Drug intelligence / Profile preview

leflunomide + rituximab

Development stage: Unknown
Lead developer: Sanofi
Modality: Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration: Oral, Intravenous

Overview

A combination therapy consisting of leflunomide (a disease-modifying antirheumatic drug) and rituximab (a monoclonal antibody targeting CD20 on B cells). This combination is used primarily for treating rheumatoid arthritis in patients who are intolerant to methotrexate or have inadequate response to methotrexate alone. Leflunomide inhibits dihydroorotate dehydrogenase, preventing de novo pyrimidine synthesis needed for lymphocyte proliferation, while rituximab eliminates B cells through antibody-dependent cellular cytotoxicity, complement-dependent cytotoxicity, and induction of apoptosis.

Targets

CD20 (B-lymphocyte antigen CD20)Tyrosine kinaseDHODH (Dihydroorotate dehydrogenase (quinone), mitochondrial)

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