leflunomide, methotrexate, and prednisone—used primarily in the management of rheumatoid arthritis (RA). Leflunomide and methotrexate are both disease-modifying antirheumatic drugs (DMARDs) with distinct mechanisms; leflunomide inhibits de novo pyrimidine synthesis via dihydroorotate dehydrogenase inhibition, while methotrexate inhibits purine metabolism as an anti-metabolite. Prednisone is a synthetic glucocorticoid corticosteroid that acts as an anti-inflammatory and immunosuppressant. This combination aims to provide additive or synergistic effects for patients with active RA who do not respond adequately to monotherapy. The regimen can improve clinical outcomes but requires careful monitoring due to increased risks of hepatotoxicity, immunosuppression, and infection[1][2][4][5].

02

Targets

GR (Glucocorticoid receptor)DHFR (Dihydrofolate reductase)DHODH (Dihydroorotate dehydrogenase (quinone), mitochondrial)

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