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Azathioprine (AZA)
Azathioprine is a purine analog prodrug that is converted to 6-mercaptopurine, which inhibits purine synthesis and suppresses T-cell and B-cell proliferation.
Azathioprine is a purine analog prodrug that is converted to 6-mercaptopurine, which inhibits purine synthesis and suppresses T-cell and B-cell proliferation. Used for Prevention of organ rejection in transplant recipients, Autoimmune diseases including rheumatoid arthritis, systemic lupus erythematosus, and inflammatory bowel disease, Chronic active hepatitis.
At a glance
| Generic name | Azathioprine (AZA) |
|---|---|
| Also known as | Imuran®, non-investigational medicinal product (NIMP), Adverse effect of Azathioprine in SLE, Imuran |
| Sponsor | University Hospital Schleswig-Holstein |
| Drug class | Purine analog immunosuppressant |
| Target | Inosine monophosphate dehydrogenase (IMPDH), purine synthesis pathway |
| Modality | Small molecule |
| Therapeutic area | Immunology |
| Phase | FDA-approved |
Mechanism of action
Azathioprine acts as an immunosuppressant by interfering with nucleotide metabolism, particularly purine synthesis. After hepatic conversion to 6-mercaptopurine and further metabolism, it inhibits the proliferation of lymphocytes and reduces the production of antibodies and cell-mediated immune responses. This makes it effective in preventing organ rejection and treating autoimmune conditions.
Approved indications
- Prevention of organ rejection in transplant recipients
- Autoimmune diseases including rheumatoid arthritis, systemic lupus erythematosus, and inflammatory bowel disease
- Chronic active hepatitis
Common side effects
- Bone marrow suppression (leukopenia, thrombocytopenia, anemia)
- Nausea and vomiting
- Hepatotoxicity
- Increased infection risk
- Pancreatitis
- Rash
Key clinical trials
- Combined Immunosuppression for Pediatric Crohn's Disease (PHASE4)
- An Open-Label Study of Effectiveness of Immunomodulatory Medications for Patients With Relapsing Polychondritis (PHASE2)
- Efficacy of Top-down Therapy With Mirikizumab Versus Standard of Care With Azathioprine in Patients With Newly Diagnosed Moderate-to-severe Ulcerative Colitis (PHASE4)
- Weaning of Immunosuppression in Nephritis of Lupus (PHASE3)
- The Frequency of Thiopurine Methyltransferase Polymorphism in Systemic Lupus Erythematosus SLE
- Comparison of Azathioprine to Methotrexate in Combination Therapy With Adalimumab in Crohn's Disease: an Open-label Randomized Controlled Trial (PHASE3)
- To Compare the Efficacy of Weekly Azathioprine Pulse Versus Betamethasone Oral Mini-Pulse in the Treatment of Moderate to Severe Alopecia Areata (PHASE2)
- A Study to Evaluate the Safety and Efficacy of Satralizumab in Participants With Neuromyelitis Optica Spectrum Disorder (NMOSD) (PHASE3)
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:
- Azathioprine (AZA) CI brief — competitive landscape report
- Azathioprine (AZA) updates RSS · CI watch RSS
- University Hospital Schleswig-Holstein portfolio CI