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Methotrexate (stable dose)
Methotrexate inhibits dihydrofolate reductase, blocking the synthesis of purines and pyrimidines required for DNA replication and cell division.
Methotrexate inhibits dihydrofolate reductase, blocking the synthesis of purines and pyrimidines required for DNA replication and cell division. Used for Acute lymphoblastic leukemia (ALL), Osteosarcoma, Breast cancer.
At a glance
| Generic name | Methotrexate (stable dose) |
|---|---|
| Sponsor | Hoffmann-La Roche |
| Drug class | Antimetabolite; Folate antagonist |
| Target | Dihydrofolate reductase (DHFR) |
| Modality | Small molecule |
| Therapeutic area | Oncology; Immunology; Rheumatology |
| Phase | FDA-approved |
Mechanism of action
By inhibiting dihydrofolate reductase, methotrexate prevents the conversion of dihydrofolate to tetrahydrofolate, disrupting one-carbon transfer reactions essential for nucleotide synthesis. This leads to suppression of rapidly dividing cells, including cancer cells and activated immune cells. At lower doses used in autoimmune conditions, it also exerts immunosuppressive effects through adenosine release and reduced T-cell proliferation.
Approved indications
- Acute lymphoblastic leukemia (ALL)
- Osteosarcoma
- Breast cancer
- Lung cancer
- Rheumatoid arthritis
- Psoriasis
- Crohn's disease
Common side effects
- Myelosuppression (anemia, leukopenia, thrombocytopenia)
- Mucositis / stomatitis
- Nausea and vomiting
- Hepatotoxicity
- Nephrotoxicity
- Alopecia
- Infection (due to immunosuppression)
Key clinical trials
- Testing the Addition of Lenalidomide and Nivolumab to the Usual Treatment for Primary CNS Lymphoma (PHASE1)
- Influence of Methotrexate Discontinuation on Immunogenicity After PCV-20 Vaccine in Patients ARDs (PHASE4)
- Efficacy and Safety Study of MP-435 in Combination With Methotrexate (MTX) in Patients With Rheumatoid Arthritis (PHASE2)
- Natrunix in Combination With Methotrexate for Rheumatoid Arthritis Treatment (PHASE2)
- Recombinant Herpes Zoster Vaccine in Patients With Autoimmune Rheumatic Diseases (PHASE4)
- Efficacy of a Sequential Treatment Strategy in Rheumatoid Arthritis (PHASE3)
- Spondyloarthritis: Inducing Drug-free Remission by Early TNF-alpha Blockade (PHASE3)
- A Study Comparing Upadacitinib (ABT-494) to Placebo and to Adalimumab in Adults With Rheumatoid Arthritis Who Are on a Stable Dose of Methotrexate and Who Have an Inadequate Response to Methotrexate (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:
- Methotrexate (stable dose) CI brief — competitive landscape report
- Methotrexate (stable dose) updates RSS · CI watch RSS
- Hoffmann-La Roche portfolio CI