Last reviewed · How we verify
Leflunomide(LEF)
Leflunomide inhibits dihydroorotate dehydrogenase, an enzyme required for pyrimidine synthesis, thereby suppressing T-cell and B-cell proliferation.
Leflunomide inhibits dihydroorotate dehydrogenase, an enzyme required for pyrimidine synthesis, thereby suppressing T-cell and B-cell proliferation. Used for Rheumatoid arthritis, Active psoriatic arthritis, Active ankylosing spondylitis.
At a glance
| Generic name | Leflunomide(LEF) |
|---|---|
| Sponsor | Nanjing Children's Hospital |
| Drug class | Immunosuppressant; DHODH inhibitor |
| Target | Dihydroorotate dehydrogenase (DHODH) |
| Modality | Small molecule |
| Therapeutic area | Immunology; Rheumatology |
| Phase | FDA-approved |
Mechanism of action
Leflunomide's active metabolite, teriflunomide, reversibly inhibits dihydroorotate dehydrogenase (DHODH), a mitochondrial enzyme critical for de novo pyrimidine nucleotide synthesis. This selectively impairs the proliferation of activated lymphocytes, which depend heavily on de novo pyrimidine synthesis, leading to immunosuppression. The drug is used to reduce inflammation and slow disease progression in autoimmune conditions.
Approved indications
- Rheumatoid arthritis
- Active psoriatic arthritis
- Active ankylosing spondylitis
Common side effects
- Diarrhea
- Elevated liver enzymes (ALT/AST)
- Alopecia (hair loss)
- Hypertension
- Nausea
- Respiratory tract infection
Key clinical trials
- Comparative Study of Leflunomide Plus Methotrexate Versus Methotrexate Monotherapy in Refractory Polyarticular Juvenile Idiopathic Arthritis Patients (PHASE4)
- Takayasu Arteritis Clinical Trial in China (NA)
- New Clinical End-points in Patients With Primary Sjögren's Syndrome (PHASE2)
- The Clinical Efficacy of Immunomodulators in RA Patients (PHASE4)
- Comparison of Disease Modifying Antirheumatic Drugs Therapy in Patients With RA Failing Methotrexate Monotherapy (PHASE3)
- The Research of Standard Diagnosis and Treatment for HSPN in Children (PHASE2)
- Predictability Studies on the Efficacy of TNF-α Inhibitors in Chinese RA From "Real World" (PHASE4)
- A Clinical Study of a Natural Remedy for Rheumatoid Arthritis vs. Commonly Used Conventional Medications (NA)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Leflunomide(LEF) CI brief — competitive landscape report
- Leflunomide(LEF) updates RSS · CI watch RSS
- Nanjing Children's Hospital portfolio CI