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AZATHIOPRINE or METHOTREXATE
Azathioprine and methotrexate are immunosuppressive agents that inhibit cell proliferation and reduce immune activation by interfering with nucleotide synthesis and cellular metabolism.
Azathioprine and methotrexate are immunosuppressive agents that inhibit cell proliferation and reduce immune activation by interfering with nucleotide synthesis and cellular metabolism. Used for Inflammatory bowel disease (Crohn's disease and ulcerative colitis), Rheumatoid arthritis, Autoimmune hepatitis.
At a glance
| Generic name | AZATHIOPRINE or METHOTREXATE |
|---|---|
| Also known as | 6 MERCAPTOPURINE |
| Sponsor | Prof. Arie Levine |
| Drug class | Immunosuppressive agents / Antimetabolites |
| Target | Hypoxanthine-guanine phosphoribosyltransferase (HGPRT) for azathioprine; Dihydrofolate reductase (DHFR) for methotrexate |
| Modality | Small molecule |
| Therapeutic area | Immunology / Rheumatology / Gastroenterology |
| Phase | FDA-approved |
Mechanism of action
Azathioprine is a purine analog prodrug that is converted to 6-mercaptopurine, which inhibits purine synthesis and reduces T-cell and B-cell proliferation. Methotrexate is a folate antagonist that inhibits dihydrofolate reductase, blocking DNA synthesis and cell division. Both drugs suppress immune responses and are used to control inflammatory and autoimmune conditions.
Approved indications
- Inflammatory bowel disease (Crohn's disease and ulcerative colitis)
- Rheumatoid arthritis
- Autoimmune hepatitis
- Systemic lupus erythematosus
- Vasculitis
Common side effects
- Myelosuppression (leukopenia, thrombocytopenia)
- Nausea and vomiting
- Hepatotoxicity
- Infection
- Mucositis
- Alopecia
- Pancreatitis (azathioprine)
Key clinical trials
- Combined Immunosuppression for Pediatric Crohn's Disease (PHASE4)
- This Study is a Non-interventional Disease Registry of Adolescent and Adult Patients With Atopic Dermatitis Who Initiate or Switch Any Systemic Treatment
- An Open-Label Study of Effectiveness of Immunomodulatory Medications for Patients With Relapsing Polychondritis (PHASE2)
- Evaluation of TNF-alpha Antagonists (Infliximab) Withdrawal in Sarcoidosis (PHASE3)
- Effects of Telitacicept vs Cyclophosphamide on Lupus Related Interstitial Lung Disease (PHASE4)
- Determination of the Optimal Treatment Target in Ulcerative Colitis (PHASE4)
- Dose-Ranging Phase 2b Study of ABX464 in Moderate to Severe Ulcerative Colitis (PHASE2)
- Prospective Cohort Establishment and Clinical Observation of Children With Crohn's Disease
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 or METHOTREXATE CI brief — competitive landscape report
- AZATHIOPRINE or METHOTREXATE updates RSS · CI watch RSS
- Prof. Arie Levine portfolio CI